Drug intelligence / Profile preview

diclofenac sodium + menthol

Development stage
Phase 1
Lead developer
Novartis
Modality
Small Molecules
Administration
Topical
01

Overview

Diclofenac sodium + menthol is an investigational fixed-dose topical gel developed by GSK as **MFC51123**, containing 1% diclofenac sodium and 3% menthol. Diclofenac is a nonsteroidal anti-inflammatory drug that inhibits cyclooxygenase enzymes and reduces prostaglandin-mediated pain and inflammation, while menthol activates cold-sensing TRPM8 channels to produce a cooling counterirritant analgesic effect. The gel was studied in tube and roll-on presentations for acute ankle sprain and other mild-to-moderate musculoskeletal pain or inflammation, including sprains and sports injuries. A pivotal Phase III ankle-sprain study was completed, and pharmacokinetic testing found systemic diclofenac exposure substantially lower than with oral diclofenac, although local skin reactions were more frequent than with topical diclofenac gel alone. ([gsk-studyregister.com](https://www.gsk-studyregister.com/trials/202179))

Brand names
DicloStream
Other names
1% diclofenac sodium + 3% mentholdiclofenac + mentholdiclofenac-menthol geldiclofenac/mentholdiclofenac sodium + menthol
02

Targets

PTGS2 (Prostaglandin-Endoperoxide Synthase 2)PGHS-1 (Prostaglandin G/H Synthase 1)TRPM8 (Transient receptor potential cation channel subfamily M member 8)

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