Payload ID	PAY0LZRXU
Name	SG3199
Synonyms	SG3199; 1595275-71-0; SCHEMBL15686377; EX-A6229; MS-30463; HY-101161; CS-0020928    Click to Show/Hide
Target(s)	Human Deoxyribonucleic acid (hDNA)					Target Info
Structure
	3D MOL			2D MOL
Formula	C33H36N4O6
Isosmiles	CC1=CN2[C@@H](C1)C=NC3=CC(=C(C=C3C2=O)OC)OCCCCCOC4=C(C=C5C(=C4)N=C[C@@H]6CC(=CN6C5=O)C)OC
PubChem CID	90132565
InChI	InChI=1S/C33H36N4O6/c1-20-10-22-16-34-26-14-30(28(40-3)12-24(26)32(38)36(22)18-20)42-8-6-5-7-9-43-31-15-27-25(13-29(31)41-4)33(39)37-19-21(2)11-23(37)17-35-27/h12-19,22-23H,5-11H2,1-4H3/t22-,23-/m0/s1
InChIKey	YMTZZJOPSATRTO-GOTSBHOMSA-N
IUPAC Name	(6aS)-3-[5-[[(6aS)-2-methoxy-8-methyl-11-oxo-6a,7-dihydropyrrolo[2,1-c][1,4]benzodiazepin-3-yl]oxy]pentoxy]-2-methoxy-8-methyl-6a,7-dihydropyrrolo[2,1-c][1,4]benzodiazepin-11-one
Pharmaceutical Properties	Molecule Weight		584.7	Polar area		102
	Complexity		1080	xlogp Value		2.8
	Heavy Count		43	Rot Bonds		10
	Hbond acc		8	Hbond Donor		0

Standard Type	Value	Units	Cell line	Disease Model	Cell line ID	Reference
Half Maximal Inhibitory Concentration (IC50)	0.79	pM	EoL-1 cells	Chronic eosinophilic leukemia	CVCL_0258	[1]
Half Maximal Inhibitory Concentration (IC50)	12.11	pM	SU-DHL-1 cells	Anaplastic large cell lymphoma	CVCL_0538	[1]
Half Maximal Inhibitory Concentration (IC50)	12.98	pM	HuT 78 cells	T lymphocytic leukemia	CVCL_0337	[1]
Half Maximal Inhibitory Concentration (IC50)	14.8	pM	L-540 cells	Hodgkin lymphoma	CVCL_1362	[1]
Half Maximal Inhibitory Concentration (IC50)	150	pM	K562 cells	Chronic myeloid leukemia	CVCL_0004	[2]
Half Maximal Inhibitory Concentration (IC50)	158.6	pM	HDLM-2 cells	Hodgkin lymphoma	CVCL_0009	[1]
Half Maximal Inhibitory Concentration (IC50)	18.11	pM	Daudi cells	Burkitt lymphoma	CVCL_0008	[1]
Half Maximal Inhibitory Concentration (IC50)	18.49	pM	Karpas-299 cells	ALK-positive anaplastic large cell lymphoma	CVCL_1324	[1]
Half Maximal Inhibitory Concentration (IC50)	20	pM	NCI-N87 cells	Gastric tubular adenocarcinoma	CVCL_1603	[2]
Half Maximal Inhibitory Concentration (IC50)	320	pM	SK-BR-3 cells	Breast adenocarcinoma	CVCL_0033	[2]
Half Maximal Inhibitory Concentration (IC50)	5.83	pM	Ramos cells	Burkitt lymphoma	CVCL_0597	[1]
Half Maximal Inhibitory Concentration (IC50)	0.033	nM	SW48 cells	Colon adenocarcinoma	CVCL_1724	[3]
Half Maximal Inhibitory Concentration (IC50)	0.3	nM	LIM1215 cells	Colon adenocarcinoma	CVCL_2574	[3]
Half Maximal Inhibitory Concentration (IC50)	0.92	nM	SW620 cells	Colon adenocarcinoma	CVCL_0547	[3]
Half Maximal Inhibitory Concentration (IC50)	1	nM	BT-474 cells	Invasive breast carcinoma	CVCL_0179	[2]
Half Maximal Inhibitory Concentration (IC50)	110.5	nM	MDA-MB-231 cells	Breast adenocarcinoma	CVCL_0062	[4]
Half Maximal Inhibitory Concentration (IC50)	174.1	nM	MDA-MB-468 cells	Breast adenocarcinoma	CVCL_0419	[4]
Half Maximal Inhibitory Concentration (IC50)	19.06	nM	SK-LU-1 cells	Lung adenocarcinoma	CVCL_0629	[4]
Half Maximal Inhibitory Concentration (IC50)	22.79	nM	A-172 cells	Glioblastoma	CVCL_0131	[4]
Half Maximal Inhibitory Concentration (IC50)	57.63	nM	SN12C cells	Renal cell carcinoma	CVCL_1705	[4]
Half Maximal Inhibitory Concentration (IC50)	60.6	nM	PANC-1 cells	Pancreatic ductal adenocarcinoma	CVCL_0480	[4]
Half Maximal Inhibitory Concentration (IC50)	62.59	nM	SK-OV-3 cells	Ovarian serous cystadenocarcinoma	CVCL_0532	[4]
Half Maximal Inhibitory Concentration (IC50)	88.8	nM	NCI-H1299 cells	Lung large cell carcinoma	CVCL_0060	[4]
Half Maximal Inhibitory Concentration (IC50)	9.18	nM	Karpas-299 cells	ALK-positive anaplastic large cell lymphoma	CVCL_1324	[4]

Experiment 1 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Objective Response Rate (ORR)	48.28%
Patients Enrolled	Relapsed or refractory diffuse large B-cell lymphoma (DLBCL) after two or more multiagent systemic treatments, who had measurable disease and Eastern Cooperative Oncology Group performance status 0-2.
Administration Dosage	Intravenously on day 1 of each 21-day cycle, at 150 ug/kg for two cycles, then 75 ug/kg thereafter, for up to 1 year or until disease relapse or progression, unacceptable toxicity, death, major protocol deviation, pregnancy, or patient, investigator, or sponsor decision.
Related Clinical Trial
NCT Number	NCT03589469	Phase Status	Phase 2
Clinical Description	A phase 2 open-label single-arm study to evaluate the efficacy and safety of loncastuximab tesirine in patients with relapsed or refractory diffuse large B-cell lymphoma (DLBCL) (LOTIS-2).
Primary Endpoint	Overall response rate assessed by central review. 70 of 145 patients had complete or partial response (overall response rate 48.28% [95% CI 39.9-56.7]); 35 had complete response and 35 had partial response.
Other Endpoint	Median time to first response (complete response or partial response) was 41.00 days (IQR 38.00-44.00). Median duration of response was 10.30 months (95% CI 6.9-not estimable); 13.40 months (10.30-not estimable) for patients with complete response and 5.70 months (1.70-not estimable) for patients with partial response. The probability of responders maintaining responses for 9 months or longer was 64.0%. Median progressionfree survival was 4.90 months (95% CI 2.90-8.30), median overall survival was 9.90 months (6.70-11.50), and median relapse-free survival was 13.40 months (10.30-not estimable).    Click to Show/Hide
Experiment 2 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Objective Response Rate (ORR)	59.40%
Patients Enrolled	R/R B-cell non Hodgkin lymphoma (NHL); had failed or were intolerant to established therapies, or for whom no other established treatment options were available.
Administration Dosage	5 to 200 ug/kg; intravenously over 1 hour, once every 3 weeks (one cycle) by a 3+3 dose-escalation design.
Related Clinical Trial
NCT Number	NCT02669017	Phase Status	Phase 1
Clinical Description	A phase 1 dose-escalation study to evaluate the tolerability, safety, pharmacokinetics, and antitumor activity of ADCT-402 in patients with relapsed or refractory b-cell lineage non Hodgkin lymphoma (B-NHL).
Primary Endpoint	The MTD was not established during the trial due to the low level of DLTs, 150 ug/kg dose for expansion and phase 2.
Other Endpoint	For loncastuximab tesirine 120 ug/kg,Median Progression-Free Survival (mPFS)=4.80 months.The median PFS OS=11.60 months.
Experiment 3 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Complete Remission (CR)	26.70%
Patients Enrolled	Adults (age 18 years) with histologically confirmed relapsed/refractory B-non Hodgkin lymphoma (World Health Organization 2008 classification18 ) who were intolerant to established therapy, for whom established therapy had failed, or for whom no other treatment options were available in the opinion of the investigator were eligible to participate.
Administration Dosage	3 + 3 dose escalation at 15 to 200 ug/kg and dose expansion at 120 and 150 ug/kg; IV infusion over 60 minutes once every 3 weeks (day 1 of each 21-day cycle).
Related Clinical Trial
NCT Number	NCT02669017	Phase Status	Phase 1
Clinical Description	A phase 1 dose-escalation study to evaluate the tolerability, safety, pharmacokinetics, and antitumor activity of ADCT-402 in patients with relapsed or refractory B-cell lineage non Hodgkin lymphoma (B-NHL).
Primary Endpoint	The recommended dose of loncastuximab tesirine for Phase 2 is 150 ug/kg Q3W for 2 doses followed by 75 ug/kg Q3W for subsequent doses. The 150 ug/kg dose was selected as a dose with encouraging responses but lower frequency of AEs than observed with the 200 u/kg dose. Overall response rate (ORR) in evaluable patients was 45.60%, including 26.70% complete responses (CR). Median PFS was 3.10 months (95% CI 2.70-4.20) in all patients with B-NHL, 2.8 months (95% CI 1.90-3.80) in patients with DLBCL, 4.80 months (95% CI 1.10-7.80) in patients with MCL, and could not be determined in those with FL due to the low number of events. Median OS was 8.3 months (95% CI 6.70-10.70) in all patients with B-NHL, 7.5 months (95% CI 6.00-9.80) in patients with DLBCL, and was not reached in patients with MCL or FL due to low number of events.    Click to Show/Hide
Other Endpoint	PK exposure similarity between loncastuximab tesirine total antibody and PBD-conjugated antibody indicated good stability in serum.Accumulation by Cycle 2 for patients on a Q6W dosing regimen was lower than that of those on Q3W dosing: mean accumulation of 1.22 and 1.33 for PBD-conjugated antibody and total antibody on Q6W regimens compared with 1.72 and 1.74 on Q3W regimens. There was substantial variability in PK exposure and PK parameters assessed for PBD-conjugated antibody, total antibody, and SG3199.    Click to Show/Hide
Experiment 4 Reporting the Activity Date of This ADC					[8]
Efficacy Data	Complete Remission (CR)	40.20%
Patients Enrolled	R/R B-acute lymphocytic leukemia (ALL) for standard therapies had failed, intolerant to standard therapies, or no other treatment options were available, in the opinion of the investigator, were eligible for the study, other key inclusion criteria included Eastern Cooperative Oncology Group (ECOG) performance status of 0 to 2.
Administration Dosage	15 to 150 ug/kg once every 3 weeks (Q3W) or 50 ug/kg IV weekly.
Related Clinical Trial
NCT Number	NCT02669264	Phase Status	Phase 1
Clinical Description	A phase 1, open-label, adaptive dose-escalation, multicenter study to evaluate the tolerability, safety, pharmacokinetics, and anti-tumor activity of ADCT-402 in patients with relapsed or refractory B-cell lineage acute lymphoblastic leukemia (B-ALL).
Primary Endpoint	Part II (dose expansion portion) utilized the doses of 120 and 150 ug/kg, selected based on antitumor activity and tolerability seen during part I. The overall response rate (ORR) in patients with DLBCL, mantle cell lymphoma, and follicular lymphoma was 42.30%, 46.70%, and 78.60%, respectively.
Other Endpoint	The median progression-free survival (PFS) was 3.10 months in all patients with B-NHL and 2.80 months in patients with DLBCL, whereas the median OS was 8.30 months in all patients and 7.50 months in patients with DLBCL.
Experiment 5 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Complete Remission (CR)	46.16%

