Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0RFTFM
ADC Name	EGFRvIII-16
Synonyms	EGFRvIII 16 Click to Show/Hide
Drug Status	Investigative
Indication	In total 2 Indication(s) Astrocytoma [ICD11:2F36] Investigative Uterine cancer [ICD11:2C78] Investigative
Drug-to-Antibody Ratio	3
	3D MOL	2D MOL
Antibody Name	Anti-EGFRvIII mAb		Antibody Info
Antigen Name	Epidermal growth factor receptor variant III (EGFRvIII)		Antigen Info
Payload Name	DM1 derivative 16		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 1 Activity Data Related to This Level

Standard Type	Value	Units	Cell Line	Disease Model
Tumor Growth Inhibition value (TGI)	≈ 90	%	MMT-060562 cells	Malignant neoplasms of the mouse mammary gland

Revealed Based on the Cell Line Data

Click To Hide/Show 3 Activity Data Related to This Level

Standard Type	Value	Units	Cell Line	Disease Model
Half Maximal Inhibitory Concentration (IC50)	0.3	nM	U-251MG cells	Astrocytoma
Half Maximal Inhibitory Concentration (IC50)	0.3	nM	MMT-060562 cells	Malignant neoplasms of the mouse mammary gland
Half Maximal Inhibitory Concentration (IC50)	0.4	nM	HEK293 cells	Normal

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)	≈ 90.00% (Day 25)	Positive EGFR vIII expression (EGFR vIII+++/++)
Method Description	ADCs were dosed at 1 and 5 mg/kg in a single dose and once weekly for 3 weeks.
In Vivo Model	MMT CDX model
In Vitro Model	Malignant neoplasms of the mouse mammary gland	MMT-060562 cells		CVCL_4241

Revealed Based on the Cell Line Data

Click To Hide/Show 3 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.30 nM	Positive EGFR vIII expression (EGFR vIII+++/++)
Method Description	Cells were seeded in PDL-coated 96 well plates at 375 for MMT/hEGFRvIII, 1500 for U251/hEGFRvIII, 2000 for HEK293/hEGFRvIII, or 3000 for C4-2, PC3, and T47D cells per well in complete growth media and grown overnight.
In Vitro Model	Astrocytoma	U-251MG cells		CVCL_0021
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.30 nM	Positive EGFR vIII expression (EGFR vIII+++/++)
Method Description	Cells were seeded in PDL-coated 96 well plates at 375 for MMT/hEGFRvIII, 1500 for U251/hEGFRvIII, 2000 for HEK293/hEGFRvIII, or 3000 for C4-2, PC3, and T47D cells per well in complete growth media and grown overnight.
In Vitro Model	Malignant neoplasms of the mouse mammary gland	MMT-060562 cells		CVCL_4241
Experiment 3 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.40 nM	Positive EGFR vIII expression (EGFR vIII+++/++)
Method Description	Cells were seeded in PDL-coated 96 well plates at 375 for MMT/hEGFRvIII, 1500 for U251/hEGFRvIII, 2000 for HEK293/hEGFRvIII, or 3000 for C4-2, PC3, and T47D cells per well in complete growth media and grown overnight.
In Vitro Model	Normal	HEK293 cells		CVCL_0045

References

Ref 1	Antibody drug conjugates of cleavable amino-alkyl and aryl maytansinoids. Bioorg Med Chem. 2018 May 15;26(9):2271-2279. doi: 10.1016/j.bmc.2018.02.025. Epub 2018 Feb 21.