General
Preferred name
fesoterodine
Synonyms
FESOTERODINE FUMARATE ()
Fesoterodine (L-mandelate) ()
Fesoterodine (fumarate) ()
SPM-8272 ()
SPM 8272 ()
SPM-907 ()
SPM 907 ()
Toviaz ()
Fesoterodina ()
P&D ID
PD009283
CAS
286930-03-8
286930-02-7
1206695-46-6
Tags
available
prodrug
drug
Approved by
EMA
PMDA
FDA
First approval
2007
Drug indication
Urinary incontinence
Overactive bladder
Drug Status
approved
Max Phase
4.0
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION Fesoterodine Fumarate 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 Fumarate is used for the overactive bladder (OAB)[1][2].
ABSORPTION Tmax (5-HMT): 5 hours post-adminitration of fesoterodine. ; AUC (0,∞)= 49.5 ng·h/ ml ; Bioavailability, 5-HMT = 52%
PHARMACODYNAMICS In-vivo the fesoteridine prodrug is broken down into its active metabolite, 5-hydroxymethyl tolterodine (5-HMT), by plasma esterases. The 5-hydroxymethyl metabolite, which exhibits an antimuscarinic activity. Both urinary bladder contraction and salivation are mediated via cholinergic muscarinic receptors. Therefore, acting as a competitive muscarinic receptor antagonist, fesoterodine ultimately acts to decrease the detrusor pressure by its muscarinic antagonism, thereby decreasing bladder contraction and consequently, the urge to urinate.
ROE Renal: 70% of fesoterodine was recovered in urine as 5-HMT; 35% carboxy metabolite; 18% carboxy-N-desisopropylmetabolite, and 1% N-desisopropyl metabolite ; Fecal: 7% ; Hepatic: fesoterodine elimination via CYP2D6 and CYP3A4
TOXICITY Rat, Oral, LD50: ~ 681 mg/kg; Mouse, Oral, LD50: ~ 316 mg/kg ; Rat, Intravenous, NOAEL: 10 mg/kg; Mouse, Intravenous, NOAEL: 10 mg/kg
METABOLISM Metabolized by ubiquitous, nonspecific esterases to transform fesoterodine into 5-HMT; Extensive metabolism via CYP2D6 and CYP3A4 into inactive metabolites
DESCRIPTION The marketed formulation contains the fumarate compound (PubChem CID 9849808). Fesoterodine is an antimuscarinic prodrug, with the active metabolite being 5-hydroxymethyl tolterodine (5-HMT, PubChem CID 9819382). (GtoPdb)
PRICE 220
DESCRIPTION Fesoterodine ((R) Fesoterodine) is an orally active, competitive mAChR antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. It is used for the overactive bladder (OAB).
DESCRIPTION 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].
Compound Sets
16
AdooQ Bioactive Compound Library
A10386
Cayman Chemical Bioactives
23777
ChEMBL Approved Drugs
CHEMBL1201765
CHEMBL1201764
ChEMBL Drugs
CHEMBL1201765
CHEMBL1201764
Drug Repurposing Hub
DrugBank
DB06702
DrugBank Approved Drugs
DB06702
DrugCentral
4191
DrugCentral Approved Drugs
4191
DrugMAP
DM13495
DrugMAP Approved Drugs
DM13495
Guide to Pharmacology
7473
MedChem Express Bioactive Compound Library
HY-A0030
HY-70053
HY-70053A
NCATS Inxight Approved Drugs
621G617227
ReFrame library
The Spectrum Collection
External IDs
60
Properties
(calculated by RDKit )
Molecular Weight
411.28
Hydrogen Bond Acceptors
4
Hydrogen Bond Donors
1
Rotatable Bonds
10
Ring Count
2
Aromatic Ring Count
2
cLogP
5.38
TPSA
49.77
Fraction CSP3
0.5
Chiral centers
1.0
Largest ring
6.0
QED
0.42
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
mAChR
Indication
urinary incontinence
MOA
acetylcholine receptor antagonist
Pathway
GPCR/G protein
Neuronal Signaling
Source data