DESFESOTERODINE FUMARATE

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C22H31NO2.C4H4O4
Molecular Weight	457.5592
Optical Activity	UNSPECIFIED
Defined Stereocenters	1 / 1
E/Z Centers	1
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

OC(=O)\C=C\C(O)=O.CC(C)N(CC[C@H](C1=CC=CC=C1)C2=C(O)C=CC(CO)=C2)C(C)C

InChI

InChIKey=CFLJDPGMBAKCIK-BOQYJDHWSA-N

InChI=1S/C22H31NO2.C4H4O4/c1-16(2)23(17(3)4)13-12-20(19-8-6-5-7-9-19)21-14-18(15-24)10-11-22(21)25;5-3(6)1-2-4(7)8/h5-11,14,16-17,20,24-25H,12-13,15H2,1-4H3;1-2H,(H,5,6)(H,7,8)/b;2-1+/t20-;/m1./s1

HIDE SMILES / InChI

Molecular Formula	C22H31NO2
Molecular Weight	341.487
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	1 / 1
E/Z Centers	0
Optical Activity	UNSPECIFIED

Molecular Formula	C4H4O4
Molecular Weight	116.0722
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	1
Optical Activity	NONE

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/19835561 | DOI: 10.1002/(SICI)1520-6777(1996)15:4<249::AID-NAU1>3.0.CO;2-F | https://www.ncbi.nlm.nih.gov/pubmed/9353847https://www.ncbi.nlm.nih.gov/pubmed/19835561
Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/18279452

Fesoterodine (trade name Toviaz) is a prodrug of 5-hydroxymethyl tolterodine, which is also the active metabolite of tolterodine. Fesoterodine and its active metabolites are nonsubtype selective, competitive antagonists of human muscarinic receptors, but 5-hydroxymethyl tolterodine has greater potency than the parent compound. A prodrug approach was necessary for systemic bioavailability of 5-hydroxymethyl tolterodine after oral administration. Fesoterodine was originated by Schwarz Pharma (later a subsidiary of UCB) and is being developed by Pfizer for the treatment of overactive bladder and urinary urge incontinence. The agent is launched in several countries for the treatment of overactive bladder, including the US, Japan, Canada, Europe and Asia.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Muscarinic acetylcholine receptor M1 168 Target ID: CHEMBL216 Sources: DOI: 10.1002/(SICI)1520-6777(1996)15:4<249::AID-NAU1>3.0.CO;2-F	Antagonist 2849	2.3 nM [Ki]
Muscarinic acetylcholine receptor M2 121 Target ID: CHEMBL211 Sources: DOI: 10.1002/(SICI)1520-6777(1996)15:4<249::AID-NAU1>3.0.CO;2-F	Antagonist 2849	2.0 nM [Ki]
Muscarinic acetylcholine receptor M3 160 Target ID: CHEMBL245 Sources: DOI: 10.1002/(SICI)1520-6777(1996)15:4<249::AID-NAU1>3.0.CO;2-F	Antagonist 2849	2.5 nM [Ki]
Muscarinic acetylcholine receptor M4 87 Target ID: CHEMBL1821 Sources: DOI: 10.1002/(SICI)1520-6777(1996)15:4<249::AID-NAU1>3.0.CO;2-F	Antagonist 2849	2.8 nM [Ki]
Muscarinic acetylcholine receptor M5 63 Target ID: CHEMBL2035 Sources: DOI: 10.1002/(SICI)1520-6777(1996)15:4<249::AID-NAU1>3.0.CO;2-F	Antagonist 2849	2.9 nM [Ki]
Muscarinic acetylcholine receptor M1 168 Target ID: CHEMBL216 Sources: https://www.ncbi.nlm.nih.gov/pubmed/23497983 \| https://www.ncbi.nlm.nih.gov/pubmed/18279452	Antagonist 2849	8.0 null [pKi]
Muscarinic acetylcholine receptor M2 121 Target ID: CHEMBL211 Sources: https://www.ncbi.nlm.nih.gov/pubmed/23497983 \| https://www.ncbi.nlm.nih.gov/pubmed/18279452	Antagonist 2849	7.7 null [pKi]
Muscarinic acetylcholine receptor M3 160 Target ID: CHEMBL245 Sources: https://www.ncbi.nlm.nih.gov/pubmed/23497983 \| https://www.ncbi.nlm.nih.gov/pubmed/18279452	Antagonist 2849	7.4 null [pKi]
Muscarinic acetylcholine receptor M4 87 Target ID: CHEMBL1821 Sources: https://www.ncbi.nlm.nih.gov/pubmed/23497983 \| https://www.ncbi.nlm.nih.gov/pubmed/18279452	Antagonist 2849	7.3 null [pKi]
Muscarinic acetylcholine receptor M5 63 Target ID: CHEMBL2035 Sources: https://www.ncbi.nlm.nih.gov/pubmed/23497983 \| https://www.ncbi.nlm.nih.gov/pubmed/18279452	Antagonist 2849	7.5 null [pKi]