Experiment 1 Reporting the Activity Date of This ADC					[10]
Efficacy Data	Objective Response Rate (ORR)	10.00%
Patients Enrolled	Extensive-stage small-cell lung cancer (ES-SCLC) who had completed four cycles of front-line platinum-based chemotherapy (cisplatin or carboplatin with etoposide or irinotecan) at least 3 weeks but not more than 9 weeks before randomization and had stable disease, PR, or CR per RECIST v.1.1.
Administration Dosage	0.30 mg/kg intravenous Rova-T on day 1 of each 6-week cycle, omitting every third cycle.
Related Clinical Trial
NCT Number	NCT03033511	Phase Status	Phase 3
Clinical Description	A randomized, double-blind, placebo-controlled phase 3 study of rovalpituzumab tesirine as maintenance therapy following first-line platinum-based chemotherapy in subjects with extensive stage small cell lung cancer (MERU).
Primary Endpoint	Median age of all randomized patients (N=748) was 64 years; 78.00% had TNM stage IV disease. At futility analysis of the subset with DLL3-high tumors, the hazard ratio for OS was 1.07 (95% confidence interval: 0.84-1.36) favoring the placebo arm,with median OS of 8.50 and 9.80 months in the Rova-T and placebo arms,respectively; futility criteria were met. Rova-T significantly improved PFS versus placebo by investigator assessment (4.00 versus 1.40 mo,hazard ratio=0.48, p < 0.001).    Click to Show/Hide
Experiment 2 Reporting the Activity Date of This ADC					[11]
Efficacy Data	Objective Response Rate (ORR)	12.40% (all) 14.30% (DLL3-high) 13.20% (DLL3-positive)
Patients Enrolled	Advanced stage DLL3-positive small-cell lung cancer (SCLC).
Administration Dosage	0.30 mg/kg Rova-T intravenously infused over 30 minutes once every 6 weeks for two cycles.
Related Clinical Trial
NCT Number	NCT02674568	Phase Status	Phase 2
Clinical Description	An Open-label, Single-Arm, Phase 2 Study Evaluating the Efficacy, Safety and Pharmacokinetics of Rovalpituzumab Tesirine (SC16LD6.5) for Third-line and Later Treatment of Subjects With Relapsed or Refractory Delta-Like Protein 3-Expressing Small Cell Lung Cancer (TRINITY).
Primary Endpoint	OrR was 12.40%, 14.30%, and 13.20% in all, DLL3-high, and DLL3-positive patients,respectively. Median OS was 5.60 months in all patients and 5.70 months in DLL3-high patients.
Experiment 3 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Objective Response Rate (ORR)	17.14% (In pooled patients with NEC/NET expressing a high level of DLL 3% (50% DLL3-positive tumor cells)) 8.82% (In those with NEC/NET expressing a low level of DLL 3% (1-49% DLL3-positive tumor cells))
Patients Enrolled	101 with NEC/NET (large-cell NEC, gastroenteropancreatic NEC, neuroendocrine prostate cancer, and other NEC/NET) and 99 with other solid tumors (melanoma, medullary thyroid cancer [MTC], glioblastoma, and other).
Administration Dosage	The recommended phase II dose (RP2D) was 0.30 mg/kg every 6 weeks (q6w) for two cycles.
Related Clinical Trial
NCT Number	NCT02709889	Phase Status	Phase 1/2
Clinical Description	An open-label study of rovalpituzumab tesirine in subjects with delta-like protein 3-expressing advanced solid tumors.
Primary Endpoint	The recommended phase II dose (RP2D) was 0.30 mg/kg every 6 weeks (q6w) for two cycles. At the RP2D, grade 3/4 adverse events included anemia (17.00%), thrombocytopenia (15.00%), and elevated aspartate aminotransferase (8.00%). Responses were confirmed in 15/145 patients (10.34%) treated at 0.30 mg/kg, including 9/69 patients (13.04%) with NEC/NET. Rova-T at 0.30 mg/kg q6w had manageable toxicity, with antitumor activity observed in patients with NEC/NET, melanoma, MTC, and glioblastoma.    Click to Show/Hide
Other Endpoint	In pooled patients with NEC/NET expressing a high level of DLL3 (50% DLL3-positive tumor cells), the ORR was 17.14% (6/35) and 34.29% (12/35) had a BOR (all PRs). In those with NEC/NET expressing a low level of DLL3 (1-49% DLL3-positive tumor cells), the ORR was 8.82% (3/34) and the BOR rate was 14.70% (5/34) (all PRs). The median PFS values for pooled patients with NEC/NET expressing high and low levels of DLL3 were 4.30 months (95% CI, 2.7-6.1) and 3.30 months (95% CI, 2.40-4.80), respectively. The median OS values for patients expressing high and low levels of DLL3 were 7.40 months (95% CI, 5.60-13.10) and 7.10 months (95% CI, 4.30-9.90), respectively.    Click to Show/Hide
Experiment 4 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Objective Response Rate (ORR)	34.50% (All evaluable patients) 31.60% (DLL3 score 75%) 50.00% (PD-L1 positive tumor cells) 50.00% (PD-L1 positive inflammatory cells with an intensity of 2+)
Patients Enrolled	Progressive small-cell lung cancer (SCLC) who had previously been treated with at least one prior line of platinum-containing chemotherapy were enrolled if they were naive to PD-1/PD-L1targeting agents, had ECOG performance status 0-1, measurable disease per RECIST v1.1 or disease evaluable by tumor antigen assessment, and adequate bone marrow, cardiac, hepatic, and renal functions.    Click to Show/Hide
Administration Dosage	Budigalimab 375 mg via intravenous infusion every 3 weeks and Rova-T was administered as a dose of 0.30 mg/kg intravenously, on day 1 of the first and third 3-week cycle.
Related Clinical Trial
NCT Number	NCT03000257	Phase Status	Phase 1
Clinical Description	A multicenter, phase 1, open-label, dose-escalation study of ABBV-181 as monotherapy and in combination with another anti-cancer therapy in subjects with advanced solid tumors.
Primary Endpoint	In patients with DLL3 score 75.00% (n = 19) the response rate was similar to the total evaluable population, with an ORR of 21.10% (90% CI: 7.50-41.90).
Experiment 5 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Objective Response Rate (ORR)	50.00% (all) 63.00% (0.1 mg/kg Rova-T) 33.00% (0.2 mg/kg Rova-T)
Patients Enrolled	Extensive-stage small-cell lung cancer (ES SCLC), with a response of stable disease or better after the prestudy CE cycle per the Response Evaluation Criteria in Solid Tumors version 1.1, Eastern Cooperative Oncology Group performance status of 0 to 1, and absent or treated central nervous system metastases.
Administration Dosage	Rova-T monotherapy (0.30 mg/kg, every 6 [q6] wk 2; cohort 1; n = 4); Rova-T induction (0.30 mg/kg, q6 wk 2) followed by CE every 21 days (q21) 4 (cohort 2; n = 5); Rova-T (0.10 or 0.20 mg/kg, q6 wk 2) overlapping with CE q21 4 (cohort 3; n = 14); and Rova-T maintenance (0.30 mg/kg, q6 wk 2) after CE q21 4 (cohort 4; n = 3).
Related Clinical Trial
NCT Number	NCT02819999	Phase Status	Phase 1
Clinical Description	A study of rovalpituzumab tesirine (SC16LD6.5) in the frontline treatment of patients with extensive stage small cell lung cancer.
Primary Endpoint	Median age was 66 years, and 73.00% had Eastern Cooperative Oncology Group performance status of 1. In cohort 3,seven patients (50%) had confirmed objective responses,with a median progression-free survival of 5.20 months and median overall survival of 10.30 months.

Experiment 1 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 16.00% (Day 9)	High DLL3 expression (DLL3+++)
Method Description	The inhibitory activity of Rova-T against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 0.1 mg/kg.
In Vivo Model	Neuroblastoma PDX model (PDX: COG-N-415x)
Experiment 2 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 30.00% (Day 9)	High DLL3 expression (DLL3+++)
Method Description	The inhibitory activity of Rova-T against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 0.3 mg/kg.
In Vivo Model	Neuroblastoma PDX model (PDX: COG-N-415x)
Experiment 3 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 33.00% (Day 28)	High DLL3 expression (DLL3+++)
Method Description	The inhibitory activity of Rova-T against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 1 mg/kg weekly x 1.
In Vivo Model	Neuroblastoma PDX model (PDX: COG-N-415x)
Experiment 4 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 40.74% (Day 9)	High DLL3 expression (DLL3+++)
Method Description	The inhibitory activity of Rova-T against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 0.1 mg/kg.
In Vivo Model	Neuroblastoma PDX model (PDX: COG-N-452x)
Experiment 5 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 50.90% (Day 10)	High DLL3 expression (DLL3+++)
Method Description	The inhibitory activity of Rova-T against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 0.1 mg/kg.
In Vivo Model	Neuroblastoma PDX model (PDX: COG-N-519x)
Experiment 6 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 59.81% (Day 9)	High DLL3 expression (DLL3+++)
Method Description	The inhibitory activity of Rova-T against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 0.3 mg/kg.
In Vivo Model	Neuroblastoma PDX model (PDX: COG-N-452x)
Experiment 7 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 73.87% (Day 10)	High DLL3 expression (DLL3+++)
Method Description	The inhibitory activity of Rova-T against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 0.3 mg/kg.
In Vivo Model	Neuroblastoma PDX model (PDX: COG-N-519x)
Experiment 8 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 78.50% (Day 9)	High DLL3 expression (DLL3+++)
Method Description	The inhibitory activity of Rova-T against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 0.6 mg/kg.
In Vivo Model	Neuroblastoma PDX model (PDX: COG-N-452x)
Experiment 9 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 83.00% (Day 9)	High DLL3 expression (DLL3+++)
Method Description	The inhibitory activity of Rova-T against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 0.6 mg/kg.
In Vivo Model	Neuroblastoma PDX model (PDX: COG-N-415x)
Experiment 10 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.14% (Day 10)	High DLL3 expression (DLL3+++)
Method Description	The inhibitory activity of Rova-T against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 0.6 mg/kg.
In Vivo Model	Neuroblastoma PDX model (PDX: COG-N-519x)
Experiment 11 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.83% (Day 10)	High DLL3 expression (DLL3+++)
Method Description	The inhibitory activity of Rova-T against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 0.6 mg/kg.
In Vivo Model	Neuroblastoma PDX model

Experiment 1 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.00% (Day 28)	High DLL3 expression (DLL3+++)
Method Description	The inhibitory activity of Rova-T against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 1 mg/kg weekly x 3.
In Vivo Model	COG-N-415 neuroblastoma model
In Vitro Model	Neuroblastoma	COG-N-415 cells		CVCL_AQ23

