Linker ID	LIN0YRUBS
Linker Name	Mal-PEG8-Val-Ala-PABC
Linker Type	Cathepsin-cleavable linker
Antibody-Linker Relation	Cleavable
Structure
	3D MOL			2D MOL
Formula	C41H65N5O15
Isosmiles	C[C@@H](C(=O)NC1=CC=C(C=C1)CO)NC(=O)[C@H](C(C)C)NC(=O)CCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)CCN2C(=O)C=CC2=O
PubChem CID	145157750
InChI	InChI=1S/C41H65N5O15/c1-31(2)39(41(53)43-32(3)40(52)44-34-6-4-33(30-47)5-7-34)45-36(49)11-14-54-16-18-56-20-22-58-24-26-60-28-29-61-27-25-59-23-21-57-19-17-55-15-12-42-35(48)10-13-46-37(50)8-9-38(46)51/h4-9,31-32,39,47H,10-30H2,1-3H3,(H,42,48)(H,43,53)(H,44,52)(H,45,49)/t32-,39-/m0/s1
InChIKey	YJYDWLGCCNOUSJ-GSSDHLSPSA-N
IUPAC Name	(2S)-2-[3-[2-[2-[2-[2-[2-[2-[2-[2-[3-(2,5-dioxopyrrol-1-yl)propanoylamino]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]propanoylamino]-N-[(2S)-1-[4-(hydroxymethyl)anilino]-1-oxopropan-2-yl]-3-methylbutanamide
Pharmaceutical Properties	Molecule Weight		868	Polar area		248
	Complexity		1280	xlogp Value		-2.1
	Heavy Count		61	Rot Bonds		37
	Hbond acc		15	Hbond Donor		5

Experiment 1 Reporting the Activity Date of This ADC					[1]
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	Clinical 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					[2]
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	Clinical 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					[3]
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	Clinical 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					[4]
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	Clinical 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					[5]
Efficacy Data	Complete Remission (CR)	46.16%

Experiment 1 Reporting the Activity Date of This ADC					[6]
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	Clinical 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					[10]
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	Clinical 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					[11]
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	Clinical 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					[12]
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					[12]
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					[12]
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					[12]
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					[12]
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					[12]
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					[12]
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					[12]
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					[12]
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					[12]
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					[12]
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					[12]
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					[12]
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					[12]
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					[12]
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					[12]
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					[12]
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					[12]
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					[7]
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	Clinical 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					[8]
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	Clinical 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					[9]
Related Clinical Trial
NCT Number	NCT03698552	Clinical 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					[13]
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	Clinical 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					[18]
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					[18]
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					[18]
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					[19]
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					[19]
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					[19]
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					[14]
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	Clinical 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					[17]
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					[17]
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					[17]
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					[17]
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					[17]
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					[17]
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					[17]
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					[15]
Related Clinical Trial
NCT Number	NCT03859752	Clinical 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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[16]
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					[20]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 91.30% (Day 49)	Positive 5T4 expression (5T4+++/++)
Method Description	A single dose of 5T4-PBD was administrated at 0.1 and 0.3 mg/kg intravenously into nude mice.
In Vivo Model	MDA-MB-361 CDX model
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620

Experiment 1 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 40.50% (Day 50)	Negative expression (HER2-)
Method Description	The antitumor activity of trastuzumab-C239i-SG3400 was evaluated in the low-HER2-expressing,trastuzumab-resistant human breast cancer model JIMT-1 and the HER2-positive human gastric cancer xenograft model NCI-N87. A sub-curative single dose of ADC of 1 mg/kg was chosen for both ADCs to observe any difference in activity.
