Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0QMQKQ
ADC Name	Trastuzumab-AJICAP-maytansinoid
Synonyms	Trastuzumab AJICAP maytansinoid Click to Show/Hide
Drug Status	Investigative
Indication	In total 1 Indication(s) Gastric cancer [ICD11:2B72] Investigative
Drug-to-Antibody Ratio	2
Structure
	3D MOL	2D MOL
Antibody Name	Trastuzumab		Antibody Info
Antigen Name	Receptor tyrosine-protein kinase erbB-2 (ERBB2)		Antigen Info
Payload Name	Mertansine DM1		Payload Info
Therapeutic Target	Microtubule (MT)		Target Info
Linker Name	AJICAP		Linker Info
Conjugate Type	AJICAP site-specific conjugation to synthesize, and ADC conjugation site-occupancy at Lys 248 in the antibody Fc region.

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
Minimal Effective Dose (MED)	< 5	mg/kg	NCI-N87 cells	Gastric tubular adenocarcinoma
Maximum Tolerated Dose (MTD)	> 120	mg/kg	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 2 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Minimal Effective Dose (MED)	< 5.00 mg/kg	High HER2 expression (HER2+++)
Method Description	Following the acclimatization period (1 week), the animals were stratified by body weight and randomly assigned to the following group: three trastuzumab-AJICAP-maytansinoid groups, treated with 20 mg/kg, 60 mg/kg, and 120 mg/kg. Each group consisted of five animals for blood chemistry test as well as five animals for clinical signs and body weight measurements. Click to Show/Hide
In Vivo Model	Gastric cancer CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Maximum Tolerated Dose (MTD)	> 120.00 mg/kg	High HER2 expression (HER2+++)
Method Description	Following the acclimatization period (1 week), the animals were stratified by body weight and randomly assigned to the following group: three trastuzumab-AJICAP-maytansinoid groups, treated with 20 mg/kg, 60 mg/kg, and 120 mg/kg. Each group consisted of five animals for blood chemistry test as well as five animals for clinical signs and body weight measurements. Click to Show/Hide
In Vivo Model	Gastric cancer CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

References

Ref 1	Biological Evaluation of Maytansinoid-Based Site-Specific Antibody-Drug Conjugate Produced by Fully Chemical Conjugation Approach: AJICAP. Front Biosci (Landmark Ed). 2022 Aug 5;27(8):234.