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.