Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0DEGEG
ADC Name	Vobramitamab duocarmazine
Synonyms	AEX4089DC1; MGC 018; Anti-B7-H3 antibody drug conjugate; MGC-018; MGC018 Click to Show/Hide
Organization	MacroGenics, Inc.
Drug Status	Phase 2/3
Indication	In total 4 Indication(s) Castration resistant prostate cancer [ICD11:2C82] Phase 3 Melanoma [ICD11:2C30] Phase 3 Non-small cell lung cancer [ICD11:2C25] Phase 3 Solid tumors [ICD11:2A00-2A0Z\|2B50-2F9Z] Phase 2
Drug-to-Antibody Ratio	2.7
Structure
	3D MOL	2D MOL
Antibody Name	Vobramitamab		Antibody Info
Antigen Name	CD276 antigen (CD276)		Antigen Info
Payload Name	seco-DUBA		Payload Info
Therapeutic Target	Human Deoxyribonucleic acid (hDNA)		Target Info
Linker Name	Mal-PEG2-Val-Cit-PABA-Cyclization Spacer		Linker Info
Conjugate Type	Random conjugation through reduced inter-chain cysteines.
Combination Type	Duocarmazine
Puchem SID	472419325 , 461454200 , 440234524 , 474489022 , 474488467
ChEBI ID	CHEMBL4594576

General Information of The Activity Data Related to This ADC

Identified from the Human Clinical Data

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

Standard Type	NCT Number	Clinical Status	Clinical Trial Description
Undisclosed	NCT05551117	Phase 2	A phase 2, randomized, open-label, study of two dose levels of obramitamab duocarmazine in participants with metastatic castration-resistant prostate cancer.
Undisclosed	NCT03729596	Phase 1/2	A phase 1/2, first-in-human, open-label, dose-escalation study of MGC018 (anti-B7-H3 antibody drug conjugate) alone and in combination with MGA012 (anti-PD-1 antibody) in patients with advanced solid tumors. Click to Show/Hide
Undisclosed	NCT05293496	Phase 1	A phase 1/1b dose escalation and cohort expansion study of MGC018 in combination with checkpoint inhibitor in participants with advanced solid tumors.

Discovered Using Patient-derived Xenograft Model

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

Standard Type	Value	Units	Animal Model (No. of PDX)
Tumor Growth Inhibition value (TGI)	≈ 96.1	%	Pancreatic cancer PDX model (PDX: PDX-PAX-13565)
Tumor Growth Inhibition value (TGI)	≈ 97.6	%	Head and neck cancer PDX model
Tumor Growth Inhibition value (TGI)	≈ 98.2	%	Triple-negative breast cancer PDX model

Discovered Using Cell Line-derived Xenograft Model

Click To Hide/Show 25 Activity Data Related to This Level

Standard Type	Value	Units	Cell Line	Disease Model
Tumor Growth Inhibition value (TGI)	≈ 22.4	%	Calu-6 cells	Lung adenocarcinoma
Tumor Growth Inhibition value (TGI)	≈ 30.1	%	PA-1 cells	Ovarian mixed germ cell tumor
Tumor Growth Inhibition value (TGI)	≈ 42.9	%	PA-1 cells	Ovarian mixed germ cell tumor
Tumor Growth Inhibition value (TGI)	≈ 43.9	%	MDA-MB-468 Luc cells	Breast adenocarcinoma
Tumor Growth Inhibition value (TGI)	≈ 59.3	%	Calu-6 cells	Lung adenocarcinoma
Tumor Growth Inhibition value (TGI)	≈ 62.7	%	MDA-MB-468 Luc cells	Breast adenocarcinoma
Tumor Growth Inhibition value (TGI)	≈ 62.8	%	PA-1 cells	Ovarian mixed germ cell tumor
Tumor Growth Inhibition value (TGI)	≈ 66.5	%	Calu-6 cells	Lung adenocarcinoma
Tumor Growth Inhibition value (TGI)	≈ 71.9	%	Calu-6 cells	Lung adenocarcinoma
Tumor Growth Inhibition value (TGI)	≈ 76.3	%	Calu-6 cells	Lung adenocarcinoma
Tumor Growth Inhibition value (TGI)	≈ 76.6	%	A375.S2 cells	Amelanotic melanoma
Tumor Growth Inhibition value (TGI)	≈ 82.8	%	Calu-6 cells	Lung adenocarcinoma
Tumor Growth Inhibition value (TGI)	≈ 83.9	%	A375.S2 cells	Amelanotic melanoma
Tumor Growth Inhibition value (TGI)	≈ 87.5	%	Calu-6 cells	Lung adenocarcinoma
Tumor Growth Inhibition value (TGI)	≈ 88.8	%	PA-1 cells	Ovarian mixed germ cell tumor
Tumor Growth Inhibition value (TGI)	≈ 90.5	%	PA-1 cells	Ovarian mixed germ cell tumor
Tumor Growth Inhibition value (TGI)	≈ 91.4	%	PA-1 cells	Ovarian mixed germ cell tumor
Tumor Growth Inhibition value (TGI)	≈ 94.6	%	PA-1 cells	Ovarian mixed germ cell tumor
Tumor Growth Inhibition value (TGI)	≈ 96.7	%	Calu-6 cells	Lung adenocarcinoma
Tumor Growth Inhibition value (TGI)	≈ 97	%	MDA-MB-468 Luc cells	Breast adenocarcinoma
Tumor Growth Inhibition value (TGI)	≈ 97.6	%	PA-1 cells	Ovarian mixed germ cell tumor
Tumor Growth Inhibition value (TGI)	≈ 97.9	%	MDA-MB-468 Luc cells	Breast adenocarcinoma
Tumor Growth Inhibition value (TGI)	≈ 98.1	%	A375.S2 cells	Amelanotic melanoma
Tumor Growth Inhibition value (TGI)	≈ 98.6	%	Calu-6 cells	Lung adenocarcinoma
Tumor Growth Inhibition value (TGI)	≈ 99.7	%	A375.S2 cells	Amelanotic melanoma