Experiment 1 Reporting the Activity Date of This ADC					[15]
Efficacy Data	Complete Remission (CR)	48.60% (In the cHL cohort, at 45 ug/kg) 35.00% (In the cHL cohort, at 30 ug/kg) 6.50% (in all patients with T-NHL) 10.00% (in all patients with T-NHL, 60 ug/kg doses) 7.10% (in all patients with T-NHL, 80 ug/kg doses) 0.00% (in all patients with T-NHL, 100 ug/kg doses)
Patients Enrolled	Relapsed or refractory classical Hodgkin lymphoma or non-Hodgkin lymphoma, an Eastern Cooperative Oncology Group performance status 0-2, who had no therapies available to them with established clinical benefit for their disease stage were enrolled.
Administration Dosage	Intravenously (3-150 ug/kg) once every 3 weeks.
Related Clinical Trial
NCT Number	NCT02432235	Phase Status	Phase 1
Clinical Description	A phase 1 adaptive dose-escalation study to evaluate the tolerability, safety, pharmacokinetics, and antitumor activity of ADCT-301 in patients with relapsed or refractory Hodgkin lymphoma and non-Hodgkin lymphoma.
Primary Endpoint	The maximum tolerated dose was not reached. The recommended doses for expansion were 30 ug/kg and 45 ug/kg for patients with classical Hodgkin lymphoma and 80 ug/kg for patients with T-cell non-Hodgkin lymphomas. No recommended doses for expansion were defined for B-cell non-Hodgkin lymphomas.
Other Endpoint	In the cHL cohort,ORR (95% CI) was 86.49% at 45 ug/kg (32/37 patients [71.20-95.50]) and 55.00% at 30 ug/kg (11/20 patients [31.50-76.90]); 48.65% (18/37 patients) and 35.00% (7/20 patients) achieved CR. Median (95% CI) DOR for the cHL population was 6.64 months (5.06-8.11),and was 7.16 months (4.57-8.51) in patients treated at 45 ug/kg.
Experiment 2 Reporting the Activity Date of This ADC					[19]
Patients Enrolled	Antecedent myelodysplastic syndrome who received treatment with hypomethylating agents and subsequently presented with CD25-positive AmL, or patients with R/R CD25-positive acute lymphocytic leukemia (ALL) who had failed or were intolerant to any established therapy, or for whom no other treatment options were available.
Administration Dosage	Intravenously at 3-92 ug/kg once every three weeks (Q3W) or 30 or 37.50 ug/kg every week (QW).
Related Clinical Trial
NCT Number	NCT02588092	Phase Status	Phase 1
Clinical Description	A phase 1, open-label, dose-escalation, multicenter study to evaluate the tolerability, safety, pharmacokinetics, and activity of ADCT 301 in patients with relapsed or refractory CD25-positive acute myeloid leukemia (AML) or CD25-positive acute lymphoblastic leukemia.
Primary Endpoint	Two patients achieved complete responses with incomplete hematologic recovery; one each at 30.00 and 37.50 ug/kg QW.
Other Endpoint	Of 16 patients with post-baseline disease assessments, two patients treated on the QW dosing regimen had a complete response (CR).
Experiment 3 Reporting the Activity Date of This ADC					[20]
Patients Enrolled	Relapsed or refractory classical Hodgkin lymphoma and non-Hodgkin lymphoma.
Administration Dosage	45 ug/kg Q3W for 2 cycles and then 30 ug/kg Q3W thereafter; intravenous administration.
Related Clinical Trial
NCT Number	NCT02432235	Phase Status	Phase 1
Clinical Description	A phase 1 adaptive dose-escalation study to evaluate the tolerability, safety, pharmacokinetics, and antitumor activity of ADCT-301 in patients with relapsed or refractory Hodgkin lymphoma and non-Hodgkin lymphoma.
Primary Endpoint	The ORR was 40%,representing 51 responders (patients achieved a best overall response of confirmed PR).
Other Endpoint	Of the 130 patients included in the safety analysis, 27 (20.77%) experienced grade2 increased GGT, 17 (13.08%) experienced a grade2 neurologic AE,and 18 (13.85%) experienced a grade2 autoimmune AE at cycle 6.

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 11.60% (Day 21)	Moderate CD25 expression (CD25++; 76,000 CD25 molecules/cell)
Method Description	Camidanlumab tesirine induces efficient tumor cell killing in CDX models of an anaplastic large cell lymphoma (ALCL) cell line Karpas 299 with moderate CD25 expression (molecules per cell surface=76000). Compared with injection of vehicle (PBS), ADCT-301 administered intravenously (i.v.) at a mean tumor volume of 160 mm3 as a single dose at 0.1 mg/kg.    Click to Show/Hide
In Vivo Model	Anaplastic large cell lymphoma CDX model
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 41.50% (Day 32)	High CD25 expression (CD25+++; 310,000 CD25 molecules/cell)
Method Description	Camidanlumab tesirine induces efficient tumor cell killing in CDX models of an anaplastic large cell lymphoma (ALCL) cell line Su-DHL-1 with high CD25 expression (molecules per cell surface=310000).ADCT-301 was administered intravenously at mean tumor volume of 155 mm3 at single doses of 0.3 mg/kg and tumor growth compared with that observed after injection of vehicle (PBS).    Click to Show/Hide
In Vivo Model	Anaplastic large cell lymphoma CDX model
In Vitro Model	Anaplastic large cell lymphoma	SU-DHL-1 cells		CVCL_0538
Experiment 3 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 51.30% (Day 21)	High CD25 expression (CD25+++; 310,000 CD25 molecules/cell)
Method Description	Camidanlumab tesirine induces efficient tumor cell killing in CDX models of an anaplastic large cell lymphoma (ALCL) cell line Su-DHL-1 with high CD25 expression (molecules per cell surface=310000).ADCT-301 was administered intravenously at mean tumor volume of 155 mm3 at single doses of 0.3 mg/kg and tumor growth compared with that observed after injection of vehicle (PBS).    Click to Show/Hide
In Vivo Model	Anaplastic large cell lymphoma CDX model
In Vitro Model	Anaplastic large cell lymphoma	SU-DHL-1 cells		CVCL_0538
Experiment 4 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 68.40% (Day 21)	Moderate CD25 expression (CD25++; 76,000 CD25 molecules/cell)
Method Description	Camidanlumab tesirine induces efficient tumor cell killing in CDX models of an anaplastic large cell lymphoma (ALCL) cell line Karpas 299 with moderate CD25 expression (molecules per cell surface=76000). Compared with injection of vehicle (PBS), ADCT-301 administered intravenously (i.v.) at a mean tumor volume of 160 mm3 as a single dose at 0.2 mg/kg.    Click to Show/Hide
In Vivo Model	Anaplastic large cell lymphoma CDX model
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324
Experiment 5 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 93.20% (Day 21)	Moderate CD25 expression (CD25++; 76,000 CD25 molecules/cell)
Method Description	Camidanlumab tesirine induces efficient tumor cell killing in CDX models of an anaplastic large cell lymphoma (ALCL) cell line Karpas 299 with moderate CD25 expression (molecules per cell surface=76000). Compared with injection of vehicle (PBS), ADCT-301 administered intravenously (i.v.) at a mean tumor volume of 160 mm3 as a single dose at 0.4 mg/kg.    Click to Show/Hide
In Vivo Model	Anaplastic large cell lymphoma CDX model
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324
Experiment 6 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.10% (Day 32)	High CD25 expression (CD25+++; 310,000 CD25 molecules/cell)
Method Description	Camidanlumab tesirine induces efficient tumor cell killing in CDX models of an anaplastic large cell lymphoma (ALCL) cell line Su-DHL-1 with high CD25 expression (molecules per cell surface=310000).ADCT-301 was administered intravenously at mean tumor volume of 155 mm3 at single doses of 0.6 mg/kg and tumor growth compared with that observed after injection of vehicle (PBS).    Click to Show/Hide
In Vivo Model	Anaplastic large cell lymphoma CDX model
In Vitro Model	Anaplastic large cell lymphoma	SU-DHL-1 cells		CVCL_0538
Experiment 7 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.10% (Day 21)	Moderate CD25 expression (CD25++; 76,000 CD25 molecules/cell)
Method Description	Camidanlumab tesirine induces efficient tumor cell killing in CDX models of an anaplastic large cell lymphoma (ALCL) cell line Karpas 299 with moderate CD25 expression (molecules per cell surface=76000).Vechicle (PBS), ADCT-301 (dar 2.2), nonbinding ADC (DAR 2.1) or Adcetris (DAR~4) were administered intravenously at a mean Karpas 299 tumor volume of 130mm3 as single doses at 0.5 mg/kg.    Click to Show/Hide
In Vivo Model	Anaplastic large cell lymphoma CDX model
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324
Experiment 8 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.40% (Day 21)	Moderate CD25 expression (CD25++; 76,000 CD25 molecules/cell)
Method Description	Camidanlumab tesirine induces efficient tumor cell killing in CDX models of an anaplastic large cell lymphoma (ALCL) cell line Karpas 299 with moderate CD25 expression (molecules per cell surface=76000). Compared with injection of vehicle (PBS), ADCT-301 administered intravenously (i.v.) at a mean tumor volume of 160 mm3 as a single dose at 0.6mg/kg.    Click to Show/Hide
In Vivo Model	Anaplastic large cell lymphoma CDX model
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324
Experiment 9 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.80% (Day 21)	High CD25 expression (CD25+++; 310,000 CD25 molecules/cell)
Method Description	Camidanlumab tesirine induces efficient tumor cell killing in CDX models of an anaplastic large cell lymphoma (ALCL) cell line Su-DHL-1 with high CD25 expression (molecules per cell surface=310000).ADCT-301 was administered intravenously at mean tumor volume of 155 mm3 at single doses of 0.6 mg/kg and tumor growth compared with that observed after injection of vehicle (PBS).    Click to Show/Hide
In Vivo Model	Anaplastic large cell lymphoma CDX model
In Vitro Model	Anaplastic large cell lymphoma	SU-DHL-1 cells		CVCL_0538

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximum Growth Inhibitory Concentration (GI50)	0.26 pM	Moderate CD25 expression (CD25++; 17,000 CD25 molecules/cell)
Method Description	The inhibitory activity of ADCT-301 against cancer cell growth was evaluated in various human cancer cell lines in vitro. CD25-positive and -negative cell lines were incubated with increasing concentrations of ADCT-301 or free warhead (SG3199) for 96 hours before processing by the MTS assay.
In Vitro Model	Chronic eosinophilic leukemia	EoL-1 cells		CVCL_0258
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximum Growth Inhibitory Concentration (GI50)	4.96 pM	High CD25 expression (CD25+++; 310,000 CD25 molecules/cell)
Method Description	The inhibitory activity of ADCT-301 against cancer cell growth was evaluated in various human cancer cell lines in vitro. CD25-positive and -negative cell lines were incubated with increasing concentrations of ADCT-301 or free warhead (SG3199) for 96 hours before processing by the MTS assay.
In Vitro Model	Anaplastic large cell lymphoma	SU-DHL-1 cells		CVCL_0538
Experiment 3 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximum Growth Inhibitory Concentration (GI50)	17.07 pM	Moderate CD25 expression (CD25++; 76,000 CD25 molecules/cell)
Method Description	The inhibitory activity of ADCT-301 against cancer cell growth was evaluated in various human cancer cell lines in vitro. CD25-positive and -negative cell lines were incubated with increasing concentrations of ADCT-301 or free warhead (SG3199) for 96 hours before processing by the MTS assay.
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324
Experiment 4 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximum Growth Inhibitory Concentration (GI50)	19.60 pM	High CD25 expression (CD25+++; 167,000 CD25 molecules/cell)
Method Description	The inhibitory activity of ADCT-301 against cancer cell growth was evaluated in various human cancer cell lines in vitro. CD25-positive and -negative cell lines were incubated with increasing concentrations of ADCT-301 or free warhead (SG3199) for 96 hours before processing by the MTS assay.
In Vitro Model	Hodgkin lymphoma	HDLM-2 cells		CVCL_0009
Experiment 5 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximum Growth Inhibitory Concentration (GI50)	> 6667.00 pM	Negative CD25 expression (CD25-; <1,000 CD25 molecules/cell)
Method Description	The inhibitory activity of ADCT-301 against cancer cell growth was evaluated in various human cancer cell lines in vitro. CD25-positive and -negative cell lines were incubated with increasing concentrations of ADCT-301 or free warhead (SG3199) for 96 hours before processing by the MTS assay.
In Vitro Model	Burkitt lymphoma	Ramos cells		CVCL_0597
Experiment 6 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximum Growth Inhibitory Concentration (GI50)	> 6667.00 pM	Negative CD25 expression (CD25-; <1,000 CD25 molecules/cell)
Method Description	The inhibitory activity of ADCT-301 against cancer cell growth was evaluated in various human cancer cell lines in vitro. CD25-positive and -negative cell lines were incubated with increasing concentrations of ADCT-301 or free warhead (SG3199) for 96 hours before processing by the MTS assay.
In Vitro Model	Burkitt lymphoma	Daudi cells		CVCL_0008
Experiment 7 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximum Growth Inhibitory Concentration (GI50)	> 6667.00 pM	Negative CD25 expression (CD25-; <1,000 CD25 molecules/cell)
Method Description	The inhibitory activity of ADCT-301 against cancer cell growth was evaluated in various human cancer cell lines in vitro. CD25-positive and -negative cell lines were incubated with increasing concentrations of ADCT-301 or free warhead (SG3199) for 96 hours before processing by the MTS assay.
In Vitro Model	T lymphocytic leukemia	HuT 78 cells		CVCL_0337
Experiment 8 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximum Growth Inhibitory Concentration (GI50)	> 6667.00 pM	Negative CD25 expression (CD25-; <1,000 CD25 molecules/cell)
Method Description	The inhibitory activity of ADCT-301 against cancer cell growth was evaluated in various human cancer cell lines in vitro. CD25-positive and -negative cell lines were incubated with increasing concentrations of ADCT-301 or free warhead (SG3199) for 96 hours before processing by the MTS assay.
In Vitro Model	Adult acute myeloid leukemia	KG-1 cells		CVCL_0374
Experiment 9 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximum Growth Inhibitory Concentration (GI50)	7.49 pM 1.11 ng/mL	Moderate CD25 expression (CD25++; 96,000 CD25 molecules/cell)
Method Description	The inhibitory activity of ADCT-301 against cancer cell growth was evaluated in various human cancer cell lines in vitro. CD25-positive and -negative cell lines were incubated with increasing concentrations of ADCT-301 or free warhead (SG3199) for 96 hours before processing by the MTS assay.
In Vitro Model	Hodgkin lymphoma	L-540 cells		CVCL_1362

