Degradation pathway of a taxane derivative DS80100717 drug substance and drug product

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Abstract

The degradation pathway of a taxane derivative and anticancer agent, DS80100717, was investigated. Several degradants were generated under acidic, basic, and oxidative stress conditions in solution. The chemical structures of eight degradants of DS80100717 were elucidated using MS and NMR. The major degradant of the DS80100717 drug substance derived by heating in solid-state was the N-oxide form via oxidation and C2′-epimer of the side chain via acid hydrolysis. We proposed previously unreported degradation pathways of DS80100717 with taxane derivatives such as paclitaxel, docetaxel, and cabazitaxel.

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Tamura, K., Ono, M., Kawabe, T., Ohara, M., & Yonemochi, E. (2020). Degradation pathway of a taxane derivative DS80100717 drug substance and drug product. Chemical and Pharmaceutical Bulletin, 68(4), 392–397. https://doi.org/10.1248/cpb.c20-00032

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