Revealed Based on the Cell Line Data

Click To Hide/Show 9 Activity Data Related to This Level

Standard Type	Value	Units	Cell Line	Disease Model
Half Maximal Inhibitory Concentration (IC50)	181	pM	A375.S2 cells	Amelanotic melanoma
Half Maximal Inhibitory Concentration (IC50)	260	pM	Calu-6 cells	Lung adenocarcinoma
Half Maximal Inhibitory Concentration (IC50)	275	pM	PA-1 cells	Ovarian mixed germ cell tumor
Half Maximal Inhibitory Concentration (IC50)	319	pM	Hs 700T cells	Neoplasm
Half Maximal Inhibitory Concentration (IC50)	585	pM	NCI-H1703 cells	Lung squamous cell carcinoma
Half Maximal Inhibitory Concentration (IC50)	767	pM	MDA-MB-468 cells	Breast adenocarcinoma
Half Maximal Inhibitory Concentration (IC50)	910	pM	LN-229 cells	Glioblastoma
Half Maximal Inhibitory Concentration (IC50)	1447	pM	SW48 cells	Colon adenocarcinoma
Half Maximal Inhibitory Concentration (IC50)	> 10	nM	Raji cells	EBV-related Burkitt lymphoma

Full List of Activity Data of This Antibody-drug Conjugate

Identified from the Human Clinical Data

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

Experiment 1 Reporting the Activity Date of This ADC				[1]
*Related Clinical Trial*
NCT Number	NCT05551117	Clinical Status	Phase 2
Clinical Description	A phase 2, randomized, open-label, study of two dose levels of obramitamab duocarmazine in participants with metastatic castration-resistant prostate cancer.
Experiment 2 Reporting the Activity Date of This ADC				[2]
Patients Enrolled	Patients of multiple tumor types, which included 3 melanoma patients refractory to 2 prior lines of checkpoint therapy.
Administration Dosage	6 dose cohorts (0.50-4.00 mg/kg) every 3 weeks.
*Related Clinical Trial*
NCT Number	NCT03729596	Clinical Status	Phase 1/2
Clinical Description	A phase 1/2, first-in-human, open-label, dose-escalation study of MGC018 (anti-B7-H3 antibody drug conjugate) alone and in combination with MGA012 (anti-PD-1 antibody) in patients with advanced solid tumors.
Experiment 3 Reporting the Activity Date of This ADC				[3]
*Related Clinical Trial*
NCT Number	NCT05293496	Clinical Status	Phase 1
Clinical Description	A phase 1/1b dose escalation and cohort expansion study of MGC018 in combination with checkpoint inhibitor in participants with advanced solid tumors.

Discovered Using Patient-derived Xenograft Model

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

Experiment 1 Reporting the Activity Date of This ADC				[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 96.10% (Day 21)	High MET expression (MET+++; IHC H-score=265)
Method Description	Female Athymic Nude-Foxn1nu from Envigo (head and neck,triple-negative breast cancer models),68 weeks of age,were used for the PDX studies. Low passage tumor fragments were implanted into stock animals. When tumors reached 1.01.5 cm3,they were reimplanted into prestudy animals unilaterally on the left flank. When tumors reached an average tumor volume of 150-300 mm³,animals were matched by tumor volume into treatment or vehicle control groups. Three animals were assigned to each group and dosed intravenously by tail vein injection (10 mL/kg). Tumor volumes were measured twice weekly by calipers. Prostate cancer subcutaneous PDX model treated with MGC018 or control ADC at 3 mg/kg (QW3). Click to Show/Hide
In Vivo Model	Pancreatic cancer PDX model (PDX: PDX-PAX-13565)
Experiment 2 Reporting the Activity Date of This ADC				[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.60% (Day 42)	Moderate MET expression (MET++; IHC H-score=130)
Method Description	Male NOG mice from Taconic (prostate cancer model),68 weeks of age,were used for the PDX studies. Low passage tumor fragments were implanted into stock animals. When tumors reached 1.01.5 cm3,they were reimplanted into prestudy animals unilaterally on the left flank. When tumors reached an average tumor volume of 150-300 mm³,animals were matched by tumor volume into treatment or vehicle control groups. Three animals were assigned to each group and dosed intravenously by tail vein injection (10 mL/kg). Tumor volumes were measured twice weekly by calipers. Head and neck cancer subcutaneous PDX model treated with MGC018 or control ADC at 3 mg/kg (Q2W 2). Click to Show/Hide
In Vivo Model	Head and neck cancer PDX model
Experiment 3 Reporting the Activity Date of This ADC				[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.20% (Day 10)	High MET expression (MET+++; IHC H-score=240)
Method Description	Female Athymic Nude-Foxn1nu from Envigo (head and neck,triple-negative breast cancer models),68 weeks of age,were used for the PDX studies. Low passage tumor fragments were implanted into stock animals. When tumors reached 1.01.5 cm3,they were reimplanted into prestudy animals unilaterally on the left flank. When tumors reached an average tumor volume of 150-300 mm³,animals were matched by tumor volume into treatment or vehicle control groups. Three animals were assigned to each group and dosed intravenously by tail vein injection (10 mL/kg). Tumor volumes were measured twice weekly by calipers. Triple-negative breast cancer subcutaneous PDX model treated with MGC018 or control ADC at 3 mg/kg (QW2). Click to Show/Hide
In Vivo Model	Triple-negative breast cancer PDX model

