抗DXd抗体

DXd is a derivative of exatecan (DX8951f), a compound with increased activity and improved solubility compared to CPT, and described not to be an ABCC2 or ABCG1 substrate. DXd was used in several proprietary ADC programs, such as DS-8201a (Enhertu), U3-1402 and DS-6157a, conjugated at DAR8 and DS-1062a and DS-7300a conjugated at lower DAR (4) to limit their toxicity, that are either approved by the FDA (DS-8201a) or currently under clinical evaluation. Although the DXd payload presented lower passive membrane permeability than exatecan mesylate, it was found to be less myelotoxic and was therefore also selected for its improved safety profile.
The anti-payload antibody is a useful reagent in ADC research by quantifying and monitoring drug levels or accumulations in tumor tissue, and more. It can be used in PK, PD analysis and ELISA.

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