Product Information
Registration Status: ActiveFEBURIC FILM COATED TABLET 80MG is approved to be sold in Singapore with effective from 2016-02-19. It is marketed by ASTELLAS PHARMA SINGAPORE PTE LTD, with the registration number of SIN14959P.
This product contains Febuxostat 80mg in the form of TABLET, FILM-COATED. It is approved for ORAL use.
This product is manufactured by Patheon France in FRANCE, andInterthai Pharmaceutical Manufacturing Ltd. in THAILAND.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Description
Febuxostat is a xanathine oxidase (XO) inhibitor indicated in patients with gout suffering from hyperuricemia and is used in its chronic management. Febuxostat is not recommended for the treatment of asymptomatic hyperuricemia. Febuxostat is marketed under the trade name Uloric by Takeda Pharmaceuticals America, Inc., and was approved by the FDA in February 2009.
Indication
For the treatment of hyperuricemia in patients with gout.
Mechanism of Action
Febuxostat, a xanthine oxidase inhibitor, achieves its therapeutic effect by decreasing serum uric acid. Febuxostat is not expected to inhibit other enzymes involved in purine and pyrimidine synthesis and metabolism at therapeutic concentrations.
Pharmacokinetics
- Absorption
- >49%
- Distribution
- The mean apparent steady state volume of distribution (Vss/F) of febuxostat was approximately 50 L (CV ~40%)
- 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. The relative contribution of each enzyme isoform in the metabolism of febuxostat is not clear. The oxidation of the isobutyl side chain leads to the formation of four pharmacologically active hydroxy metabolites, all of which occur in plasma of humans at a much lower extent than febuxostat. In urine and feces, acyl glucuronide metabolites of febuxostat (~35% of the dose), and oxidative metabolites, 67M-1 (~10% of the dose), 67M-2 (~11% of the dose), and 67M-4, a secondary metabolite from 67M-1 (~14% of the dose), appeared to be the major metabolites of febuxostat in vivo.
- Elimination
Toxicity
The FDA adverse event reporting system database, AERS, indicated potential signals of febuxostat-associated cardiovascular thromboembolic events. AERS is not capable of establishing the causal link and detecting the true frequency of an adverse event associated with a drug. The positive IC value found in this study merits continued surveillance and assessment of cardiovascular thromboembolic events associated with Febuxostat.
Active Ingredient/Synonyms
2-(3-cyano-4-isobutoxyphenyl)-4-methyl- 1,3-thiazole-5-carboxylic acid | Fébuxostat | Febuxostat | Febuxostatum | Febuxostat |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.