Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0ZYOJI
ADC Name	EGFR ADC-21
Synonyms	EGFR-ADC-21 Click to Show/Hide
Drug Status	Investigative
Indication	In total 1 Indication(s) Lung cancer [ICD11:2C25] Investigative
Drug-to-Antibody Ratio	4
	3D MOL	2D MOL
Antibody Name	Cetuximab		Antibody Info
Antigen Name	Epidermal growth factor receptor (EGFR)		Antigen Info
Payload Name	Monomethyl auristatin E		Payload Info
Therapeutic Target	Microtubule (MT)		Target Info
Linker Name	Vinylsulfonamide based linker 15		Linker Info
Conjugate Type	Site-specific 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)	≈ 0	%	NCI-H2228 cells	Lung adenocarcinoma
Tumor Growth Inhibition value (TGI)	≈ 98.65	%	HCC827 cells	Lung 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)	0.5	nM	HCC827 cells	Lung adenocarcinoma
Half Maximal Inhibitory Concentration (IC50)	> 500	nM	NCI-H2228 cells	Lung 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)	≈ 0.00% (Day 40)	Negative EGFR expression (EGFR -)
Method Description	After acclimatization for one week, healthy mice were subcutaneously implanted with 5 x 10⁶ NCI-H2228 cells. Fourteen days after implantation the mice were divided into three groups (n = 8 each): 21, 22 and PBS as control. All the groups received four doses of 20 mg/kg on days 0, 4, 8 and 12, injected intravenously.
In Vivo Model	NCI-H2228 CDX model
In Vitro Model	Lung adenocarcinoma	NCI-H2228 cells		CVCL_1543
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.65% (Day 40)	Positive EGFR expression (EGFR +++/++)
Method Description	After acclimatization for one week, healthy mice were subcutaneously implanted with 5 x 10⁶ HCC827 cells. Fourteen days after implantation the mice were divided into three groups (n = 8 each): 21, 22 and PBS as control. All the groups received four doses of 20 mg/kg on days 0, 4, 8 and 12, injected intravenously.
In Vivo Model	HCC827 CDX model
In Vitro Model	Lung adenocarcinoma	HCC827 cells		CVCL_2063

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)	0.50 nM±0.10 nM	Positive EGFR expression (EGFR +++/++)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 10³ cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Lung adenocarcinoma	HCC827 cells		CVCL_2063
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 nM	Negative EGFR expression (EGFR -)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 10³ cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Lung adenocarcinoma	NCI-H2228 cells		CVCL_1543

References

Ref 1	Divinylsulfonamides enable the construction of homogeneous antibody-drug conjugates. Bioorg Med Chem. 2020 Dec 1;28(23):115793. doi: 10.1016/j.bmc.2020.115793. Epub 2020 Oct 6.