Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0PQQJW
ADC Name
GPC-1 ADC 1
Synonyms
GPC-1-ADC-1
   Click to Show/Hide
Drug Status
Investigative
Indication
In total 3 Indication(s)
Adenocarcinoma [ICD11:2D40]
Investigative
Ovarian cancer [ICD11:2C73]
Investigative
Squamous cell cancer [ICD11:2D60-2D61]
Investigative
Drug-to-Antibody Ratio
4.1
Antibody Name
Anti-GPC1 mAb 01a033
  Antibody Info 
Antigen Name
Glypican-1 (GPC1)
  Antigen Info 
Payload Name
Monomethyl auristatin F
  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.
Combination Type
VcMMAF
General Information of The Activity Data Related to This ADC
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 6 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Tumor Growth Inhibition value (TGI) 
≈ 21.71
%
HeLa cells
Endocervical adenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 28.13
%
ME-180 cells
Cervical squamous cell carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 33.65
%
ME-180 cells
Cervical squamous cell carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 43.94
%
HeLa cells
Endocervical adenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 69.65
%
HeLa cells
Endocervical adenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 99.49
%
ME-180 cells
Cervical squamous cell carcinoma
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) 
0.04
nM
HeLa cells
Endocervical adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
0.09
nM
ME-180 cells
Cervical squamous cell carcinoma
Half Maximal Inhibitory Concentration (IC50) 
> 100
nM
RMG-I cells
Ovarian clear cell adenocarcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 6 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 21.71% (Day 24) Positive GPC1 expression (GPC1 +++/++)
Method Description
Antitumor efficacy of GPC1-ADC in HeLa (n = 6/group) xenograft models. When the mean tumor size of each cancer type reached approximately 130 mm3 , PBS, control-ADC or GPC1-ADC (1 mg/kg) was intravenously injected every four days for a total of 4 times.
In Vivo Model HeLa CDX model
In Vitro Model Endocervical adenocarcinoma HeLa cells CVCL_0030
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 28.13% (Day 32) Positive GPC1 expression (GPC1 +++/++)
Method Description
Antitumor efficacy of GPC1-ADC in ME180 (n = 7/group) xenograft models. When the mean tumor size of each cancer type reached approximately 130 mm3 , PBS, control-ADC or GPC1-ADC (1 mg/kg) was intravenously injected every four days for a total of 4 times.
In Vivo Model ME180 CDX model
In Vitro Model Cervical squamous cell carcinoma ME-180 cells CVCL_1401
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 33.65% (Day 32) Positive GPC1 expression (GPC1 +++/++)
Method Description
Antitumor efficacy of GPC1-ADC in ME180 (n = 7/group) xenograft models. When the mean tumor size of each cancer type reached approximately 130 mm3 , PBS, control-ADC or GPC1-ADC (3 mg/kg) was intravenously injected every four days for a total of 4 times.
In Vivo Model ME180 CDX model
In Vitro Model Cervical squamous cell carcinoma ME-180 cells CVCL_1401
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 43.94% (Day 24) Positive GPC1 expression (GPC1 +++/++)
Method Description
Antitumor efficacy of GPC1-ADC in HeLa (n = 6/group) xenograft models. When the mean tumor size of each cancer type reached approximately 130 mm3 , PBS, control-ADC or GPC1-ADC (3 mg/kg) was intravenously injected every four days for a total of 4 times.
In Vivo Model HeLa CDX model
In Vitro Model Endocervical adenocarcinoma HeLa cells CVCL_0030
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 69.65% (Day 24) Positive GPC1 expression (GPC1 +++/++)
Method Description
Antitumor efficacy of GPC1-ADC in HeLa (n = 6/group) xenograft models. When the mean tumor size of each cancer type reached approximately 130 mm3 , PBS, control-ADC or GPC1-ADC (10 mg/kg) was intravenously injected every four days for a total of 4 times.
In Vivo Model HeLa CDX model
In Vitro Model Endocervical adenocarcinoma HeLa cells CVCL_0030
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 99.49% (Day 32) Positive GPC1 expression (GPC1 +++/++)
Method Description
Antitumor efficacy of GPC1-ADC in ME180 (n = 7/group) xenograft models. When the mean tumor size of each cancer type reached approximately 130 mm3 , PBS, control-ADC or GPC1-ADC (10 mg/kg) was intravenously injected every four days for a total of 4 times.
In Vivo Model ME180 CDX model
In Vitro Model Cervical squamous cell carcinoma ME-180 cells CVCL_1401
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) 0.04 nM Positive GPC1 expression (GPC1 +++/++)
Method Description
HeLa, ME180, and RMG-1 cells were treated with anti-GPC1 monoclonal antibody (clone 01a033) or control IgG antibody for 144 h.
In Vitro Model Endocervical adenocarcinoma HeLa cells CVCL_0030
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 0.09 nM Positive GPC1 expression (GPC1 +++/++)
Method Description
HeLa, ME180, and RMG-1 cells were treated with anti-GPC1 monoclonal antibody (clone 01a033) or control IgG antibody for 144 h.
In Vitro Model Cervical squamous cell carcinoma ME-180 cells CVCL_1401
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) > 100 nM Negative GPC1 expression (GPC1 -)
Method Description
HeLa, ME180, and RMG-1 cells were treated with anti-GPC1 monoclonal antibody (clone 01a033) or control IgG antibody for 144 h.
In Vitro Model Ovarian clear cell adenocarcinoma RMG-I cells CVCL_1662
References
Ref 1 Anti-glypican-1 antibody-drug conjugate exhibits potent preclinical antitumor activity against glypican-1 positive uterine cervical cancer. Int J Cancer. 2018 Mar 1;142(5):1056-1066. doi: 10.1002/ijc.31124. Epub 2017 Oct 31.

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