Discovered Using Cell Line-derived Xenograft Model

Click To Hide/Show 25 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 22.40% (Day 50)	High MET expression (MET+++; IHC H-score=287)
Method Description	Human tumor cells (5x10⁶) were resuspended in 1:1 medium (DMEM/F-12) and Matrigel basement membrane matrix (Corning) and implanted subcutaneously into the flank (A375.S2,Calu-6,PA-1) or mammary fat pad (MDA-MB-468) of mice. Mice were randomized into groups of 5-7 individuals per group. ADCs or vehicle control (PBS) were administered intravenously by tail vein injection (10 mL/kg) following growth of established tumors (100-150 mm³). Calu-6 lung cancer subcutaneous xenografts were treated with MGC018 or control ADC at 0.3 mg/kg QWx4. Click to Show/Hide
In Vivo Model	Lung cancer CDX model
In Vitro Model	Lung adenocarcinoma	Calu-6 cells		CVCL_0236
Experiment 2 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 30.10% (Day 80)	Moderate MET expression (MET++; IHC H-score=150)
Method Description	Human tumor cells (5x10⁶) were resuspended in 1:1 medium (DMEM/F-12) and Matrigel basement membrane matrix (Corning) and implanted subcutaneously into the flank (A375.S2,Calu-6,PA-1) or mammary fat pad (MDA-MB-468) of mice. Mice were randomized into groups of 5-7 individuals per group. ADCs or vehicle control (PBS) were administered intravenously by tail vein injection (10 mL/kg) following growth of established tumors (100-150 mm³). PA-1 ovarian cancer subcutaneous xenografts were treated with MGC018 or control ADC at 3 mg/kg as a single dose,QW1. Click to Show/Hide
In Vivo Model	Ovarian cancer CDX model
In Vitro Model	Ovarian mixed germ cell tumor	PA-1 cells		CVCL_0479
Experiment 3 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 42.90% (Day 60)	High MET expression (MET+++; IHC H-score=287)
Method Description	Human tumor cells (5x10⁶) were resuspended in 1:1 medium (DMEM/F-12) and Matrigel basement membrane matrix (Corning) and implanted subcutaneously into the flank (A375.S2,Calu-6,PA-1) or mammary fat pad (MDA-MB-468) of mice. Mice were randomized into groups of 5-7 individuals per group. ADCs or vehicle control (PBS) were administered intravenously by tail vein injection (10 mL/kg) following growth of established tumors (100-150 mm³). A-1 ovarian cancer subcutaneous xenografts were treated with MGC018 or control ADC at 3 mg/kg. Click to Show/Hide
In Vivo Model	Ovarian cancer CDX model
In Vitro Model	Ovarian mixed germ cell tumor	PA-1 cells		CVCL_0479
Experiment 4 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 43.90% (Day 100)	NegativeCD276 expression (CD276-)
Method Description	Human tumor cells (5x10⁶) were resuspended in 1:1 medium (DMEM/F-12) and Matrigel basement membrane matrix (Corning) and implanted subcutaneously into the flank (A375.S2,Calu-6,PA-1) or mammary fat pad (MDA-MB-468) of mice. Mice were randomized into groups of 5-7 individuals per group. ADCs or vehicle control (PBS) were administered intravenously by tail vein injection (10 mL/kg) following growth of established tumors (100-150 mm³). MDA-MB-468 triple-negative breast cancer orthotopic xenografts were treated with MGC018 or control ADC at 3 mg/kg. Click to Show/Hide
In Vivo Model	Triple-negative breast cancer CDX model
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 Luc cells		CVCL_0419
Experiment 5 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 59.30% (Day 70)	High MET expression (MET+++; IHC H-score=255)
Method Description	Human tumor cells (5x10⁶) were resuspended in 1:1 medium (DMEM/F-12) and Matrigel basement membrane matrix (Corning) and implanted subcutaneously into the flank (A375.S2,Calu-6,PA-1) or mammary fat pad (MDA-MB-468) of mice. Mice were randomized into groups of 5-7 individuals per group. ADCs or vehicle control (PBS) were administered intravenously by tail vein injection (10 mL/kg) following growth of established tumors (100-150 mm³). Calu-6 lung cancer subcutaneous xenografts were treated with MGC018 or control ADC at 3 mg/kg. Click to Show/Hide
In Vivo Model	Lung cancer CDX model
In Vitro Model	Lung adenocarcinoma	Calu-6 cells		CVCL_0236
Experiment 6 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 62.70% (Day 100)	Moderate MET expression (MET++; IHC H-score=150)
Method Description	Human tumor cells (5x10⁶) were resuspended in 1:1 medium (DMEM/F-12) and Matrigel basement membrane matrix (Corning) and implanted subcutaneously into the flank (A375.S2,Calu-6,PA-1) or mammary fat pad (MDA-MB-468) of mice. Mice were randomized into groups of 5-7 individuals per group. ADCs or vehicle control (PBS) were administered intravenously by tail vein injection (10 mL/kg) following growth of established tumors (100-150 mm³).MDA-MB-468 triple-negative breast cancer orthotopic xenografts were treated with MGC018 or control ADC at 0.3 mg/kg QW4. Click to Show/Hide
In Vivo Model	Triple-negative breast cancer CDX model
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 Luc cells		CVCL_0419
Experiment 7 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 62.80% (Day 70)	High MET expression (MET+++; IHC H-score=287)
