ABSTRACT

Fesoterodine is a newly identified selective muscarinic M3 receptor antagonist which is currently being considered for regulatory approval in the treatment of overactive bladder. The chemical name of fesoterodine is 2-methylpropionic acid 2-[3-(N, N-diisopropylamino)-1(R)-phenylpropyl]- 4-(hydroxymethyl)phenyl ester. The molecular formula is C26H37NO3. Fesoterodine is extensively and rapidly hydrolyzed in both humans and rodents to its primary active metabolite, SPM 7605 (Figure 24.1). The conversion of fesoterodine to its primary metabolite is by hepatic hydrolysis. The active metabolite has demonstrated potentspecific and non-subtype selective antimuscarinic activity in both in vitro and in vivo preclinical studies. In vitro studies have shown tissue selectivity three times greater for the bladder than for the salivary gland for SPM 7605.