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开发并验证新的LC-MS/MS方法，用于定量人血浆中达拉非尼及其主要代谢物羟基达拉非尼 (OHD)。OHD（纯度>99%）通过美迪西合成

2023-06-28
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14-hydroxy-dabrafenib-1.jpg

Increased understanding of molecular pathways leads to the development of effective targeted therapies for the treatment of solid tumors. Dabrafenib (DAB) undergoes oxidative metabolism via cytochrome P450 (CYP) 3A4 and CYP2C8 to form hydroxy-dabrafenib (OHD), an active metabolite, with a twofold higher potency than an inhibitor of mutant BRAF. OHD (purity >99 %) was synthesized by Medicilon. Medicilon synthetic chemistry team is capable of the independent design of synthesis pathways and complex compound treatments, key to helping accelerate drug discovery.

Reference

David Balakirouchenane, et al. Simultaneous quantification of dabrafenib, hydroxy-dabrafenib and trametinib in human plasma by liquid chromatography-tandem mass spectrometry. J Pharm Biomed Anal. 2021 Jan 30;193:113718. doi: 10.1016/j.jpba.2020.113718.

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