Drug intelligence / Profile preview

antrafenine

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

Overview

Antrafenine is a phenylpiperazine derivative and small molecule drug developed in the late 1970s as a non-narcotic analgesic and anti-inflammatory agent, with efficacy similar to naproxen. Its primary mechanism of action is believed to be inhibition of cyclooxygenase (COX) enzymes, specifically both COX-1 (prostaglandin G/H synthase 1) and COX-2 (prostaglandin G/H synthase 2), leading to reduced prostaglandin synthesis. This results in anti-inflammatory and analgesic effects. Antrafenine was studied for the treatment of mild to moderate pain and osteoarthritis but has largely been replaced by newer drugs due to limited use. It shows long duration of action and good tolerance in pharmacological studies[1][2][3][5][7].

Brand names
Stakane
Other names
2-[4-[3-(trifluoromethyl)phenyl]-1-piperazinyl]ethyl 2-[[7-(trifluoromethyl)-4-quinolinyl]amino]benzoate
02

Targets

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

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