Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0PBWRV
ADC Name
Anti-FucGM1-45 ADC
Synonyms
Anti-FucGM1 45 ADC
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Drug Status
Investigative
Indication
In total 1 Indication(s)
Small cell lung cancer [ICD11:2C25]
Investigative
Drug-to-Antibody Ratio
2.5
Antibody Name
Anti-FucGM1 mAb
  Antibody Info 
Antigen Name
Fucosylated monosialotetrahexosylganglioside (FucGM1)
  Antigen Info 
Payload Name
Tetrahydroisoquinoline-based PBD dimer 17
  Payload Info 
Therapeutic Target
Human Deoxyribonucleic acid (hDNA)
  Target Info 
Linker Name
Mc-Val-Cit-PABC
  Linker Info 
Conjugate Type
Random heterogeneous lysine conjugation
General Information of The Activity Data Related to This ADC
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 5 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Tumor Growth Inhibition value (TGI) 
≈ 30.8
%
NCI-H187 cells
Lung small cell carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 86.48
%
NCI-H187 cells
Lung small cell carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 97.07
%
NCI-H187 cells
Lung small cell carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 100
%
NCI-H187 cells
Lung small cell carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 100
%
NCI-H187 cells
Lung small cell carcinoma
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Half Maximal Inhibitory Concentration (IC50) 
1
nM
NCI-H187 cells
Lung small cell carcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 5 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 30.80% Positive FucGM1 expression (FucGM1+++/++)
Method Description
Female CB-17 SCID mice were each inoculated in the flank area with the 5 million tumor cells. To examine the efficacy of anti-FucGM1 ADC-45, mice were dosed with a single IP administration of 0.005 mol/kg.
In Vivo Model H187 CDX model
In Vitro Model Lung small cell carcinoma NCI-H187 cells CVCL_1501
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 86.48% Positive FucGM1 expression (FucGM1+++/++)
Method Description
Female CB-17 SCID mice were each inoculated in the flank area with the 5 million tumor cells. To examine the efficacy of anti-FucGM1 ADC-45, mice were dosed with a single IP administration of 0.02 mol/kg.
In Vivo Model H187 CDX model
In Vitro Model Lung small cell carcinoma NCI-H187 cells CVCL_1501
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 97.07% Positive FucGM1 expression (FucGM1+++/++)
Method Description
Female CB-17 SCID mice were each inoculated in the flank area with the 5 million tumor cells. To examine the efficacy of anti-FucGM1 ADC-45, mice were dosed with a single IP administration of 0.01 mol/kg.
In Vivo Model H187 CDX model
In Vitro Model Lung small cell carcinoma NCI-H187 cells CVCL_1501
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00% Positive FucGM1 expression (FucGM1+++/++)
Method Description
Female CB-17 SCID mice were each inoculated in the flank area with the 5 million tumor cells. To examine the efficacy of anti-FucGM1 ADC-45, mice were dosed with a single IP administration of 0.03 mol/kg.
In Vivo Model H187 CDX model
In Vitro Model Lung small cell carcinoma NCI-H187 cells CVCL_1501
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 100.00% Positive FucGM1 expression (FucGM1+++/++)
Method Description
Female CB-17 SCID mice were each inoculated in the flank area with the 5 million tumor cells. To examine the efficacy of anti-FucGM1 ADC-45, mice were dosed with a single IP administration of 0.06 mol/kg.
In Vivo Model H187 CDX model
In Vitro Model Lung small cell carcinoma NCI-H187 cells CVCL_1501
Revealed Based on the Cell Line Data
Click To Hide/Show 1 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 1.00 nM Positive FucGM1 expression (FucGM1+++/++)
Method Description
Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model Lung small cell carcinoma NCI-H187 cells CVCL_1501
References
Ref 1 Design, Synthesis, and Structure-Activity Relationships of Novel Tetrahydroisoquinolino Benzodiazepine Dimer Antitumor Agents and Their Application in Antibody-Drug Conjugates. J Med Chem. 2020 Nov 25;63(22):13913-13950. doi: 10.1021/acs.jmedchem.0c01385.

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