Experiment 1 Reporting the Activity Date of This ADC					[16]
Patients Enrolled	R/R B-acute lymphocytic leukemia (ALL).
Administration Dosage	A 3+3 dose-escalation design was used for phase 1. ADCT-602 was initially given IV once every 3 weeks (30 ug/kg, n=3; 60 ug/kg, n=4; 90 ug/kg, n=4); based on the PK data, the administration schedule was later amended to weekly infusions (30 ug/kg, n=3; 40 ug/kg, n=4; 50 ug/kg, n=3).
Related Clinical Trial
NCT Number	NCT03698552	Phase Status	Phase 1
Clinical Description	A phase 1/2 study to evaluate the safety and anti-tumor activity of ADCT-602 targeting CD22 in patients with relapsed or refractory B-cell acute lymphoblastic leukemia.
Primary Endpoint	In this phase 1 study in pts with very heavily pretreated R/R B-ALL with a median of 5 prior lines of therapy and high baseline bone marrow tumor burden, single-agent ADCT-602 was well tolerated with one pt with DLT noted at the 50 mg/kg weekly dose level. Notably, all 3 pts treated at this dose level had evidence of clinical activity with 2/3 pts achieving MRD negative CR.    Click to Show/Hide
Experiment 2 Reporting the Activity Date of This ADC					[17]
Patients Enrolled	R/R B-acute lymphocytic leukemia (ALL).
Administration Dosage	A 3+3 dose-escalation design was used for phase 1. ADCT-602 was initially given IV once every 3 weeks (30 ug/kg, n=3; 60 ug/kg, n=4; 90 ug/kg, n=4); based on the PK data, the administration schedule was later amended to weekly infusions (30 ug/kg, n=3; 40 ug/kg, n=4; 50 ug/kg, n=3).
Related Clinical Trial
NCT Number	NCT03698552	Phase Status	Phase 1
Clinical Description	A phase 1/2 study to evaluate the safety and anti-tumor activity of ADCT-602 targeting CD22 in patients with relapsed or refractory b-cell acute lymphoblastic leukemia.
Primary Endpoint	In this phase 1 study in pts with very heavily pretreated R/R B-ALL with a median of 5 prior lines of therapy and high baseline bone marrow tumor burden, single-agent ADCT-602 was well tolerated with no DLTs noted. Two pts achieved MRD-negative remission. Dose escalation in the weekly schedule continues and 2 additional dose levels (40 ug/kg weekly and 50 ug/kg weekly) are planned. PK data, available for 9 pts treated at every 3-week schedule [30 ug/kg, n=3; 60 ug/kg, n=4; 90 ug/kg, n=2] showed rapid clearance of antibody with mean apparent half-life of <1 day during Cycle 1. This supported transitioning ADCT-602 administration to the weekly dosing.    Click to Show/Hide
Experiment 3 Reporting the Activity Date of This ADC					[18]
Related Clinical Trial
NCT Number	NCT03698552	Phase Status	Phase 1
Clinical Description	A phase 1/2 study to evaluate the safety and anti-tumor activity of ADCT-602 targeting CD22 in patients with relapsed or refractory B-cell acute lymphoblastic leukemia.

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Objective Response Rate (ORR)	14.29%
Patients Enrolled	Small-cell lung cancer (either limited or extensive disease) or large cell neuroendocrine carcinoma that had relapsed or was refractory to treatment following 1 prior systemic chemotherapy and for which no curative therapy was available were eligible for the phase 1a dose-escalation.
Administration Dosage	7 dose levels (0.025-0.40 mg/kg), 3+3 design.
Related Clinical Trial
NCT Number	NCT02500914	Phase Status	Phase 1a/1b
Clinical Description	A phase 1a/1b dose escalation and expansion study of single-agent SC-002 in subjects with relapsed or refractory small cell lung cancer and large cell neuroendocrine carcinoma.
Primary Endpoint	All patients (N = 35) were included in response analyses. Five patients (14.29%) overall achieved a PR per investigator assessment,with no patients achieving a CR. One patient each had a PR in the 0.20 and 0.30 mg/kg Q3W dose groups, and 3 patients in the 0.40 mg/kg Q9W dose group, fourteen (40.00%) patients achieved stable disease as their best overall response,and 5 had no or an non-evaluable posttreatment scan.    Click to Show/Hide
Other Endpoint	Nineteen patients had tumor samples that were able to be assessed for DLL3 expression by immunohistochemistry. DLL3-positive expression by immunohistochemistry (DLL3 >0%) was confirmed in 17 patients; 5 were DLL3 high (75.00% DLL3 positive cells). Of DLL3-positive patients, 2 (11.80%) achieved a PR, including 1 patient in the 0.20 mg/kg Q3W cohort and 1 DLL3-high patient in the 0.40 mg/kg Q9W cohort.    Click to Show/Hide
Experiment 2 Reporting the Activity Date of This ADC					[26]
Related Clinical Trial
NCT Number	NCT02500914	Phase Status	Phase 1
Clinical Description	A phase 1a/1b dose escalation and expansion study of single-agent SC-002 in subjects with relapsed or refractory small cell lung cancer and large cell neuroendocrine carcinoma.

Experiment 1 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Objective Response Rate (ORR)	61.00% (MTD)
Patients Enrolled	Eligible pts were 18 years old with confirmed relapsed/refractory multiple myeloma (R/R MM) as defined by International Myeloma Working Group consensus criteria, had measurable disease, and had an Eastern Cooperative Oncology Group performance status 1. Pts had to have progressed after treatment with three classes of standard-of-care anti-myeloma drugs, including proteasome inhibitors (PIs), immunomodulatory drugs (IMiDs), and monoclonal antibodies (mAbs).    Click to Show/Hide
Administration Dosage	Administered in the dose of 0.0125-0.20 mg/kg intravenously every 3 weeks (Q3W); The maximum tolerated dose was 0.14 mg/kg Q3W.
Related Clinical Trial
NCT Number	NCT03489525	Phase Status	Phase 1
Clinical Description	A phase 1, open-label study to evaluate the safety, pharmacokinetics, immunogenicity, and preliminary efficacy of MEDI2228 in subjects with relapsed/refractory multiple myeloma.

Experiment 1 Reporting the Activity Date of This ADC					[29]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 82.05% (Day 31)
Method Description	The inhibitory activity of MEDI-2228 against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 0.3 mg/kg MEDI-2228.
In Vivo Model	NSG mice model
In Vitro Model	Plasma cell myeloma	MM1.S cells		CVCL_8792
Experiment 2 Reporting the Activity Date of This ADC					[29]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90.46% (Day 31)
Method Description	The inhibitory activity of MEDI-2228+NK against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 0.3 mg/kg MEDI-2228.
In Vivo Model	NSG mice model
In Vitro Model	Plasma cell myeloma	MM1.S cells		CVCL_8792
Experiment 3 Reporting the Activity Date of This ADC					[29]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.94% (Day 31)
Method Description	The inhibitory activity of MEDI-2228+NK+Dara against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 0.3 mg/kg MEDI-2228.
In Vivo Model	NSG mice model
In Vitro Model	Plasma cell myeloma	MM1.S cells		CVCL_8792

Experiment 1 Reporting the Activity Date of This ADC					[30]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 67.99% (Day 24)
Method Description	The inhibitory activity of MEDI-2228 against cancer cell growth was evaluated in various human cancer cell lines in vivo.The cells were treated with 0.4 mg/kg MEDI-2228.
In Vivo Model	CB17 SCID mice model
Experiment 2 Reporting the Activity Date of This ADC					[30]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90.12% (Day 24)
Method Description	The inhibitory activity combination of M2 and btz for 2 weeks against cancer cell growth was evaluated in various human cancer cell lines in vivo.
In Vivo Model	CB17 SCID mice model

Experiment 1 Reporting the Activity Date of This ADC					[30]
Efficacy Data	Half Maximal Effective Dose (EC50)	189.70 ng/mL
Method Description	The inhibitory activity of MEDI-2228 against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Plasma cell myeloma	RPMI-8226 cells		CVCL_0014

Experiment 1 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Composite Response Rate (RR)	12.10%
Patients Enrolled	Patients with metastatic castration-resistant prostate cancer after disease progression on abiraterone and/or enzalutamide and taxane-based chemotherapy.
Administration Dosage	Administered at 0.015-0.30 mg/kg intravenously every 3 weeks until disease progression/unacceptable toxicity; The MTD was not identified; the MAD was 0.30 mg/kg.
Related Clinical Trial
NCT Number	NCT02991911	Phase Status	Phase 1
Clinical Description	A phase 1/1b multicenter, open-label, dose-escalation and dose-expansion study to evaluate the safety, pharmacokinetics, immunogenicity, and antitumor activity of MEDI3726 in subjects with metastatic castration resistant prostate cancer who have received prior treatment with abiraterone or enzalutamide.

