Payload Information

General Information of This Payload

Payload ID	PAY0AKDAM
Name	SGD-1882
Synonyms	SGD-1882 Click to Show/Hide
Target	Human deoxyribonucleic acid (hDNA)			Target Info
Structure
Structure	3D MOL		2D MOL
Formula	C42H39N5O7
Isosmiles	COc1ccc(C2=CN3C(=O)c4cc(OC)c(OCCCOc5cc6c(cc5OC)C(=O)N5C=C(c7ccc(N)cc7)CC5C=N6)cc4N=CC3C2)cc1
InChI	InChI=1S/C42H39N5O7/c1-50-32-11-7-26(8-12-32)28-16-31-22-45-36-20-40(38(52-3)18-34(36)42(49)47(31)24-28)54-14-4-13-53-39-19-35-33(17-37(39)51-2)41(48)46-23-27(15-30(46)21-44-35)25-5-9-29(43)10-6-25/h5-12,17-24,30-31H,4,13-16,43H2,1-3H3
InChIKey	OMRPLUKQNWNZAV-UHFFFAOYSA-N
Pharmaceutical Properties	Molecule Weight	725.802	Polar area	137.51
	Complexity	54	xlogp Value	7.0855
	Heavy Count	54	Rot Bonds	11
	Hbond acc	10	Hbond Donor	1

Each Antibody-drug Conjugate Related to This Payload

Full Information of The Activity Data of The ADC(s) Related to This Payload

Vadastuximab talirine [Phase 3 (discontinued)]

