Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0KPUHG
ADC Name	WO2021115426A1 ADC-1
Synonyms	WO2021115426A1 ADC 1 Click to Show/Hide
Organization	Jiangsu Hengrui Pharmaceuticals Co., Ltd.
Drug Status	Investigative
Indication	In total 2 Indication(s) Gastric cancer [ICD11:2B72] Investigative Pancreatic cancer [ICD11:2C10] Investigative
Drug-to-Antibody Ratio	6.8
Structure
	3D MOL	2D MOL
Antibody Name	h1902-5		Antibody Info
Antigen Name	Claudin-18.2 (CLDN18.2)		Antigen Info
Payload Name	Undisclosed
Linker Name	WO2021115426A1 ADC-1 linker

General Information of The Activity Data Related to This ADC

Discovered Using Cell Line-derived Xenograft Model

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

Standard Type	Value	Units	Cell Line	Disease Model
Tumor Growth Inhibition value (TGI)	≈ 83.65	%	NUGC-4 cells	Gastric signet ring cell adenocarcinoma
Tumor Growth Inhibition value (TGI)	≈ 94.04	%	NUGC-4 cells	Gastric signet ring cell adenocarcinoma

Revealed Based on the Cell Line Data

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

Standard Type	Value	Units	Cell Line	Disease Model
Half Maximal Inhibitory Concentration (IC50)	0.12	nM	SK-BR-3 cells	Breast adenocarcinoma
Half Maximal Inhibitory Concentration (IC50)	0.23	nM	U-87MG cells	Glioblastoma

Full List of Activity Data of This Antibody-drug Conjugate

Discovered Using Cell Line-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)	≈ 83.65% (Day 31)	Moderate CLDN18.2 expression (CLDN18.2 ++)
Method Description	Conjugates of the exemplary anti-CLDN18.2 antibodies were tested using an established xenograft model of NUGC4 cells implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 3mpk of one of the conjugates listed above or with PBS only.
In Vivo Model	NUGC4 CDX model
In Vitro Model	Gastric signet ring cell adenocarcinoma	NUGC-4 cells		CVCL_3082
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.04% (Day 31)	Moderate CLDN18.2 expression (CLDN18.2 ++)
Method Description	Conjugates of the exemplary anti-CLDN18.2 antibodies were tested using an established xenograft model of NUGC4 cells implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 10mpk of one of the conjugates listed above or with PBS only.
In Vivo Model	NUGC4 CDX model
In Vitro Model	Gastric signet ring cell adenocarcinoma	NUGC-4 cells		CVCL_3082

Revealed Based on the Cell Line Data

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

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.12 nM	Positive CLDN18.2 expression (CLDN18.2 +++/++)
Method Description	Conjugate in various concentrations was added to CLDN18.2-expressing cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.23 nM	Positive CLDN18.2 expression (CLDN18.2 +++/++)
Method Description	Conjugate in various concentrations was added to CLDN18.2-expressing cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium.
In Vitro Model	Glioblastoma	U-87MG cells		CVCL_0022

References

Ref 1	Anti-claudin antibody-drug conjugate and pharmaceutical use thereof; 2021-06-17.