Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0AVDEL
ADC Name	Trastuzumab-PNUEDAGly5
Synonyms	Trastuzumab PNU EDA Gly5; Tras PNU EDA Gly5; Tras-PNUEDAGly5 Click to Show/Hide
Organization	NBE Therapeutics AG
Drug Status	Investigative
Indication	In total 1 Indication(s) Breast cancer [ICD11:2C60-2C65] Investigative
Drug-to-Antibody Ratio	3.9
Structure
	3D MOL	2D MOL
Antibody Name	Trastuzumab		Antibody Info
Antigen Name	Receptor tyrosine-protein kinase erbB-2 (ERBB2)		Antigen Info
Payload Name	PNU-159682		Payload Info
Therapeutic Target	DNA topoisomerase 2-alpha (TOP2A)		Target Info
Linker Name	LPETG-Gly5-EDA		Linker Info
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 1 Activity Data Related to This Level

Standard Type	Value	Units	Cell Line	Disease Model
Tumor Growth Inhibition value (TGI)	≈ 100	%	EMT6 cells (High HER2 expression)	Mammary gland malignant neoplasms

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)	6.9	ng/mL	Karpas-299 cells	ALK-positive anaplastic large cell lymphoma
Half Maximal Effective Concentration (EC50)	< 10	ug/mL	L-428 cells	Hodgkin lymphoma

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 60)	Positive HER2 expression (HER2 +++/++)
Method Description	1,000,000 EMT6 mouse breast cancer cells expressing human HER-2 previously determined to be suitable for in vivo growth, were implanted into theright mammary fat pads of female Balb/c mice. Animals were treated onthe same day (day 13) and 7 days later (day 20) byintravenous injection of the reference ADC Kadcyla (15 mg/kg), Trastuzumab-PNU-EDA-Glys (1 mg/kg) or vehicle control. Click to Show/Hide
In Vivo Model	EMT6 CDX model (Expressing hHER2)
In Vitro Model	Mammary gland malignant neoplasms	EMT6 cells (High HER2 expression)		CVCL_1923

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					[2]
Efficacy Data	Half Maximal Effective Concentration (EC50)	6.90 ng/mL	High CD30 expression (CD30 +++)
Method Description	Dose response of the cytotoxic effects of the indicated ADCs on human Non-Hodgkin lymphoma cell line Karpas-299, and on human Hodgkin lymphoma cell line L428 cells.
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324
Experiment 2 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Effective Concentration (EC50)	< 10.00 ug/mL	Low CD30 expression (CD30 +)
Method Description	Dose response of the cytotoxic effects of the indicated ADCs on human Non-Hodgkin lymphoma cell line Karpas-299, and on human Hodgkin lymphoma cell line L428 cells.
In Vitro Model	Hodgkin lymphoma	L-428 cells		CVCL_1361

References

Ref 1	Novel b7-h3 binding molecules, antibody drug conjugates thereof and methods of use thereof; 2017-10-19.
Ref 2	Binding protein drug conjugates comprising anthracycline derivatives; 2016-06-30.