ADC Info

Identified from the Human Clinical Data

Click To Hide/Show 12 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC				[1]
Patients Enrolled	Eligibility required untreated MDS (WHO 2008) patients ≥18 years with ECOG ≤2 and adequate organ function, excluding prior lenalidomide/HMA treatment, active secondary malignancies (except hormonal therapies), or candidates for immediate stem cell transplant.
Administration Dosage	Intravenous (IV) push every 4 weeks
*Related Clinical Trial*
NCT Number	NCT02706899	Phase Status	PHASE1\|\|\|PHASE2
Clinical Description	A Phase 1/2 Study of Vadastuximab Talirine (SGN-CD33A) in Combination With Azacitidine in Patients With Previously Untreated International Prognostic Scoring System (IPSS) Intermediate-2 or High Risk Myelodysplastic Syndrome (MDS)
Primary Endpoint	The phase 1 study evaluating vadastuximab talirine was terminated before establishing a recommended phase 2 dose, with only dose delays/reductions reported, while phase 2 efficacy endpoints (ORR, CR, HI, DOR, PFS, AML transformation, OS) were not assessed due to study discontinuation.
Other Endpoint	Safety analysis captured adverse events and lab abnormalities over 1 year, though all planned phase 2 efficacy comparisons per IWG 2006 criteria (including CR rate, hematologic improvement, and survival outcomes) remained unevaluated following early trial termination.
Experiment 2 Reporting the Activity Date of This ADC				[2]
Patients Enrolled	Eligible patients had untreated intermediate/adverse-risk AML (WHO-classified, excluding APL/favorable karyotypes) suitable for HMA therapy, while excluding prior MDS treatment recipients, transplant candidates, and those with myeloproliferative neoplasm histories.
Administration Dosage	33A, 10 mcg/kg, every 4 weeks via intravenous (IV) push
*Related Clinical Trial*
NCT Number	NCT02785900	Phase Status	PHASE3
Clinical Description	A Randomized, Double-blind Phase 3 Study of Vadastuximab Talirine (SGN-CD33A) Versus Placebo in Combination With Azacitidine or Decitabine in the Treatment of Older Patients With Newly Diagnosed Acute Myeloid Leukemia (AML)
Primary Endpoint	The study evaluated overall survival (1.5 years) and composite complete remission (CRc) rate per Cheson 2003 criteria, while assessing MRD-negative CRc status and time to CR/CRi within the same timeframe.
Other Endpoint	Secondary endpoints included duration of remission (9.5 months), event-free survival (11.24 months), leukemia-free survival (9.49 months), safety profile (TEAEs, grade ≥3 lab abnormalities over 1.5 years), and 30-/60-day mortality rates, with censoring rules applied for patients receiving subsequent therapies.
Experiment 3 Reporting the Activity Date of This ADC				[3]
Patients Enrolled	Eligible participants had CD33+ AML with ECOG 0-1, adequate organ function, and either relapsed after ≥12-week remission or were untreated with ≥20% blasts, excluding recent transplant recipients (except designated cohort) or those receiving recent antileukemic therapy.
Administration Dosage	Given intravenously on Day 1 or Days 1 and 4 every 3 weeks (SGN-CD33A Monotherapy) or given intravenously on the final HMA dosing day every 4 weeks (SGN-CD33A+HMA)
*Related Clinical Trial*
NCT Number	NCT01902329	Phase Status	PHASE1
Clinical Description	A Phase 1 Trial of SGN-CD33A in Patients With CD33-positive Acute Myeloid Leukemia
Primary Endpoint	The study monitored adverse events and laboratory abnormalities through 1 month post-treatment, while evaluating pharmacokinetics (SGN-CD33A blood concentrations for 3 weeks) and immunogenicity (antitherapeutic antibody incidence).
Other Endpoint	Efficacy assessments included complete remission rate (3 months), duration of response (3 years), relapse-free survival (3 years), and overall survival (3 years) in CD33-positive AML patients.
Experiment 4 Reporting the Activity Date of This ADC				[4]
Patients Enrolled	The trial enrolled AML patients (excluding APL) with ECOG 0-1 and adequate organ function, stratifying by treatment phase (induction/consolidation/maintenance), while excluding those with prior MDS/MPN therapy or cardiopulmonary dysfunction in dose-escalation cohorts.
Administration Dosage	7+3 (Standard dose cytarabine for induction and daunorubicin) + SGN-CD33A Drug: SGN-CD33A, Given intravenously Day 1 or Days 1 and 4 of each cycle
*Related Clinical Trial*
NCT Number	NCT02326584	Phase Status	PHASE1
Clinical Description	A Phase 1b Dose-escalation Study of SGN-CD33A in Combination With Standard-of-care for Patients With Newly Diagnosed Acute Myeloid Leukemia
Primary Endpoint	Safety assessments included adverse events, laboratory abnormalities, and dose-limiting toxicities monitored through 1 month post-treatment, establishing the preliminary safety profile of SGN-CD33A in AML patients.
Other Endpoint	Efficacy outcomes measured CR rate post-induction, leukemia-free survival, and overall survival (up to 3 years), while pharmacokinetic parameters (drug concentrations, ATA incidence) and MRD clearance rates were tracked longitudinally throughout the study duration.
Experiment 5 Reporting the Activity Date of This ADC				[5]
Patients Enrolled	Inclusion criteria: Adults ≥18 with isolated distal femur fractures requiring LISS plating, compliant with 1-year MGH follow-ups. Exclusion: Life expectancy <1 year, pre-injury non-ambulatory status, pregnancy, non-LISS implants, bone disorders, neoplasm-related fractures, severe open fractures with vascular damage, or inability to attend follow-ups. Click to Show/Hide
*Related Clinical Trial*
NCT Number	NCT01593176	Phase Status	N.A.
Clinical Description	Radiostereometric Analysis of Fracture Healing in Distal Femur Fractures
Primary Endpoint	The study evaluates inter-fragmentary motion changes in distal femoral fractures using radiostereometric analysis at postoperative intervals (2 weeks, 6 weeks, 3/6/12 months) to assess healing dynamics.
Experiment 6 Reporting the Activity Date of This ADC				[6]
Efficacy Data	Incomplete Count Recovery (CRi)	26%
Patients Enrolled	Older patients with newly diagnosed acute myeloid leukemia (AML).
Administration Dosage	33A, iv, 10 mcg/kg, every 4 weeks plus azacitidine 75 mg/m², SC or IV x 7 days, every 4 weeks or decitabine 20 mg/m², iv x 5 days, every 4 weeks; placebo plus plus azacitidine 75 mg/m², SC or IV x 7 days, every 4 weeks or decitabine 20 mg/m², iv x 5 days, every 4 weeks.
*Related Clinical Trial*
NCT Number	NCT02326584	Phase Status	Phase 1
Clinical Description	A phase 1b dose-escalation study of SGN-CD33A in combination with standard-of-care for patients with newly diagnosed acute myeloid leukemia.
Experiment 7 Reporting the Activity Date of This ADC				[7]
Efficacy Data	Complete Remission (CR)	66.70%
Patients Enrolled	Patients With Relapsed or Refractory AmL.
Administration Dosage	Post-allo after stem cell transplant in Day 1 of each cycle; Pre-allo in Day 1 of each cycle plus melphalan 30 mg/m²/day iv and fludarabine 140 mg/m² iv before stem cell transplant.
*Related Clinical Trial*
NCT Number	NCT02785900	Phase Status	Phase 3
Clinical Description	A randomized, double-blind phase 3 study of vadastuximab talirine (SGN-CD33A) versus placebo in combination with azacitidine or decitabine in the treatment of older patients with newly diagnosed acute myeloid leukemia (AML).
Experiment 8 Reporting the Activity Date of This ADC				[8]
Efficacy Data	Complete Remission (CR)	11.00 12.00 22.00 23.00 %
Patients Enrolled	CD33-positive AmL (any level of CD33 expression as detected by local flow cytometric assessment) and had either newly diagnosed AmL (declining intensive induction/consolidation chemotherapy) or AmL relapsed after a minimum remission duration of 12 weeks after intensive induction/consolidation.
Administration Dosage	Slow IV push on day 1 (5-60 ug/kg) or on days 1 and 4 (20 ug/kg) of 21-day cycles.
*Related Clinical Trial*
NCT Number	NCT01902329	Phase Status	Phase 1
Clinical Description	A phase 1 trial of SGN-CD33A in patients with CD33-positive acute myeloid leukemia.
Primary Endpoint	The recommended monotherapy dose is 4.00 mg/kg.
Other Endpoint	The complete remission rate (CRc) among the 69 patients in the dose-finding cohorts, was 19.00% (6.00% CR + 13.00% CRi, 95% confidence interval [CI], 10.40-30.10).
Experiment 9 Reporting the Activity Date of This ADC				[6]
Efficacy Data	Complete Remission (CR)	30.00 26.00 %
Patients Enrolled	Older patients with newly diagnosed acute myeloid leukemia (AML).
Administration Dosage	33A, iv, 10 mcg/kg, every 4 weeks plus azacitidine 75 mg/m², SC or IV x 7 days, every 4 weeks or decitabine 20 mg/m², iv x 5 days, every 4 weeks; placebo plus plus azacitidine 75 mg/m², SC or IV x 7 days, every 4 weeks or decitabine 20 mg/m², iv x 5 days, every 4 weeks.
*Related Clinical Trial*
NCT Number	NCT02326584	Phase Status	Phase 1
Clinical Description	A phase 1b dose-escalation study of SGN-CD33A in combination with standard-of-care for patients with newly diagnosed acute myeloid leukemia.
Experiment 10 Reporting the Activity Date of This ADC				[9]
Efficacy Data	Complete Remission (CR)	43.00 42.00 34.00 80.00 50.00 39.00 %
Patients Enrolled	New diagnosis of CD33-expressing AmL, they could not have received prior therapy with HMAs; however, prior low-intensity treatment, such as hydroxyurea for cytoreduction or other low-intensity therapies for preceding myelodysplastic syndrome (MDS), an Eastern Cooperative Oncology Group (ECOG) performance status 0 or 1, with adequate baseline renal, hepatic, and pulmonary function. Click to Show/Hide
Administration Dosage	Azacitidine (75 mg/m² subcutaneous/intravenous 7 days) or decitabine (20 mg/m² intravenous 5 days) was administered per institutional standard. On the final day of HMA administration (day 7 of azacitidine treatment and day 5 of decitabine treatment), vadastuximab talirine (10 ug/kg) was administered via slow intravenous push (1-2 mL/min), after infusion of the HMA, as 28-day cycles for up to 4 cycles of treatment. Click to Show/Hide
*Related Clinical Trial*
NCT Number	NCT01902329	Phase Status	Phase 1
Clinical Description	A phase 1 trial of SGN-CD33A in patients with CD33-positive acute myeloid leukemia.
Primary Endpoint	The 30- and 60-day mortality rates were 2% and 8%, respectively. No DLTs or infusion-related reactions were observed in the combination cohort of this study.
Other Endpoint	CR and CRi, was 70.00% (43% CR + 26% CRi, 95% CI, 55.70-81.70). Median RFS was 7.70 months (95% CI, 4.90-15.40) with 11.30 months (95% CI, 8.80-13.20) median OS.
Experiment 11 Reporting the Activity Date of This ADC				[10]
Patients Enrolled	Patients with operable HER2-positive primary breast cancer.
Administration Dosage	Anthracycline then Trastuzumab Emtansine and Pertuzumab ; Anthracycline then Trastuzumab, Pertuzumab, and Taxane.
*Related Clinical Trial*
NCT Number	NCT02614560	Phase Status	Phase 1/2
Clinical Description	A phase 1/2 study of vadastuximab talirine administered in sequence with allogeneic hematopoietic stem cell transplant in patients with relapsed or refractory acute myeloid leukemia (AML).
Experiment 12 Reporting the Activity Date of This ADC				[11]
Patients Enrolled	Patients With acute myeloid leukemia (AML).
Administration Dosage	SGN-CD33A iv in Day 1 or Days 1 and 4 of each cycle; High dose cytarabine + SGN-CD33A (28-day cycles); Standard dose cytarabine and daunorubicin + SGN-CD33A; standard dose cytarabine and daunorubicin + SGN-CD33A and High dose cytarabine + SGN-CD33A.
*Related Clinical Trial*
NCT Number	NCT01902329	Phase Status	Phase 1
Clinical Description	A phase 1 trial of SGN-CD33A in patients with CD33-positive acute myeloid leukemia.

