Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0BCLOV
ADC Name	WO2022057651A1 ADC-20
Synonyms	WO2022057651A1 ADC 20 Click to Show/Hide
Organization	Sichuan Kelun Pharmaceutical Co., Ltd.
Drug Status	Investigative
Indication	In total 4 Indication(s) Bladder cancer [ICD11:2C94] Investigative Breast cancer [ICD11:2C60-2C65] Investigative Lung cancer [ICD11:2C25] Investigative Non-small cell lung cancer [ICD11:2C25] Investigative
Drug-to-Antibody Ratio	7.71
Structure
	3D MOL	2D MOL
Antibody Name	56HZ		Antibody Info
Antigen Name	Nectin-4 (NECTIN4)		Antigen Info
Payload Name	Undisclosed
Linker Name	WO2022057651A1 ADC-20 linker

General Information of The Activity Data Related to This ADC

Discovered Using Patient-derived Xenograft Model

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

Standard Type	Value	Units	Animal Model (No. of PDX)
Tumor Growth Inhibition value (TGI)	≈ 100	%	Bladder cancer PDX model (PDX: BL9200)

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)	≈ 98.33	%	NCI-H322M cells	Minimally invasive lung adenocarcinoma
Tumor Growth Inhibition value (TGI)	≈ 100	%	NCI-H322M cells	Minimally invasive lung 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 Effective Concentration (EC50)	1.1	ug/mL	NCI-N87 cells	Gastric tubular adenocarcinoma
Half Maximal Effective Concentration (EC50)	1.57	ug/mL	T24 cells	Bladder carcinoma

Full List of Activity Data of This Antibody-drug Conjugate

Discovered Using Patient-derived Xenograft Model

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

Experiment 1 Reporting the Activity Date of This ADC				[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 20)	Positive NECTIN4 expression (NECTIN4 +++/++)
Method Description	Conjugates of the exemplary antibodies were tested using an established PDX model of bladder cancer cell implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 3 mg/kg of one of the conjugates listed above or with PBS only.
In Vivo Model	Bladder cancer PDX model (PDX: BL9200)

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)	≈ 98.33% (Day 21)	Positive NECTIN4 expression (NECTIN4 +++/++)
Method Description	Conjugates of the exemplary antibodies were tested using an established xenograft model implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 3 mg/kg of one of the conjugates listed above or with PBS only.
In Vivo Model	NCI-H322M CDX model
In Vitro Model	Minimally invasive lung adenocarcinoma	NCI-H322M cells		CVCL_1557
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 21)	Positive NECTIN4 expression (NECTIN4 +++/++)
Method Description	Conjugates of the exemplary antibodies were tested using an established xenograft model implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 10 mg/kg of one of the conjugates listed above or with PBS only.
In Vivo Model	NCI-H322M CDX model
In Vitro Model	Minimally invasive lung adenocarcinoma	NCI-H322M cells		CVCL_1557

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 Effective Concentration (EC50)	1.10 ug/mL	Positive NECTIN4 expression (NECTIN4 +++/++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.57 ug/mL	High NECTIN4 expression (NECTIN4 +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Bladder carcinoma	T24 cells		CVCL_0554

References

Ref 1	Anti-nectin-4 antibody, conjugate including same, and application thereof; 2022-03-24.