General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0GYZHE
ADC Name
WO2016205176A1 ADC-102
Synonyms
Thio Hu Anti-Ly6E 9B12.v12 LC K149C-(LD-2)
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Organization
Genentech, Inc.
Drug Status
Investigative
Indication
In total 3 Indication(s)
Breast cancer [ICD11:2C60-2C65]
Investigative
Lung cancer [ICD11:2C25]
Investigative
Non-small cell lung cancer [ICD11:2C25]
Investigative
Drug-to-Antibody Ratio
2
Antibody Name
Thio hu Anti-Ly6E 9B12.v12 LC K149C
 Antibody Info 
Antigen Name
Lymphocyte antigen 6E (LY6E)
 Antigen Info 
Payload Name
Undisclosed
Linker Name
WO2016205176A1_ADC-102 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) 
≈ 0
%
Triple negative breast cancer PDX model (PDX: HBCx9)
Tumor Growth Inhibition value (TGI) 
≈ 32.11
%
Triple negative breast cancer PDX model (PDX: HBCx9)
Tumor Growth Inhibition value (TGI) 
≈ 73.25
%
Triple negative breast cancer PDX model (PDX: HBCx9)
Tumor Growth Inhibition value (TGI) 
≈ 79.64
%
Triple negative breast cancer PDX model (PDX: HCI-009)
Tumor Growth Inhibition value (TGI) 
≈ 83.52
%
Triple negative breast cancer PDX model (PDX: HCI-009)
Tumor Growth Inhibition value (TGI) 
≈ 83.52
%
Triple negative breast cancer PDX model (PDX: HCI-009)
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 11 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Tumor Growth Inhibition value (TGI) 
≈ 0
%
NCI-H1781 cells
Minimally invasive lung adenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 39.52
%
PC-9 cells
Lung adenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 45.74
%
NCI-H1781 cells
Minimally invasive lung adenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 53.26
%
HCC1569 cells
Breast ductal carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 67.78
%
PC-9 cells
Lung adenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 71.88
%
PC-9 cells
Lung adenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 73.9
%
PC-9 cells
Lung adenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 85.2
%
HCC1569 cells
Breast ductal carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 92.27
%
NCI-H1781 cells
Minimally invasive lung adenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 93.78
%
NCI-H1781 cells
Minimally invasive lung adenocarcinoma
Tumor Growth Inhibition value (TGI) 
≈ 95.33
%
HCC1569 cells
Breast ductal carcinoma
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) ≈ 0.00% (Day 28) Low LY6E expression (LY6E+)
Method Description
Female C.B-17 SCD-beige mice were each inoculated in the thoracic mammary fat pad area with 5 million breast cancer cells suspended in HBSS/matrigel. When the xenograft tumors reached an average tumor volume of 100-300 mm(referred to as Day 0), animals were received a single intravenous injection of the antibody-drug conjugate (0.1 mg/kg) through tail vein.

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In Vivo Model Triple negative breast cancer PDX model (PDX: HBCx9)
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 32.11% (Day 28) Low LY6E expression (LY6E+)
Method Description
Female C.B-17 SCD-beige mice were each inoculated in the thoracic mammary fat pad area with 5 million breast cancer cells suspended in HBSS/matrigel. When the xenograft tumors reached an average tumor volume of 100-300 mm(referred to as Day 0), animals were received a single intravenous injection of the antibody-drug conjugate (0.3 mg/kg) through tail vein.

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In Vivo Model Triple negative breast cancer PDX model (PDX: HBCx9)
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 73.25% (Day 28) Low LY6E expression (LY6E+)
Method Description
Female C.B-17 SCD-beige mice were each inoculated in the thoracic mammary fat pad area with 5 million breast cancer cells suspended in HBSS/matrigel. When the xenograft tumors reached an average tumor volume of 100-300 mm(referred to as Day 0), animals were received a single intravenous injection of the antibody-drug conjugate (0.6 mg/kg) through tail vein.