Discovered Using Cell Line-derived Xenograft Model

Click To Hide/Show 8 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 0%	High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was compared with control ADC against various human cancer cell lines in vivo. The cells were treated with 100mcg/kg.
In Vitro Model	Erythroleukemia	HEL 92.1.7 cells (Multidrug resistance)		CVCL_2481
Experiment 2 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 29.44%	High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was compared with control ADC against various human cancer cell lines in vivo. The cells were treated with 30mcg/kg.
In Vitro Model	Adult acute myeloid leukemia	HL-60 cells		CVCL_0002
Experiment 3 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 47.77%	High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was compared with control ADC against various human cancer cell lines in vivo. The cells were treated with 300mcg/kg.
In Vitro Model	Erythroleukemia	HEL 92.1.7 cells (Multidrug resistance)		CVCL_2481
Experiment 4 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 78.95%	Negative CD33 expression (CD33-)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was compared with control ADC against various human cancer cell lines in vivo. The cells were treated with 100mcg/kg.
In Vitro Model	Anaplastic thyroid cancer	TF1-alpha cells (Multidrug resistance)		Homo sapiens
Experiment 5 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.41%	High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was compared with control ADC against various human cancer cell lines in vivo. The cells were treated with 1000mcg/kg.
In Vitro Model	Erythroleukemia	HEL 92.1.7 cells (Multidrug resistance)		CVCL_2481
Experiment 6 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.53%	Negative CD33 expression (CD33-)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was compared with control ADC against various human cancer cell lines in vivo. The cells were treated with 300mcg/kg.
In Vitro Model	Anaplastic thyroid cancer	TF1-alpha cells (Multidrug resistance)		Homo sapiens
Experiment 7 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.99%	Negative CD33 expression (CD33-)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was compared with control ADC against various human cancer cell lines in vivo. The cells were treated with 300mcg/kg.
In Vitro Model	Anaplastic thyroid cancer	TF1-alpha cells (Multidrug resistance)		Homo sapiens
Experiment 8 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.99%	High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was compared with control ADC against various human cancer cell lines in vivo. The cells were treated with 100mcg/kg.
In Vitro Model	Adult acute myeloid leukemia	HL-60 cells		CVCL_0002

Revealed Based on the Cell Line Data

Click To Hide/Show 33 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 ng/mL	Moderate CD33 expression (CD33++; CD33 MFI=3,919)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model	Acute myeloid leukemia	Acute myeloid leukemia cells #SG019		Homo sapiens
Experiment 2 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 ng/mL	Moderate CD33 expression (CD33++; 6,000 CD33 receptor copy number)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Childhood acute monocytic leukemia	MV4-11 cells		CVCL_0064
Experiment 3 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.2 ng/mL	High CD33 expression (CD33+++; CD33 MFI=11,850)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model	Acute myeloid leukemia	Acute myeloid leukemia cells #SG015		Homo sapiens
Experiment 4 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.2 ng/mL	High CD33 expression (CD33+++; CD33 MFI=10,762)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model	Acute myeloid leukemia	Acute myeloid leukemia cells #SG018		Homo sapiens
Experiment 5 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.2 ng/mL	High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model	Acute myeloid leukemia	Acute myeloid leukemia cells #SG023		Homo sapiens
Experiment 6 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.2 ng/mL	Moderate CD33 expression (CD33++; CD33 MFI=1,355)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model	Acute myeloid leukemia	Acute myeloid leukemia cells #SG014		Homo sapiens
Experiment 7 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.2 ng/mL	High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model	Acute myeloid leukemia	Acute myeloid leukemia cells #SG022		Homo sapiens
Experiment 8 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.4 ng/mL	Low CD33 expression (CD33+; CD33 MFI=107)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model	Acute myeloid leukemia	Acute myeloid leukemia cells #SG003		Homo sapiens
Experiment 9 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.9 ng/mL	Moderate CD33 expression (CD33++; CD33 MFI=5,817)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model	Acute myeloid leukemia	Acute myeloid leukemia cells #SG002		Homo sapiens
Experiment 10 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1 ng/mL	High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Adult acute myeloid leukemia	HL-60 cells		CVCL_0002
Experiment 11 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3 ng/mL	High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Adult acute myeloid leukemia	KG-1 cells		CVCL_0374
Experiment 12 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5 ng/mL	Negative CD33 expression (CD33-; CD33 MFI=20)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model	Acute myeloid leukemia	Acute myeloid leukemia cells #SG017		Homo sapiens
Experiment 13 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6 ng/mL	Negative CD33 expression (CD33-; CD33 MFI=49)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model	Acute myeloid leukemia	Acute myeloid leukemia cells #SG001		Homo sapiens
Experiment 14 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6 ng/mL	High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Acute myeloid leukemia	SH-1 cells		CVCL_2191
Experiment 15 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7 ng/mL	High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Childhood acute monocytic leukemia	THP-1 cells		CVCL_0006
Experiment 16 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7 ng/mL	High CD33 expression (CD33+++; CD33 MFI=23,223)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Erythroleukemia	HEL 92.1.7 cells		CVCL_2481
Experiment 17 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 7.5 ng/mL	High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Acute myeloid leukemia	SIG-M5 cells		CVCL_1694
Experiment 18 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	11 ng/mL	Low CD33 expression (CD33+; CD33 MFI=216)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model	Acute myeloid leukemia	Acute myeloid leukemia cells #SG013		Homo sapiens
Experiment 19 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	11 ng/mL	Moderate CD33 expression (CD33++; CD33 MFI=1,035)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model	Acute myeloid leukemia	Acute myeloid leukemia cells #SG008		Homo sapiens
Experiment 20 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	22 ng/mL	High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Adult acute monocytic leukemia	U-937 cells		CVCL_0007
Experiment 21 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	23 ng/mL	Low CD33 expression (CD33+; CD33 MFI=299)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model	Acute myeloid leukemia	Acute myeloid leukemia cells #SG010		Homo sapiens
Experiment 22 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	26 ng/mL	High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Acute myeloid leukemia	HNT-34 cells		CVCL_2071
Experiment 23 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	32 ng/mL	Moderate CD33 expression (CD33++; CD33 MFI=1,184)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model	Acute myeloid leukemia	Acute myeloid leukemia cells #SG004		Homo sapiens
Experiment 24 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	33 ng/mL	Moderate CD33 expression (CD33++; CD33 MFI=6,598)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model	Acute myeloid leukemia	Acute myeloid leukemia cells #SG011		Homo sapiens
Experiment 25 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	49 ng/mL	Moderate CD33 expression (CD33++; CD33 MFI=2,278)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Anaplastic thyroid cancer	TF1-alpha cells (Multidrug resistance)		Homo sapiens
Experiment 26 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	61 ng/mL	Moderate CD33 expression (CD33++; 7,000 CD33 receptor copy number)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Esophageal squamous cell carcinoma	TF-1 cells		CVCL_1759
Experiment 27 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	68 ng/mL	High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Adult acute myeloid leukemia	SH-2 cells		CVCL_2190
Experiment 28 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 ng/mL	Negative CD33 expression (CD33-; CD33 MFI=0)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model	Acute myeloid leukemia	Acute myeloid leukemia cells #SG009		Homo sapiens
Experiment 29 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 110 ng/mL	Low CD33 expression (CD33+; CD33 MFI=353)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model	Acute myeloid leukemia	Acute myeloid leukemia cells #SG012		Homo sapiens
Experiment 30 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 110 ng/mL	High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in primary AmL samples in vitro.
In Vitro Model	Acute myeloid leukemia	Acute myeloid leukemia cells #SG020		Homo sapiens
Experiment 31 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 ng/mL	Low CD33 expression (CD33+; CD33 MFI=318)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Ovarian clear cell adenocarcinoma	ES-2 cells		CVCL_3509
Experiment 32 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 ng/mL	High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Burkitt lymphoma	Ramos cells		CVCL_0597
Experiment 33 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 5000 ng/mL	High CD33 expression (CD33+++; 23,000 CD33 receptor copy number)
Method Description	The inhibitory activity of SGN-CD33A against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532

SC-004 [Phase 1 (discontinued)]

