Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0AWQJG
ADC Name	PF-06804103
Synonyms	PF 06804103; PF06804103; anti-HER2-vc0101; anti-HER2-vcAur0101 ADC; Anti-NG-HER2 ADC; NG-HER2 ADC; Anti-HER2 ADC (Pfizer Inc.) Click to Show/Hide
Organization	Pfizer Inc.
Drug Status	Phase 1
Indication	In total 1 Indication(s) Breast cancer [ICD11:2C60-2C65] Phase 1
Drug-to-Antibody Ratio	4
Structure
	3D MOL	2D MOL
Antibody Name	T-(kK183C+K290C)		Antibody Info
Antigen Name	Receptor tyrosine-protein kinase erbB-2 (ERBB2)		Antigen Info
Payload Name	Auristatin 0101		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	Vc0101
TTD ID	D09ATR

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)	100	%	NCI-N87 cells	Gastric tubular adenocarcinoma
Tumor Growth Inhibition value (TGI)	100	%	BT474-M1 cells	Invasive breast carcinoma

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)	100.00%	High HER2 expression (HER2+++)
Method Description	In cell line xenograft (CLX) studies, nude mice were injected subcutaneously in the flank with suspensions of 1 x10⁶ NCI-N87, in 50% Matrigel (BD Biosciences). Mice were randomized into study groups when tumors reached approximately 150-300 mm³. Either PBS (Gibco, catalog no., 14190-144, as vehicle), PF-06804103, or PT-DM1 at different doses was administered intravenously starting on day 0 for a total of four doses, 4 days apart (four times every 4 days). Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100.00%	Moderate HER2 expression (HER2++)
Method Description	In cell line xenograft (CLX) studies, nude mice were injected subcutaneously in the flank with suspensions of 10 x10⁶ BT474 cells, in 50% Matrigel (BD Biosciences). Mice were randomized into study groups when tumors reached approximately 150-300 mm³. Either PBS (Gibco, catalog no., 14190-144, as vehicle), PF-06804103, or PT-DM1 at different doses was administered intravenously starting on day 0 for a total of four doses, 4 days apart (four times every 4 days). Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT474-M1 cells		CVCL_0179

References

Ref 1	PF-06804103, A Site-specific Anti-HER2 Antibody-Drug Conjugate for the Treatment of HER2-expressing Breast, Gastric, and Lung Cancers. Mol Cancer Ther. 2020 Oct;19(10):2068-2078.