Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0IDJLV
ADC Name
WO2018135501A1 ADC-13
Synonyms
WO2018135501A1 ADC13
   Click to Show/Hide
Organization
Daiichi Sankyo Co., Ltd.
Drug Status
Investigative
Indication
In total 1 Indication(s)
Gastrointestinal stromal tumor [ICD11:2B5B]
Investigative
Drug-to-Antibody Ratio
7.7
Antibody Name
h046-H4e/L7
  Antibody Info 
Antigen Name
G-protein coupled receptor 20 (GPR20)
  Antigen Info 
Payload Name
Undisclosed
Linker Name
WO2018135501A1_ADC-13 linker
General Information of The Activity Data Related to This ADC
Discovered Using Patient-derived Xenograft Model
Click To Hide/Show 6 Activity Data Related to This Level
Standard Type Value Units Animal Model (No. of PDX)
Tumor Growth Inhibition value (TGI) 
≔ 38
%
Gastrointestinal stromal tumor (GIST) PDX model (PDX: GIST-T1/GPR20)
Tumor Growth Inhibition value (TGI) 
≙ 50
%
Gastrointestinal stromal tumor (GIST) PDX model (PDX: GIST1)
Tumor Growth Inhibition value (TGI) 
≘ 56.3
%
Gastrointestinal stromal tumor (GIST) PDX model (PDX: GIST020)
Tumor Growth Inhibition value (TGI) 
≕ 83
%
Gastrointestinal stromal tumor (GIST) PDX model (PDX: GIST-T1/GPR20)
Tumor Growth Inhibition value (TGI) 
≖ 90.4
%
Gastrointestinal stromal tumor (GIST) PDX model (PDX: GIST-T1/GPR20)
Tumor Growth Inhibition value (TGI) 
≚ 92
%
Gastrointestinal stromal tumor (GIST) PDX model (PDX: GIST1)
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Patient-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) ≔ 38.00% (Day 45) Positive GPR20 expression (GPR20+++/++)
Method Description
To establish gastrointestinal stromal tumor model, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 0.3mpk.
In Vivo Model Gastrointestinal stromal tumor (GIST) PDX model (PDX: GIST-T1/GPR20)
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≙ 50.00% (Day 70) Positive GPR20 expression (GPR20+++/++)
Method Description
To establish gastrointestinal stromal tumor model, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 3 mg/kg, i.v. at day38, day 59.
In Vivo Model Gastrointestinal stromal tumor (GIST) PDX model (PDX: GIST1)
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≘ 56.30% (Day 89) Positive GPR20 expression (GPR20+++/++)
Method Description
To establish gastrointestinal stromal tumor model, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 10 mg/kg, i.v. at day55, day 75.
In Vivo Model Gastrointestinal stromal tumor (GIST) PDX model (PDX: GIST020)
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≕ 83.00% (Day 45) Positive GPR20 expression (GPR20+++/++)
Method Description
To establish gastrointestinal stromal tumor model, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 1mpk.
In Vivo Model Gastrointestinal stromal tumor (GIST) PDX model (PDX: GIST-T1/GPR20)
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≖ 90.40% (Day 45) Positive GPR20 expression (GPR20+++/++)
Method Description
To establish gastrointestinal stromal tumor model, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 3mpk.
In Vivo Model Gastrointestinal stromal tumor (GIST) PDX model (PDX: GIST-T1/GPR20)
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≚ 92.00% (Day 70) Positive GPR20 expression (GPR20+++/++)
Method Description
To establish gastrointestinal stromal tumor model, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 10 mg/kg, i.v. at day38, day 59.
In Vivo Model Gastrointestinal stromal tumor (GIST) PDX model (PDX: GIST1)
References
Ref 1 Anti-gpr20 antibody and anti-gpr20 antibody-drug conjugate; 2018-07-26.

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