Darifenacin, an orally active, once a day selective M3
receptor antagonist, was launched for the treatment of overactive
bladder in patients with symptoms of urge urinary
incontinence, urgency and frequency. The drug selectively
inhibits M3 receptor in the detrusor muscle while sparing the M1 and M2 receptors that are believed to be involved
in central nervous system and cardiovascular function respectively.
The compound was originally developed by
Pfizer and licensed to Novartis and Bayer.
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Darifenacin hydrobromide is used as a medication to treat urinary incontinence. It works by blocking the M3 muscarinic acetylcholine receptor.
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ChEBI: The hydrobromide salt of darifenacin. A selective antagonist for the M3 muscarinic acetylcholine receptor, which is primarily responsible for bladder muscle contractions, it is used in the management of urinary incontinence.
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Darfenacin (Enablex),(s)-2-{1-[2-(2,3-dihydrobenzofuran-5-yl)ethyl]-3-pyrrolidinyl}-2,2-diphen-ylacetamide, is an antimuscarinicagent that has selectivity for the M3 muscarinicsubtype receptor. By competitively blocking of the muscarinicreceptors results in a reduction of the smoothmuscle tone, allowing for greater volume of urine to bestored in the bladder. This results in less urinary incontinence,urgency, and frequency. It is a white to almostwhite, crystalline powder, with a molecular weight of507.5. Darifenacin is metabolized by the isozymesCYP2D6 and CYP3A4 with the primary metabolic routesbeing monohydroxylation of the dihydrobenzofuran ring,opening of the dihydrobenzofuran ring, and N-dealkylationof the pyrrolidine nitrogen.
