Reaction: Dabrafenib to 1 product

Reaction
Dabrafenib
DB08912
Hydroxy-dabrafenib
DBMET03510
Reaction type
Aliphatic hydroxylation
Direction
Major circulating metabolite?
Yes
Spontaneous?
No
Activity
active
References
  1. Bershas DA, Ouellet D, Mamaril-Fishman DB, Nebot N, Carson SW, Blackman SC, Morrison RA, Adams JL, Jurusik KE, Knecht DM, Gorycki PD, Richards-Peterson LE: Metabolism and disposition of oral dabrafenib in cancer patients: proposed participation of aryl nitrogen in carbon-carbon bond cleavage via decarboxylation following enzymatic oxidation. Drug Metab Dispos. 2013 Dec;41(12):2215-24. doi: 10.1124/dmd.113.053785. Epub 2013 Oct 4. [Article]
  2. Puszkiel A, Noe G, Bellesoeur A, Kramkimel N, Paludetto MN, Thomas-Schoemann A, Vidal M, Goldwasser F, Chatelut E, Blanchet B: Clinical Pharmacokinetics and Pharmacodynamics of Dabrafenib. Clin Pharmacokinet. 2019 Apr;58(4):451-467. doi: 10.1007/s40262-018-0703-0. [Article]
  3. Ellens H, Johnson M, Lawrence SK, Watson C, Chen L, Richards-Peterson LE: Prediction of the Transporter-Mediated Drug-Drug Interaction Potential of Dabrafenib and Its Major Circulating Metabolites. Drug Metab Dispos. 2017 Jun;45(6):646-656. doi: 10.1124/dmd.116.073932. Epub 2017 Mar 20. [Article]
  4. FDA Approved Drug Proucts: TAFINLAR® (dabrafenib) capsules, for oral use [Link]
Comments
Not Available
Enzymes
EnzymeKmVmaxRole
Cytochrome P450 3A4Not AvailableNot Availableconfirmed
Cytochrome P450 2C8Not AvailableNot Availableimplied