Drug intelligence / Profile preview

nabumetone

Development stage
Approved
Lead developer
GSK
Modality
Small Molecules
Administration
Oral
01

Overview

Nabumetone is a nonsteroidal anti-inflammatory drug (NSAID) of the naphthylalkanone class, primarily indicated for the symptomatic relief of osteoarthritis and rheumatoid arthritis. It is a non-acidic prodrug that undergoes extensive hepatic metabolism to form its active metabolite, 6-methoxy-2-naphthylacetic acid (6-MNA). This metabolite acts as a potent inhibitor of cyclooxygenase (COX) enzymes, with some evidence suggesting a degree of partial selectivity for COX-2. Nabumetone is distinguished by its relatively low incidence of gastrointestinal side effects compared to traditional acidic NSAIDs, likely due to its non-acidic nature and the fact that its active form is generated post-absorption. It is typically administered once daily and has been evaluated for its safety profile in elderly patients and its minimal impact on platelet aggregation.

Brand names
RelafenCenatone
Other names
nabumetone
02

Targets

PGHS-1 (Prostaglandin G/H Synthase 1)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)

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