Drug intelligence / Profile preview

loxoprofen

Development stage
Phase 4
Lead developer
Daiichi Sankyo
Modality
Small Molecules
Administration
Oral, Topical, Transdermal
01

Overview

Loxoprofen is a nonsteroidal anti-inflammatory drug (NSAID) of the propionic acid derivative class, related to ibuprofen and naproxen. It is primarily indicated for the treatment of pain and inflammation associated with musculoskeletal and joint disorders, as well as rheumatism, soft tissue injury, and other conditions such as headache, toothache, menstrual cramps, neuralgia, and postoperative pain. Loxoprofen acts as a prodrug that is rapidly metabolized in the body to its active trans-alcohol form. The active metabolite functions as a potent non-selective inhibitor of cyclooxygenase (COX), blocking both COX‑1 and COX‑2 isoforms. This inhibition reduces the synthesis of prostaglandins from arachidonic acid—key mediators involved in pain, inflammation, and fever responses[1][2][3][5][6]. Developed originally by Sankyo (now Daiichi Sankyo), it is widely used in Japan and several other countries.

Brand names
LoxoninOxenoLoxomacJaproloxRoxoninRoxonin TapeOxotronLoxonin S PlusLoxonin S Premium
Other names
2-(4-(2-Oxocyclopentyl)methyl)phenyl)propanoic acidloxoprofeneloxoprofeno
02

Targets

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

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