In Vivo Model	Breast cancer CDX model
In Vitro Model	Breast cancer	Breast cancer cells		Homo sapiens
Experiment 2 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 48.00% (Day 50)	Low HER2 expression (HER2+)
Method Description	The antitumor activity of trastuzumab-C239i-SG3400 was evaluated in the low-HER2-expressing,trastuzumab-resistant human breast cancer model JIMT-1 and the HER2-positive human gastric cancer xenograft model NCI-N87. A sub-curative single dose of ADC of 1 mg/kg was chosen for both ADCs to observe any difference in activity.
In Vivo Model	Gastric cancer CDX model
In Vitro Model	Gastric cancer	Gastric cancer cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	10.70 ng/mL	Low HER2 expression (HER2+)
Method Description	The cytotoxicity of the HER2-targeting ADCs was examined in vitro. Every cell line after treatment for 144h with doses ranging from 0.01 to 10, 000 ng/mL. Results are meanSEM of three replicate experiments.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	20.90 ng/mL	Low HER2 expression (HER2+)
Method Description	The cytotoxicity of the HER2-targeting ADCs was examined in vitro. Every cell line after treatment for 144h with doses ranging from 0.01 to 10, 000 ng/mL. Results are meanSEM of three replicate experiments.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 3 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	23.30 ng/mL	Low HER2 expression (HER2+)
Method Description	The cytotoxicity of the HER2-targeting ADCs was examined in vitro. Every cell line after treatment for 144h with doses ranging from 0.01 to 10, 000 ng/mL. Results are meanSEM of three replicate experiments.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 4 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 50.00 ng/mL	Negative expression (HER2-)
Method Description	The cytotoxicity of the HER2-targeting ADCs was examined in vitro. Every cell line after treatment for 144h with doses ranging from 0.01 to 10, 000 ng/mL. Results are meanSEM of three replicate experiments.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 5 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 250.00 ng/mL	Negative expression (HER2-)
Method Description	The cytotoxicity of the HER2-targeting ADCs was examined in vitro. Every cell line after treatment for 144h with doses ranging from 0.01 to 10, 000 ng/mL. Results are meanSEM of three replicate experiments.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 62.20% (Day 50)	Low HER2 expression (HER2+)
Method Description	The antitumor activity of trastuzumab-C239i-SG3600 was evaluated in the low-HER2-expressing,trastuzumab-resistant human breast cancer model JIMT-1 and the HER2-positive human gastric cancer xenograft model NCI-N87. A sub-curative single dose of ADC of 1 mg/kg was chosen for both ADCs to observe any difference in activity.
In Vivo Model	Gastric cancer CDX model
In Vitro Model	Gastric cancer	Gastric cancer cells		Homo sapiens
Experiment 2 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 65.10% (Day 50)	Negative expression (HER2-)
Method Description	The antitumor activity of trastuzumab-C239i-SG3600 was evaluated in the low-HER2-expressing,trastuzumab-resistant human breast cancer model JIMT-1 and the HER2-positive human gastric cancer xenograft model NCI-N87. A sub-curative single dose of ADC of 1 mg/kg was chosen for both ADCs to observe any difference in activity.
In Vivo Model	Breast cancer CDX model
In Vitro Model	Breast cancer	Breast cancer cells		Homo sapiens
Experiment 3 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 50)	Low HER2 expression (HER2+)
Method Description	The antitumor activity of trastuzumab-C239i-SG3600 was evaluated in the low-HER2-expressing,trastuzumab-resistant human breast cancer model JIMT-1 and the HER2-positive human gastric cancer xenograft model NCI-N87. A sub-curative single dose of ADC of 3 mg/kg was chosen for both ADCs to observe any difference in activity.
