ADC ID	DRG0JBTBO
ADC Name	GPC-1-ADC
Synonyms	GPC-1-mc-vc-PABC-MMAF    Click to Show/Hide
Drug Status	Investigative
Indication	In total 1 Indication(s) Pancreatic cancer [ICD11:2C10] Investigative
Drug-to-Antibody Ratio	4.1
	3D MOL			2D MOL
Antibody Name	Anti-GPC1 mAb clone 01a033					Antibody Info
Antigen Name	Glypican-1 (GPC1)					Antigen Info
Payload Name	Monomethyl auristatin F					Payload Info
Therapeutic Target	Microtubule (MT)					Target Info
Linker Name	Mc-Val-Cit-PABC					Linker Info
Conjugate Type	Random conjugation through reduced inter-chain cysteines.

Standard Type	Value	Units	Animal Model (No. of PDX)
Tumor Growth Inhibition value (TGI)	≈ 22.63	%	Pancreatic cancer PDX model
Tumor Growth Inhibition value (TGI)	≈ 29.66	%	Pancreatic cancer PDX model
Tumor Growth Inhibition value (TGI)	≈ 69.22	%	Pancreatic cancer PDX model

Standard Type	Value	Units	Cell Line	Disease Model
Tumor Growth Inhibition value (TGI)	≈ 71.97	%	BxPC-3 cells	Pancreatic ductal adenocarcinoma
Tumor Growth Inhibition value (TGI)	≈ 85	%	BxPC-3 cells	Pancreatic ductal adenocarcinoma
Tumor Growth Inhibition value (TGI)	≈ 96	%	BxPC-3 cells	Pancreatic ductal adenocarcinoma

Standard Type	Value	Units	Cell Line	Disease Model
Half Maximal Inhibitory Concentration (IC50)	0.06	nM	BxPC-3 cells	Pancreatic ductal adenocarcinoma
Half Maximal Inhibitory Concentration (IC50)	0.24	nM	T3M-4 cells	Pancreatic ductal adenocarcinoma
Half Maximal Inhibitory Concentration (IC50)	> 100	nM	SUIT-2 cells	Pancreatic ductal adenocarcinoma

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 22.63% (Day 28)	Positive GPC-1 expression (GPC-1 +++/++)
Method Description	Tumour volumes reached >100 mm3, the mice were randomly divided into five groups (six per group). PBS, control ADC (10 mg/kg) or GPC-1-ADC (1 mg/kg) was injected from caudal veins every 4 days until four doses had been administered.
In Vivo Model	Pancreatic cancer PDX model
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 29.66% (Day 28)	Positive GPC-1 expression (GPC-1 +++/++)
Method Description	Tumour volumes reached >100 mm3, the mice were randomly divided into five groups (six per group). PBS, control ADC (10 mg/kg) or GPC-1-ADC (3 mg/kg) was injected from caudal veins every 4 days until four doses had been administered.
In Vivo Model	Pancreatic cancer PDX model
Experiment 3 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 69.22% (Day 28)	Positive GPC-1 expression (GPC-1 +++/++)
Method Description	Tumour volumes reached >100 mm3, the mice were randomly divided into five groups (six per group). PBS, control ADC (10 mg/kg) or GPC-1-ADC (10 mg/kg) was injected from caudal veins every 4 days until four doses had been administered.
In Vivo Model	Pancreatic cancer PDX model

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 71.97% (Day 36)	Positive GPC-1 expression (GPC-1 +++/++)
Method Description	Tumour-bearing mice were intravenously administered PBS, control ADC or GPC-1-ADC (1 mg/kg) on days 0, 4, 8 and 12.
In Vivo Model	BxPC-3 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 85.00% (Day 36)	Positive GPC-1 expression (GPC-1 +++/++)
Method Description	Tumour-bearing mice were intravenously administered PBS, control ADC or GPC-1-ADC (3 mg/kg) on days 0, 4, 8 and 12.
In Vivo Model	BxPC-3 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 3 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 96.00% (Day 36)	Positive GPC-1 expression (GPC-1 +++/++)
Method Description	Tumour-bearing mice were intravenously administered PBS, control ADC (10 mg/kg ) or GPC-1-ADC (10 mg/kg) on days 0, 4, 8 and 12, once every 4 days for a total of four doses.
In Vivo Model	BxPC-3 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.06 nM	Positive GPC-1 expression (GPC-1 +++/++)
Method Description	IC50 of MMAF and anti-glypican-1 ADC in human pancreatic cancer cell lines.
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.24 nM	Positive GPC-1 expression (GPC-1 +++/++)
Method Description	IC50 of MMAF and anti-glypican-1 ADC in human pancreatic cancer cell lines.
In Vitro Model	Pancreatic ductal adenocarcinoma	T3M-4 cells		CVCL_4056
Experiment 3 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative GPC-1 expression (GPC-1 -)
Method Description	IC50 of MMAF and anti-glypican-1 ADC in human pancreatic cancer cell lines.
In Vitro Model	Pancreatic ductal adenocarcinoma	SUIT-2 cells		CVCL_3172

Ref 1	Anti-glypican-1 antibody-drug conjugate is a potential therapy against pancreatic cancer. Br J Cancer. 2020 Apr;122(9):1333-1341. doi: 10.1038/s41416-020-0781-2. Epub 2020 Mar 10.