Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0BWNUI
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| ADC Name |
H01L02-DXd
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| Synonyms |
H01L02 DXd
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| Organization |
Daiichi Sankyo Co., Ltd.;
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| Drug Status |
Investigative
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| Indication |
In total 2 Indication(s)
Ovarian cancer [ICD11:2C73]
Investigative
Renal cell carcinoma [ICD11:2C90]
Investigative
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| Drug-to-Antibody Ratio |
7.7
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| Antibody Name |
Anti-CDH6 mAb H01L02
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Antibody Info | ||||
| Antigen Name |
Cadherin-6 (CDH6)
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Antigen Info | ||||
| Payload Name |
DX-8951 derivative (DXd)
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Payload Info | ||||
| Therapeutic Target |
DNA topoisomerase 1 (TOP1)
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Target Info | ||||
| Linker Name |
Mc-Gly-Gly-Phe-Gly
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Linker Info | ||||
| Conjugate Type |
Random conjugation through reduced inter-chain cysteines.
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| Combination Type |
Deruxtecan
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General Information of The Activity Data Related to This ADC
Discovered Using Cell Line-derived Xenograft Model
Revealed Based on the Cell Line Data
| Standard Type | Value | Units | Cell Line | Disease Model |
|---|---|---|---|---|
| Half Maximal Inhibitory Concentration (IC50) |
0.01-0.10
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nM
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CVCL_0479
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Ovarian mixed germ cell tumor
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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) | ≈ 0.00% (Day 13) | Negative CDH6 expression (CDH6-) | ||
| Method Description |
The CDH6-negative human ovarian tumor cell line ES-2 was subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate H01L02-DXd was intravenously administered at doses of 1 mg/kg to thetail of each mouse.
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| In Vivo Model | ES-2 CDX model | ||||
| In Vitro Model | Ovarian clear cell adenocarcinoma | ES-2 cells | CVCL_3509 | ||
| Experiment 2 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 0.00% (Day 13) | Negative CDH6 expression (CDH6-) | ||
| Method Description |
The CDH6-negative human ovarian tumor cell line ES-2 was subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate H01L02-DXd was intravenously administered at doses of 3 mg/kg to thetail of each mouse.
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| In Vivo Model | ES-2 CDX model | ||||
| In Vitro Model | Ovarian clear cell adenocarcinoma | ES-2 cells | CVCL_3509 | ||
| Experiment 3 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 41.87% (Day 23) | Positive CDH6 expression (CDH6+++/++) | ||
| Method Description |
The CDH6-positive human renal cell tumor cell line786-O was subcutaneously inoculated at a dose of 5,000,000 cells to the right flank regionof each male SCID mouse (Day 0). On the day 20 of grouping, the anti-body-drug conjugate H01L02-DXd was intravenously administered at doses of 1 mg/kg to thetail of each mouse.
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| In Vivo Model | 786-O CDX model | ||||
| In Vitro Model | Renal cell carcinoma | 786-O cells | CVCL_1051 | ||
| Experiment 4 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 75.34% (Day 23) | Positive CDH6 expression (CDH6+++/++) | ||
| Method Description |
The CDH6-positive human renal cell tumor cell line786-O was subcutaneously inoculated at a dose of 5,000,000 cells to the right flank regionof each male SCID mouse (Day 0). On the day 20 of grouping, the anti-body-drug conjugate H01L02-DXd was intravenously administered at doses of 3 mg/kg to thetail of each mouse.
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| In Vivo Model | 786-O CDX model | ||||
| In Vitro Model | Renal cell carcinoma | 786-O cells | CVCL_1051 | ||
| Experiment 5 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 79.79% (Day 28) | Positive CDH6 expression (CDH6+++/++) | ||
| Method Description |
The CDH6-positive human ovarian tumor cell line OVCAR-3 was subcutane-ously inoculated at a dose of 10,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 22 of grouping, theantibody-drug conjugate H01L02-DXd was intravenously administered at doses of 1 mg/kg to the tail of each mouse.
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| In Vivo Model | OVCAR-3 CDX model | ||||
| In Vitro Model | Ovarian serous adenocarcinoma | OVCAR-3 cells | CVCL_0465 | ||
| Experiment 6 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 85.25% (Day 24) | Positive CDH6 expression (CDH6+++/++) | ||
| Method Description |
The CDH6-positive human renal cell tumor cell line 786-O was subcutaneously inoculated at a dose of 5,000,000 cells to the right flank regionof each male SCID mouse (Day 0). On the day 18 of grouping, H01L02-DXd was intravenously administered at a dose of 3 mg/kg to the tail of each mouse.
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| In Vivo Model | 786-O CDX model | ||||
| In Vitro Model | Renal cell carcinoma | 786-O cells | CVCL_1051 | ||
| Experiment 7 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 88.96% (Day 21) | Positive CDH6 expression (CDH6+++/++) | ||
| Method Description |
The CDH6-positive human ovarian tumor cell line PA-1 was subcutaneously inoculatedat a dose of 8,500,000 cells to the right flank region of eachfemale nude mouse (Day 0). On the day 11 of grouping, the antibody-drug conjugate H01L02-DXd was intravenously administered at doses of 1 mg/kg to the tail of each mouse.
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| In Vivo Model | PA-1 CDX model | ||||
| In Vitro Model | Ovarian mixed germ cell tumor | PA-1 cells | CVCL_0479 | ||
| Experiment 8 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 92.76% (Day 28) | Positive CDH6 expression (CDH6+++/++) | ||
| Method Description |
The CDH6-positive human ovarian tumor cell line OVCAR-3 was subcutane-ously inoculated at a dose of 10,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 22 of grouping, theantibody-drug conjugate H01L02-DXd was intravenously administered at doses of 3 mg/kg to the tail of each mouse.
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| In Vivo Model | OVCAR-3 CDX model | ||||
| In Vitro Model | Ovarian serous adenocarcinoma | OVCAR-3 cells | CVCL_0465 | ||
| Experiment 9 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) | ≈ 98.37% (Day 21) | Positive CDH6 expression (CDH6+++/++) | ||
| Method Description |
The CDH6-positive human ovarian tumor cell line PA-1 was subcutaneously inoculatedat a dose of 8,500,000 cells to the right flank region of eachfemale nude mouse (Day 0). On the day 11 of grouping, the antibody-drug conjugate H01L02-DXd was intravenously administered at doses of 3 mg/kg to the tail of each mouse.
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| In Vivo Model | PA-1 CDX model | ||||
| In Vitro Model | Ovarian mixed germ cell tumor | PA-1 cells | CVCL_0479 | ||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Date of This ADC | [1] | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) | 0.01-0.10 nM | Positive CDH6 expression (CDH6+++/++) | ||
| Method Description |
CDH6-positive human ovarian tumor cell line PA-1 was seeded over a 96-well plate at 2,000 cells/100 L/well in MEM medium supplemented with 10% FBS, and the cells were then cultured overnight. On the next day, each of the 4 humanized hG019-drug conjugates or NOV0712-DM4 was added to the cells.
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| In Vitro Model | Ovarian mixed germ cell tumor | PA-1 cells | CVCL_0479 | ||
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