ADC Info

Identified from the Human Clinical Data

Click To Hide/Show 2 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC				[13]
Efficacy Data	progressive disease (PD)	21%
Patients Enrolled	Eligible patients must have platinum-resistant ovarian or endometrial cancer (≤3 prior lines), ECOG 0-1, adequate organ function, with exclusion for prior PBD/IND-based therapy.
*Related Clinical Trial*
NCT Number	NCT03138408	Phase Status	PHASE1
Clinical Description	An Open Label, Phase 1 Study of SC-004 as Monotherapy and in Combination With ABBV-181 in Subjects With Epithelial Ovarian, Including Fallopian Tube and Primary Peritoneal and Endometrial Cancers
Primary Endpoint	Safety evaluation includes DLT assessment (NCI CTCAE v4.03) during the first 21-day cycle and QTcF monitoring over 9 weeks.
Other Endpoint	PK parameters (Ctrough, Cmax, Tmax, T1/2, AUC) will be analyzed for 1 year; efficacy endpoints (ORR, CBR, PFS, OS, DOR, DOCB) will be tracked for 2 years.
Experiment 2 Reporting the Activity Date of This ADC				[13]
Efficacy Data	partial response (PR)	5%
Patients Enrolled	Eligible patients must have platinum-resistant ovarian or endometrial cancer (≤3 prior lines), ECOG 0-1, adequate organ function, with exclusion for prior PBD/IND-based therapy.
*Related Clinical Trial*
NCT Number	NCT03138408	Phase Status	PHASE1
Clinical Description	An Open Label, Phase 1 Study of SC-004 as Monotherapy and in Combination With ABBV-181 in Subjects With Epithelial Ovarian, Including Fallopian Tube and Primary Peritoneal and Endometrial Cancers
Primary Endpoint	Safety evaluation includes DLT assessment (NCI CTCAE v4.03) during the first 21-day cycle and QTcF monitoring over 9 weeks.
Other Endpoint	PK parameters (Ctrough, Cmax, Tmax, T1/2, AUC) will be analyzed for 1 year; efficacy endpoints (ORR, CBR, PFS, OS, DOR, DOCB) will be tracked for 2 years.

SGN-CD123A [Phase 1 (discontinued)]

ADC Info

Identified from the Human Clinical Data

Click To Hide/Show 1 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC				[14]
Patients Enrolled	Eligibility requires CD123-positive AML patients with 1-3 prior regimens (high-risk cases may qualify after 1 regimen), adequate organ function and ECOG 0-1, excluding those with CNS involvement, promyelocytic leukemia, significant pulmonary dysfunction, recent transplants, or recent antileukemia/experimental treatments within 4 weeks (hydroxyurea/6-MP allowed). Click to Show/Hide
Administration Dosage	Intravenous infusion in 3-week cycles
*Related Clinical Trial*
NCT Number	NCT02848248	Phase Status	PHASE1
Clinical Description	A Phase 1 Study of SGN-CD123A in Patients With Relapsed or Refractory Acute Myeloid Leukemia (AML)
Primary Endpoint	The primary safety endpoints assess adverse event profiles (type/incidence/severity/seriousness/relatedness) and lab abnormalities during treatment and 1-month post-treatment, along with dose-limiting toxicity incidence during the initial 3-week cycle.
Other Endpoint	Secondary objectives include pharmacokinetic analysis (SGN-CD123A blood concentrations), immunogenicity (antitherapeutic antibodies), and efficacy measures (remission rate, complete remission duration, leukemia-free survival, and overall survival) monitored for approximately 1 year in relapsed/refractory AML patients.

SGN-CD19B [Phase 1 (discontinued)]

ADC Info

Identified from the Human Clinical Data

Click To Hide/Show 1 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC				[15]
Patients Enrolled	Eligibility requires measurable disease after ≥2 prior systemic therapies with ECOG 0-1 and adequate organ function, excluding patients with prior CD19-targeted therapy (unless CD19+ confirmed), active infections, allogeneic transplants, or recent anticancer treatments within 4 weeks (2 weeks if progressive disease).
Administration Dosage	Given intravenously Day 1 of 28-day or 42-day cycles
*Related Clinical Trial*
NCT Number	NCT02702141	Phase Status	PHASE1
Clinical Description	A Phase 1, Open-label, Dose-escalation Study of SGN-CD19B in Patients With Relapsed or Refractory Aggressive B-cell Non-Hodgkin Lymphoma
Primary Endpoint	The primary endpoints evaluate safety profiles including adverse event incidence and laboratory abnormalities monitored through 1 month post-treatment in relapsed/refractory patients.
Other Endpoint	Secondary objectives assess pharmacokinetics (SGN-CD19B blood concentrations for 3 weeks), immunogenicity (antitherapeutic antibodies), and efficacy measures (objective response rate, progression-free survival up to 3 years) in this heavily pretreated population.

Serclutamab talirine [Phase 1 (discontinued)]

ADC Info

Identified from the Human Clinical Data

Click To Hide/Show 4 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC				[16]
Patients Enrolled	Eligibility requires ECOG 0-1 patients with progressive EGFR+ tumors (GBM/CRC/HNSCC/NSCLC/others) refractory to prior therapies (≤3 cytotoxic lines), measurable disease, and ≥12-week life expectancy, excluding those with uncontrolled CNS metastases, cardiac dysfunction (NYHA III-IV/EF<40%), active infections (CTCAE≥G3), recent major surgery (21 days), or significant effusions/keratitis. Washout periods apply for prior therapies (21 days for most, 5 half-lives for targeted agents). Click to Show/Hide
Administration Dosage	ABBV-321 will be administered via intravenous infusion at escalating dose levels until the maximum tolerated dose is reached and a recommended Phase 2 dose is determined.
*Related Clinical Trial*
NCT Number	NCT03234712	Phase Status	PHASE1
Clinical Description	A Phase 1 Study Evaluating the Safety, Pharmacokinetics, and Anti-tumor Activity of ABBV-321 in Subjects With Advanced Solid Tumors Associated With Overexpression of the Epidermal Growth Factor Receptor (EGFR)
Primary Endpoint	The primary pharmacokinetic endpoints evaluate ABBV-321 exposure (AUCt, AUC), peak concentration (Cmax), time to peak (Tmax), elimination characteristics (beta, t1/2) over 78 days, along with dose-escalation outcomes (MTD, RPTD) during the first 28-day cycle in EGFR-overexpressing solid tumor patients.
Other Endpoint	Secondary efficacy measures assess long-term outcomes (PFS, DOR, DCR, TTP, OS up to 5 years) using RECIST 1.1/RANO criteria, QTcF interval changes through 61 days, and ORR in both solid tumors and glioblastoma populations.
Experiment 2 Reporting the Activity Date of This ADC				[18]
Efficacy Data	Partial Response (PR)	4.17%	High EGFR expression (EGFR+++)
Patients Enrolled	Advanced, histologically confirmed solid tumors associated with EGFR overexpression (centralized testing).
Administration Dosage	Ser-T intravenously once every 4 weeks (Q4W; 5-50 ug/kg) in the dose-escalation phase.
*Related Clinical Trial*
NCT Number	NCT03234712	Phase Status	Phase 1
Clinical Description	A phase 1 study evaluating the safety, pharmacokinetics, and anti-tumor activity of ABBV-321 in subjects with advanced solid tumors associated with overexpression of the epidermal growth factor receptor (EGFR).
Primary Endpoint	One patient was PR (N=1/24, 4.17%), 6 patients was SD (N=6/24,25.00%). Median DOR (CR + PR + SD)=6.40 months (95% CI 3.0not reached). The median PFS=1.8 months (95% CI 1.3-5.8), median OS=7.10 months (95% CI: 4.1-12.3).
Other Endpoint	Ser-T RP2D regimen=25 ug/kg Q4W.
Experiment 3 Reporting the Activity Date of This ADC				[18]
Efficacy Data	Partial Response (PR)	4.20%	High EGFR expression (EGFR+++)
Patients Enrolled	Advanced, histologically confirmed solid tumors associated with EGFR overexpression (centralized testing).
Administration Dosage	Ser-T intravenously once every 4 weeks (Q4W; 5-50 ug/kg) in the dose-escalation phase.
*Related Clinical Trial*
NCT Number	NCT03234712	Phase Status	Phase 1
Clinical Description	A phase 1 study evaluating the safety, pharmacokinetics, and anti-tumor activity of ABBV-321 in subjects with advanced solid tumors associated with overexpression of the epidermal growth factor receptor (EGFR).
Primary Endpoint	Responses included 1 partial response (PR), 6 stable disease (SD), 14 progressive disease (PD); 3 patients were not evaluable for response. Median duration of clinical benefit (complete response + PR + SD) was 6.40 months (95% CI: 3.00-not reached).
Other Endpoint	The median PFS was 1.80 months (95% CI: 1.30-5.80) and the median OS was 7.10 months (95% CI: 4.10-12.30).
Experiment 4 Reporting the Activity Date of This ADC				[20]
*Related Clinical Trial*
NCT Number	NCT03234712	Phase Status	Phase 1
Clinical Description	A phase 1 study evaluating the safety, pharmacokinetics, and anti-tumor activity of ABBV-321 in subjects with advanced solid tumors associated with overexpression of the epidermal growth factor receptor (EGFR).