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 15.86% (Day 26)	High PSMA expression (PSMA+++; 250,494 PSMA molecules/cell)
Method Description	The inhibitory activity of MEDI3726 against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 0.33 mg/kg MEDI3726.
In Vivo Model	PC-3 CDX model
In Vitro Model	Prostate carcinoma	PC-3 cells		CVCL_0035
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 36.17% (Day 19)	Moderate PSMA expression (PSMA++; 43,766 PSMA molecules/cell)
Method Description	The inhibitory activity of MEDI3726 against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 0.11 mg/kg MEDI3726.
In Vivo Model	PC-3 CDX model
In Vitro Model	Prostate carcinoma	LNCaP cells		CVCL_0395
Experiment 3 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 45.68% (Day 26)	High PSMA expression (PSMA+++; 250,494 PSMA molecules/cell)
Method Description	The inhibitory activity of MEDI3726 against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 1 mg/kg MEDI3726.
In Vivo Model	PC-3 CDX model
In Vitro Model	Prostate carcinoma	PC-3 cells		CVCL_0035
Experiment 4 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 68.20% (Day 19)	Moderate PSMA expression (PSMA++; 43,766 PSMA molecules/cell)
Method Description	The inhibitory activity of MEDI3726 against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 0.33 mg/kg MEDI3726.
In Vivo Model	PC-3 CDX model
In Vitro Model	Prostate carcinoma	LNCaP cells		CVCL_0395
Experiment 5 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 76.95% (Day 19)	High PSMA expression (PSMA+++; 250,494 PSMA molecules/cell)
Method Description	The inhibitory activity of MEDI3726 against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 1 mg/kg MEDI3726.
In Vivo Model	PC-3 CDX model
In Vitro Model	Prostate carcinoma	LNCaP cells		CVCL_0395
Experiment 6 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 93.55% (Day 20)	Negative PSMA expression (PSMA-)
Method Description	The inhibitory activity of MEDI3726 against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 0.33 mg/kg MEDI3726.
In Vivo Model	PC-3 CDX model
In Vitro Model	Prostate carcinoma	22RV1 cells		CVCL_1045
Experiment 7 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.71% (Day 20)	Negative PSMA expression (PSMA-)
Method Description	The inhibitory activity of MEDI3726 against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 1 mg/kg MEDI3726.
In Vivo Model	PC-3 CDX model
In Vitro Model	Prostate carcinoma	22RV1 cells		CVCL_1045

Experiment 1 Reporting the Activity Date of This ADC					[25]
Related Clinical Trial
NCT Number	NCT03859752	Phase Status	Phase 1
Clinical Description	A phase 1, open label, first-in-human study of TR1801-ADC, an antibody drug conjugate (ADC), in patients with select solid tumors expressing c-met.

Experiment 1 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 1.02% (Day 25)	High MET expression (MET+++)
Method Description	Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 0.125 mg/kg.    Click to Show/Hide
In Vivo Model	Colorectal cancer PDX model (PDX: CR3150)
Experiment 2 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 30.20% (Day 28)	High MET expression (MET+++)
Method Description	Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 0.125 mg/kg.    Click to Show/Hide
In Vivo Model	Head and neck squamous cell carcinoma PDX model (PDX: HN0635)
Experiment 3 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 30.40% (Day 45)	Moderate MET expression (MET++)
Method Description	Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 0.125 mg/kg.    Click to Show/Hide
In Vivo Model	Head and neck squamous cell carcinoma PDX model (PDX: HN0696)
Experiment 4 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 34.80% (Day 42)	Moderate MET expression (MET++)
Method Description	Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 0.25 mg/kg.    Click to Show/Hide
In Vivo Model	Colorectal cancer PDX model (PDX: CR0126)
Experiment 5 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 35.40% (Day 28)	Moderate MET expression (MET++)
Method Description	Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 0.125 mg/kg.    Click to Show/Hide
In Vivo Model	Head and neck squamous cell carcinoma PDX model (PDX: HN3533)
Experiment 6 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 37.50% (Day 25)	Moderate MET expression (MET++)
Method Description	Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 0.25 mg/kg.    Click to Show/Hide
In Vivo Model	Colorectal cancer PDX model (PDX: CR3150)
Experiment 7 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 44.60% (Day 42)	High MET expression (MET+++)
Method Description	Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 0.5 mg/kg.    Click to Show/Hide
In Vivo Model	Colorectal cancer PDX model (PDX: CR0126)
Experiment 8 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 45.70% (Day 28)	Moderate MET expression (MET++)
Method Description	Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 0.25 mg/kg.    Click to Show/Hide
In Vivo Model	Head and neck squamous cell carcinoma PDX model (PDX: HN3533)
Experiment 9 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 45.70% (Day 45)	Negative MET expression (MET-)
Method Description	Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 0.25 mg/kg.    Click to Show/Hide
In Vivo Model	Head and neck squamous cell carcinoma PDX model (PDX: HN0696)
Experiment 10 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 47.30% (Day 28)	High MET expression (MET+++)
Method Description	Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 0.25 mg/kg.    Click to Show/Hide
In Vivo Model	Head and neck squamous cell carcinoma PDX model (PDX: HN0635)
Experiment 11 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 53.20% (Day 28)	Moderate MET expression (MET++)
Method Description	Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 0.5 mg/kg.    Click to Show/Hide
In Vivo Model	Head and neck squamous cell carcinoma PDX model (PDX: HN0635)
Experiment 12 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 59.10% (Day 28)	High MET expression (MET+++)
Method Description	Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 0.5 mg/kg.    Click to Show/Hide
In Vivo Model	Head and neck squamous cell carcinoma PDX model (PDX: HN3533)
Experiment 13 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 60.40% (Day 45)	High MET expression (MET+++)
Method Description	Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 0.5 mg/kg.    Click to Show/Hide
In Vivo Model	Head and neck squamous cell carcinoma PDX model (PDX: HN0696)
Experiment 14 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 70.30% (Day 25)	High MET expression (MET+++; IHC H-score=300)
Method Description	Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 0.5 mg/kg.    Click to Show/Hide
In Vivo Model	Colorectal cancer PDX model (PDX: CR3150)
Experiment 15 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 70.80% (Day 28)	High MET expression (MET+++; IHC H-score=295)
Method Description	Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 1 mg/kg.    Click to Show/Hide
In Vivo Model	Head and neck squamous cell carcinoma PDX model (PDX: HN0635)
Experiment 16 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 70.90% (Day 42)	Moderate MET expression (MET++; IHC H-score=173)
Method Description	Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 1 mg/kg.    Click to Show/Hide
In Vivo Model	Colorectal cancer PDX model (PDX: CR0126)
Experiment 17 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 76.50% (Day 45)	Moderate MET expression (MET++; IHC H-score=130)
Method Description	Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 1 mg/kg.    Click to Show/Hide
In Vivo Model	Head and neck squamous cell carcinoma PDX model (PDX: HN0696)
Experiment 18 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 79.40% (Day 60)	Moderate MET expression (MET++; IHC H-score=180)
Method Description	Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 0.125 mg/kg.    Click to Show/Hide
In Vivo Model	Gastric cancer PDX models (PDX: GA0152)
Experiment 19 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 80.50% (Day 28)	Moderate MET expression (MET++; IHC H-score=190)
Method Description	Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 1 mg/kg.    Click to Show/Hide
In Vivo Model	Head and neck squamous cell carcinoma PDX model (PDX: HN3533)
Experiment 20 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 80.90% (Day 42)	High MET expression (MET+++; IHC H-score=300)
Method Description	Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 0.125 mg/kg.    Click to Show/Hide
In Vivo Model	Colorectal cancer PDX model (PDX: CR0126)
Experiment 21 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 81.40% (Day 60)	High MET expression (MET+++; IHC H-score=300)
Method Description	Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 0.125 mg/kg.    Click to Show/Hide
In Vivo Model	Gastric cancer PDX models (PDX: GA3121)
Experiment 22 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 89.20% (Day 60)	Moderate MET expression (MET++; IHC H-score=190)
Method Description	Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 0.25 mg/kg.    Click to Show/Hide
In Vivo Model	Gastric cancer PDX models (PDX: GA0152)
Experiment 23 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 95.10% (Day 25)	High MET expression (MET+++; IHC H-score=300)
Method Description	Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 1 mg/kg.    Click to Show/Hide
In Vivo Model	Colorectal cancer PDX model (PDX: CR3150)
Experiment 24 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 96.30% (Day 60)	Moderate MET expression (MET++; IHC H-score=180)
Method Description	Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 0.25 mg/kg.    Click to Show/Hide
In Vivo Model	Gastric cancer PDX models (PDX: GA3121)
Experiment 25 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.60% (Day 60)	Moderate MET expression (MET++; IHC H-score=130)
Method Description	Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 0.5 mg/kg.    Click to Show/Hide
In Vivo Model	Gastric cancer PDX models (PDX: GA0152)
Experiment 26 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.10% (Day 60)	Moderate MET expression (MET++; IHC H-score=130)
Method Description	Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 0.5 mg/kg.    Click to Show/Hide
In Vivo Model	Gastric cancer PDX models (PDX: GA3121)
Experiment 27 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 60)	Moderate MET expression (MET++)
Method Description	Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 1 mg/kg.    Click to Show/Hide
In Vivo Model	Gastric cancer PDX models (PDX: GA3121)
Experiment 28 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 60)	Moderate MET expression (MET++)
Method Description	Each mouse was subcutaneously inoculated at the right flank with a 23 mm (diameter) tumor piece of one of the tested PDX models. Mice were randomly grouped into six groups (n = 10 animals) according to the tumor size average of 200 mm3.A single dose of test articles was administered intravenously into the tail vein at the dose concentrations indicated. TR1801-ADC 1 mg/kg.    Click to Show/Hide
In Vivo Model	Gastric cancer PDX models (PDX: GA0152)

Experiment 1 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Maximum inhibition efficiency (MIE)	68.30%	High MET expression (MET+++; IHC H-score=300)
Method Description	Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model	Pharyngeal squamous cell carcinoma	Detroit 562 cells		CVCL_1171
Experiment 2 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Maximum inhibition efficiency (MIE)	88.80%	Moderate MET expression (MET++; IHC H-score=190)
Method Description	Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model	Lung adenocarcinoma	NCI-H1573 cells		CVCL_1478
Experiment 3 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Maximum inhibition efficiency (MIE)	90.50%	High MET expression (MET+++; IHC H-score=295)
Method Description	Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076
Experiment 4 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Maximum inhibition efficiency (MIE)	92.40%	Moderate MET expression (MET++; IHC H-score=190)
Method Description	Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model	Colon adenocarcinoma	SW480 cells		CVCL_0546
Experiment 5 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Maximum inhibition efficiency (MIE)	92.90%	Moderate MET expression (MET++; IHC H-score=180)
Method Description	Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model	Colon adenocarcinoma	SW1417 cells		CVCL_1717
Experiment 6 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Maximum inhibition efficiency (MIE)	95.20%	Moderate MET expression (MET++; IHC H-score=173)
Method Description	Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model	Lung papillary adenocarcinoma	NCI-H441 cells		CVCL_1561
Experiment 7 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Maximum inhibition efficiency (MIE)	95.50%	Moderate MET expression (MET++; IHC H-score=180)
Method Description	Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model	Lung adenocarcinoma	NCI-H1373 cells		CVCL_1465
Experiment 8 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Maximum inhibition efficiency (MIE)	97.40%	Moderate MET expression (MET++; IHC H-score=173)
Method Description	Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model	Gastric adenocarcinoma	SNU-1 cells		CVCL_0099
Experiment 9 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Maximum inhibition efficiency (MIE)	97.50%	High MET expression (MET+++; IHC H-score=300)
Method Description	Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model	Gastric adenocarcinoma	SNU-5 cells		CVCL_0078
Experiment 10 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Maximum inhibition efficiency (MIE)	97.60%	Moderate MET expression (MET++; IHC H-score=130)
Method Description	Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model	Lung adenocarcinoma	NCI-H1975 cells		CVCL_1511
Experiment 11 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Maximum inhibition efficiency (MIE)	97.80%	High MET expression (MET+++; IHC H-score=295)
Method Description	Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model	Gastric adenocarcinoma	MKN45 cells		CVCL_0434
Experiment 12 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Maximum inhibition efficiency (MIE)	98.10%	Moderate MET expression (MET++; IHC H-score=173)
Method Description	Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model	Hypopharyngeal squamous cell carcinoma	FaDu cells		CVCL_1218
Experiment 13 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Maximum inhibition efficiency (MIE)	98.90%	High MET expression (MET+++; IHC H-score=295)
Method Description	Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model	Colon carcinoma	HCT 116 cells		CVCL_0291
Experiment 14 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Maximum inhibition efficiency (MIE)	99.10%	High MET expression (MET+++; IHC H-score=300)
Method Description	Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model	Cecum adenocarcinoma	NCI-H747 cells		CVCL_1587
Experiment 15 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Maximum inhibition efficiency (MIE)	99.30%	High MET expression (MET+++; IHC H-score=300)
Method Description	Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model	Gastric adenocarcinoma	SNU-620 cells		CVCL_5079
Experiment 16 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.20 pM	Moderate MET expression (MET++; IHC H-score=173)
Method Description	Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model	Lung papillary adenocarcinoma	NCI-H441 cells		CVCL_1561
Experiment 17 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	15.60 pM	High MET expression (MET+++; IHC H-score=300)
Method Description	Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model	Gastric adenocarcinoma	SNU-5 cells		CVCL_0078
Experiment 18 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	15.80 pM	High MET expression (MET+++; IHC H-score=295)
Method Description	Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model	Gastric adenocarcinoma	MKN45 cells		CVCL_0434
Experiment 19 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	190.20 pM	High MET expression (MET+++; IHC H-score=295)
Method Description	Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model	Colon carcinoma	HCT 116 cells		CVCL_0291
Experiment 20 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	197.90 pM	High MET expression (MET+++; IHC H-score=300)
Method Description	Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model	Gastric adenocarcinoma	SNU-620 cells		CVCL_5079
Experiment 21 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	327.50 pM	Moderate MET expression (MET++; IHC H-score=173)
Method Description	Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model	Hypopharyngeal squamous cell carcinoma	FaDu cells		CVCL_1218
Experiment 22 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	346.40 pM	Moderate MET expression (MET++; IHC H-score=130)
Method Description	Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model	Lung adenocarcinoma	NCI-H1975 cells		CVCL_1511
Experiment 23 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1380.00 pM	Moderate MET expression (MET++; IHC H-score=190)
Method Description	Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model	Colon adenocarcinoma	SW480 cells		CVCL_0546
Experiment 24 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2272.70 pM	Moderate MET expression (MET++; IHC H-score=180)
Method Description	Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model	Lung adenocarcinoma	NCI-H1373 cells		CVCL_1465
Experiment 25 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3230.00 pM	High MET expression (MET+++; IHC H-score=300)
Method Description	Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model	Cecum adenocarcinoma	NCI-H747 cells		CVCL_1587
Experiment 26 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3494.00 pM	Moderate MET expression (MET++; IHC H-score=180)
Method Description	Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model	Colon adenocarcinoma	SW1417 cells		CVCL_1717
Experiment 27 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4664.00 pM	High MET expression (MET+++; IHC H-score=295)
Method Description	Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076
Experiment 28 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	11.03 nM	High MET expression (MET+++; IHC H-score=300)
Method Description	Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model	Pharyngeal squamous cell carcinoma	Detroit 562 cells		CVCL_1171
Experiment 29 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	13.44 nM	Moderate MET expression (MET++; IHC H-score=190)
Method Description	Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model	Lung adenocarcinoma	NCI-H1573 cells		CVCL_1478
Experiment 30 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	24.37 nM	Moderate MET expression (MET++; IHC H-score=173)
Method Description	Cell viability was determined by measuring the luminescence after adding the CellTiter-Glo 2.0 reagent. Cancer cells were seeded overnight in growth media and incubated at 37°C, 5% CO2,and 95% humidity. starting with concentrations of 100 nM for ADCs for free drug. Cells were exposed to test articlesfor 5 days.
In Vitro Model	Gastric adenocarcinoma	SNU-1 cells		CVCL_0099

