Antibody-drug Conjugate Information
General Information of This Antibody-drug Conjugate (ADC)
| ADC ID |
DRG0VROXA
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| ADC Name |
Tras-Bel
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| Synonyms |
Trastuzumab + Val-Cit-Belotecan dendrimer
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| Organization |
Tel Aviv University.; Inter-Lab, a subsidiary of Merck KGaA.
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| Drug Status |
Investigative
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| Drug-to-Antibody Ratio |
3.9
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| Structure |
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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 |
Belotecan
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Payload Info | ||||
| Therapeutic Target |
DNA topoisomerase 1 (TOP1)
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Target Info | ||||
| Linker Name |
AB2 self-immolative dendritic scaffold
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Linker Info | ||||
| Conjugate Type |
Random conjugation through reduced inter-chain cysteines.
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ADC-specific functional property(2027 Update)
Circulating Stability
| Incubation Time | 96h | Release | 0.2% | Reference |
[1]
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| Incubation Medium | Mouse serum | ||||
| Description |
First, we assessed the linker-drug stability of our trastuzumab-based ADCs in serum. To this end, Tras-Exa (DAR4), Tras-Bel (DAR4) and T-DXd (DAR8) were monitored overtime for their payload release in mouse and human sera (Table 2, Fig. S28) by the detection of free exatecan, belotecan and DXd via LC-MS/MS. Following 96 h incubation of the ADCs in sera, minimal amounts of the conjugated payload were released from both Tras-Exa and Tras-Bel ADCs in mouse (0.4% and 0.2%, respectively) and human (0.3% and 0.2%, respectively) sera.
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| Incubation Time | 96h | Release | 0.2% | Reference |
[1]
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| Incubation Medium | Human serum | ||||
| Description |
First, we assessed the linker-drug stability of our trastuzumab-based ADCs in serum. To this end, Tras-Exa (DAR4), Tras-Bel (DAR4) and T-DXd (DAR8) were monitored overtime for their payload release in mouse and human sera (Table 2, Fig. S28) by the detection of free exatecan, belotecan and DXd via LC-MS/MS. Following 96 h incubation of the ADCs in sera, minimal amounts of the conjugated payload were released from both Tras-Exa and Tras-Bel ADCs in mouse (0.4% and 0.2%, respectively) and human (0.3% and 0.2%, respectively) sera.
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References