In Vivo Model	Gastric cancer CDX model
In Vitro Model	Gastric cancer	Gastric cancer cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	16.10 ng/mL	Low HER2 expression (HER2+)
Method Description	The cytotoxicity of the HER2-targeting ADCs was examined in vitro. Every cell line after treatment for 144h with doses ranging from 0.01 to 10, 000 ng/mL. Results are meanSEM of three replicate experiments.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	24.10 ng/mL	Low HER2 expression (HER2+)
Method Description	The cytotoxicity of the HER2-targeting ADCs was examined in vitro. Every cell line after treatment for 144h with doses ranging from 0.01 to 10, 000 ng/mL. Results are meanSEM of three replicate experiments.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 3 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	33.90 ng/mL	Low HER2 expression (HER2+)
Method Description	The cytotoxicity of the HER2-targeting ADCs was examined in vitro. Every cell line after treatment for 144h with doses ranging from 0.01 to 10, 000 ng/mL. Results are meanSEM of three replicate experiments.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 4 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10.00 ug/mL	Negative expression (HER2-)
Method Description	The cytotoxicity of the HER2-targeting ADCs was examined in vitro. Every cell line after treatment for 144h with doses ranging from 0.01 to 10, 000 ng/mL. Results are meanSEM of three replicate experiments.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 5 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10.00 ug/mL	Negative expression (HER2-)
Method Description	The cytotoxicity of the HER2-targeting ADCs was examined in vitro. Every cell line after treatment for 144h with doses ranging from 0.01 to 10, 000 ng/mL. Results are meanSEM of three replicate experiments.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[22]
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					[22]
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					[22]
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					[22]
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					[22]
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					[22]
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					[22]
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					[23]
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					[24]
Efficacy Data	Maximum inhibition efficiency (MIE)	41.50 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 2 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Maximum inhibition efficiency (MIE)	46.00 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 3 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	19.70 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 4 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.15 nM	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 1 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Maximum inhibition efficiency (MIE)	49.00 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	Lung adenocarcinoma	NCI-H1373 cells		CVCL_1465
Experiment 2 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Maximum inhibition efficiency (MIE)	61.50 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 3 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	11.10 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 4 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	91.00 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 1 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Maximum inhibition efficiency (MIE)	56.00 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 2 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Maximum inhibition efficiency (MIE)	77.50 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 3 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	24.40 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 4 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	31.30 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 1 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Maximum inhibition efficiency (MIE)	66.00 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	Lung adenocarcinoma	NCI-H1373 cells		CVCL_1465
Experiment 2 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Maximum inhibition efficiency (MIE)	76.50 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 3 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	27.50 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 4 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.41 nM	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 1 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Maximum inhibition efficiency (MIE)	76.80 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 2 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Maximum inhibition efficiency (MIE)	78.70 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 3 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	21.80 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 4 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.15 nM	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 1 Reporting the Activity Date of This ADC					[25]
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					[25]
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					[26]
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					[26]
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					[26]
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					[26]
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					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	235.60 nM	High HER2 expression (HER2+++)
Method Description	SKOV-3, BT474 HerDR, MDA-MB-231 and MCF-7 cells were cultured under various concentrations of Mil40, SN-38 and ADCs for 10days, 9days, 6days, and 6days, respectively. Cytotoxicity assays were established using the CellTiter-Go assay kit (CTG).
In Vitro Model	Invasive breast carcinoma	BT474 HerDR cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	283.80 nM	High HER2 expression (HER2+++)
Method Description	SKOV-3, BT474 HerDR, MDA-MB-231 and MCF-7 cells were cultured under various concentrations of Mil40, SN-38 and ADCs for 10days, 9days, 6days, and 6days, respectively. Cytotoxicity assays were established using the CellTiter-Go assay kit (CTG).
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 3 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000.00 nM	Negative HER2 expression (HER2-)
Method Description	SKOV-3, BT474 HerDR, MDA-MB-231 and MCF-7 cells were cultured under various concentrations of Mil40, SN-38 and ADCs for 10days, 9days, 6days, and 6days, respectively. Cytotoxicity assays were established using the CellTiter-Go assay kit (CTG).
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 4 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000.00 nM	Negative HER2 expression (HER2-)
Method Description	SKOV-3, BT474 HerDR, MDA-MB-231 and MCF-7 cells were cultured under various concentrations of Mil40, SN-38 and ADCs for 10days, 9days, 6days, and 6days, respectively. Cytotoxicity assays were established using the CellTiter-Go assay kit (CTG).