Experiment 1 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 35.00% (Day 65)	Positive AXL expression (AXL+++/++)
Method Description	In vivo antitumor activity of ADCT-601 in BRCA1-mutated ovarian cancer PDX model. Single-dose (0.15 mg/kg,q.d.) ADCT-601 and isotype-control ADC (B12-PL1601) were administered intravenously (day 1) to treatment groups of 8 mice.
In Vivo Model	BRCA1-mutated ovarian cancer PDX model (PDX: CTG-0703)
Experiment 2 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 57.40% (Day 21)	Positive AXL expression (AXL+++/++)
Method Description	The antitumor activity of ADCT-601 was tested in a range of human solid tumor xenograft models covering multiple indications. Single-dose (0.075 mg/kg,q.d.). ADCT-601 and isotype-control ADC (B12-PL1601) were administered intravenously (day 1) to treatment groups of 8 mice.
In Vivo Model	Pancreatic cancer PDX model (PDX: PAXF1657)
Experiment 3 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 65.80% (Day 65)	Negative AXL expression (AXL-)
Method Description	In vivo antitumor activity of ADCT-601 in BRCA1-mutated ovarian cancer PDX model. Single-dose (0.15 mg/kg,q.d.) ADCT-601 in combination with olaparib (50 mg/kg) and isotype-control ADC (B12-PL1601) were administered intravenously (day 1) to treatment groups of 8 mice.
In Vivo Model	BRCA1-mutated ovarian cancer PDX model (PDX: CTG-0703)
Experiment 4 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 68.70% (Day 30)	Negative AXL expression (AXL-)
Method Description	In vivo antitumor activity of ADCT-601 in a MMAE-resistant NCI-H1299 NSCLC model. Single-dose (0.50 mg/kg,q.d.) ADCT-601 and isotype-control ADC (B12-PL1601) were administered intravenously (day 1) to treatment groups of 8 mice.
In Vivo Model	MMAE-resistant non-small cell lung cancer PDX model (PDX: NCI-H1299)
Experiment 5 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 72.10% (Day 30)	Positive AXL expression (AXL+++/++; 88,000 copy number)
Method Description	In vivo antitumor activity of ADCT-601 in a MMAE-resistant NCI-H1299 NSCLC model. Single-dose (1.00 mg/kg,q.d.) ADCT-601 and isotype-control ADC (B12-PL1601) were administered intravenously (day 1) to treatment groups of 8 mice.
In Vivo Model	MMAE-resistant non-small cell lung cancer PDX model (PDX: NCI-H1299)
Experiment 6 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 84.90% (Day 21)	Positive AXL expression (AXL+++/++; 88,000 copy number)
Method Description	The antitumor activity of ADCT-601 was tested in a range of human solid tumor xenograft models covering multiple indications. Single-dose (0.15 mg/kg,q.d.). ADCT-601 and isotype-control ADC (B12-PL1601) were administered intravenously (day 1) to treatment groups of 8 mice.
In Vivo Model	Pancreatic cancer PDX model (PDX: PAXF1657)
Experiment 7 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 96.90% (Day 21)	Positive AXL expression (AXL+++/++; 88,000 copy number)
Method Description	The antitumor activity of ADCT-601 was tested in a range of human solid tumor xenograft models covering multiple indications. Single-dose (0.30 mg/kg,q.d.). ADCT-601 and isotype-control ADC (B12-PL1601) were administered intravenously (day 1) to treatment groups of 8 mice.
In Vivo Model	Pancreatic cancer PDX model (PDX: PAXF1657)
Experiment 8 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.50% (Day 51)	Positive AXL expression (AXL+++/++; 36,000 copy number)
Method Description	The antitumor activity of ADCT-601 was tested in a range of human solid tumor xenograft models covering multiple indications. Single-dose (1 mg/kg,q.d.) 0.ADCT-601 and isotype-control ADC (B12-PL1601) were administered intravenously (day 1) to treatment groups of 8 mice.
In Vivo Model	Esophageal caner PDX model (PDX: ES0195)

Experiment 1 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 69.40% (Day 60)	Positive AXL expression (AXL+++/++)
Method Description	The antitumor activity of ADCT-601 was tested in a range of human solid tumor xenograft models covering multiple indications. Single-dose (0.30 mg/kg,q.d.). ADCT-601 and isotype-control ADC (B12-PL1601) were administered intravenously (day 1) to treatment groups of 8 mice.
In Vivo Model	kidney cancer CDX model
In Vitro Model	Renal cell carcinoma	SN12C cells		CVCL_1705
Experiment 2 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 86.20% (Day 60)	Positive AXL expression (AXL+++/++)
Method Description	The antitumor activity of ADCT-601 was tested in a range of human solid tumor xenograft models covering multiple indications. Single-dose (0.60 mg/kg,q.d.). ADCT-601 and isotype-control ADC (B12-PL1601) were administered intravenously (day 1) to treatment groups of 8 mice.
In Vivo Model	kidney cancer CDX model
In Vitro Model	Renal cell carcinoma	SN12C cells		CVCL_1705
Experiment 3 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.60% (Day 23)	Positive AXL expression (AXL+++/++)
Method Description	The antitumor activity of ADCT-601 was tested in a range of human solid tumor xenograft models covering multiple indications. Single-dose (1.00 mg/kg,q.d.). ADCT-601 and isotype-control ADC were administered intravenously (day 1) to treatment groups of 10 mice.
In Vivo Model	Triple-negative breast cancer CDX model
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 4 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.50% (Day 60)	Positive AXL expression (AXL+++/++)
Method Description	The antitumor activity of ADCT-601 was tested in a range of human solid tumor xenograft models covering multiple indications. Single-dose (1.00 mg/kg,q.d.). ADCT-601 and isotype-control ADC (B12-PL1601) were administered intravenously (day 1) to treatment groups of 8 mice.
In Vivo Model	Kidney cancer CDX model
In Vitro Model	Renal cell carcinoma	SN12C cells		CVCL_1705

Experiment 1 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	Positive AXL expression (AXL+++/++; 46,000 copy number)
Method Description	In vitro cytotoxicity was determined by incubation of cell lines with serial dilutions of ADCT-601,the nonbinding control ADC,or the free PBD dimer cytotoxin SG3199 for 5-8 days at 37°C in a 5% CO2-gassed,humidified incubator. ADCT-601 selectively inhibited the growth of a panel of seven AXL-positive human cancer cell lines and two AXL-negative cell lines.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	SK-LU-1 cells		CVCL_0629
Experiment 2 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.11 nM	Positive AXL expression (AXL+++/++; 88,000 copy number)
Method Description	In vitro cytotoxicity was determined by incubation of cell lines with serial dilutions of ADCT-601,the nonbinding control ADC,or the free PBD dimer cytotoxin SG3199 for 5-8 days at 37°C in a 5% CO2-gassed,humidified incubator. ADCT-601 selectively inhibited the growth of a panel of seven AXL-positive human cancer cell lines and two AXL-negative cell lines.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 3 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.35 nM	Positive AXL expression (AXL+++/++; 79,000 copy number)
Method Description	In vitro cytotoxicity was determined by incubation of cell lines with serial dilutions of ADCT-601,the nonbinding control ADC,or the free PBD dimer cytotoxin SG3199 for 5-8 days at 37°C in a 5% CO2-gassed,humidified incubator. ADCT-601 selectively inhibited the growth of a panel of seven AXL-positive human cancer cell lines and two AXL-negative cell lines.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 4 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.47 nM	Positive AXL expression (AXL+++/++; 24,000 copy number)
Method Description	In vitro cytotoxicity was determined by incubation of cell lines with serial dilutions of ADCT-601,the nonbinding control ADC,or the free PBD dimer cytotoxin SG3199 for 5-8 days at 37°C in a 5% CO2-gassed,humidified incubator. ADCT-601 selectively inhibited the growth of a panel of seven AXL-positive human cancer cell lines and two AXL-negative cell lines.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	PANC-1 cells		CVCL_0480
Experiment 5 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.59 nM	Positive AXL expression (AXL+++/++; 23,000 copy number)
Method Description	In vitro cytotoxicity was determined by incubation of cell lines with serial dilutions of ADCT-601,the nonbinding control ADC,or the free PBD dimer cytotoxin SG3199 for 5-8 days at 37°C in a 5% CO2-gassed,humidified incubator. ADCT-601 selectively inhibited the growth of a panel of seven AXL-positive human cancer cell lines and two AXL-negative cell lines.    Click to Show/Hide
In Vitro Model	Glioblastoma	A-172 cells		CVCL_0131
Experiment 6 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.83 nM	Positive AXL expression (AXL+++/++; 79,000 copy number)
Method Description	In vitro cytotoxicity was determined by incubation of cell lines with serial dilutions of ADCT-601,the nonbinding control ADC,or the free PBD dimer cytotoxin SG3199 for 5-8 days at 37°C in a 5% CO2-gassed,humidified incubator. ADCT-601 selectively inhibited the growth of a panel of seven AXL-positive human cancer cell lines and two AXL-negative cell lines.    Click to Show/Hide
In Vitro Model	Renal cell carcinoma	SN12C cells		CVCL_1705
Experiment 7 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.20 nM	Positive AXL expression (AXL+++/++; 20,000 copy number)
Method Description	In vitro cytotoxicity was determined by incubation of cell lines with serial dilutions of ADCT-601,the nonbinding control ADC,or the free PBD dimer cytotoxin SG3199 for 5-8 days at 37°C in a 5% CO2-gassed,humidified incubator. ADCT-601 selectively inhibited the growth of a panel of seven AXL-positive human cancer cell lines and two AXL-negative cell lines.    Click to Show/Hide
In Vitro Model	Lung large cell carcinoma	NCI-H1299 cells		CVCL_0060
Experiment 8 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	9.29 nM	Positive AXL expression (AXL+++/++; 79,000 copy number)
Method Description	In vitro cytotoxicity was determined by incubation of cell lines with serial dilutions of ADCT-601,the nonbinding control ADC,or the free PBD dimer cytotoxin SG3199 for 5-8 days at 37°C in a 5% CO2-gassed,humidified incubator. ADCT-601 selectively inhibited the growth of a panel of seven AXL-positive human cancer cell lines and two AXL-negative cell lines.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620
Experiment 9 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	14.62 nM	Positive AXL expression (AXL+++/++; 36,000 copy number)
Method Description	In vitro cytotoxicity was determined by incubation of cell lines with serial dilutions of ADCT-601,the nonbinding control ADC,or the free PBD dimer cytotoxin SG3199 for 5-8 days at 37°C in a 5% CO2-gassed,humidified incubator. ADCT-601 selectively inhibited the growth of a panel of seven AXL-positive human cancer cell lines and two AXL-negative cell lines.    Click to Show/Hide
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324

