Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0ESHDB
ADC Name	M9346A-CX-DM1
Synonyms	M9346A CX DM1 Click to Show/Hide
Drug Status	Investigative
Indication	In total 1 Indication(s) Cervical cancer [ICD11:2C77] Investigative
Drug-to-Antibody Ratio	3-4
	3D MOL	2D MOL
Antibody Name	Mirvetuximab		Antibody Info
Antigen Name	Folate receptor alpha (FOLR1)		Antigen Info
Payload Name	Mertansine DM1		Payload Info
Therapeutic Target	Microtubule (MT)		Target Info
Linker Name	triglycyl peptide linker CX		Linker Info
Conjugate Type	Random conjugation through nucleophilic lysines.

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)	≈ 87.77	%	KB cells	Human papillomavirus-related endocervical adenocarcinoma
Tumor Growth Inhibition value (TGI)	≈ 88.3	%	KB cells	Human papillomavirus-related endocervical adenocarcinoma

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)	0.07	nM	KB cells	Human papillomavirus-related endocervical adenocarcinoma
Half Maximal Inhibitory Concentration (IC50)	8	nM	KB cells	Human papillomavirus-related endocervical 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	Tumor Growth Inhibition value (TGI)	≈ 87.77% (Day 23)	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	M9436A-CX-DM1 (200 ug/kg, every seven days x3) induces efficient tumor cell killing in cell line-derived models of KB cells with HER2 expression with high expression.
In Vivo Model	KB CDX model
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 88.30% (Day 23)	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	M9436A-CX-DM1 (100 ug/kg, every seven days x3) induces efficient tumor cell killing in cell line-derived models of KB cells with HER2 expression with high expression.
In Vivo Model	KB CDX model
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372

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)	0.07 nM	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	Cytotoxic IC50 Values (as a Function of [ADC] and [DM1]) for Various M9346A-CX-DM1 ADCs against FR-Expressing KB Cells in the absence of 1 M unconjugated M9346A antibody.
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	8.00 nM	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	Cytotoxic IC50 Values (as a Function of [ADC] and [DM1]) for Various M9346A-CX-DM1 ADCs against FOLR1-Expressing KB Cells in the presence of 1 M unconjugated M9346A antibody.
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372

References

Ref 1	A Case Study Comparing Heterogeneous Lysine- and Site-Specific Cysteine-Conjugated Maytansinoid Antibody-Drug Conjugates (ADCs) Illustrates the Benefits of Lysine Conjugation. Mol Pharm. 2019 Sep 3;16(9):3926-3937. doi: 10.1021/acs.molpharmaceut.9b00529. Epub 2019 Jul 31.