Discovered Using Patient-derived Xenograft Model

Click To Hide/Show 10 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC				[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 34%	High EGFR expression (EGFR+++)
Method Description	ABBV-321 induces efficient tumor cell killing in cell line-derived models of SNO199 and U87NG cells with mAb806 expression with high expression.
In Vivo Model	Glioblastoma PDX model (PDX: SNO199)
Experiment 2 Reporting the Activity Date of This ADC				[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 40%	Low EGFR expression (EGFR+)
Method Description	ABBV-321 induces efficient tumor cell killing in cell line-derived models of SNO199 and U87NG cells with mAb806 expression with high expression.
In Vivo Model	Glioblastoma PDX model (PDX: SNO199)
Experiment 3 Reporting the Activity Date of This ADC				[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 76%	High EGFR expression (EGFR+++)
Method Description	Serclutamab talirine induces efficient tumor cell killing in PDX models of head and neck cancer cell with EGFR expression,demonstrated with ABBV-321 dosed at 0.15 mg/kg 2 every seven days 3.
In Vivo Model	EGFR-expressing malignant mesothelioma PDX model (PDX: 1174)
Experiment 4 Reporting the Activity Date of This ADC				[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 88.57%	Moderate EGFR expression (EGFR++)
Method Description	ABBV-321 induces efficient tumor cell killing in cell line-derived models of SNO199 and U87NG cells with mAb806 expression with high expression.
In Vivo Model	Glioblastoma PDX model (PDX: SNO207)
Experiment 5 Reporting the Activity Date of This ADC				[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90.20%	Moderate EGFR expression (EGFR++)
Method Description	Serclutamab talirine induces efficient tumor cell killing in PDX models of brain cancer cell with EGFR expression,dosed 0.2 mg/kg,every seven days 3.
In Vivo Model	EGFR-expressing GBM brain cancer PDX model (PDX: SNO199)
Experiment 6 Reporting the Activity Date of This ADC				[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 91.60%	Moderate EGFR expression (EGFR++)
Method Description	ABBV-321 induces efficient tumor cell killing in cell line-derived models of SNO199 and U87NG cells with mAb806 expression with high expression.
In Vivo Model	Glioblastoma PDX model (PDX: SNO207)
Experiment 7 Reporting the Activity Date of This ADC				[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 93.70%	High EGFR expression (EGFR+++)
Method Description	Serclutamab talirine induces efficient tumor cell killing in PDX models of brain cancer cell with EGFR expression,dosed 0.2 mg/kg,every seven days 3.
In Vivo Model	EGFR-expressing GBM brain cancer PDX model (PDX: SNO207)
Experiment 8 Reporting the Activity Date of This ADC				[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 93.80%	High EGFR expression (EGFR+++)
Method Description	Serclutamab talirine induces efficient tumor cell killing in PDX models of head and neck cancer cell with EGFR expression, administered at 0.5 mg/kg on a Q7D 6 regimen.
In Vivo Model	EGFR-expressing colorectal adenocarcinoma PDX model (PDX: LoVo)
Experiment 9 Reporting the Activity Date of This ADC				[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 96.40%	Moderate EGFR expression (EGFR++)
Method Description	Serclutamab talirine induces efficient tumor cell killing in PDX models of brain cancer cell with EGFR expression,dosed 0.4 mg/kg,every seven days 3.
In Vivo Model	EGFR-expressing GBM brain cancer PDX model (PDX: SNO207)
Experiment 10 Reporting the Activity Date of This ADC				[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.20%	High EGFR expression (EGFR+++)
Method Description	Serclutamab talirine induces efficient tumor cell killing in PDX models of brain cancer cell with EGFR expression,dosed 0.4 mg/kg,every seven days 3.
In Vivo Model	EGFR-expressing GBM brain cancer PDX model (PDX: SNO199)