Experiment 1 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 16.02% (Day 21)	Moderate BCMA expression (BCMA++)
Method Description	Mice were treated with either a single intravenous dose of ADCs at 1 mg/kg, or dosed intravenously with J6M0-mc-MMAF ADC weekly at a dose of 1 mg/kg for 3 weeks. Control mice were left untreated.
In Vivo Model	JJN-3 CDX model
In Vitro Model	Plasma cell myeloma	JJN-3 cells		CVCL_2078

Experiment 1 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 82.20% (Day 50)	Low HER2 expression (HER2+)
Method Description	The in vivo efficacy of trastuzumab-Flexmab-SG3710 was investigated after single-dose injections (0.30 mg/kg) in female athymic mice bearing NCI-N87 HER2-positive subcutaneous xenografts. NCI-N87 cells (5 x106) in 50% Matrigel were inoculated subcutaneously into 46 week-old female athymic nude mice. Five mice per group were dosed intravenously five days after their tumors reached a volume of 200 mm3.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 92.20% (Day 50)	Low HER2 expression (HER2+)
Method Description	The in vivo efficacy of trastuzumab-Flexmab-SG3710 was investigated after single-dose injections (0.6 mg/kg) in female athymic mice bearing NCI-N87 HER2-positive subcutaneous xenografts. NCI-N87 cells (5 x106) in 50% Matrigel were inoculated subcutaneously into 46 week-old female athymic nude mice. Five mice per group were dosed intravenously five days after their tumors reached a volume of 200 mm3.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 92.80% (Day 40)	Low HER2 expression (HER2+)
Method Description	The in vivo efficacy of trastuzumab-Flexmab-SG3710 and trastuzumab-C239i-SG3249 ADCs was investigated after single-dose injections (1 mg/kg) in female athymic mice bearing NCI-N87 HER2-positive subcutaneous xenografts,and tumor growth was monitored for 85 days. NCI-N87 cells (5 x106) in 50% Matrigel were inoculated subcutaneously into 46 week-old female athymic nude mice. Five mice per group were dosed intravenously five days after their tumors reached a volume of 200 mm3.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	35.50 pM	Low HER2 expression (HER2+)
Method Description	The cytotoxic effect of Trastuzumab-Flexmab-SG3710 was assessed in cell viability assays for a diverse panel of human solid tumor cell lines representing breast and gastric cancers. The potency of trastuzumab-Flexmab-SG3710 was assessed on the SKBR-3 cell line after five days of incubation.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.00% (Day 50)	Low HER2 expression (HER2+)
Method Description	The in vivo efficacy of trastuzumab-C239i-SG3249 was investigated after single-dose injections (0.30 mg/kg) in female athymic mice bearing NCI-N87 HER2-positive subcutaneous xenografts. NCI-N87 cells (5 x106) in 50% Matrigel were inoculated subcutaneously into 46 week-old female athymic nude mice. Five mice per group were dosed intravenously five days after their tumors reached a volume of 200 mm3.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.20% (Day 40)	Low HER2 expression (HER2+)
Method Description	The in vivo efficacy of trastuzumab-Flexmab-SG3710 and trastuzumab-C239i-SG3249 ADCs was investigated after single-dose injections (1 mg/kg) in female athymic mice bearing NCI-N87 HER2-positive subcutaneous xenografts,and tumor growth was monitored for 85 days. NCI-N87 cells (5 x106) in 50% Matrigel were inoculated subcutaneously into 46 week-old female athymic nude mice. Five mice per group were dosed intravenously five days after their tumors reached a volume of 200 mm3.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	14.40 pM	Low HER2 expression (HER2+)
Method Description	The cytotoxic effect of Trastuzumab-C239i-SG32490 was assessed in cell viability assays for a diverse panel of human solid tumor cell lines representing breast and gastric cancers. The potency of trastuzumab-Flexmab-SG3710 was assessed on the SKBR-3 cell line after five days of incubation.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.55% (Day 21)	High BCMA expression (BCMA+++)
Method Description	Mice were treated with either a single intravenous dose of the ADCs at 0.3 mg/kg or dosed intravenously with J6M0-mc-MMAFweekly at a dose of 0.3 mg/kg for 2 weeks.
In Vivo Model	NCI-H929 CDX model
In Vitro Model	Plasma cell myeloma	NCI-H929 cells		CVCL_1600
Experiment 2 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 95.16% (Day 21)	Moderate BCMA expression (BCMA++)
Method Description	Mice were treated with either a single intravenous dose of ADCs at 1 mg/kg, or dosed intravenously with J6M0-mc-MMAF ADC weekly at a dose of 1 mg/kg for 3 weeks. Control mice were left untreated.
In Vivo Model	JJN-3 CDX model
In Vitro Model	Plasma cell myeloma	JJN-3 cells		CVCL_2078
Experiment 3 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 96.37% (Day 32)	Moderate BCMA expression (BCMA++)
Method Description	Mice were treated with either a single intravenous dose of ADCs at 1 mg/kg, or dosed intravenously with J6M0-mc-MMAF ADC weekly at a dose of 1 mg/kg for 4 weeks. Control mice were left untreated.
In Vivo Model	MM.1S CDX model
In Vitro Model	Plasma cell myeloma	MM1.S cells		CVCL_8792

Experiment 1 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.81 nM	Moderate BCMA expression (BCMA++)
Method Description	The ability of the ADCs to kill multiple myeloma cells in vitro inthe presence of soluble BCMA (sBCMA, 0 ng/ml) as compared to the 09-SG3249 ADC was evaluated in MM.1S cells, except that tested cell lines also were treated with BCMA-containing conditioned media collected from Ad293 cells expressing human BCMA.
In Vitro Model	Plasma cell myeloma	MM1.S cells		CVCL_8792
Experiment 2 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.55 nM	Moderate BCMA expression (BCMA++)
Method Description	The ability of the ADCs to kill multiple myeloma cells in vitro inthe presence of soluble BCMA (sBCMA, 270 ng/ml) as compared to the 09-SG3249 ADC was evaluated in MM.1S cells, except that tested cell lines also were treated with BCMA-containing conditioned media collected from Ad293 cells expressing human BCMA.
In Vitro Model	Plasma cell myeloma	MM1.S cells		CVCL_8792
Experiment 3 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.79 nM	Moderate BCMA expression (BCMA++)
Method Description	The ability of the ADCs to kill multiple myeloma cells in vitro inthe presence of soluble BCMA (sBCMA, 75 ng/ml) as compared to the 09-SG3249 ADC was evaluated in MM.1S cells, except that tested cell lines also were treated with BCMA-containing conditioned media collected from Ad293 cells expressing human BCMA.
In Vitro Model	Plasma cell myeloma	MM1.S cells		CVCL_8792
Experiment 4 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	16.16 nM	Moderate BCMA expression (BCMA++)
Method Description	The ability of the ADCs to kill multiple myeloma cells in vitro inthe presence of soluble BCMA (sBCMA, 720 ng/ml) as compared to the 09-SG3249 ADC was evaluated in MM.1S cells, except that tested cell lines also were treated with BCMA-containing conditioned media collected from Ad293 cells expressing human BCMA.
In Vitro Model	Plasma cell myeloma	MM1.S cells		CVCL_8792

Experiment 1 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 95.16% (Day 21)	Moderate BCMA expression (BCMA++)
Method Description	Mice were treated with either a single intravenous dose of ADCs at 1 mg/kg, or dosed intravenously with J6M0-mc-MMAF ADC weekly at a dose of 1 mg/kg for 3 weeks. Control mice were left untreated.
In Vivo Model	JJN-3 CDX model
In Vitro Model	Plasma cell myeloma	JJN-3 cells		CVCL_2078
Experiment 2 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 96.37% (Day 32)	Moderate BCMA expression (BCMA++)
Method Description	Mice were treated with either a single intravenous dose of ADCs at 1 mg/kg, or dosed intravenously with J6M0-mc-MMAF ADC weekly at a dose of 1 mg/kg for 4 weeks. Control mice were left untreated.
In Vivo Model	MM.1S CDX model
In Vitro Model	Plasma cell myeloma	MM1.S cells		CVCL_8792
Experiment 3 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.35% (Day 21)	High BCMA expression (BCMA+++)
Method Description	Mice were treated with either a single intravenous dose of the ADCs at 0.3 mg/kg or dosed intravenously with J6M0-mc-MMAFweekly at a dose of 0.3 mg/kg for 2 weeks.
In Vivo Model	NCI-H929 CDX model
In Vitro Model	Plasma cell myeloma	NCI-H929 cells		CVCL_1600

Experiment 1 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 95.59% (Day 21)	High BCMA expression (BCMA+++)
Method Description	Mice were treated with either a single intravenous dose of the ADCs at 0.3 mg/kg or dosed intravenously with J6M0-mc-MMAFweekly at a dose of 0.3 mg/kg for 2 weeks.
In Vivo Model	NCI-H929 CDX model
In Vitro Model	Plasma cell myeloma	NCI-H929 cells		CVCL_1600

Experiment 1 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 96.37% (Day 32)	Moderate BCMA expression (BCMA++)
Method Description	Mice were treated with either a single intravenous dose of ADCs at 1 mg/kg, or dosed intravenously with J6M0-mc-MMAF ADC weekly at a dose of 1 mg/kg for 4 weeks. Control mice were left untreated.
In Vivo Model	MM.1S CDX model
In Vitro Model	Plasma cell myeloma	MM1.S cells		CVCL_8792
Experiment 2 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.73% (Day 35)	High BCMA expression (BCMA+++)
Method Description	Mice were treated with either a single intravenous dose of ADCs at 1 mg/kg, or dosed intravenously with J6M0-mc-MMAF ADC weekly at a dose of 3 mg/kg for 4 weeks. Control mice were left untreated.
In Vivo Model	MM.1R CDX model
In Vitro Model	Plasma cell myeloma	MM1.R cells		CVCL_8794

