Drug intelligence / Profile preview

flurbiprofen axetil (Kaken Pharmaceutical Co., Ltd., 044777)

Development stage
Unknown
Lead developer
Kaken Pharmaceutical
Modality
Small Molecules
Administration
Intravenous
01

Overview

Flurbiprofen axetil is an injectable prodrug of the nonsteroidal anti-inflammatory drug (NSAID) flurbiprofen, specifically formulated within lipid microspheres (a lipid emulsion) to enhance its delivery and solubility. Upon intravenous administration, the drug is rapidly hydrolyzed by esterases in the blood to release the active moiety, flurbiprofen. Flurbiprofen acts as a non-selective inhibitor of the enzymes cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2), thereby reducing the synthesis of prostaglandins that mediate pain and inflammation. The lipid microsphere formulation provides a high affinity for surgical incision sites and inflammatory tissues, allowing for targeted analgesic effects. It is primarily indicated for the management of postoperative pain, cancer-related pain, and chronic inflammatory conditions such as arthritis. Initially developed by Kaken Pharmaceutical, it is also marketed by companies including Beijing Tide Pharmaceutical and Shanxi Pude Pharmaceutical.

Brand names
RopionKaifenPude
Other names
flubiprofen axetilflurbiprofen axetilflurbiprofen 1-acetoxyethyl esterflurbiprofen1-acetoxyethyl esterflurbiprofen-1-acetoxyethyl ester
02

Targets

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

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