Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0NYYUB
ADC Name
WO2021249228A1 ADC-61
Synonyms
WO2021249228A1 ADC61
   Click to Show/Hide
Organization
Sichuan Baili Pharmaceutical Co., Ltd.
Drug Status
Investigative
Indication
In total 2 Indication(s)
Breast cancer [ICD11:2C60-2C65]
Investigative
Gastric cancer [ICD11:2B72]
Investigative
Drug-to-Antibody Ratio
7.59
Antibody Name
Trastuzumab
  Antibody Info 
Antigen Name
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
  Antigen Info 
Payload Name
Undisclosed
Linker Name
WO2021249228A1_ADC-61 linker
General Information of The Activity Data Related to This ADC
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 4 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Tumor Growth Inhibition value (TGI) 
≈ 4
%
NCI-H1975 cells
Lung adenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 71.2
%
NCI-H1975 cells
Lung adenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 92
%
NCI-N87 cells
Gastric tubular adenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 92
%
NCI-H1975 cells
Lung adenocarcinoma
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) 
> 500
nM
NCI-N87 cells
Gastric tubular adenocarcinoma
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 4 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 4.00% (Day 31) Positive HER2 expression (EPHA2+++/++)
Method Description
To establish lung adenocarcinoma 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 11.25 mg/kg, i.v.
In Vivo Model NCI-H1975 CDX model
In Vitro Model Lung adenocarcinoma NCI-H1975 cells CVCL_1511
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 71.20% (Day 31) Positive EGFR expression (EGFR+++/++)
Method Description
To establish lung adenocarcinoma 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 3.75 mg/kg, i.v.
In Vivo Model NCI-H1975 CDX model
In Vitro Model Lung adenocarcinoma NCI-H1975 cells CVCL_1511
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 92.00% (Day 31) Positive HER2 expression (EPHA2+++/++)
Method Description
To establish gastric tubular adenocarcinoma 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 3.75 mg/kg, i.v.
In Vivo Model NCI-N87 CDX model
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 92.00% (Day 31) Positive EGFR expression (EGFR+++/++)
Method Description
To establish lung adenocarcinoma 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 11.25 mg/kg, i.v.
In Vivo Model NCI-H1975 CDX model
In Vitro Model Lung adenocarcinoma NCI-H1975 cells CVCL_1511
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) > 500 nM Positive HER2 expression (EPHA2+++/++)
Method Description
Potency of compounds and ADCs was evaluated using the NCI-N87 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
In Vitro Model Gastric tubular adenocarcinoma NCI-N87 cells CVCL_1603
References
Ref 1 Camptothecin drug having high-stability hydrophilic connecting unit and conjugate thereof; 2021-12-16.

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