Method Description	Human tumor cells (5x10⁶) were resuspended in 1:1 medium (DMEM/F-12) and Matrigel basement membrane matrix (Corning) and implanted subcutaneously into the flank (A375.S2,Calu-6,PA-1) or mammary fat pad (MDA-MB-468) of mice. Mice were randomized into groups of 5-7 individuals per group. ADCs or vehicle control (PBS) were administered intravenously by tail vein injection (10 mL/kg) following growth of established tumors (100-150 mm³). PA-1 ovarian cancer subcutaneous xenografts were treated with MGC018 or control ADC at 0.3 mg/kg QW4. Click to Show/Hide
In Vivo Model	Ovarian cancer CDX model
In Vitro Model	Ovarian mixed germ cell tumor	PA-1 cells		CVCL_0479
Experiment 8 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 66.50% (Day 50)	High MET expression (MET+++; IHC H-score=255)
Method Description	Human tumor cells (5x10⁶) were resuspended in 1:1 medium (DMEM/F-12) and Matrigel basement membrane matrix (Corning) and implanted subcutaneously into the flank (A375.S2,Calu-6,PA-1) or mammary fat pad (MDA-MB-468) of mice. Mice were randomized into groups of 5-7 individuals per group. ADCs or vehicle control (PBS) were administered intravenously by tail vein injection (10 mL/kg) following growth of established tumors (100-150 mm³). Calu-6 lung cancer subcutaneous xenografts were treated with MGC018 or control ADC at 3 mg/kg. Click to Show/Hide
In Vivo Model	Lung cancer CDX model
In Vitro Model	Lung adenocarcinoma	Calu-6 cells		CVCL_0236
Experiment 9 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 71.90% (Day 50)	High MET expression (MET+++; IHC H-score=255)
Method Description	Human tumor cells (5x10⁶) were resuspended in 1:1 medium (DMEM/F-12) and Matrigel basement membrane matrix (Corning) and implanted subcutaneously into the flank (A375.S2,Calu-6,PA-1) or mammary fat pad (MDA-MB-468) of mice. Mice were randomized into groups of 5-7 individuals per group. ADCs or vehicle control (PBS) were administered intravenously by tail vein injection (10 mL/kg) following growth of established tumors (100-150 mm³). Calu-6 lung cancer subcutaneous xenografts were treated with MGC018 or control ADC at 1 mg/kg QWx4. Click to Show/Hide
In Vivo Model	Lung cancer CDX model
In Vitro Model	Lung adenocarcinoma	Calu-6 cells		CVCL_0236
Experiment 10 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 76.30% (Day 50)	High MET expression (MET+++; IHC H-score=255)
Method Description	Human tumor cells (5x10⁶) were resuspended in 1:1 medium (DMEM/F-12) and Matrigel basement membrane matrix (Corning) and implanted subcutaneously into the flank (A375.S2,Calu-6,PA-1) or mammary fat pad (MDA-MB-468) of mice. Mice were randomized into groups of 5-7 individuals per group. ADCs or vehicle control (PBS) were administered intravenously by tail vein injection (10 mL/kg) following growth of established tumors (100-150 mm³). Calu-6 lung cancer subcutaneous xenografts were treated with MGC018 or control ADC at 6 mg/kg. Click to Show/Hide
In Vivo Model	Lung cancer CDX model
In Vitro Model	Lung adenocarcinoma	Calu-6 cells		CVCL_0236
Experiment 11 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 76.60% (Day 60)	High MET expression (MET+++; IHC H-score=255)
Method Description	Human tumor cells (5x10⁶) were resuspended in 1:1 medium (DMEM/F-12) and Matrigel basement membrane matrix (Corning) and implanted subcutaneously into the flank (A375.S2,Calu-6,PA-1) or mammary fat pad (MDA-MB-468) of mice. Mice were randomized into groups of 5-7 individuals per group. ADCs or vehicle control (PBS) were administered intravenously by tail vein injection (10 mL/kg) following growth of established tumors (100-150 mm³). A375.S2 melanoma subcutaneous xenografts were treated with MGC018 or control ADC at 0.3 mg/kg QW4. Click to Show/Hide
In Vivo Model	Melanoma CDX model
In Vitro Model	Amelanotic melanoma	A375.S2 cells		CVCL_0136
Experiment 12 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 82.80% (Day 50)	High MET expression (MET+++; IHC H-score=255)
Method Description	Human tumor cells (5x10⁶) were resuspended in 1:1 medium (DMEM/F-12) and Matrigel basement membrane matrix (Corning) and implanted subcutaneously into the flank (A375.S2,Calu-6,PA-1) or mammary fat pad (MDA-MB-468) of mice. Mice were randomized into groups of 5-7 individuals per group. ADCs or vehicle control (PBS) were administered intravenously by tail vein injection (10 mL/kg) following growth of established tumors (100-150 mm³). Calu-6 lung cancer subcutaneous xenografts were treated with MGC018 or control ADC at 3 mg/kg QWx4. Click to Show/Hide
In Vivo Model	Lung cancer CDX model
In Vitro Model	Lung adenocarcinoma	Calu-6 cells		CVCL_0236
Experiment 13 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 83.90% (Day 60)	High MET expression (MET+++; IHC H-score=265)
