Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0GVDPA
ADC Name
40H3-Deruxtecan
Synonyms
40H3 Deruxtecan
   Click to Show/Hide
Drug Status
Investigative
Indication
In total 1 Indication(s)
Triple negative breast cancer [ICD11:2C60-2C65]
Investigative
Drug-to-Antibody Ratio
7
Structure
Antibody Name
Anti-EGFR mAb 40H3
  Antibody Info 
Antigen Name
Epidermal growth factor receptor (EGFR)
  Antigen Info 
Payload Name
DX-8951 derivative (DXd)
  Payload Info 
Therapeutic Target
DNA topoisomerase 1 (TOP1)
  Target Info 
Linker Name
Mc-Gly-Gly-Phe-Gly
  Linker Info 
Conjugate Type
The free sulfhydryl group obtained by the reduction of interchain cysteine is site-specific conjugated with maleimide, michael addition reaction.
Combination Type
Deruxtecan
General Information of The Activity Data Related to This ADC
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal Inhibitory Concentration (IC50) 
9.32
nM
MDA-MB-468 cells
Breast adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
70.36
nM
BT-20 cells
Invasive breast carcinoma of no special type
Half Maximal Inhibitory Concentration (IC50) 
90.21
nM
A431 cells
Skin squamous cell carcinoma
Half Maximal Inhibitory Concentration (IC50) 
> 100
nM
MDA-MB-231 cells
Breast adenocarcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Revealed Based on the Cell Line Data
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 9.32 nM High EGFR expression (EGFR+++)
Method Description
1 x104 cells per well in a volume of 100 ul were plated in 96-well tissue culture plates. After 24 h, ADCs were added at the indicated concentrations. After 72 h, the medium was removed and the viability was determined using the CellTiter-Glo luminescent cell viability assay kit.
In Vitro Model Breast adenocarcinoma MDA-MB-468 cells CVCL_0419
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 70.36 nM Moderate EGFR expression (EGFR++)
Method Description
1 x104 cells per well in a volume of 100 ul were plated in 96-well tissue culture plates. After 24 h, ADCs were added at the indicated concentrations. After 72 h, the medium was removed and the viability was determined using the CellTiter-Glo luminescent cell viability assay kit.
In Vitro Model Invasive breast carcinoma of no special type BT-20 cells CVCL_0178
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 90.21 nM High EGFR expression (EGFR+++)
Method Description
1 x104 cells per well in a volume of 100 ul were plated in 96-well tissue culture plates. After 24 h, ADCs were added at the indicated concentrations. After 72 h, the medium was removed and the viability was determined using the CellTiter-Glo luminescent cell viability assay kit.
In Vitro Model Skin squamous cell carcinoma A431 cells CVCL_0037
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 100.00 nM Negative EGFR expression (EGFR-)
Method Description
1 x104 cells per well in a volume of 100 ul were plated in 96-well tissue culture plates. After 24 h, ADCs were added at the indicated concentrations. After 72 h, the medium was removed and the viability was determined using the CellTiter-Glo luminescent cell viability assay kit.
In Vitro Model Breast adenocarcinoma MDA-MB-231 cells CVCL_0062
References
Ref 1 Antibody drug conjugates, targeting cancer-expressed EGFR, exhibit potent and specific antitumor activity. Biomed Pharmacother. 2023 Jan;157:114047.

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