Experiment 1 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.99 nM	High BCMA expression (BCMA+++)
Method Description	Treatments were then serially diluted 1:3 in RPMI+10% FBS. 20uL of this series was added to the cells in duplicate, resulting in a 12-point dose curve of antibody-drug conjugate and media-only controls also were included. Plates were incubated at 37°C, 5% CO for 9 hours.
In Vitro Model	Plasma cell myeloma	NCI-H929 cells		CVCL_1600
Experiment 2 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	8.64 nM	High BCMA expression (BCMA+++)
Method Description	Treatments were then serially diluted 1:3 in RPMI+10% FBS. 20uL of this series was added to the cells in duplicate, resulting in a 12-point dose curve of antibody-drug conjugate and media-only controls also were included. Plates were incubated at 37°C, 5% CO for 9 hours.
In Vitro Model	Plasma cell myeloma	MM1.R cells		CVCL_8794
Experiment 3 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	14.47 nM	Moderate BCMA expression (BCMA++)
Method Description	The ability of the ADCs to kill multiple myeloma cells in vitro inthe presence of soluble BCMA (sBCMA, 0 ng/ml) as compared to the 09-SG3249 ADC was evaluated in MM.1S cells, except that tested cell lines also were treated with BCMA-containing conditioned media collected from Ad293 cells expressing human BCMA.
In Vitro Model	Plasma cell myeloma	MM1.S cells		CVCL_8792
Experiment 4 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	16.09 nM	Moderate BCMA expression (BCMA++)
Method Description	The ability of the ADCs to kill multiple myeloma cells in vitro inthe presence of soluble BCMA (sBCMA, 75 ng/ml) as compared to the 09-SG3249 ADC was evaluated in MM.1S cells, except that tested cell lines also were treated with BCMA-containing conditioned media collected from Ad293 cells expressing human BCMA.
In Vitro Model	Plasma cell myeloma	MM1.S cells		CVCL_8792
Experiment 5 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	16.80 nM	Moderate BCMA expression (BCMA++)
Method Description	Treatments were then serially diluted 1:3 in RPMI+10% FBS. 20uL of this series was added to the cells in duplicate, resulting in a 12-point dose curve of antibody-drug conjugate and media-only controls also were included. Plates were incubated at 37°C, 5% CO for 9 hours.
In Vitro Model	Plasma cell myeloma	MM1.S cells		CVCL_8792
Experiment 6 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	22.86 nM	Moderate BCMA expression (BCMA++)
Method Description	The ability of the ADCs to kill multiple myeloma cells in vitro inthe presence of soluble BCMA (sBCMA, 270 ng/ml) as compared to the 09-SG3249 ADC was evaluated in MM.1S cells, except that tested cell lines also were treated with BCMA-containing conditioned media collected from Ad293 cells expressing human BCMA.
In Vitro Model	Plasma cell myeloma	MM1.S cells		CVCL_8792
Experiment 7 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	29.12 nM	Moderate BCMA expression (BCMA++)
Method Description	The ability of the ADCs to kill multiple myeloma cells in vitro inthe presence of soluble BCMA (sBCMA, 720 ng/ml) as compared to the 09-SG3249 ADC was evaluated in MM.1S cells, except that tested cell lines also were treated with BCMA-containing conditioned media collected from Ad293 cells expressing human BCMA.
In Vitro Model	Plasma cell myeloma	MM1.S cells		CVCL_8792
Experiment 8 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	31.40 nM	Low BCMA expression (BCMA+)
Method Description	Treatments were then serially diluted 1:3 in RPMI+10% FBS. 20uL of this series was added to the cells in duplicate, resulting in a 12-point dose curve of antibody-drug conjugate and media-only controls also were included. Plates were incubated at 37°C, 5% CO for 9 hours.
In Vitro Model	Plasma cell myeloma	L-363 cells		CVCL_1357
Experiment 9 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	36.28 nM	Moderate BCMA expression (BCMA++)
Method Description	Treatments were then serially diluted 1:3 in RPMI+10% FBS. 20uL of this series was added to the cells in duplicate, resulting in a 12-point dose curve of antibody-drug conjugate and media-only controls also were included. Plates were incubated at 37°C, 5% CO for 9 hours.
In Vitro Model	Plasma cell myeloma	JJN-3 cells		CVCL_2078
Experiment 10 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	39.00 nM	Moderate BCMA expression (BCMA++)
Method Description	Treatments were then serially diluted 1:3 in RPMI+10% FBS. 20uL of this series was added to the cells in duplicate, resulting in a 12-point dose curve of antibody-drug conjugate and media-only controls also were included. Plates were incubated at 37°C, 5% CO for 9 hours.
In Vitro Model	Plasma cell myeloma	U266B1 cells		CVCL_0566
Experiment 11 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	153.00 nM	High BCMA expression (BCMA+++)
Method Description	Treatments were then serially diluted 1:3 in RPMI+10% FBS. 20uL of this series was added to the cells in duplicate, resulting in a 12-point dose curve of antibody-drug conjugate and media-only controls also were included. Plates were incubated at 37°C, 5% CO for 9 hours.
In Vitro Model	Plasma cell myeloma	EJM cells		CVCL_2030
Experiment 12 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	201.00 nM	Moderate BCMA expression (BCMA++)
Method Description	Treatments were then serially diluted 1:3 in RPMI+10% FBS. 20uL of this series was added to the cells in duplicate, resulting in a 12-point dose curve of antibody-drug conjugate and media-only controls also were included. Plates were incubated at 37°C, 5% CO for 9 hours.
In Vitro Model	Plasma cell myeloma	OPM-2 cells		CVCL_1625
Experiment 13 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500.00 nM	Negative BCMA expression (BCMA-)
Method Description	Treatments were then serially diluted 1:3 in RPMI+10% FBS. 20uL of this series was added to the cells in duplicate, resulting in a 12-point dose curve of antibody-drug conjugate and media-only controls also were included. Plates were incubated at 37°C, 5% CO for 9 hours.
In Vitro Model	EBV-related Burkitt lymphoma	Raji cells		CVCL_0511
Experiment 14 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500.00 nM	Negative BCMA expression (BCMA-)
Method Description	Treatments were then serially diluted 1:3 in RPMI+10% FBS. 20uL of this series was added to the cells in duplicate, resulting in a 12-point dose curve of antibody-drug conjugate and media-only controls also were included. Plates were incubated at 37°C, 5% CO for 9 hours.
In Vitro Model	T acute lymphoblastic leukemia	Jurkat cells		CVCL_0065

Experiment 1 Reporting the Activity Date of This ADC					[33]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 96.50% (Day 14)	Positive La/SSB expression (La/SSB +++/++)
Method Description	ChDAB4-SG3249 (3 mg/kg, the day after chemotherapy (Day 3)) induces efficient tumor cell killing in cell line-derived models of Lewis lung carcinoma cell with HER3 expression with high expression.
In Vivo Model	LL2 CDX model
In Vitro Model	Normal	LL2 cells		CVCL_C4MM

Experiment 1 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximum Growth Inhibitory Concentration (GI50)	1.74 ng/mL	Low HER2 expression (HER2+)
Method Description	The cytotoxic effect of Her-SG3249 was assessed in cell viability assays for breast cancer. The potency of Her-SG3249 was assessed on the SKBR-3 cell line. Process aggregation assessed by SEC.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximum Growth Inhibitory Concentration (GI50)	2.62 ng/mL	Low HER2 expression (HER2+)
Method Description	The cytotoxic effect of site-specific Her-SG3249 was assessed in cell viability assays for breast cancer. The potency of site-specific Her-SG3249 was assessed on the SKBR-3 cell line. Process aggregation assessed by SEC.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[34]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.13 nM	Positive CD276 expression (CD276 +++/++)
Method Description	The anti-tumor activity of these ADCs was tested in cytotoxicity assaysusing the HCC38 cell line. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Breast ductal carcinoma	HCC38 cells		CVCL_1267

Experiment 1 Reporting the Activity Date of This ADC					[35]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.31 nM	High EGFR expression (EGFR+++)
Method Description	1 x104 cells per well in a volume of 100 ul were plated in 96-well tissue culture plates. After 24 h, ADCs were added at the indicated concentrations. After 72 h, the medium was removed and the viability was determined using the CellTiter-Glo luminescent cell viability assay kit.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 2 Reporting the Activity Date of This ADC					[35]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.85 nM	High EGFR expression (EGFR+++)
Method Description	1 x104 cells per well in a volume of 100 ul were plated in 96-well tissue culture plates. After 24 h, ADCs were added at the indicated concentrations. After 72 h, the medium was removed and the viability was determined using the CellTiter-Glo luminescent cell viability assay kit.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 3 Reporting the Activity Date of This ADC					[35]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	9.07 nM	Moderate EGFR expression (EGFR++)
Method Description	1 x104 cells per well in a volume of 100 ul were plated in 96-well tissue culture plates. After 24 h, ADCs were added at the indicated concentrations. After 72 h, the medium was removed and the viability was determined using the CellTiter-Glo luminescent cell viability assay kit.
In Vitro Model	Invasive breast carcinoma of no special type	BT-20 cells		CVCL_0178
Experiment 4 Reporting the Activity Date of This ADC					[35]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100.00 nM	Negative EGFR expression (EGFR-)
Method Description	1 x104 cells per well in a volume of 100 ul were plated in 96-well tissue culture plates. After 24 h, ADCs were added at the indicated concentrations. After 72 h, the medium was removed and the viability was determined using the CellTiter-Glo luminescent cell viability assay kit.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.82 nM	Moderate BCMA expression (BCMA++)
Method Description	The ability of the ADCs to kill multiple myeloma cells in vitro inthe presence of soluble BCMA (sBCMA, 0 ng/ml) as compared to the 09-SG3249 ADC was evaluated in MM.1S cells, except that tested cell lines also were treated with BCMA-containing conditioned media collected from Ad293 cells expressing human BCMA.
In Vitro Model	Plasma cell myeloma	MM1.S cells		CVCL_8792
Experiment 2 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	12.83 nM	Moderate BCMA expression (BCMA++)
Method Description	The ability of the ADCs to kill multiple myeloma cells in vitro inthe presence of soluble BCMA (sBCMA, 75 ng/ml) as compared to the 09-SG3249 ADC was evaluated in MM.1S cells, except that tested cell lines also were treated with BCMA-containing conditioned media collected from Ad293 cells expressing human BCMA.
In Vitro Model	Plasma cell myeloma	MM1.S cells		CVCL_8792
Experiment 3 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	32.26 nM	Moderate BCMA expression (BCMA++)
Method Description	The ability of the ADCs to kill multiple myeloma cells in vitro inthe presence of soluble BCMA (sBCMA, 270 ng/ml) as compared to the 09-SG3249 ADC was evaluated in MM.1S cells, except that tested cell lines also were treated with BCMA-containing conditioned media collected from Ad293 cells expressing human BCMA.
In Vitro Model	Plasma cell myeloma	MM1.S cells		CVCL_8792
Experiment 4 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	92.92 nM	Moderate BCMA expression (BCMA++)
Method Description	The ability of the ADCs to kill multiple myeloma cells in vitro inthe presence of soluble BCMA (sBCMA, 720 ng/ml) as compared to the 09-SG3249 ADC was evaluated in MM.1S cells, except that tested cell lines also were treated with BCMA-containing conditioned media collected from Ad293 cells expressing human BCMA.
In Vitro Model	Plasma cell myeloma	MM1.S cells		CVCL_8792

Experiment 1 Reporting the Activity Date of This ADC					[36]
Efficacy Data	Objective Response Rate (ORR)	20.00% (150 ug/kg)
Patients Enrolled	Patients with HER2-positive advanced solid tumors.
Administration Dosage	Seven dose cohorts (30, 60, 120, 150, 180, 210, 240 ug/kg on day 1, iv once every 3 weeks.
Related Clinical Trial
NCT Number	NCT03125200	Phase Status	Phase 1
Clinical Description	A phase 1, open-label, dose-escalation study to evaluate the safety, tolerability, pharmacokinetics, and antitumor activity of ADCT-502 in patients with advanced solid tumors with HER2 expression.

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