Fesoterodine L-mandelate

Fesoterodine L-mandelate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine L-mandelate is used for the overactive bladder (OAB)[1][2].

Signaling Pathways >> Neuronal Signaling >> mAChR

Signaling Pathways >> GPCR/G Protein >> mAChR

Research Areas >> Metabolic Disease

Research Areas >> Neurological Disease

pKi: 8.0 (M1), 7.7 (M2), 7.4 (M3), 7.3 (M4) and 7.5 (M5)[3]

Fesoterodine L-mandelate decreases micturition frequency, urgency severity and urgency incontinence episodes and increases the volume voided with each micturition[1]. After oral administration, Fesoterodine L-mandelate is rapidly and extensively hydrolysed in plasma by nonspecific esterases to Desfesoterodine (5-hydroxymethyl tolterodine; SPM 7605; HY-76569; an active metabolite of Fesoterodine)[3][4].

Fesoterodine L-mandelate (0.01-1 mg/kg; IV) reduces the micturition pressure and increases bladder capacity and ICIs (intercontraction intervas) at the lowest dose tested of 0.01 mg/kg[3]. Animal Model: Bladders from female Sprague-Dawley rats (225-275 g)[3] Dosage: 0.01, 0.1 and 1 mg/kg Administration: IV Result: Reduced the micturition pressure and increased bladder capacity and ICIs at the lowest dose tested of 0.01 mg/kg.

[1]. Ellsworth P, et al. Fesoterodine for the treatment of urinary incontinence and overactive bladder. Ther Clin Risk Manag. 2009;5:869-76. Epub 2009 Nov 18.

[2]. Didem Yilmaz-Oral, et al. The Beneficial Effect of Fesoterodine, a Competitive Muscarinic Receptor Antagonist on Erectile Dysfunction in Streptozotocin-induced Diabetic Rats

[3]. Peter Ney, et al. Pharmacological Characterization of a Novel Investigational Antimuscarinic Drug, Fesoterodine, in Vitro and in Vivo. BJU Int. 2008 Apr;101(8):1036-42.

[4]. Martin C Michel, et al. Fesoterodine: A Novel Muscarinic Receptor Antagonist for the Treatment of Overactive Bladder Syndrome. Expert Opin Pharmacother. 2008 Jul;9(10):1787-96.