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.60 ng/mL	Low HER2 expression (HER2+)
Method Description	The cytotoxicity of the HER2-targeting ADCs was examined in vitro. Every cell line after treatment for 144h with doses ranging from 0.01 to 10, 000 ng/mL. Results are meanSEM of three replicate experiments.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 2 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.37 ng/mL	Low HER2 expression (HER2+)
Method Description	The cytotoxicity of the HER2-targeting ADCs was examined in vitro. Every cell line after treatment for 144h with doses ranging from 0.01 to 10, 000 ng/mL. Results are meanSEM of three replicate experiments.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 3 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.90 ng/mL	Low HER2 expression (HER2+)
Method Description	The cytotoxicity of the HER2-targeting ADCs was examined in vitro. Every cell line after treatment for 144h with doses ranging from 0.01 to 10, 000 ng/mL. Results are meanSEM of three replicate experiments.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	36.10 ng/mL	Negative expression (HER2-)
Method Description	The cytotoxicity of the HER2-targeting ADCs was examined in vitro. Every cell line after treatment for 144h with doses ranging from 0.01 to 10, 000 ng/mL. Results are meanSEM of three replicate experiments.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10.00 ug/mL	Negative expression (HER2-)
Method Description	The cytotoxicity of the HER2-targeting ADCs was examined in vitro. Every cell line after treatment for 144h with doses ranging from 0.01 to 10, 000 ng/mL. Results are meanSEM of three replicate experiments.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[28]
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	Clinical 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.

Ref 1	Loncastuximab tesirine in relapsed or refractory diffuse large B-cell lymphoma (LOTIS-2): a multicentre, open-label, single-arm, phase 2 trial. Lancet Oncol. 2021 Jun;22(6):790-800.
Ref 2	A Phase I Study of ADCT-402 (Loncastuximab Tesirine), a Novel Pyrrolobenzodiazepine-Based Antibody-Drug Conjugate, in Relapsed/Refractory B-Cell Non-Hodgkin Lymphoma. Clin Cancer Res. 2019 Dec 1;25(23):6986-6994.
Ref 3	Final results of a phase 1 study of loncastuximab tesirine in relapsed/refractory B-cell non-Hodgkin lymphoma. Blood. 2021 May 13;137(19):2634-2645.
Ref 4	Loncastuximab tesirine, an anti-CD19 antibody-drug conjugate, in relapsed/refractory B-cell acute lymphoblastic leukemia. Blood Adv. 2020 Feb 11;4(3):449-457.
Ref 5	The AntiCD19 Antibody Drug Immunoconjugate Loncastuximab Achieves Responses in DLBCL Relapsing After AntiCD19 CAR-T Cell Therapy. Clin Lymphoma Myeloma Leuk. 2022 May;22(5):e335-e339.
Ref 6	Camidanlumab tesirine in patients with relapsed or refractory lymphoma: a phase 1, open-label, multicentre, dose-escalation, dose-expansion study. Lancet Haematol. 2021 Jun;8(6):e433-e445.
Ref 7	Adct-602, a CD22 Targeting Antibody Drug Conjugate Bound to PBD Toxin in Adult Patients with Relapsed or Refractory B-Cell Acute Lymphoblastic Leukemia: A Phase 1 Trial. Blood (2022) 140 (Supplement 1): 521522.
Ref 8	A Phase 1 Trial of Adct-602, a CD22 Targeting Antibody Drug Conjugate Bound to PBD Toxin in Adult Patients with Relapsed or Refractory CD22+ B-Cell Acute Lymphoblastic Leukemia. Blood (2021) 138 (Supplement 1): 1237.