Method Description	Human tumor cells (5x10⁶) were resuspended in 1:1 medium (DMEM/F-12) and Matrigel basement membrane matrix (Corning) and implanted subcutaneously into the flank (A375.S2,Calu-6,PA-1) or mammary fat pad (MDA-MB-468) of mice. Mice were randomized into groups of 5-7 individuals per group. ADCs or vehicle control (PBS) were administered intravenously by tail vein injection (10 mL/kg) following growth of established tumors (100-150 mm³). A375.S2 melanoma subcutaneous xenografts were treated with MGC018 or control ADC at 1 mg/kg. Click to Show/Hide
In Vivo Model	Melanoma CDX model
In Vitro Model	Amelanotic melanoma	A375.S2 cells		CVCL_0136
Experiment 14 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 87.50% (Day 50)	High MET expression (MET+++; IHC H-score=255)
Method Description	Human tumor cells (5x10⁶) were resuspended in 1:1 medium (DMEM/F-12) and Matrigel basement membrane matrix (Corning) and implanted subcutaneously into the flank (A375.S2,Calu-6,PA-1) or mammary fat pad (MDA-MB-468) of mice. Mice were randomized into groups of 5-7 individuals per group. ADCs or vehicle control (PBS) were administered intravenously by tail vein injection (10 mL/kg) following growth of established tumors (100-150 mm³). Calu-6 lung cancer subcutaneous xenografts were treated with MGC018 or control ADC at 10 mg/kg. Click to Show/Hide
In Vivo Model	Lung cancer CDX model
In Vitro Model	Lung adenocarcinoma	Calu-6 cells		CVCL_0236
Experiment 15 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 88.80% (Day 60)	High MET expression (MET+++; IHC H-score=287)
Method Description	Human tumor cells (5x10⁶) were resuspended in 1:1 medium (DMEM/F-12) and Matrigel basement membrane matrix (Corning) and implanted subcutaneously into the flank (A375.S2,Calu-6,PA-1) or mammary fat pad (MDA-MB-468) of mice. Mice were randomized into groups of 5-7 individuals per group. ADCs or vehicle control (PBS) were administered intravenously by tail vein injection (10 mL/kg) following growth of established tumors (100-150 mm³). A-1 ovarian cancer subcutaneous xenografts were treated with MGC018 or control ADC at 6 mg/kg. Click to Show/Hide
In Vivo Model	Ovarian cancer CDX model
In Vitro Model	Ovarian mixed germ cell tumor	PA-1 cells		CVCL_0479
Experiment 16 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90.50% (Day 60)	High MET expression (MET+++; IHC H-score=287)
Method Description	Human tumor cells (5x10⁶) were resuspended in 1:1 medium (DMEM/F-12) and Matrigel basement membrane matrix (Corning) and implanted subcutaneously into the flank (A375.S2,Calu-6,PA-1) or mammary fat pad (MDA-MB-468) of mice. Mice were randomized into groups of 5-7 individuals per group. ADCs or vehicle control (PBS) were administered intravenously by tail vein injection (10 mL/kg) following growth of established tumors (100-150 mm³). A-1 ovarian cancer subcutaneous xenografts were treated with MGC018 or control ADC at 10 mg/kg. Click to Show/Hide
In Vivo Model	Ovarian cancer CDX model
In Vitro Model	Ovarian mixed germ cell tumor	PA-1 cells		CVCL_0479
Experiment 17 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 91.40% (Day 80)	High MET expression (MET+++; IHC H-score=287)
Method Description	Human tumor cells (5x10⁶) were resuspended in 1:1 medium (DMEM/F-12) and Matrigel basement membrane matrix (Corning) and implanted subcutaneously into the flank (A375.S2,Calu-6,PA-1) or mammary fat pad (MDA-MB-468) of mice. Mice were randomized into groups of 5-7 individuals per group. ADCs or vehicle control (PBS) were administered intravenously by tail vein injection (10 mL/kg) following growth of established tumors (100-150 mm³). PA-1 ovarian cancer subcutaneous xenografts were treated with MGC018 or control ADC at 3 mg/kg as a single dose,QW4. Click to Show/Hide
In Vivo Model	Ovarian cancer CDX model
In Vitro Model	Ovarian mixed germ cell tumor	PA-1 cells		CVCL_0479
Experiment 18 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.60% (Day 70)	High MET expression (MET+++; IHC H-score=287)
Method Description	Human tumor cells (5x10⁶) were resuspended in 1:1 medium (DMEM/F-12) and Matrigel basement membrane matrix (Corning) and implanted subcutaneously into the flank (A375.S2,Calu-6,PA-1) or mammary fat pad (MDA-MB-468) of mice. Mice were randomized into groups of 5-7 individuals per group. ADCs or vehicle control (PBS) were administered intravenously by tail vein injection (10 mL/kg) following growth of established tumors (100-150 mm³). PA-1 ovarian cancer subcutaneous xenografts were treated with MGC018 or control ADC at 1 mg/kg QW4. Click to Show/Hide
In Vivo Model	Ovarian cancer CDX model
In Vitro Model	Ovarian mixed germ cell tumor	PA-1 cells		CVCL_0479
Experiment 19 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 96.70% (Day 70)	High MET expression (MET+++; IHC H-score=255)
Method Description	Human tumor cells (5x10⁶) were resuspended in 1:1 medium (DMEM/F-12) and Matrigel basement membrane matrix (Corning) and implanted subcutaneously into the flank (A375.S2,Calu-6,PA-1) or mammary fat pad (MDA-MB-468) of mice. Mice were randomized into groups of 5-7 individuals per group. ADCs or vehicle control (PBS) were administered intravenously by tail vein injection (10 mL/kg) following growth of established tumors (100-150 mm³). Calu-6 lung cancer subcutaneous xenografts were treated with MGC018 or control ADC at 6 mg/kg. Click to Show/Hide