Discovered Using Cell Line-derived Xenograft Model

Click To Hide/Show 16 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 52.40%	Moderate EGFR expression (EGFR++)
Method Description	Serclutamab talirine induces efficient tumor cell killing in PDX models of head and neck cancer cell with EGFR expression,a single dose of 0.0125 mg/kg.
In Vivo Model	EGFR-expressing SW48 CDX model
In Vitro Model	Colon adenocarcinoma	SW48 cells		CVCL_1724
Experiment 2 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 55.30%	Low EGFR expression (EGFR+)
Method Description	Serclutamab talirine induces efficient tumor cell killing in PDX models of lung squamous cell carcinoma cell with EGFR expression,a single dose of 0.1 mg/kg.
In Vivo Model	EGFR-expressing EBC-1 CDX model
In Vitro Model	Lung squamous cell carcinoma	EBC-1 cells		CVCL_2891
Experiment 3 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 70.60%	High EGFR expression (EGFR+++)
Method Description	Serclutamab talirine induces efficient tumor cell killing in PDX models of head and neck cancer cell with EGFR expression,a single dose of 0.025 mg/kg.
In Vivo Model	EGFR-expressing SW48 CDX model
In Vitro Model	Colon adenocarcinoma	SW48 cells		CVCL_1724
Experiment 4 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 73.80%	High EGFR expression (EGFR+++)
Method Description	Serclutamab talirine induces efficient tumor cell killing in PDX models of head and neck cancer cell with EGFR expression,a single dose of 0.1 mg/kg.
In Vivo Model	EGFR-expressing A-253 CDX model
In Vitro Model	Submandibular gland squamous cell carcinoma	A-253 cells		CVCL_1060
Experiment 5 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 81.10%	Moderate EGFR expression (EGFR++)
Method Description	Serclutamab talirine induces efficient tumor cell killing in PDX models of head and neck cancer cell with EGFR expression,a single dose of 0.3 mg/kg.
In Vivo Model	EGFR-expressing A-253 CDX model
In Vitro Model	Submandibular gland squamous cell carcinoma	A-253 cells		CVCL_1060
Experiment 6 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 82.80%	Moderate EGFR expression (EGFR++)
Method Description	Serclutamab talirine induces efficient tumor cell killing in PDX models of head and neck cancer cell with EGFR expression,a single dose of 0.1 mg/kg.
In Vivo Model	EGFR-expressing SW48 CDX model
In Vitro Model	Colon adenocarcinoma	SW48 cells		CVCL_1724
Experiment 7 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 82.80%	High EGFR expression (EGFR+++)
Method Description	Serclutamab talirine induces efficient tumor cell killing in PDX models of head and neck cancer cell with EGFR expression,a single dose of 0.05 mg/kg.
In Vivo Model	EGFR-expressing SW48 CDX model
In Vitro Model	Colon adenocarcinoma	SW48 cells		CVCL_1724
Experiment 8 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 83.10%	Moderate EGFR expression (EGFR++)
Method Description	Serclutamab talirine induces efficient tumor cell killing in PDX models of head and neck cancer cell with EGFR expression,a single dose of 0.1 mg/kg.
In Vivo Model	EGFR-expressing FaDu CDX model
In Vitro Model	Hypopharyngeal squamous cell carcinoma	FaDu cells		CVCL_1218
Experiment 9 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 89.90%	Low EGFR expression (EGFR+)
Method Description	Serclutamab talirine induces efficient tumor cell killing in PDX models of head and neck cancer cell with EGFR expression,administered 0.4 mg/kg,at every seven days 3.
In Vivo Model	EGFR-expressing HCT 116 CDX model
In Vitro Model	Colon carcinoma	HCT 116 cells		CVCL_0291
Experiment 10 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 89.90%	High EGFR expression (EGFR+++)
Method Description	Serclutamab talirine induces efficient tumor cell killing in PDX models of head and neck cancer cell with EGFR expression,a single dose of 0.1 mg/kg.
In Vivo Model	EGFR-expressing HCT 116 CDX model
In Vitro Model	Colon carcinoma	HCT 116 cells		CVCL_0291
Experiment 11 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 91.80%	Negative EGFR expression (EGFR-)
Method Description	Serclutamab talirine induces efficient tumor cell killing in PDX models of head and neck cancer cell with EGFR expression,a single dose of 0.3 mg/kg.
In Vivo Model	EGFR-expressing FaDu CDX model
In Vitro Model	Hypopharyngeal squamous cell carcinoma	FaDu cells		CVCL_1218
Experiment 12 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	High EGFR expression (EGFR+++)
Method Description	ABBV-321 induces efficient tumor cell killing in cell line-derived models of SNO199 and U87NG cells with mAb806 expression with high expression.
In Vivo Model	Glioblastoma U-87MG CDX model
In Vitro Model	Glioblastoma	U-87MG ATCC cells		CVCL_0022
Experiment 13 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Low EGFR expression (EGFR+)
Method Description	ABBV-321 induces efficient tumor cell killing in cell line-derived models of SNO199 and U87NG cells with mAb806 expression with high expression.
In Vivo Model	Glioblastoma U-87MG CDX model
In Vitro Model	Glioblastoma	U-87MG ATCC cells		CVCL_0022
Experiment 14 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Low EGFR expression (EGFR+)
Method Description	Serclutamab talirine induces efficient tumor cell killing in PDX models of lung squamous cell carcinoma cell with EGFR expression,a single dose of 0.3 mg/kg.
In Vivo Model	EGFR-expressing EBC-1 CDX model
In Vitro Model	Lung squamous cell carcinoma	EBC-1 cells		CVCL_2891
Experiment 15 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	High EGFR expression (EGFR+++)
Method Description	Serclutamab talirine induces efficient tumor cell killing in PDX models of brain cancer cell with EGFR expression,dosed 0.4 mg/kg,every seven days 3.
In Vivo Model	EGFR-expressing U-87MG CDX model
In Vitro Model	Glioblastoma	U-87MG ATCC cells		CVCL_0022
Experiment 16 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	High EGFR expression (EGFR+++)
Method Description	Serclutamab talirine induces efficient tumor cell killing in PDX models of brain cancer cell with EGFR expression,dosed 0.2 mg/kg,every seven days 3.
In Vivo Model	EGFR-expressing U-87MG CDX model
In Vitro Model	Glioblastoma	U-87MG ATCC cells		CVCL_0022