Ref 9	A Phase I/II 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, NCT03698552
Ref 10	Camidanlumab tesirine, an antibody-drug conjugate, in relapsed/refractory CD25-positive acute myeloid leukemia or acute lymphoblastic leukemia: A phase I study. Leuk Res. 2020 Aug;95:106385.
Ref 11	Exposure-response analysis of Camidanlumab tesirine in patients with relapsed or refractory classical Hodgkin lymphoma and non-Hodgkin lymphoma. Cancer Chemother Pharmacol. 2023 Jan;91(1):1-12.
Ref 12	ADCT-301, a Pyrrolobenzodiazepine (PBD) Dimer-Containing Antibody-Drug Conjugate (ADC) Targeting CD25-Expressing Hematological Malignancies. Mol Cancer Ther. 2016 Nov;15(11):2709-2721.
Ref 13	Phase 1, First-in-Human Study of MEDI2228, a BCMA-Targeted ADC in Patients with Relapsed/Refractory Multiple Myeloma. Blood (2020) 136 (Supplement 1): 2627.
Ref 14	Phase I Study of MEDI3726: A Prostate-Specific Membrane Antigen-Targeted Antibody-Drug Conjugate, in Patients with mCRPC after Failure of Abiraterone or Enzalutamide. Clin Cancer Res. 2021 Jul 1;27(13):3602-3609.
Ref 15	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
Ref 16	TR1801-ADC: a highly potent cMet antibody-drug conjugate with high activity in patient-derived xenograft models of solid tumors. Mol Oncol. 2020 Jan;14(1):54-68.
Ref 17	CMB-401
Ref 18	BCMA-Specific ADC MEDI2228 and Daratumumab Induce Synergistic Myeloma Cytotoxicity via IFN-Driven Immune Responses and Enhanced CD38 Expression. Clin Cancer Res. 2021 Oct 1;27(19):5376-5388.
Ref 19	A novel BCMA PBD-ADC with ATM/ATR/WEE1 inhibitors or bortezomib induce synergistic lethality in multiple myeloma. Leukemia. 2020 Aug;34(8):2150-2162.
Ref 20	Improved Therapeutic Window in BRCA-mutant Tumors with Antibody-linked Pyrrolobenzodiazepine Dimers with and without PARP Inhibition. Mol Cancer Ther. 2019 Jan;18(1):89-99. doi: 10.1158/1535-7163.MCT-18-0314. Epub 2018 Oct 23.
Ref 21	Synthesis and evaluation of pyrrolobenzodiazepine dimer antibody-drug conjugates with dual -glucuronide and dipeptide triggers. Eur J Med Chem. 2019 Oct 1;179:591-607.
Ref 22	Design and characterization of homogenous antibody-drug conjugates with a drug-to-antibody ratio of one prepared using an engineered antibody and a dual-maleimide pyrrolobenzodiazepine dimer. MAbs. 2019 Apr;11(3):500-515.
Ref 23	Tumour-associated macrophages process drug and radio-conjugates of the dead tumour cell-targeting APOMAB antibody. J Control Release. 2020 Nov 10;327:779-787. doi: 10.1016/j.jconrel.2020.09.027.
Ref 24	TR1801-ADC: a highly potent cMet antibody-drug conjugate with high activity in patient-derived xenograft models of solid tumors. Mol Oncol. 2020 Jan;14(1):54-68. doi: 10.1002/1878-0261.12600. Epub 2019 Dec 3.
Ref 25	Design and Synthesis of Tesirine, a Clinical Antibody-Drug Conjugate Pyrrolobenzodiazepine Dimer Payload. ACS Med Chem Lett. 2016 May 24;7(11):983-987.
Ref 26	Antibody drug conjugates, targeting cancer-expressed EGFR, exhibit potent and specific antitumor activity. Biomed Pharmacother. 2023 Jan;157:114047.
Ref 27	Synthesis and evaluation of highly releasable and structurally stable antibody-SN-38-conjugates. Drug Deliv. 2021 Dec;28(1):2603-2617.
Ref 28	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