Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0YHHWC
ADC Name	N501-SN38
Synonyms	N501 SN38 Click to Show/Hide
Drug Status	Investigative
Indication	In total 2 Indication(s) Hepatocellular carcinoma [ICD11:2C12] Investigative Pancreatic cancer [ICD11:2C10] Investigative
Drug-to-Antibody Ratio	1
Structure
	3D MOL	2D MOL
Antibody Name	Anti-5T4 n501 (nanobody)		Antibody Info
Antigen Name	Trophoblast glycoprotein (TPBG)		Antigen Info
Payload Name	Active metabolite of irinotecan SN38		Payload Info
Therapeutic Target	DNA topoisomerase 1 (TOP1)		Target Info
Linker Name	CL2A		Linker Info
Conjugate Type	Site-specific conjugation through the engineered cysteine (THIOMAB).
Combination Type	Govitecan

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)	≈ 0	%	Pancreatic cancer cells	Pancreatic cancer
Tumor Growth Inhibition value (TGI)	≈ 62.93	%	Pancreatic cancer cells	Pancreatic cancer

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)	11.9	nM	BxPC-3 cells	Pancreatic ductal adenocarcinoma
Half Maximal Inhibitory Concentration (IC50)	49.8	nM	Huh-7 cells	Adult hepatocellular 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)	≈ 0.00% (Day 25)	High 5T4 expression (5T4+++)
Method Description	Treated with n501.
In Vivo Model	Pancreatic cancer CDX model
In Vitro Model	Pancreatic cancer	Pancreatic cancer cells		Homo sapiens
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 62.93% (Day 25)	High 5T4 expression (5T4+++)
Method Description	Treated with n501-SN38.
In Vivo Model	Pancreatic cancer CDX model
In Vitro Model	Pancreatic cancer	Pancreatic cancer cells		Homo sapiens

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)	11.90 nM	High 5T4 expression (5T4+++)
Method Description	Cells in the logarithmic phase of growth were collected and seeded in 96-well plates at a density of 510 3 cells/well and cultured overnight. The culture medium was removed and serial dilution ADCs or naked antibodies were added into the wells of 96-well plates in 200 L medium.
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	49.80 nM	Moderate 5T4 expression (5T4++)
Method Description	Cells in the logarithmic phase of growth were collected and seeded in 96-well plates at a density of 510 3 cells/well and cultured overnight. The culture medium was removed and serial dilution ADCs or naked antibodies were added into the wells of 96-well plates in 200 L medium.
In Vitro Model	Adult hepatocellular carcinoma	Huh-7 cells		CVCL_0336

References

Ref 1	A highly stable human single-domain antibody-drug conjugate exhibits superior penetration and treatment of solid tumors. Mol Ther. 2022 Aug 3;30(8):2785-2799.