The Sound of Evolution
Nabumetone
Mechanism of action:
Nabumetone is a naphthylalkanone derivative. Nabumetone is a prodrug that is metabolized in the liver into its major active product, 6-methoxy-2-naphthylacetic acid (6-MNA). 6-MNA is a cyclooxygenase inhibitor with slightly greater inhibitory activity against COX-2 than COX-1. 6-MNA blocks the production of prostaglandins.
Reference(s):
1. Davies NM et al. (1997). Clinical pharmacokinetics of nabumetone. The dawn of selective cyclo-oxygenase-2 inhibition? Clin Pharmacokinet.
2. Matsumoto K et al. (2015). Reductive metabolism of nabumetone by human liver microsomal and cytosolic fractions: exploratory prediction using inhibitors and substrates as marker probes. Eur J Drug Metab Pharmacokinet.
3. Nobilis M et al. (2013). Analytical power of LLE-HPLC-PDA-MS/MS in drug metabolism studies: identification of new nabumetone metabolites. J Pharm Biomed Anal.