Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0ZQKIT
ADC Name	Anti-FucGM1-46 ADC
Synonyms	Anti-FucGM1 46 ADC Click to Show/Hide
Drug Status	Investigative
Indication	In total 1 Indication(s) Small cell lung cancer [ICD11:2C25] Investigative
Drug-to-Antibody Ratio	1.9
	3D MOL	2D MOL
Antibody Name	Anti-FucGM1 mAb		Antibody Info
Antigen Name	Fucosylated monosialotetrahexosylganglioside (FucGM1)		Antigen Info
Payload Name	Tetrahydroisoquinoline-based PBD dimer 17		Payload Info
Therapeutic Target	Human Deoxyribonucleic acid (hDNA)		Target Info
Linker Name	PEG2-Val-Cit-PABC		Linker Info
Conjugate Type	Bacterial transglutaminase (BTGase)-mediated site-specific conjugation (Q295).

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)	≈ 61.24	%	NCI-H187 cells	Lung small cell carcinoma
Tumor Growth Inhibition value (TGI)	≈ 97.58	%	NCI-H187 cells	Lung small cell carcinoma

Revealed Based on the Cell Line Data

Click To Hide/Show 1 Activity Data Related to This Level

Standard Type	Value	Units	Cell Line	Disease Model
Half Maximal Inhibitory Concentration (IC50)	2.2	nM	NCI-H187 cells	Lung small cell 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)	≈ 61.24%	Positive FucGM1 expression (FucGM1+++/++)
Method Description	Female CB-17 SCID mice were each inoculated in the flank area with the 5 million tumor cells. To examine the efficacy of anti-FucGM1 ADC-45, mice were dosed with a single IP administration of 0.005 mol/kg.
In Vivo Model	H187 CDX model
In Vitro Model	Lung small cell carcinoma	NCI-H187 cells		CVCL_1501
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.58%	Positive FucGM1 expression (FucGM1+++/++)
Method Description	Female CB-17 SCID mice were each inoculated in the flank area with the 5 million tumor cells. To examine the efficacy of anti-FucGM1 ADC-45, mice were dosed with a single IP administration of 0.02 mol/kg.
In Vivo Model	H187 CDX model
In Vitro Model	Lung small cell carcinoma	NCI-H187 cells		CVCL_1501

Revealed Based on the Cell Line Data

Click To Hide/Show 1 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.20 nM	Positive FucGM1 expression (FucGM1+++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Lung small cell carcinoma	NCI-H187 cells		CVCL_1501

References

Ref 1	Design, Synthesis, and Structure-Activity Relationships of Novel Tetrahydroisoquinolino Benzodiazepine Dimer Antitumor Agents and Their Application in Antibody-Drug Conjugates. J Med Chem. 2020 Nov 25;63(22):13913-13950. doi: 10.1021/acs.jmedchem.0c01385.