Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0IVKDI
ADC Name	Trastuzumab-alpha-amanitin conjugate 3
Synonyms	Trastuzumab alpha-amanitin conjugate 3 Click to Show/Hide
Organization	Heidelberg Pharma AG
Drug Status	Investigative
Indication	In total 2 Indication(s) Breast cancer [ICD11:2C60-2C65] Investigative Ovarian cancer [ICD11:2C73] Investigative
Drug-to-Antibody Ratio	2
	3D MOL	2D MOL
Antibody Name	Trastuzumab		Antibody Info
Antigen Name	Receptor tyrosine-protein kinase erbB-2 (ERBB2)		Antigen Info
Payload Name	Alpha-amanitin		Payload Info
Therapeutic Target	DNA-directed RNA polymerase II subunit RPB2 (POLR2B); DNA-directed RNA polymerase III subunit RPC7 (POLR3G)		Target Info
Linker Name	Trastuzumab-alpha-amanitin conjugate 3 linker
Conjugate Type	Random conjugation through nucleophilic lysines.

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)	≈ 71.25	%	CVCL_0532	Ovarian serous cystadenocarcinoma
Tumor Growth Inhibition value (TGI)	≈ 85.43	%	CVCL_0532	Ovarian serous cystadenocarcinoma

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)	≈ 71.25% (Day 87)	High HER2 expression (HER2 +++)
Method Description	A mouse tumor xenograft model, wherein 250,000,000 SKOV-3 ovarial carcinoma cellsare implated sub-cutaneously (s.c,) into SCID mice and allowed to grow for 10 days. After 10 days a single dose of 30 ug/kg body weight of various a-amanitin-Herceptin conjugates.
In Vivo Model	SK-OV-3 CDX model
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 85.43% (Day 87)	High HER2 expression (HER2 +++)
Method Description	A mouse tumor xenograft model, wherein 250,000,000 SKOV-3 ovarial carcinoma cellsare implated sub-cutaneously (s.c,) into SCID mice and allowed to grow for 10 days. After 10 days a single dose of 150 ug/kg body weight of various a-amanitin-Herceptin conjugates.
In Vivo Model	SK-OV-3 CDX model
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532

References

Ref 1	Amatoxin-armed therapeutic cell surface binding components designed for tumour therapy.