Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0UYWZI
ADC Name	GPC1-ADC-MMAE
Synonyms	GPC1 ADC (MMAE) Click to Show/Hide
Drug Status	Investigative
Indication	In total 2 Indication(s) Esophageal squamous cell carcinoma [ICD11:2B71] Investigative Pancreatic cancer [ICD11:2C10] Investigative
Drug-to-Antibody Ratio	4.01
Structure
	3D MOL	2D MOL
Antibody Name	Anti-GPC1 GPC1-ADC (MMAE) mAb		Antibody Info
Antigen Name	Glypican-1 (GPC1)		Antigen Info
Payload Name	Monomethyl auristatin E		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.
Combination Type	Vedotin

General Information of The Activity Data Related to This ADC

Discovered Using Patient-derived Xenograft Model

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

Standard Type	Value	Units	Animal Model (No. of PDX)
Tumor Growth Inhibition value (TGI)	≈ 88.8	%	Pancreatic cancer PDX model (PDX: PK645)
Tumor Growth Inhibition value (TGI)	≈ 98.7	%	Pancreatic cancer PDX model (PDX: PK565)

Revealed Based on the Cell Line Data

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

Standard Type	Value	Units	Cell Line	Disease Model
Half Maximal Inhibitory Concentration (IC50)	80.9	pM	KP-2 cells	Pancreatic carcinoma
Half Maximal Inhibitory Concentration (IC50)	0.55	nM	PK-8 cells	Pancreatic ductal adenocarcinoma
Half Maximal Inhibitory Concentration (IC50)	0.68	nM	BxPC-3 cells	Pancreatic ductal adenocarcinoma

Full List of Activity Data of This Antibody-drug Conjugate

Discovered Using Patient-derived Xenograft Model

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

Experiment 1 Reporting the Activity Date of This ADC				[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 88.80% (Day 35)	High GPC1 expression (GPC1+++)
In Vivo Model	Pancreatic cancer PDX model (PDX: PK645)
Experiment 2 Reporting the Activity Date of This ADC				[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.70% (Day 28)	High GPC1 expression (GPC1+++)
In Vivo Model	Pancreatic cancer PDX model (PDX: PK565)

Revealed Based on the Cell Line Data

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

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	80.90 pM	High GPC1 expression (GPC1+++)
Method Description	GPC1-ADC(MMAE) induces efficient tumor cell killing in cells PDX models from a Pancreatic ductal adenocarcinoma (PDAC) patient with GPC1 expression.
In Vitro Model	Pancreatic carcinoma	KP-2 cells		CVCL_3004
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.55 nM	High GPC1 expression (GPC1+++)
Method Description	GPC1-ADC(MMAE) induces efficient tumor cell killing in cells PDX models from a Pancreatic ductal adenocarcinoma (PDAC) patient with GPC1 expression.
In Vitro Model	Pancreatic ductal adenocarcinoma	PK-8 cells		CVCL_4718
Experiment 3 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.68 nM	High GPC1 expression (GPC1+++)
Method Description	GPC1-ADC(MMAE) induces efficient tumor cell killing in cells PDX models from a Pancreatic ductal adenocarcinoma (PDAC) patient with GPC1 expression.
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186

References

Ref 1	Glypican-1 Is a Novel Target for Stroma and Tumor Cell Dual-Targeting Antibody-Drug Conjugates in Pancreatic Cancer. Mol Cancer Ther. 2021 Dec;20(12):2495-2505.