Revealed Based on the Cell Line Data

Click To Hide/Show 38 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	15 pM
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Colon adenocarcinoma	SW48 cells		CVCL_1724
Experiment 2 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.23 nM	Negative EGFR expression (EGFR-)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Glioblastoma	U-87 MGvIII cells		CVCL_0022
Experiment 3 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.7 nM	High EGFR expression (EGFR+++; IHC 3+)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Colon adenocarcinoma	LoVo cells		CVCL_0399
Experiment 4 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.7 nM	High EGFR expression (EGFR+++; IHC 3+)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Astrocytoma	U-251MG cells		CVCL_0021
Experiment 5 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1 nM	Moderate EGFR expression (EGFR++; IHC 2+)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Colon adenocarcinoma	LS174T cells		CVCL_1384
Experiment 6 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.1 nM	High EGFR expression (EGFR+++; IHC 3+)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Colon adenocarcinoma	SK-CO-1 cells		CVCL_0626
Experiment 7 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.4 nM	Negative EGFR expression (EGFR-)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Astrocytoma	SF268 cells		CVCL_1689
Experiment 8 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.5 nM	Moderate EGFR expression (EGFR++)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Colon cancer	HT29 cells		CVCL_A8EZ
Experiment 9 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.5 nM	Low EGFR expression (EGFR+; IHC 1+)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Glioblastoma	M059K cells		CVCL_0401
Experiment 10 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.8 nM	Moderate EGFR expression (EGFR++; IHC 2+)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Colon adenocarcinoma	SW403 cells		CVCL_0545
Experiment 11 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.9 nM	High EGFR expression (EGFR+++)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Primitive neuroectodermal tumor	PFSK-1 cells		CVCL_1642
Experiment 12 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.5 nM	High EGFR expression (EGFR+++)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Gliosarcoma	SF539 cells		CVCL_1691
Experiment 13 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.6 nM	Moderate EGFR expression (EGFR++)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Colon adenocarcinoma	COLO 201 cells		CVCL_1987
Experiment 14 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.8 nM	High EGFR expression (EGFR+++; IHC 3+)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Glioblastoma	M059J cells		CVCL_0400
Experiment 15 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.3 nM	High EGFR expression (EGFR+++; IHC 3+)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Colon adenocarcinoma	COLO 205 cells		CVCL_0218
Experiment 16 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.7 nM	High EGFR expression (EGFR+++; IHC 3+)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Astrocytoma	SNB-19 cells		CVCL_0535
Experiment 17 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.3 nM	High EGFR expression (EGFR+++; IHC 3+)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Colon adenocarcinoma	SW620 cells		CVCL_0547
Experiment 18 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.6 nM	High EGFR expression (EGFR+++; IHC 3+)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Colon adenocarcinoma	SW1116 cells		CVCL_0544
Experiment 19 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.6 nM	Low EGFR expression (EGFR+; IHC 1+)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Glioblastoma	U-87MG cells		CVCL_0022
Experiment 20 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.7 nM	Low EGFR expression (EGFR+; IHC 1+)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Colon carcinoma	RKO cells		CVCL_0504
Experiment 21 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.8 nM	Moderate EGFR expression (EGFR++)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Rectal adenocarcinoma	SW1463 cells		CVCL_1718
Experiment 22 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.8 nM	Negative EGFR expression (EGFR-)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Anaplastic astrocytoma	CHLA-03-AA cells		CVCL_U616
Experiment 23 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.5 nM	Moderate EGFR expression (EGFR++)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Colon adenocarcinoma	WiDr cells		CVCL_2760
Experiment 24 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	8 nM	Moderate EGFR expression (EGFR++; IHC 2+)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Colon adenocarcinoma	SW480 cells		CVCL_0546
Experiment 25 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	8.4 nM	High EGFR expression (EGFR+++; IHC 3+)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Glioblastoma	LN-18 cells		CVCL_0392
Experiment 26 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	9 nM	High EGFR expression (EGFR+++; IHC 3+)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Colon adenocarcinoma	DLD-1 cells		CVCL_0248
Experiment 27 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	9.5 nM	Moderate EGFR expression (EGFR++; IHC 2+)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Cecum adenocarcinoma	LS1034 cells		CVCL_1382
Experiment 28 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	10.6 nM	Negative EGFR expression (EGFR-)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Glioblastoma	SNB-75 cells		CVCL_1706
Experiment 29 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	11.8 nM	High EGFR expression (EGFR+++; IHC 3+)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Colon adenocarcinoma	T84 cells		CVCL_0555
Experiment 30 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	12 nM	High EGFR expression (EGFR+++; IHC 3+)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Colon carcinoma	HCT 116 cells		CVCL_0291
Experiment 31 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	13.9 nM	Low EGFR expression (EGFR+; IHC 1+)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Colon adenocarcinoma	Caco-2 cells		CVCL_0025
Experiment 32 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	14.5 nM	High EGFR expression (EGFR+++; IHC 3+)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Glioblastoma	T98G cells		CVCL_0556
Experiment 33 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	16.1 nM	Low EGFR expression (EGFR+; IHC 1+)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Astrocytoma	U-138MG cells		CVCL_0020
Experiment 34 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	17.6 nM	Low EGFR expression (EGFR+; IHC 1+)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Colon adenocarcinoma	COLO 320DM cells		CVCL_0219
Experiment 35 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	18 nM	High EGFR expression (EGFR+++; IHC 3+)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Anaplastic astrocytoma	DBTRG-05MG cells		CVCL_1169
Experiment 36 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	23.2 nM
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Glioblastoma	A-172 cells		CVCL_0131
Experiment 37 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	24.9 nM	High EGFR expression (EGFR+++; IHC 3+)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Colon adenocarcinoma	COLO 320HSR cells		CVCL_0220
Experiment 38 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	28.4 nM	High EGFR expression (EGFR+++; IHC 3+)
Method Description	The inhibitory activity of serclutamab talirine against cancer cell growth was compared with ABBV-221 against various human cancer cell lines in vitro. The cells were treated with serclutamab talirine and ABBV-221.
In Vitro Model	Colon adenocarcinoma	HCT 15 cells		CVCL_0292

Rolinsatamab talirine [Phase 1 (discontinued)]

ADC Info

Identified from the Human Clinical Data

Click To Hide/Show 2 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC				[17]
Patients Enrolled	Eligibility requires ECOG 0-1 patients with PRLR+ advanced tumors (breast/colorectal/adrenocortical/chromophobe RCC in escalation; breast cancer in expansion) refractory to ≤4 cytotoxic lines, excluding prior PBD agents, uncontrolled comorbidities, significant immunotherapy reactions, active gallbladder disease, major liver resection, or ongoing CTCAE >G1 toxicities, with 21-day washout for most prior therapies (14 days for targeted agents). Click to Show/Hide
Administration Dosage	ABBV-176 will be administered via intravenous infusion at escalating dose levels until the maximum tolerated dose is reached.
*Related Clinical Trial*
NCT Number	NCT03145909	Phase Status	PHASE1
Clinical Description	A Phase 1 Study Evaluating the Safety, Pharmacokinetics and Anti-Tumor Activity of ABBV-176 in Subjects With Advanced Solid Tumors Likely to Express Prolactin Receptor (PRLR)
Primary Endpoint	The dose escalation phase evaluates ABBV-176 pharmacokinetics over 57 days and establishes safety parameters (MTD/RPTD) during the first 21-day cycle in PRLR-expressing solid tumors, with expanded cohort assessing ORR per RECIST 1.1 over 2 years.
Other Endpoint	Secondary endpoints include PK monitoring (AUCt, Cmax, Tmax) over 15 days and long-term efficacy outcomes (PFS, DOR, OS up to 2 years) in expanded cohort, alongside ECOG status changes and cardiac safety (QTcF changes over 47 days) in dose escalation phase.
Experiment 2 Reporting the Activity Date of This ADC				[19]
Efficacy Data	Objective Response Rate (ORR)	0%
Patients Enrolled	Locally advanced or metastatic solid tumor types associated with PRLR expression, including breast cancer, colorectal cancer, and adrenocortical carcinoma. Patients had progressed on prior treatment, were not amenable to treatment with curative intent, and had no other therapy options known to provide clinical benefit, or were ineligible for such therapies. Patients had an Eastern Cooperative Oncology Group performance status of 0 or 1, and adequate bone marrow, renal, and hepatic function. Click to Show/Hide
Administration Dosage	Initial dose was 2.70 ug/kg, dose increment was capped at a 100% increase, or at a 50% increase if a grade2 drug-related toxicity had been observed, intravenously every 21 days.
*Related Clinical Trial*
NCT Number	NCT03145909	Phase Status	Phase 1
Clinical Description	A phase 1 study evaluating the safety, pharmacokinetics and anti-tumor activity of ABBV-176 in subjects with advanced solid tumors likely to express prolactin receptor (PRLR).
Primary Endpoint	MtD was not formally determined, as identification of a tolerable dose was confounded by late-onset toxicities. ABBV-176 was associated with significant toxicity in this phase 1, dose-escalation study.
Other Endpoint	No patient had an objective response.