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In Vivo Model Triple negative breast cancer PDX model (PDX: HBCx9)
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 79.64% (Day 21) Moderate LY6E expression (LY6E++)
Method Description
Female C.B-17 SCD-beige mice were each inoculated in the thoracic mammary fat pad area with 5 million breast cancer cells suspended in HBSS/matrigel. When the xenograft tumors reached an average tumor volume of 100-300 mm(referred to as Day 0), animals were received a single intravenous injection of the antibody-drug conjugate (0.2 mg/kg) through tail vein.

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In Vivo Model Triple negative breast cancer PDX model (PDX: HCI-009)
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 83.52% (Day 21) Moderate LY6E expression (LY6E++)
Method Description
Female C.B-17 SCD-beige mice were each inoculated in the thoracic mammary fat pad area with 5 million breast cancer cells suspended in HBSS/matrigel. When the xenograft tumors reached an average tumor volume of 100-300 mm(referred to as Day 0), animals were received a single intravenous injection of the antibody-drug conjugate (0.5 mg/kg) through tail vein.

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In Vivo Model Triple negative breast cancer PDX model (PDX: HCI-009)
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 83.52% (Day 21) Moderate LY6E expression (LY6E++)
Method Description
Female C.B-17 SCD-beige mice were each inoculated in the thoracic mammary fat pad area with 5 million breast cancer cells suspended in HBSS/matrigel. When the xenograft tumors reached an average tumor volume of 100-300 mm(referred to as Day 0), animals were received a single intravenous injection of the antibody-drug conjugate (0.1 mg/kg) through tail vein.

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In Vivo Model Triple negative breast cancer PDX model (PDX: HCI-009)
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 11 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 0.00% (Day 22) Low LY6E expression (LY6E+)
Method Description
Female C.B-17 SCD-beige mice were each inoculated in the thoracic mammary fat pad area with 5 million NCI-H1781 cells suspended in HBSS/matrigel. When the xenograft tumors reached an average tumor volume of 100-300 mm(referred to as Day 0), animals were received a single intravenous injection of the antibody-drug conjugate (0.2 mg/kg) through tail vein.

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In Vivo Model NCI-H1781 CDX model
In Vitro Model Minimally invasive lung adenocarcinoma NCI-H1781 cells CVCL_1494
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 39.52% (Day 21) Low LY6E expression (LY6E+)
Method Description
Female C.B-17 SCD-beige mice were each inoculated in the thoracic mammary fat pad area with 5 million PC-9 cells suspended in HBSS/matrigel. When the xenograft tumors reached an average tumor volume of 100-300 mm(referred to as Day 0), animals were received a single intravenous injection of the antibody-drug conjugate (0.2 mg/kg) through tail vein.
In Vivo Model PC-9 CDX model
In Vitro Model Lung adenocarcinoma PC-9 cells CVCL_B260
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 45.74% (Day 22) Low LY6E expression (LY6E+)
Method Description
Female C.B-17 SCD-beige mice were each inoculated in the thoracic mammary fat pad area with 5 million NCI-H1781 cells suspended in HBSS/matrigel. When the xenograft tumors reached an average tumor volume of 100-300 mm(referred to as Day 0), animals were received a single intravenous injection of the antibody-drug conjugate (0.5 mg/kg) through tail vein.

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In Vivo Model NCI-H1781 CDX model
In Vitro Model Minimally invasive lung adenocarcinoma NCI-H1781 cells CVCL_1494
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 53.26% (Day 14) Moderate LY6E expression (LY6E++)
Method Description
Female C.B-17 SCD-beige mice were each inoculated in the thoracic mammary fat pad area with 5 million HCC1569 cells suspended in HBSS/matrigel. When the xenograft tumors reached an average tumor volume of 100-300 mm(referred to as Day 0), animals were received a single intravenous injection of the antibody-drug conjugate (0.2 mg/kg) through tail vein.

