Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0YUEUP
ADC Name	EGFR-MMAU ADC
Synonyms	EGFR-MMAU-PABC-Cit-Val-MC-ADC Click to Show/Hide
Drug Status	Investigative
Indication	In total 1 Indication(s) Head and neck squamous carcinoma [ICD11:2C31] Investigative
Drug-to-Antibody Ratio	8
	3D MOL	2D MOL
Antibody Name	Cetuximab		Antibody Info
Antigen Name	Epidermal growth factor receptor (EGFR)		Antigen Info
Payload Name	Glucuronyl-monomethyl-auristatin E (MMAU)		Payload Info
Therapeutic Target	Microtubule (MT)		Target Info
Linker Name	Mc-Val-Cit-PABC		Linker Info
Conjugate Type	Random conjugation through reduced inter-chain cysteines.

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)	≈ 84.2	%	HSC-2 cells	Oral cavity squamous cell carcinoma
Tumor Growth Inhibition value (TGI)	≈ 86.3	%	HSC-2 cells	Oral cavity squamous cell carcinoma

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)	25	pM	NCI-H522 cells	Non-small cell lung carcinoma
Half Maximal Inhibitory Concentration (IC50)	30	pM	HCC1954 cells	Breast ductal 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)	≈ 84.20% (Day 33)	Positive EGFR expression (EGFR+++/++)
Method Description	MMAU ADCs (3 mg/kg, intravenously four times at seven day intervals) induces efficient tumor cell killing in cell line-derived models of HSC-2 cells with EGFR expression with high expression.
In Vivo Model	HSC-2 CDX model
In Vitro Model	Oral cavity squamous cell carcinoma	HSC-2 cells		CVCL_1287
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 86.30% (Day 33)	Positive EGFR expression (EGFR+++/++)
Method Description	MMAU ADCs (10 mg/kg, intravenously four times at seven day intervals) induces efficient tumor cell killing in cell line-derived models of HSC-2 cells with EGFR expression with high expression.
In Vivo Model	HSC-2 CDX model
In Vitro Model	Oral cavity squamous cell carcinoma	HSC-2 cells		CVCL_1287

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)	25.00 pM	Low EGFR expression (EGFR+)
Method Description	Cells were seeded in a culture-treated 96-well clear plate and incubated at 37°C under 5% CO₂ for 24h. Serially diluted samples (50L) were added to each well and the plate was incubated at 37°C for 72h.
In Vitro Model	Non-small cell lung carcinoma	NCI-H522 cells		CVCL_1567
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	30.00 pM	High EGFR expression (EGFR+++)
Method Description	Cells were seeded in a culture-treated 96-well clear plate and incubated at 37°C under 5% CO₂ for 24h. Serially diluted samples (50L) were added to each well and the plate was incubated at 37°C for 72h.
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259

References

Ref 1	Hydrophilic Auristatin Glycoside Payload Enables Improved Antibody-Drug Conjugate Efficacy and Biocompatibility. Antibodies (Basel). 2018 Mar 22;7(2):15. doi: 10.3390/antib7020015.