In Vivo Model	Lung cancer CDX model
In Vitro Model	Lung adenocarcinoma	Calu-6 cells		CVCL_0236
Experiment 20 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.00% (Day 100)	Moderate MET expression (MET++; IHC H-score=150)
Method Description	Human tumor cells (5x10⁶) were resuspended in 1:1 medium (DMEM/F-12) and Matrigel basement membrane matrix (Corning) and implanted subcutaneously into the flank (A375.S2,Calu-6,PA-1) or mammary fat pad (MDA-MB-468) of mice. Mice were randomized into groups of 5-7 individuals per group. ADCs or vehicle control (PBS) were administered intravenously by tail vein injection (10 mL/kg) following growth of established tumors (100-150 mm³).MDA-MB-468 triple-negative breast cancer orthotopic xenografts were treated with MGC018 or control ADC at 1 mg/kg QW4. Click to Show/Hide
In Vivo Model	Triple-negative breast cancer CDX model
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 Luc cells		CVCL_0419
Experiment 21 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.60% (Day 80)	High MET expression (MET+++; IHC H-score=287)
Method Description	Human tumor cells (5x10⁶) were resuspended in 1:1 medium (DMEM/F-12) and Matrigel basement membrane matrix (Corning) and implanted subcutaneously into the flank (A375.S2,Calu-6,PA-1) or mammary fat pad (MDA-MB-468) of mice. Mice were randomized into groups of 5-7 individuals per group. ADCs or vehicle control (PBS) were administered intravenously by tail vein injection (10 mL/kg) following growth of established tumors (100-150 mm³). PA-1 ovarian cancer subcutaneous xenografts were treated with MGC018 or control ADC at 3 mg/kg as a single dose,Q2W4. Click to Show/Hide
In Vivo Model	Ovarian cancer CDX model
In Vitro Model	Ovarian mixed germ cell tumor	PA-1 cells		CVCL_0479
Experiment 22 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.90% (Day 100)	Moderate MET expression (MET++; IHC H-score=150)
Method Description	Human tumor cells (5x10⁶) were resuspended in 1:1 medium (DMEM/F-12) and Matrigel basement membrane matrix (Corning) and implanted subcutaneously into the flank (A375.S2,Calu-6,PA-1) or mammary fat pad (MDA-MB-468) of mice. Mice were randomized into groups of 5-7 individuals per group. ADCs or vehicle control (PBS) were administered intravenously by tail vein injection (10 mL/kg) following growth of established tumors (100-150 mm³). MDA-MB-468 triple-negative breast cancer orthotopic xenografts were treated with MGC018 or control ADC at 6 mg/kg. Click to Show/Hide
In Vivo Model	Triple-negative breast cancer CDX model
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 Luc cells		CVCL_0419
Experiment 23 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.10% (Day 60)	High MET expression (MET+++; IHC H-score=265)
Method Description	Human tumor cells (5x10⁶) were resuspended in 1:1 medium (DMEM/F-12) and Matrigel basement membrane matrix (Corning) and implanted subcutaneously into the flank (A375.S2,Calu-6,PA-1) or mammary fat pad (MDA-MB-468) of mice. Mice were randomized into groups of 5-7 individuals per group. ADCs or vehicle control (PBS) were administered intravenously by tail vein injection (10 mL/kg) following growth of established tumors (100-150 mm³). A375.S2 melanoma subcutaneous xenografts were treated with MGC018 or control ADC at 3 mg/kg. Click to Show/Hide
In Vivo Model	Melanoma CDX model
In Vitro Model	Amelanotic melanoma	A375.S2 cells		CVCL_0136
Experiment 24 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.60% (Day 70)	High MET expression (MET+++; IHC H-score=255)
Method Description	Human tumor cells (5x10⁶) were resuspended in 1:1 medium (DMEM/F-12) and Matrigel basement membrane matrix (Corning) and implanted subcutaneously into the flank (A375.S2,Calu-6,PA-1) or mammary fat pad (MDA-MB-468) of mice. Mice were randomized into groups of 5-7 individuals per group. ADCs or vehicle control (PBS) were administered intravenously by tail vein injection (10 mL/kg) following growth of established tumors (100-150 mm³). Calu-6 lung cancer subcutaneous xenografts were treated with MGC018 or control ADC at 10 mg/kg. Click to Show/Hide
In Vivo Model	Lung cancer CDX model
In Vitro Model	Lung adenocarcinoma	Calu-6 cells		CVCL_0236
Experiment 25 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.70% (Day 60)	High MET expression (MET+++; IHC H-score=265)
Method Description	Human tumor cells (5x10⁶) were resuspended in 1:1 medium (DMEM/F-12) and Matrigel basement membrane matrix (Corning) and implanted subcutaneously into the flank (A375.S2,Calu-6,PA-1) or mammary fat pad (MDA-MB-468) of mice. Mice were randomized into groups of 5-7 individuals per group. ADCs or vehicle control (PBS) were administered intravenously by tail vein injection (10 mL/kg) following growth of established tumors (100-150 mm³). A375.S2 melanoma subcutaneous xenografts were treated with MGC018 or control ADC at 1 mg/kg QW4. Click to Show/Hide
In Vivo Model	Melanoma CDX model
In Vitro Model	Amelanotic melanoma	A375.S2 cells		CVCL_0136

