PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 19473600-3 2009 The sustained-release formulation of fesoterodine delivers 5-HMT with linear, dose-proportional pharmacokinetics (PK) suitable for once-daily dosing. fesoterodine 37-49 histamine N-methyltransferase Homo sapiens 61-64 23497983-6 2013 Fesoterodine, 5-HMT, and tolterodine resulted in significantly increased (two- to five-fold) values of the apparent dissociation constant for specific [N-methyl-(3)H] scopolamine methyl chloride binding in the detrusor muscle and parotid gland, with little effect on the corresponding values of the maximal number of binding sites. fesoterodine 0-12 histamine N-methyltransferase Homo sapiens 16-19 23266359-2 2013 A highly sensitive, selective and rapid method has been developed for the simultaneous determination of fesoterodine and its active metabolite, 5-hydroxymethyl tolterodine (5-HMT) in human plasma by liquid chromatography-tandem mass spectrometry (LC-ESI-MS/MS). fesoterodine 104-116 histamine N-methyltransferase Homo sapiens 175-178 21352267-1 2011 WHAT IS ALREADY KNOWN ABOUT THIS SUBJECT: Tolterodine and 5-hydroxymethyl tolterodine (5-HMT) are equipotent active moieties of tolterodine; 5-HMT is the singular active moiety of fesoterodine. fesoterodine 180-192 histamine N-methyltransferase Homo sapiens 89-92 21352267-3 2011 On the other hand, the formation of 5-HMT from fesoterodine occurs via ubiquitous esterases. fesoterodine 47-59 histamine N-methyltransferase Homo sapiens 38-41 21352267-6 2011 The data suggest that fesoterodine delivers 5-HMT consistently, regardless of CYP2D6 status, with up to 40% higher bioavailability compared with tolterodine. fesoterodine 22-34 histamine N-methyltransferase Homo sapiens 46-49 21352267-7 2011 AIMS: Tolterodine and 5-hydroxymethyl tolterodine (5-HMT) are equipotent active moieties of tolterodine; 5-HMT is the singular active moiety of fesoterodine. fesoterodine 144-156 histamine N-methyltransferase Homo sapiens 107-110 21352267-8 2011 Formation of 5-HMT from fesoterodine and tolterodine occurs via esterases and CYP2D6 respectively. fesoterodine 24-36 histamine N-methyltransferase Homo sapiens 15-18 21352267-16 2011 Mean urinary excretion of 5-HMT following fesoterodine 4 and 8 mg, respectively, was 0.44 and 0.89 mg in EMs and 0.60 and 1.32 mg in PMs. fesoterodine 42-54 histamine N-methyltransferase Homo sapiens 28-31 21352267-20 2011 Fesoterodine delivers 5-HMT with less variability than tolterodine, regardless of CYP2D6 status, with up to 40% higher bioavailability. fesoterodine 0-12 histamine N-methyltransferase Homo sapiens 24-27 21545485-6 2011 RESULTS: Concomitant administration of fesoterodine with fluconazole increased AUC(0, ) and C(max) of 5-HMT by approximately 27% and 19%, respectively, with corresponding 90% confidence intervals of (18%, 36%) and (11%, 28%). fesoterodine 39-51 histamine N-methyltransferase Homo sapiens 104-107 20371737-1 2011 Fesoterodine, a new antimuscarinic for the treatment of overactive bladder, is rapidly and extensively hydrolyzed by nonspecific esterases to its principal active moiety, 5-hydroxymethyl tolterodine (5-HMT). fesoterodine 0-12 histamine N-methyltransferase Homo sapiens 202-205 22853865-1 2012 OBJECTIVE: Fesoterodine is a pro-drug of the active metabolite 5-hydroxymethyl tolterodine (5-HMT), a muscarinic receptor antagonist. fesoterodine 11-23 histamine N-methyltransferase Homo sapiens 94-97 21391941-6 2011 The different USDs (tolterodine, oxybutynin, solifenacin, darifenacin, and 5-hydroxy-methyl-tolterodine (5-HMT; the active metabolite of fesoterodine) were dissolved in plasma in their respective therapeutic concentration ranges. fesoterodine 137-149 histamine N-methyltransferase Homo sapiens 107-110 19915829-3 2010 We estimated the relative bioavailability of 5-hydroxymethyl tolterodine (5-HMT), the active metabolite of fesoterodine, following nighttime and daytime administration. fesoterodine 107-119 histamine N-methyltransferase Homo sapiens 76-79 24198608-4 2009 Fesoterodine is broken down to the active metabolite, 5-hydroxy-methyl-tolterodine (5-HMT) by non-specific esterases. fesoterodine 0-12 histamine N-methyltransferase Homo sapiens 86-89 24198608-9 2009 However the incidence of dry mouth is reduced with fesoterodine, compared to