Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0ZSNLZ
ADC Name	ADAPT6-ABD-mcDM1
Synonyms	ADAPT6 ABD mcDM1 Click to Show/Hide
Drug Status	Investigative
Indication	In total 1 Indication(s) Ovarian cancer [ICD11:2C73] Investigative
Structure
	3D MOL	2D MOL
Antibody Name	ADAPT6-ABD		Antibody Info
Antigen Name	Receptor tyrosine-protein kinase erbB-2 (ERBB2)		Antigen Info
Payload Name	Mertansine DM1		Payload Info
Therapeutic Target	Microtubule (MT)		Target Info
Linker Name	Maleimidocaproyl (Ser3-Gly)3		Linker Info
Conjugate Type	The ADAPT fusion proteins were conjugated with mcDM1 at a molar ratio of 3:1 through coupling of the maleimide group in the mc-linker with the free thiol group of the C-terminal cysteine in the fusion proteins.

General Information of The Activity Data Related to This ADC

Discovered Using Cell Line-derived Xenograft Model

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

Standard Type	Value	Units	Cell Line	Disease Model
Tumor Growth Inhibition value (TGI)	≈ 83.3	%	SK-OV-3 cells	Ovarian serous cystadenocarcinoma

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)	5	nM	SK-BR-3 cells	Breast adenocarcinoma
Half Maximal Inhibitory Concentration (IC50)	7	nM	AU565 cells	Breast adenocarcinoma
Half Maximal Inhibitory Concentration (IC50)	80	nM	SK-OV-3 cells	Ovarian serous cystadenocarcinoma

Full List of Activity Data of This Antibody-drug Conjugate

Discovered Using Cell Line-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)	≈ 83.30% (Day 23)	High HER2 expression (HER2+++)
Method Description	The SKOV3 xenografts were established in female BALB/c nu/nu mice by subcutaneous implantation of 1 x10⁷ SKOV3 cells in 100 uL of medium in the abdominal region. The therapy started one week after the implantation. The mice were randomized in three groups (n = 910). One group of mice received intravenous (i.v.) injections of 13.3 mg/kg of ADAPT6-ABD-mcDM1 in 100 uL of PBS, the second group of mice received i.v. injections of the same dose of ADAPTNeg-ABD-mcDM1 in 100 uL of PBS, and the third group of mice received i.v. injections of 100 uL of PBS. Click to Show/Hide
In Vivo Model	ER2-expressing SKOV3 ovarian cancer xenograft model
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532

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					[2]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.00 nM	High HER2 expression (HER2+++)
Method Description	The cytotoxic potential of ADAPT6-ABD-mcDM1 was investigated by incubation of dilution series of the conjugate with cell lines having different HER2-expression levels.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.00 nM	High HER2 expression (HER2+++)
Method Description	The cytotoxic potential of ADAPT6-ABD-mcDM1 was investigated by incubation of dilution series of the conjugate with cell lines having different HER2-expression levels.
In Vitro Model	Breast adenocarcinoma	AU565 cells		CVCL_1074
Experiment 3 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	80.00 nM	High HER2 expression (HER2+++)
Method Description	The cytotoxic potential of ADAPT6-ABD-mcDM1 was investigated by incubation of dilution series of the conjugate with cell lines having different HER2-expression levels.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532

References

Ref 1	Experimental HER2-Targeted Therapy Using ADAPT6-ABD-mcDM1 in Mice Bearing SKOV3 Ovarian Cancer Xenografts: Efficacy and Selection of Companion Imaging Counterpart. Pharmaceutics. 2022 Aug 2;14(8):1612.
Ref 2	Targeting HER2 Expressing Tumors with a Potent Drug Conjugate Based on an Albumin Binding Domain-Derived Affinity Protein. Pharmaceutics. 2021 Nov 3;13(11):1847.