Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0MCKPB
ADC Name
Anti-KIT NEG085?SPP-DM1
Synonyms
Anti-KIT-NEG085?SPP-DM4
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Organization
Novartis AG
Drug Status
Investigative
Indication
In total 3 Indication(s)
Acute myeloid leukaemia [ICD11:2A60]
Investigative
Melanoma [ICD11:2C30]
Investigative
Small cell lung cancer [ICD11:2C25]
Investigative
Drug-to-Antibody Ratio
3-4
Antibody Name
Anti-KIT mAb NEG085
  Antibody Info 
Antigen Name
Mast/stem cell growth factor receptor Kit (KIT)
  Antigen Info 
Payload Name
Mertansine DM1
  Payload Info 
Therapeutic Target
Microtubule (MT)
  Target Info 
Linker Name
N-succinimidyl 4-(2-pyridyldithio) pentanoate (SPP)
  Linker Info 
General Information of The Activity Data Related to This ADC
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 3 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Tumor Growth Inhibition value (TGI) 
≈ 41.55
%
CVCL_1453
Lung small cell carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 87.55
%
CVCL_1453
Lung small cell carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 91.32
%
CVCL_1453
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 3 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 41.55% (Day 27) Positive KIT expression (KIT+++/++)
Method Description
Female SCID-beige mice were implanted subcutaneously with 10,000,000 NCI-H1048 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of 2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (2.5 mg/kg).

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In Vivo Model NCI-H1048 CDX model
In Vitro Model Lung small cell carcinoma NCI-H1048 cells CVCL_1453
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 87.55% (Day 27) Positive KIT expression (KIT+++/++)
Method Description
Female SCID-beige mice were implanted subcutaneously with 10,000,000 NCI-H1048 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of 2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (5 mg/kg).

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In Vivo Model NCI-H1048 CDX model
In Vitro Model Lung small cell carcinoma NCI-H1048 cells CVCL_1453
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 91.32% (Day 27) Positive KIT expression (KIT+++/++)
Method Description
Female SCID-beige mice were implanted subcutaneously with 10,000,000 NCI-H1048 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of 2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (10 mg/kg).

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In Vivo Model NCI-H1048 CDX model
In Vitro Model Lung small cell carcinoma NCI-H1048 cells CVCL_1453
References
Ref 1 Antibody drug conjugates.

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