Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0QVUMQ
ADC Name	Trastuzumab-Gelonin
Synonyms	Trastuzumab Gelonin Click to Show/Hide
Drug Status	Investigative
Indication	In total 1 Indication(s) Gastric cancer [ICD11:2B72] Investigative
	3D MOL	2D MOL
Antibody Name	Trastuzumab		Antibody Info
Antigen Name	Receptor tyrosine-protein kinase erbB-2 (ERBB2)		Antigen Info
Payload Name	Gelonin		Payload Info
Therapeutic Target	Ribosome (RB)		Target Info
Linker Name	N-succinimidyl 4-(2-pyridyldithio) butanoate (SPDB)		Linker Info

General Information of The Activity Data Related to This ADC

Discovered Using Cell Line-derived Xenograft Model

Click To Hide/Show 3 Activity Data Related to This Level

Standard Type	Value	Units	Cell Line	Disease Model
Tumor Growth Inhibition value (TGI)	≈ 13.34	%	Gastric cancer cells	Gastric cancer
Tumor Growth Inhibition value (TGI)	≈ 50.57	%	Gastric cancer cells	Gastric cancer
Tumor Growth Inhibition value (TGI)	≈ 59.79	%	Gastric cancer cells	Gastric 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)	0.22±0.08	nM	NCI-N87 cells	Gastric tubular adenocarcinoma
Half Maximal Inhibitory Concentration (IC50)	555.00±69.60	nM	NCI-N87 cells	Gastric tubular adenocarcinoma

Full List of Activity Data of This Antibody-drug Conjugate

Discovered Using Cell Line-derived Xenograft Model

Click To Hide/Show 3 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 13.34% (Day 36)	High HER2 expression (HER2+++)
Method Description	The inhibitory activity of trastuzumab-gelonin against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 2.5 mg/kg.
In Vivo Model	Gastric cancer CDX model
In Vitro Model	Gastric cancer	Gastric cancer cells		Homo sapiens
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 50.57% (Day 36)	High HER2 expression (HER2+++)
Method Description	The inhibitory activity of trastuzumab-gelonin+LE8 against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 2.5 mg/kg.
In Vivo Model	Gastric cancer CDX model
In Vitro Model	Gastric cancer	Gastric cancer cells		Homo sapiens
Experiment 3 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 59.79% (Day 36)	High HER2 expression (HER2+++)
Method Description	The inhibitory activity of trastuzumab-gelonin+1HE against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 2.5 mg/kg.
In Vivo Model	Gastric cancer CDX model
In Vitro Model	Gastric cancer	Gastric 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)	0.22±0.08 nM	High HER2 expression (HER2+++)
Method Description	The inhibitory activity of trastuzumab-gelonin against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	555.00±69.60 nM	High HER2 expression (HER2+++)
Method Description	The inhibitory activity of unconjugated rGel against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

References

Ref 1	Transient Inhibition of Trastuzumab-Tumor Binding to Overcome the "Binding-Site Barrier" and Improve the Efficacy of a Trastuzumab-Gelonin Immunotoxin. Mol Cancer Ther. 2022 Oct 7;21(10):1573-1582.