Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0FWMEA
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| ADC Name |
aU2023279443A1 Example A11
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| Synonyms |
AU2023279443A1 Example A11
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| Organization |
UBE CORPORATION
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| Drug Status |
Investigative
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| Drug-to-Antibody Ratio |
8
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| Antibody Name |
Trastuzumab
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Antibody Info | ||||
| Antigen Name |
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
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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 |
AU2023279443A1, Example A10, Linker
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Linker Info | ||||
| Conjugate Type |
Random conjugation through reduced inter-chain cysteines.
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| Combination Type |
Exemplification A3-11
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ADC-specific functional property(2027 Update)
Payload Release Efficiency
| Incubation Time | 24hr | Release | 64% | Reference |
[1]
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| Description |
Metabolism test using human liver lysosomal fraction. To a reaction composition solution in which human liver lysosome (corresponding to 0.125 mg of protein) was suspended and distilled water (10 uL) was added 1.2 uM test compound (25 uL) dissolved in PBS to prepare a reaction solution. After the reaction solution was incubated at 37 °C for 24 hours, Dxd released from the Example A11 into the reaction solution was quantified by LC-MS/MS.
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| Incubation Time | 24hr | Release | 30% | Reference |
[1]
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| Description |
Metabolism test using human liver Cathepsin B. To human liver Cathepsin B (corresponding to 400 Unit/mL) (5 pL), X10 Catabolic Buffer (10 uL), 2.5 mM Bovine Serum Albumin (5 uL), and distilled water (55 uL) was added 1.2 uM test compound (25 uL) dissolved in PBS to prepare a reaction solution. After the reaction solution was incubated at 37°C for 24 hours, Dxd released from the Example A11 into the reaction solution was quantified by LC-MS/MS.
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General Information of The Activity Data Related to This ADC
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 lnhibition value (TGl) | > 50% | Positive HER2 expression (HER2+++/++) | ||
| Method Description |
A mixed solvent of PBS and and Matrigel was used to prepare a cell suspension of 5.0x107 cells / mL. The prepared cell suspension was subcutaneously injected to the right flank region of female BALB/c-nu/nu mice at 0.1 mL per mouse. Individuals having a tumor volume within a range of 50 to 500 mm 3 were selected. test compound at a concentration of 3 mg/kg or the solvent alone was intravenously administered. the tumor volume was measured at Day 0 and Day 21.
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| In Vivo Model | NCI-N87 female BALB/c-nu/nu mice model | ||||