Drug intelligence / Profile preview

ketoprofen + cyclobenzaprine + caffeine

Development stage
Phase 3
Lead developer
Sanofi
Modality
Small Molecules
Administration
Oral
01

Overview

A fixed-dose combination of three active pharmaceutical ingredients: ketoprofen, cyclobenzaprine, and caffeine. Ketoprofen is a nonsteroidal anti-inflammatory drug (NSAID) that inhibits prostaglandin synthesis by blocking cyclooxygenase enzymes, providing analgesic and anti-inflammatory effects. Cyclobenzaprine is a centrally acting muscle relaxant that acts primarily at the brainstem to reduce tonic somatic motor activity influencing both alpha and gamma motor neurons, thereby relieving skeletal muscle spasm associated with acute musculoskeletal conditions. Caffeine is a central nervous system stimulant that can counteract drowsiness caused by cyclobenzaprine and may enhance the analgesic effect of NSAIDs like ketoprofen. This combination has been studied for use in treating musculoskeletal pain and acute muscle spasm[1][2][3][6].

02

Targets

ADORA1 (Adenosine receptor A1 subtype)ADORA2A (Adenosine A₂A Receptor)ADORA2B (Adenosine A2B receptor)ADORA3 (Adenosine A3 receptor)HRH1 (Histamine H1 Receptor)5-HT (Serotonin receptors)PDE (Phosphodiesterase family)PGHS-1 (Prostaglandin G/H Synthase 1)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)

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