Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)
ADC ID
DRG0XCQTC
ADC Name
WO2017059289A1 ADC-106
Synonyms
Thio anti-HER2 hu7C2 LC K149C-51
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Organization
Genentech, Inc.
Drug Status
Investigative
Indication
In total 1 Indication(s)
Breast cancer [ICD11:2C60-2C65]
Investigative
Drug-to-Antibody Ratio
2
Antibody Name
Thio Anti-HER2 hu7C2 LC K149C
  Antibody Info 
Antigen Name
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
  Antigen Info 
Payload Name
Undisclosed
Linker Name
WO2017059289A1_ADC-106 linker
General Information of The Activity Data Related to This ADC
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 7 Activity Data Related to This Level
Standard Type Value Units Cell Line Disease Model
Tumor Growth Inhibition value (TGI) 
≈ 0
%
WSU-DLCL2 cells
Diffuse large B-cell lymphoma
Tumor Growth Inhibition value (TGI) 
≈ 49.65
%
KPL-4 cells
Breast inflammatory carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 49.9
%
KPL-4 cells
Breast inflammatory carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 53.48
%
KPL-4 cells
Breast inflammatory carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 53.81
%
KPL-4 cells
Breast inflammatory carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 82.9
%
KPL-4 cells
Breast inflammatory carcinoma
Tumor Growth Inhibition value (TGI) 
≈ 84.39
%
KPL-4 cells
Breast inflammatory carcinoma
Obtained from the Model Organism Data
Click To Hide/Show 2 Activity Data Related to This Level
Standard Type Value Units Animal Model (No. of PDX)
Tumor Growth Inhibition value (TGI) 
≈ 58.22
%
Breast cancer model MMTV-HER2 Fo5
Tumor Growth Inhibition value (TGI) 
≈ 73.26
%
Breast cancer model MMTV-HER2 Fo5
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Cell Line-derived Xenograft Model
Click To Hide/Show 7 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 14) Positive CD22 expression (CD22+++/++)
Method Description
Inoculate 150 mice with WSU-DLCL2 cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped out into 10 groups of 8-10 mice each. A single treatment will be administered intravenously (16.2 mg/kg) via the tail vein on Day 0.

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In Vivo Model WSU-DLCL2 CDX model
In Vitro Model Diffuse large B-cell lymphoma WSU-DLCL2 cells CVCL_1902
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 49.65% (Day 24) Positive HER2 expression (HER2+++/++)
Method Description
Inoculate 150 mice with KPL-4 cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped out into 10 groups of 8-10 mice each. A single treatment will be administered intravenously (5 mg/kg) via the tail vein on Day 0.

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In Vivo Model KPL-4 CDX model
In Vitro Model Breast inflammatory carcinoma KPL-4 cells CVCL_5310
Experiment 3 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 49.90% (Day 24) Positive HER2 expression (HER2+++/++)
Method Description
Inoculate 150 mice with KPL-4 cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped out into 10 groups of 8-10 mice each. A single treatment will be administered intravenously (5 mg/kg) via the tail vein on Day 0.

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In Vivo Model KPL-4 CDX model
In Vitro Model Breast inflammatory carcinoma KPL-4 cells CVCL_5310
Experiment 4 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 53.48% (Day 24) Positive HER2 expression (HER2+++/++)
Method Description
Inoculate 150 mice with KPL-4 cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped out into 10 groups of 8-10 mice each. A single treatment will be administered intravenously (1 mg/kg) via the tail vein on Day 0.

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In Vivo Model KPL-4 CDX model
In Vitro Model Breast inflammatory carcinoma KPL-4 cells CVCL_5310
Experiment 5 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 53.81% (Day 24) Positive HER2 expression (HER2+++/++)
Method Description
Inoculate 150 mice with KPL-4 cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped out into 10 groups of 8-10 mice each. A single treatment will be administered intravenously (1 mg/kg) via the tail vein on Day 0.

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In Vivo Model KPL-4 CDX model
In Vitro Model Breast inflammatory carcinoma KPL-4 cells CVCL_5310
Experiment 6 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 82.90% (Day 24) Positive HER2 expression (HER2+++/++)
Method Description
Inoculate 150 mice with KPL-4 cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped out into 10 groups of 8-10 mice each. A single treatment will be administered intravenously (ADC-211, 1 mg/kg plus ADC-106, 5 mg/kg) via the tail vein on Day 0.

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In Vivo Model KPL-4 CDX model
In Vitro Model Breast inflammatory carcinoma KPL-4 cells CVCL_5310
Experiment 7 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 84.39% (Day 24) Positive HER2 expression (HER2+++/++)
Method Description
Inoculate 150 mice with KPL-4 cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped out into 10 groups of 8-10 mice each. A single treatment will be administered intravenously (ADC-211, 1 mg/kg plus ADC-106, 1 mg/kg) via the tail vein on Day 0.

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In Vivo Model KPL-4 CDX model
In Vitro Model Breast inflammatory carcinoma KPL-4 cells CVCL_5310
Obtained from the Model Organism Data
Click To Hide/Show 2 Activity Data Related to This Level
Experiment 1 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 58.22% (Day 7) Positive HER2 expression (HER2+++/++)
Method Description
Before being used for an in vivo efficacy study, the MMTV-HER2 Fo5 transgenic mammary tumor was surgically transplanted into the mammary fat pad of nu/nu mice in fragments that measured approximately 2x2 mm. MMTV-HER2 Fo5 mammary allograft tumors inoculated into CRL nu/nu mice aftersingle,then iv 5 mg/kg ADC dosing on day 0.
In Vivo Model Breast cancer model MMTV-HER2 Fo5
Experiment 2 Reporting the Activity Date of This ADC [1]
Efficacy Data Tumor Growth Inhibition value (TGI) ≈ 73.26% (Day 7) Positive HER2 expression (HER2+++/++)
Method Description
Before being used for an in vivo efficacy study, the MMTV-HER2 Fo5 transgenic mammary tumor was surgically transplanted into the mammary fat pad of nu/nu mice in fragments that measured approximately 2x2 mm. MMTV-HER2 Fo5 mammary allograft tumors inoculated into CRL nu/nu mice aftersingle,then iv 10 mg/kg ADC dosing on day 0.
In Vivo Model Breast cancer model MMTV-HER2 Fo5
References
Ref 1 Pyrrolobenzodiazepine antibody drug conjugates and methods of use; 2017-04-06.

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