Discovered Using Cell Line-derived Xenograft Model

Click To Hide/Show 3 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC				[22]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90.50%
Method Description	Mice implanted with BT-474 breast cancer model and dosed with a single dose of ABBV-176 at 0.5 mg/kg.
In Vivo Model	BT-474 CDX
In Vitro Model	Invasive breast carcinoma	BT-474 cells	CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC				[22]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%
Method Description	Mice implanted with BT-474 breast cancer model and dosed with a single dose of ABBV-176 at 0.1 mg/kg.
In Vivo Model	BT-474 CDX
In Vitro Model	Invasive breast carcinoma	BT-474 cells	CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC				[22]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%
Method Description	Mice implanted with BT-474 breast cancer model and dosed with a single dose of ABBV-176 at 0.3 mg/kg.
In Vivo Model	BT-474 CDX
In Vitro Model	Invasive breast carcinoma	BT-474 cells	CVCL_0179

Revealed Based on the Cell Line Data

Click To Hide/Show 14 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC				[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.5 pM
Method Description	The inhibitory activity of ABBV-176 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 144 hours.
In Vitro Model	Invasive breast carcinoma	T-47D cells	CVCL_0553
Experiment 2 Reporting the Activity Date of This ADC				[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 nM
Method Description	The inhibitory activity of ABBV-176 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 144 hours.
In Vitro Model	Prostate carcinoma	22RV1 cells	CVCL_1045
Experiment 3 Reporting the Activity Date of This ADC				[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 nM
Method Description	The inhibitory activity of ABBV-176 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 144 hours.
In Vitro Model	Breast adenocarcinoma	CAMA-1 cells	CVCL_1115
Experiment 4 Reporting the Activity Date of This ADC				[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.11 nM
Method Description	The inhibitory activity of ABBV-176 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 144 hours.
In Vitro Model	Colon adenocarcinoma	SW403 cells	CVCL_0545
Experiment 5 Reporting the Activity Date of This ADC				[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.16 nM
Method Description	The inhibitory activity of ABBV-176 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 144 hours.
In Vitro Model	Ovarian clear cell adenocarcinoma	SMOV-2 cells	CVCL_S920
Experiment 6 Reporting the Activity Date of This ADC				[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.24 nM
Method Description	The inhibitory activity of ABBV-176 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 144 hours.
In Vitro Model	Invasive breast carcinoma	BT-474 cells	CVCL_0179
Experiment 7 Reporting the Activity Date of This ADC				[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.26 nM
Method Description	The inhibitory activity of ABBV-176 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 144 hours.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells	CVCL_0033
Experiment 8 Reporting the Activity Date of This ADC				[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.32 nM
Method Description	The inhibitory activity of ABBV-176 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 144 hours.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells	CVCL_0031
Experiment 9 Reporting the Activity Date of This ADC				[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.6 nM
Method Description	The inhibitory activity of ABBV-176 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 144 hours.
In Vitro Model	Endometrial adenocarcinoma	AN3-CA cells	CVCL_0028
Experiment 10 Reporting the Activity Date of This ADC				[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.77 nM
Method Description	The inhibitory activity of ABBV-176 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 144 hours.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells	CVCL_0062
Experiment 11 Reporting the Activity Date of This ADC				[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.2 nM
Method Description	The inhibitory activity of ABBV-176 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 144 hours.
In Vitro Model	Adult hepatocellular carcinoma	Huh-7 cells	CVCL_0336
Experiment 12 Reporting the Activity Date of This ADC				[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	8.6 nM
Method Description	The inhibitory activity of ABBV-176 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 144 hours.
In Vitro Model	Hepatoblastoma	Hep-G2 cells	CVCL_0027
Experiment 13 Reporting the Activity Date of This ADC				[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 22 nM
Method Description	The inhibitory activity of ABBV-176 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 144 hours.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells	CVCL_0062
Experiment 14 Reporting the Activity Date of This ADC				[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 22 nM
Method Description	The inhibitory activity of ABBV-176 against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 144 hours.
In Vitro Model	Invasive breast carcinoma of no special type	UACC-812 cells	CVCL_1781

References

Ref 1	Study of Vadastuximab Talirine (SGN-CD33A; 33A) in Combination With Azacitidine in Patients With Previously Untreated Higher Risk MDS
Ref 2	Vadastuximab Talirine (SGN-CD33A; 33A) Combined With Azacitidine or Decitabine in Older Patients With Newly Diagnosed Acute Myeloid Leukemia
Ref 3	A Safety Study of SGN-CD33A in AML Patients
Ref 4	A Safety Study of SGN-CD33A in Combination With Standard-of-care in Patients With AML
Ref 5	Radiostereometric Analysis of Fracture Healing in Distal Femur Fractures
Ref 6	A Phase 1b Dose-escalation Study of SGN-CD33A in Combination With Standard-of-care for Patients With Newly Diagnosed Acute Myeloid Leukemia, NCT02326584
Ref 7	A Randomized, Double-blind Phase 3 Study of Vadastuximab Talirine (SGN-CD33A) Versus Placebo in Combination With Azacitidine or Decitabine in the Treatment of Older Patients With Newly Diagnosed Acute Myeloid Leukemia (AML), NCT02785900
Ref 8	A phase 1 trial of vadastuximab talirine as monotherapy in patients with CD33-positive acute myeloid leukemia. Blood. 2018 Jan 25;131(4):387-396.
Ref 9	A phase 1 trial of vadastuximab talirine combined with hypomethylating agents in patients with CD33-positive AML. Blood. 2018 Sep 13;132(11):1125-1133.
Ref 10	A Phase 1/2 Study of Vadastuximab Talirine Administered in Sequence With Allogeneic Hematopoietic Stem Cell Transplant in Patients With Relapsed or Refractory Acute Myeloid Leukemia (AML), NCT02614560
Ref 11	A Phase 1 Trial of SGN-CD33A in Patients With CD33-positive Acute Myeloid Leukemia, NCT01902329
Ref 12	SGN-CD33A: a novel CD33-targeting antibody-drug conjugate using a pyrrolobenzodiazepine dimer is active in models of drug-resistant AML. Blood. 2013 Aug 22;122(8):1455-63.
Ref 13	SC-004 Alone or With ABBV-181 in Subjects With Epithelial Ovarian, Fallopian Tube, Primary Peritoneal and Endometrial Cancers
Ref 14	A Safety Study of SGN-CD123A in Patients With Acute Myeloid Leukemia
Ref 15	A Safety Study of SGN-CD19B in Patients With B-cell Non-Hodgkin Lymphoma
Ref 16	A Study Evaluating the Safety, Pharmacokinetics, and Anti-tumor Activity of ABBV-321 in Subjects With Advanced Solid Tumors Associated With Overexpression of the Epidermal Growth Factor Receptor (EGFR)
Ref 17	A Study Evaluating the Safety, Pharmacokinetics and Anti-Tumor Activity of ABBV-176 in Subjects With Advanced Solid Tumors Likely to Express Prolactin Receptor (PRLR)
Ref 18	Phase I study of anti-epidermal growth factor receptor antibody-drug conjugate serclutamab talirine: Safety, pharmacokinetics, and antitumor activity in advanced glioblastoma. Neurooncol Adv. 2022 Dec 21;5(1):vdac183.
Ref 19	A first-in-human, phase 1, dose-escalation study of ABBV-176, an antibody-drug conjugate targeting the prolactin receptor, in patients with advanced solid tumors. Invest New Drugs. 2020 Dec;38(6):1815-1825.
Ref 20	A Phase 1 Study Evaluating the Safety, Pharmacokinetics, and Anti-tumor Activity of ABBV-321 in Subjects With Advanced Solid Tumors Associated With Overexpression of the Epidermal Growth Factor Receptor (EGFR)
Ref 21	Targeting Multiple EGFR-expressing Tumors with a Highly Potent Tumor-selective Antibody-Drug Conjugate. Mol Cancer Ther. 2020 Oct;19(10):2117-2125.
Ref 22	ABBV-176, a PRLR antibody drug conjugate with a potent DNA-damaging PBD cytotoxin and enhanced activity with PARP inhibition. BMC Cancer. 2021 Jun 9;21(1):681.

Payload Information

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Correspondence

Prof. Feng ZHU (zhufeng@zju.edu.cn)

Prof. Xiaowu DONG (dongxw@zju.edu.cn)

Prof. Luo FANG (fangluo@zjcc.org.cn)