Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0DIGSK
ADC Name	VCit ADC 3a
Synonyms	VCit-ADC-3a Click to Show/Hide
Drug Status	Investigative
Indication	In total 1 Indication(s) Breast cancer [ICD11:2C60-2C65] Investigative
Drug-to-Antibody Ratio	3.9
	3D MOL	2D MOL
Antibody Name	Anti-HER2 mAb glutamine 295 (Q295)		Antibody Info
Antigen Name	Receptor tyrosine-protein kinase erbB-2 (ERBB2)		Antigen Info
Payload Name	Monomethyl auristatin F		Payload Info
Therapeutic Target	Microtubule (MT)		Target Info
Linker Name	DBCO-PEG-VCit-PABC		Linker Info
Conjugate Type	MTGase-mediated conjugation (N297)

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)	≈ 100	%	KPL-4 cells	Breast inflammatory carcinoma

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)	0.1	nM	KPL-4 cells	Breast inflammatory carcinoma
Half Maximal Inhibitory Concentration (IC50)	> 100	nM	MDA-MB-231 cells	Breast adenocarcinoma

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)	≈ 100.00% (Day 18)	Positive HER2 expression (HER2+++/++)
Method Description	VCit ADC 3a (3 mg/kg, single dose) induces efficient tumor cell killing in cell line-derived models of KPL-4 cells with HER2 expression with high expression.
In Vivo Model	KPL-4 CDX model
In Vitro Model	Breast inflammatory carcinoma	KPL-4 cells		CVCL_5310

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)	0.10 nM-0.12 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were seeded in a culture-treated 96-well clear plate and incubated at 37°C under 5% CO₂ for 24h. Serially diluted samples (50L) were added to each well and the plate was incubated at 37°C for 72h.
In Vitro Model	Breast inflammatory carcinoma	KPL-4 cells		CVCL_5310
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative HER2 expression (HER2-)
Method Description	Cells were seeded in a culture-treated 96-well clear plate and incubated at 37°C under 5% CO₂ for 24h. Serially diluted samples (50L) were added to each well and the plate was incubated at 37°C for 72h.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

References

Ref 1	Glutamic acid-valine-citrulline linkers ensure stability and efficacy of antibody-drug conjugates in mice. Nat Commun. 2018 Jun 28;9(1):2512. doi: 10.1038/s41467-018-04982-3.