Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0YTNKP
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| ADC Name |
WO2017059289A1 ADC-201
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| Synonyms |
Thio anti-HER2 hu7C2 LC K149C-CLD-1
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| Organization |
Genentech, Inc.
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| Drug Status |
Investigative
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| Indication |
In total 1 Indication(s)
Breast cancer [ICD11:2C60-2C65]
Investigative
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| Drug-to-Antibody Ratio |
1.84
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| Antibody Name |
Thio Anti-HER2 hu7C2 LC K149C
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Antibody Info | ||||
| Antigen Name |
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
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Antigen Info | ||||
| Payload Name |
Undisclosed
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| Linker Name |
WO2017059289A1_ADC-201 linker
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General Information of The Activity Data Related to This ADC
Discovered Using Cell Line-derived Xenograft Model
Obtained from the Model Organism Data
Revealed Based on the Cell Line Data
Full List of Activity Data of This Antibody-drug Conjugate
Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 15.63% (Day 25) | 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 (3 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 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 37.61% (Day 11) | Moderate CD22 expression (CD22++) | ||
| Method Description |
Inoculate 150 mice with BJAB 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 (0.4 mg/kg) via the tail vein on Day 0.
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| In Vivo Model | BJAB CDX model | ||||
| In Vitro Model | Burkitt lymphoma | BJAB cells | CVCL_5711 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 83.58% (Day 25) | 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 (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
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 35.37% (Day 10) | 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 0.5 mg/kg ADC dosing on day 0.
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| 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) | ≈ 87.28% (Day 10) | 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 1 mg/kg ADC dosing on day 0.
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| In Vivo Model | Breast cancer model MMTV-HER2 Fo5 | ||||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 0.10 ng/mL | High HER2 expression (HER2 +++) | ||
| Method Description |
Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
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| In Vitro Model | Breast adenocarcinoma | SK-BR-3 cells | CVCL_0033 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 0.30 ng/mL | High HER2 expression (HER2+++) | ||
| Method Description |
Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
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| In Vitro Model | Breast inflammatory carcinoma | KPL-4 cells | CVCL_5310 | ||
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