Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0UJXGX
ADC Name	HuIgG1-19
Synonyms	HuIgG1 19 Click to Show/Hide
Drug Status	Investigative
Indication	In total 1 Indication(s) Uterine sarcoma [ICD11:2C72] Investigative
	3D MOL	2D MOL
Antibody Name	Undisclosed
Antigen Name	Epidermal growth factor receptor (EGFR); Receptor tyrosine-protein kinase erbB-3 (ERBB3)		Antigen Info
Payload Name	PNU-159682		Payload Info
Therapeutic Target	DNA topoisomerase 2-alpha (TOP2A)		Target Info
Linker Name	Hydrophilic cleavable linker 19		Linker Info

General Information of The Activity Data Related to This ADC

Discovered Using Patient-derived Xenograft Model

Click To Hide/Show 2 Activity Data Related to This Level

Standard Type	Value	Units	Animal Model (No. of PDX)
Tumor Growth Inhibition value (TGI)	≈ 13.33	%	Non-small cell lung cancer PDX model (PDX: LU253 PDX)
Tumor Growth Inhibition value (TGI)	≈ 21.34	%	Colorectal cancer PDX model (PDX: CR188 PDX)

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)	> 3	nM	MES-SA cells	Uterine sarcoma
Half Maximal Effective Concentration (EC50)	3.8	nM	HEK293T cells	Normal

Full List of Activity Data of This Antibody-drug Conjugate

Discovered Using Patient-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)	≈ 13.33% (Day 30	Positive CD46 expression (CD46 +++/++)
Method Description	In vivo efficacy of PNU-conjugated ADCs in NSCLC LU253 PDX subcutaneous models in NOD/SCID mice. A single dose of 1.0 mg/kg HuIgG1-19 ADC.
In Vivo Model	Non-small cell lung cancer PDX model (PDX: LU253 PDX)
Experiment 2 Reporting the Activity Date of This ADC				[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 21.34% (Day 15)	Positive CD46 expression (CD46 +++/++)
Method Description	In vivo efficacy of PNU-conjugated ADCs in colorectal CR188 PDX subcutaneous models in NOD/SCID mice. A single dose of 1.0 mg/kg HuIgG1-19 ADC.
In Vivo Model	Colorectal cancer PDX model (PDX: CR188 PDX)

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 Effective Concentration (EC50)	> 3.00 nM	Positive CD46 expression (CD46 +++/++)
Method Description	Cells were seeded at 5000 per well in a 96-well plate in complete RPMI 1640. Antibody-ZAP complexes (Advanced Targeting Systems; produced according to manufacturer's instructions) or ADCs were added to the cells and plates incubated for 72 hours and 5% carbon dioxide.
In Vitro Model	Uterine sarcoma	MES-SA cells		CVCL_1404
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	3.80 nM	Positive CD46 expression (CD46 +++/++)
Method Description	Cells were seeded at 5000 per well in a 96-well plate in complete RPMI 1640. Antibody-ZAP complexes (Advanced Targeting Systems; produced according to manufacturer's instructions) or ADCs were added to the cells and plates incubated for 72 hours and 5% carbon dioxide.
In Vitro Model	Normal	HEK293T cells		CVCL_0063

References

Ref 1	Evaluation of PNU-159682 antibody drug conjugates (ADCs). Bioorg Med Chem Lett. 2020 Dec 15;30(24):127640. doi: 10.1016/j.bmcl.2020.127640. Epub 2020 Oct 28.