Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0AVUFT
ADC Name
HuM25-S239C-PBD-E2
Synonyms
HuM25-S239C PBD-E2; huM25-S239C PBD-E2
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Organization
AbbVie, Inc.
Drug Status
Investigative
Indication
In total 1 Indication(s)
Non-small cell lung cancer [ICD11:2C25]
Investigative
Drug-to-Antibody Ratio
2
Structure
Antibody Name
huM25-S239C
  Antibody Info 
Antigen Name
Leucine-rich repeat-containing protein 15 (LRRC15)
  Antigen Info 
Payload Name
PBD dimer
  Payload Info 
Therapeutic Target
Human Deoxyribonucleic acid (hDNA)
  Target Info 
Linker Name
Mc-Val-Ala
  Linker Info 
Conjugate Type
Random conjugation through reduced inter-chain cysteines.
Combination Type
VaPBD
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) 
60.13
%
EBC-1 cells
Lung squamous cell carcinoma
Tumor Growth Inhibition value (TGI) 
73.58
%
NCI-H1650 cells
Lung adenocarcinoma
Tumor Growth Inhibition value (TGI) 
92.33
%
NCI-H1650 cells
Lung adenocarcinoma
Tumor Growth Inhibition value (TGI) 
94.51
%
NCI-H1650 cells
Lung adenocarcinoma
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) 
1
pM
BALB/3T12-3 cells (huLRRC15 transfection)
Squamous non-small cell lung cancer
Half Maximal Inhibitory Concentration (IC50) 
10.00 - 100.00
nM
A-549 cells
Lung adenocarcinoma
Half Maximal Inhibitory Concentration (IC50) 
10.00 - 100.00
nM
A-549 cells
Lung 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) 60.13% (Day 13) High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description
EBC-1 squamous NSCLC cells (5 million) were implanted subcutaneously into SCID mice, and micewere randomized when the tumors reached 175 mm and dosed with ADC or isotype antibody at 0.6 mg/kg intraperitoneally on day 0.
In Vivo Model EBC-1 CDX model
In Vitro Model Lung squamous cell carcinoma EBC-1 cells CVCL_2891
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) 73.58% (Day 17) High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description
NCI-H1650 NSCLC cancer cells (5 million) were implanted subcutaneously into SCID/Beigemice. and mice were randomized when the tumors reached -200 mm and dosed on day 0 with isotype orADC at 0.1 mg/kg intraperitoneally.
In Vivo Model NCI-H1650 CDX model
In Vitro Model Lung adenocarcinoma NCI-H1650 cells CVCL_1483
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) 92.33% (Day 17) High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description
NCI-H1650 NSCLC cancer cells (5 million) were implanted subcutaneously into SCID/Beigemice. and mice were randomized when the tumors reached -200 mm and dosed on day 0 with isotype orADC at 0.3 mg/kg intraperitoneally.
In Vivo Model NCI-H1650 CDX model
In Vitro Model Lung adenocarcinoma NCI-H1650 cells CVCL_1483
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) 94.51% (Day 17) High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description
NCI-H1650 NSCLC cancer cells (5 million) were implanted subcutaneously into SCID/Beigemice. and mice were randomized when the tumors reached -200 mm and dosed on day 0 with isotype orADC at 6 mg/kg intraperitoneally.
In Vivo Model NCI-H1650 CDX model
In Vitro Model Lung adenocarcinoma NCI-H1650 cells CVCL_1483
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) 1.00 pM Positive LRRC15 expression (LRRC15 +++/++)
Method Description
In vitro cell killing in LRRC15 transfected 3T12 cells by isotype-S239C-PBD-E2 or huM25-S239CPBD-E2. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model Squamous non-small cell lung cancer BALB/3T12-3 cells (huLRRC15 transfection) CVCL_0637
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 10.00 nM-100.00 Nm Positive LRRC15 expression (LRRC15 +++/++)
Method Description
In vitro cell killing in A549 cells that have undergone epithelial tomesenchymal transition (EMT) in the presence of 10 ng/mL TGFB by isotype-S239C-PBD-E2huM25-S239C-PBD-E2, or huM25-S239C antibody.
In Vitro Model Lung adenocarcinoma A-549 cells CVCL_0023
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Half Maximal Inhibitory Concentration (IC50) 10.00 nM-100.00 Nm Positive LRRC15 expression (LRRC15 +++/++)
Method Description
In vitro cell killing in A549 lung cancer cells in the presence of 10 ng/mL TGFB by isotype-S239C-PBD-E2huM25-S239C-PBD-E2, or huM25-S239C antibody.
In Vitro Model Lung adenocarcinoma A-549 cells CVCL_0023
References
Ref 1 Anti-huLRRC15 antibody drug conjugates and methods for their use. 2017-06-08

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