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In Vivo Model HCC1569 CDX model
In Vitro Model Breast ductal carcinoma HCC1569 cells CVCL_1255
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 67.78% (Day 21) Low LY6E expression (LY6E+)
Method Description
Female C.B-17 SCD-beige mice were each inoculated in the thoracic mammary fat pad area with 5 million PC-9 cells suspended in HBSS/matrigel. When the xenograft tumors reached an average tumor volume of 100-300 mm(referred to as Day 0), animals were received a single intravenous injection of the antibody-drug conjugate (0.5 mg/kg) through tail vein.
In Vivo Model PC-9 CDX model
In Vitro Model Lung adenocarcinoma PC-9 cells CVCL_B260
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 71.88% (Day 21) Low LY6E expression (LY6E+)
Method Description
Female C.B-17 SCD-beige mice were each inoculated in the thoracic mammary fat pad area with 5 million PC-9 cells suspended in HBSS/matrigel. When the xenograft tumors reached an average tumor volume of 100-300 mm(referred to as Day 0), animals were received a single intravenous injection of the antibody-drug conjugate (1 mg/kg) through tail vein.
In Vivo Model PC-9 CDX model
In Vitro Model Lung adenocarcinoma PC-9 cells CVCL_B260
Experiment 7 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 73.90% (Day 21) Low LY6E expression (LY6E+)
Method Description
Female C.B-17 SCD-beige mice were each inoculated in the thoracic mammary fat pad area with 5 million PC-9 cells suspended in HBSS/matrigel. When the xenograft tumors reached an average tumor volume of 100-300 mm(referred to as Day 0), animals were received a single intravenous injection of the antibody-drug conjugate (2 mg/kg) through tail vein.
In Vivo Model PC-9 CDX model
In Vitro Model Lung adenocarcinoma PC-9 cells CVCL_B260
Experiment 8 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 85.20% (Day 14) Moderate LY6E expression (LY6E++)
Method Description
Female C.B-17 SCD-beige mice were each inoculated in the thoracic mammary fat pad area with 5 million HCC1569 cells suspended in HBSS/matrigel. When the xenograft tumors reached an average tumor volume of 100-300 mm(referred to as Day 0), animals were received a single intravenous injection of the antibody-drug conjugate (0.5 mg/kg) through tail vein.

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In Vivo Model HCC1569 CDX model
In Vitro Model Breast ductal carcinoma HCC1569 cells CVCL_1255
Experiment 9 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 92.27% (Day 22) Low LY6E expression (LY6E+)
Method Description
Female C.B-17 SCD-beige mice were each inoculated in the thoracic mammary fat pad area with 5 million NCI-H1781 cells suspended in HBSS/matrigel. When the xenograft tumors reached an average tumor volume of 100-300 mm(referred to as Day 0), animals were received a single intravenous injection of the antibody-drug conjugate (2 mg/kg) through tail vein.

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In Vivo Model NCI-H1781 CDX model
In Vitro Model Minimally invasive lung adenocarcinoma NCI-H1781 cells CVCL_1494
Experiment 10 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 93.78% (Day 22) Low LY6E expression (LY6E+)
Method Description
Female C.B-17 SCD-beige mice were each inoculated in the thoracic mammary fat pad area with 5 million NCI-H1781 cells suspended in HBSS/matrigel. When the xenograft tumors reached an average tumor volume of 100-300 mm(referred to as Day 0), animals were received a single intravenous injection of the antibody-drug conjugate (1 mg/kg) through tail vein.

   Click to Show/Hide
In Vivo Model NCI-H1781 CDX model
In Vitro Model Minimally invasive lung adenocarcinoma NCI-H1781 cells CVCL_1494
Experiment 11 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 95.33% (Day 14) Moderate LY6E expression (LY6E++)
Method Description
Female C.B-17 SCD-beige mice were each inoculated in the thoracic mammary fat pad area with 5 million HCC1569 cells suspended in HBSS/matrigel. When the xenograft tumors reached an average tumor volume of 100-300 mm(referred to as Day 0), animals were received a single intravenous injection of the antibody-drug conjugate (1 mg/kg) through tail vein.

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In Vivo Model HCC1569 CDX model
In Vitro Model Breast ductal carcinoma HCC1569 cells CVCL_1255
References
Ref 1 Antibodies and immunoconjugates; 2016-12-22.

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