Revealed Based on the Cell Line Data

Click To Hide/Show 9 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	181.00 pM	High CD276 expression (CD276+++; 138,000 CD276 molecules/cell)
Method Description	MGC018-mediated in vitro cytotoxicity was evaluated across a set of tumor cell lines representing multiple cancer types expressing varying levels of B7-H3. MDA-MB-468,A375.S2,PA-1,Calu-6,Hs700T,SW48,and LN-229 tumor cell lines were obtained from ATCC and cultured in DMEM/F-12 media containing 10% FBS. NCI-H1703 and Raji tumor cell lines were obtained from ATCC and cultured in RPMI1640 media containing 10% FBS. Click to Show/Hide
In Vitro Model	Amelanotic melanoma	A375.S2 cells		CVCL_0136
Experiment 2 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	260.00 pM	High CD276 expression (CD276+++; 139,000 CD276 molecules/cell)
Method Description	MGC018-mediated in vitro cytotoxicity was evaluated across a set of tumor cell lines representing multiple cancer types expressing varying levels of B7-H3. MDA-MB-468,A375.S2,PA-1,Calu-6,Hs700T,SW48,and LN-229 tumor cell lines were obtained from ATCC and cultured in DMEM/F-12 media containing 10% FBS. NCI-H1703 and Raji tumor cell lines were obtained from ATCC and cultured in RPMI1640 media containing 10% FBS. Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	Calu-6 cells		CVCL_0236
Experiment 3 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	275.00 pM	High CD276 expression (CD276+++; 310,000 CD276 molecules/cell)
Method Description	MGC018-mediated in vitro cytotoxicity was evaluated across a set of tumor cell lines representing multiple cancer types expressing varying levels of B7-H3. MDA-MB-468,A375.S2,PA-1,Calu-6,Hs700T,SW48,and LN-229 tumor cell lines were obtained from ATCC and cultured in DMEM/F-12 media containing 10% FBS. NCI-H1703 and Raji tumor cell lines were obtained from ATCC and cultured in RPMI1640 media containing 10% FBS. Click to Show/Hide
In Vitro Model	Ovarian mixed germ cell tumor	PA-1 cells		CVCL_0479
Experiment 4 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	319.00 pM	High CD276 expression (CD276+++; 122,000 CD276 molecules/cell)
Method Description	MGC018-mediated in vitro cytotoxicity was evaluated across a set of tumor cell lines representing multiple cancer types expressing varying levels of B7-H3. MDA-MB-468,A375.S2,PA-1,Calu-6,Hs700T,SW48,and LN-229 tumor cell lines were obtained from ATCC and cultured in DMEM/F-12 media containing 10% FBS. NCI-H1703 and Raji tumor cell lines were obtained from ATCC and cultured in RPMI1640 media containing 10% FBS. Click to Show/Hide
In Vitro Model	Neoplasm	Hs 700T cells		CVCL_0858
Experiment 5 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	585.00 pM	Moderate MET expression (MET++; IHC H-score=180)
Method Description	MGC018-mediated in vitro cytotoxicity was evaluated across a set of tumor cell lines representing multiple cancer types expressing varying levels of B7-H3. MDA-MB-468,A375.S2,PA-1,Calu-6,Hs700T,SW48,and LN-229 tumor cell lines were obtained from ATCC and cultured in DMEM/F-12 media containing 10% FBS. NCI-H1703 and Raji tumor cell lines were obtained from ATCC and cultured in RPMI1640 media containing 10% FBS. Click to Show/Hide
In Vitro Model	Lung squamous cell carcinoma	NCI-H1703 cells		CVCL_1490
Experiment 6 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	767.00 pM	Moderate CD276 expression (CD276++; 57,000 CD276 molecules/cell)