oxybutynin, due to the improved bladder selectivity of 5-HMT. fesoterodine 51-63 histamine N-methyltransferase Homo sapiens 134-137 19761716-1 2009 OBJECTIVE: Fesoterodine, a new antimuscarinic agent for overactive bladder, undergoes immediate and extensive hydrolysis by nonspecific esterases to 5-hydroxymethyl tolterodine (5-HMT), the metabolite principally responsible for its antimuscarinic activity. fesoterodine 11-23 histamine N-methyltransferase Homo sapiens 180-183 19145494-2 2009 Fesoterodine itself is inactive and is rapidly and extensively converted by ubiquitous esterases to its principal active moiety, 5-hydroxymethyl tolterodine (5-HMT). fesoterodine 0-12 histamine N-methyltransferase Homo sapiens 160-163 19145494-3 2009 5-HMT is formed via biotransformation of both fesoterodine and tolterodine, albeit by different metabolising enzymes, viz. fesoterodine 46-58 histamine N-methyltransferase Homo sapiens 2-5 19145494-11 2009 RESULTS: The mean peak plasma concentration (Cmax) of 5-HMT and the mean area under the time versus concentration curve (AUC) increased proportionally with the fesoterodine dose. fesoterodine 160-172 histamine N-methyltransferase Homo sapiens 56-59 19246724-2 2009 Compared with findings in healthy subjects, the maximum concentration in plasma of 5-hydroxymethyl tolterodine (5-HMT), the principal active moiety of fesoterodine, increases by 1.4-, 1.5-, and 2.0-fold and area under the curve increases by 1.6-, 1.8-, and 2.3-fold in subjects with mild, moderate, and severe renal impairment, respectively. fesoterodine 151-163 histamine N-methyltransferase Homo sapiens 114-117 19473600-10 2009 Mean values of both primary PK parameters of 5-HMT (AUC(0-tz) and C(max)) were approximately 19% higher after fesoterodine administration in the fed versus the fasted state. fesoterodine 110-122 histamine N-methyltransferase Homo sapiens 47-50 19835561-4 2009 Fesoterodine was selected amongst a series of ester analogues of 5-HMT to develop an advanced OAB treatment with an optimum biopharmaceutics profile, while maintaining a pharmacological link to tolterodine. fesoterodine 0-12 histamine N-methyltransferase Homo sapiens 67-70 19835561-0 2009 The design and development of fesoterodine as a prodrug of 5-hydroxymethyl tolterodine (5-HMT), the active metabolite of tolterodine. fesoterodine 30-42 histamine N-methyltransferase Homo sapiens 90-93 19835561-1 2009 This review highlights the design and development of fesoterodine (Toviaz) as a prodrug of 5-hydroxymethyl tolterodine (5-HMT), which is also the active metabolite of tolterodine, for the treatment of overactive bladder (OAB). fesoterodine 53-65 histamine N-methyltransferase Homo sapiens 122-125 19835561-1 2009 This review highlights the design and development of fesoterodine (Toviaz) as a prodrug of 5-hydroxymethyl tolterodine (5-HMT), which is also the active metabolite of tolterodine, for the treatment of overactive bladder (OAB). fesoterodine 67-73 histamine N-methyltransferase Homo sapiens 122-125 19835561-6 2009 In contrast to the cytochrome P450 (CYP) 2D6-mediated metabolism of tolterodine, 5-HMT formation from fesoterodine occurs via ubiquitous nonspecific esterases. fesoterodine 102-114 histamine N-methyltransferase Homo sapiens 83-86 19835561-7 2009 Consequently, treatment with fesoterodine results in consistent, genotype-independent exposure to a singular active moiety (5-HMT); treatment with tolterodine results in CYP2D6 genotype-dependent exposure to varying proportions of two active moieties (5-HMT and tolterodine). fesoterodine 29-41 histamine N-methyltransferase Homo sapiens 126-129 29338933-2 2018 Fesoterodine is a prodrug which is extensively hydrolyzed by non-specific esterases to the active metabolite 5-hydroxymethyl tolterodine (5-HMT). fesoterodine 0-12 histamine N-methyltransferase Homo sapiens 140-143 19000553-2 2008 Following oral administration, fesoterodine is rapidly and extensively hydrolyzed by nonspecific esterases to its active moiety: 5-hydroxymethyl tolterodine (5-HMT). fesoterodine 31-43 histamine N-methyltransferase Homo sapiens 160-163 30742396-4 2018 As a result of fesoterodine cleavage by non-specific esterase, the active metabolite 5-hydroxymethyl tolterodine (5-HMT) is formed. fesoterodine 15-27 histamine N-methyltransferase Homo sapiens 116-119