Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0VUUXD
ADC Name	Trastuzumab-L6
Synonyms	Trastuzumab L6; TrastuzumabL6 Click to Show/Hide
Drug Status	Investigative
Indication	In total 3 Indication(s) Breast cancer [ICD11:2C60-2C65] Investigative Gastric tubular adenocarcinoma [ICD11:2E92] Investigative Pancreatic ductal adenocarcinoma [ICD11:2C10] Investigative
Drug-to-Antibody Ratio	4
	3D MOL	2D MOL
Antibody Name	Trastuzumab		Antibody Info
Antigen Name	Receptor tyrosine-protein kinase erbB-2 (ERBB2)		Antigen Info
Payload Name	MF-6		Payload Info
Therapeutic Target	DNA topoisomerase 1 (TOP1)		Target Info
Linker Name	Bridged PEG4-valine-alanine		Linker Info
Conjugate Type	Conjugated to two free sulfhydryl groups of the reduced antibody cysteine residues to form a bridge structure.
Combination Type	TS-L6

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)	≈ 95.8	%	NCI-N87 cells	Gastric tubular adenocarcinoma

Revealed Based on the Cell Line Data

Click To Hide/Show 4 Activity Data Related to This Level

Standard Type	Value	Units	Cell Line	Disease Model
Half Maximal Inhibitory Concentration (IC50)	0.24	nM	NCI-N87 cells	Gastric tubular adenocarcinoma
Half Maximal Inhibitory Concentration (IC50)	0.37	nM	SK-BR-3 cells	Breast adenocarcinoma
Half Maximal Inhibitory Concentration (IC50)	0.5	nM	BT-474 cells	Invasive breast carcinoma
Half Maximal Inhibitory Concentration (IC50)	3.25	nM	CT26.WT cells	Colon adenocarcinoma

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)	≈ 95.80%±14.40%	Positive HER2 expression (HER2+++/++)
Method Description	10 mg/kg TS-L6 administrated once weekly2 inhibited tumor growth in nude and nave mice.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Revealed Based on the Cell Line Data

Click To Hide/Show 4 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.24 nM	Positive HER2 expression (HER2+++/++)
Method Description	The cytotoxicity of MF-6, TS, and TS-L6 was assessed with three human cancer cell lines and a mouse cell line.
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)	0.37 nM	Positive HER2 expression (HER2+++/++)
Method Description	The cytotoxicity of MF-6, TS, and TS-L6 was assessed with three human cancer cell lines and a mouse cell line.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.50 nM	Positive HER2 expression (HER2+++/++)
Method Description	The cytotoxicity of MF-6, TS, and TS-L6 was assessed with three human cancer cell lines and a mouse cell line.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.25 nM	Low HER2 expression (HER2+)
Method Description	The cytotoxicity of MF-6, TS, and TS-L6 was assessed with three human cancer cell lines and a mouse cell line.
In Vitro Model	Colon adenocarcinoma	CT26.WT cells		CVCL_7256

References

Ref 1	A HER2-targeted antibody-novel DNA topoisomerase I inhibitor conjugate induces durable adaptive antitumor immunity by activating dendritic cells. MAbs. 2023 Jan-Dec;15(1):2220466. doi: 10.1080/19420862.2023.2220466.