Description
PHARMACOLOGY
PHARMACOKINETICS:
- Absorption: – The absorption of radio labeled febuxostat following oral dose administration was estimated to be at least 49% (based on total radioactivity recovered in urine). Maximum plasma concentrations of febuxostat occurred between 1 and 1.5 hours post-dose
- Distribution: – The mean apparent steady state volume of distribution (Vss/F) of febuxostat was approximately 50 L (CV ~40%). The plasma protein binding of febuxostat is approximately 99.2%.
- Metabolism: – Febuxostat is extensively metabolized by both conjugation via uridine diphosphate glucuronosyltransferase (UGT) enzymes including UGT1A1, UGT1A3, UGT1A9, and UGT2B7 and oxidation via cytochrome P450 (CYP) enzymes including CYP1A2, 2C8 and 2C9 and non-P450 enzymes.
- Elimination: – Febuxostat is eliminated by both hepatic and renal pathways.
INDICATIONS:
- Febuxostat is a xanthine oxidase (XO) inhibitor indicated for the chronic management of hyperuricemia in patients with gout.
- Febuxostat is not recommended for the treatment of asymptomatic hyperuricemia.
