Drug intelligence / Profile preview

amfenac

Development stage
Unknown
Lead developer
Alcon
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral, Ophthalmic
01

Overview

Amfenac is a non-steroidal anti-inflammatory drug (NSAID) with antipyretic and analgesic properties. It acts as a potent inhibitor of cyclooxygenase enzymes (COX-1 and COX-2), thereby reducing the synthesis of prostaglandins involved in inflammation, pain, and fever[1][3][6]. Amfenac is the active metabolite of nepafenac, which is used primarily for ocular indications such as pain and inflammation following cataract surgery. Amfenac itself has been studied for use in various inflammatory conditions including rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, gout, headache, dental pain, post-operative pain, menstrual pain (dysmenorrhea), arthralgia (joint pain), muscle pain and fever[5]. Its mechanism involves both reversible inhibition and unique time-dependent irreversible binding to COX enzymes[6][7].

Brand names
Amfenac
Other names
amfenaco2-(2-amino-3-benzoylphenyl)acetic acidamfenacum
02

Targets

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

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