Method Description	MGC018-mediated in vitro cytotoxicity was evaluated across a set of tumor cell lines representing multiple cancer types expressing varying levels of B7-H3. MDA-MB-468,A375.S2,PA-1,Calu-6,Hs700T,SW48,and LN-229 tumor cell lines were obtained from ATCC and cultured in DMEM/F-12 media containing 10% FBS. NCI-H1703 and Raji tumor cell lines were obtained from ATCC and cultured in RPMI1640 media containing 10% FBS. Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 7 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	910.00 pM	Moderate CD276 expression (CD276++; 73,700 CD276 molecules/cell)
Method Description	MGC018-mediated in vitro cytotoxicity was evaluated across a set of tumor cell lines representing multiple cancer types expressing varying levels of B7-H3. MDA-MB-468,A375.S2,PA-1,Calu-6,Hs700T,SW48,and LN-229 tumor cell lines were obtained from ATCC and cultured in DMEM/F-12 media containing 10% FBS. NCI-H1703 and Raji tumor cell lines were obtained from ATCC and cultured in RPMI1640 media containing 10% FBS. Click to Show/Hide
In Vitro Model	Glioblastoma	LN-229 cells		CVCL_0393
Experiment 8 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1447.00 pM	High CD276 expression (CD276+++; 153,000 CD276 molecules/cell)
Method Description	MGC018-mediated in vitro cytotoxicity was evaluated across a set of tumor cell lines representing multiple cancer types expressing varying levels of B7-H3. MDA-MB-468,A375.S2,PA-1,Calu-6,Hs700T,SW48,and LN-229 tumor cell lines were obtained from ATCC and cultured in DMEM/F-12 media containing 10% FBS. NCI-H1703 and Raji tumor cell lines were obtained from ATCC and cultured in RPMI1640 media containing 10% FBS. Click to Show/Hide
In Vitro Model	Colon adenocarcinoma	SW48 cells		CVCL_1724
Experiment 9 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10.00 nM	Moderate CD276 expression (CD276++; 59,800 CD276 molecules/cell)
Method Description	MGC018-mediated in vitro cytotoxicity was evaluated across a set of tumor cell lines representing multiple cancer types expressing varying levels of B7-H3. MDA-MB-468,A375.S2,PA-1,Calu-6,Hs700T,SW48,and LN-229 tumor cell lines were obtained from ATCC and cultured in DMEM/F-12 media containing 10% FBS. NCI-H1703 and Raji tumor cell lines were obtained from ATCC and cultured in RPMI1640 media containing 10% FBS. Click to Show/Hide
In Vitro Model	EBV-related Burkitt lymphoma	Raji cells		CVCL_0511

References

Ref 1	A Phase 2, Randomized, Open-label, Study of Two Dose Levels of Obramitamab Duocarmazine in Participants With Metastatic Castration-resistant Prostate Cancer, NCT05551117
Ref 2	Zilovertamab vedotin (MK 2140) in relapsed/refractory (R/R) diffuse large B-cell lymphoma (DLBCL): Early results from the phase 2 waveLINE-004 study. J Clin Oncol. 2023 41:16_suppl, 7531-7531.
Ref 3	A Phase 1/1b Dose Escalation and Cohort Expansion Study of MGC018 in Combination With Checkpoint Inhibitor in Participants With Advanced Solid Tumors, NCT05293496
Ref 4	Preclinical Development of MGC018, a Duocarmycin-based Antibody-drug Conjugate Targeting B7-H3 for Solid Cancer. Mol Cancer Ther. 2020 Nov;19(11):2235-2244.

If you find any error in data or bug in web service, please kindly report it to Dr. Shen et al.

Antibody-drug Conjugate Information

Citation

Visitor Map

Correspondence

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

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

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