Conditions

Condition	Modality	Highest Phase	Product
Urinary incontinence 14 Sources: DOI: 10.1002/(SICI)1520-6777(1996)15:4<249::AID-NAU1>3.0.CO;2-F https://www.ncbi.nlm.nih.gov/pubmed/9353847	Primary	Preclinical	Unknown Approved Use Unknown
Partial urethral obstruction 5 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19888972 https://www.ncbi.nlm.nih.gov/pubmed/20639056	Primary	Preclinical	Unknown Approved Use Unknown
Overactive bladder 39 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022030s014lbl.pdf	Palliative	Approved 8583	TOVIAZ Approved Use Toviaz is a muscarinic antagonist indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and frequency. Launch Date 2008
Overactive bladder 39 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2008/022030lbl.pdf	Primary	Approved 8583	TOVIAZ Approved Use Toviaz® is a muscarinic antagonist indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and frequency. Toviaz is a muscarinic antagonist indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and frequency. Launch Date 2008

C_max

Value	Dose	Analyte	Population
1.89 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022030s014lbl.pdf	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	5-HYDROXYMETHYL TOLTERODINE plasma	Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN
2.464 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022030s000_ClinPharmR.pdf#page=23	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	DESFESOTERODINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
5.519 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022030s000_ClinPharmR.pdf#page=23	8 mg single, oral dose: 8 mg route of administration: Oral experiment type: SINGLE co-administered:	DESFESOTERODINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
10.863 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022030s000_ClinPharmR.pdf#page=23	16 mg single, oral dose: 16 mg route of administration: Oral experiment type: SINGLE co-administered:	DESFESOTERODINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1.96 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022030s000_ClinPharmR.pdf#page=25	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	DESFESOTERODINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
2.89 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022030s000_ClinPharmR.pdf#page=25	8 mg 1 times / day single, oral dose: 8 mg route of administration: Oral experiment type: SINGLE co-administered:	DESFESOTERODINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
2.32 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022030s000_ClinPharmR.pdf#page=25	4 mg 1 times / day multiple, oral dose: 4 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DESFESOTERODINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
3.59 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022030s000_ClinPharmR.pdf#page=25	8 mg 1 times / day multiple, oral dose: 8 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DESFESOTERODINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED

AUC

Value	Dose	Analyte	Population
24.461 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022030s000_ClinPharmR.pdf#page=23	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	DESFESOTERODINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
53.715 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022030s000_ClinPharmR.pdf#page=23	8 mg single, oral dose: 8 mg route of administration: Oral experiment type: SINGLE co-administered:	DESFESOTERODINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
111.091 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022030s000_ClinPharmR.pdf#page=23	16 mg single, oral dose: 16 mg route of administration: Oral experiment type: SINGLE co-administered:	DESFESOTERODINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
19.9 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022030s000_ClinPharmR.pdf#page=25	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	DESFESOTERODINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
26.9 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022030s000_ClinPharmR.pdf#page=25	8 mg 1 times / day single, oral dose: 8 mg route of administration: Oral experiment type: SINGLE co-administered:	DESFESOTERODINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
23.4 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022030s000_ClinPharmR.pdf#page=25	4 mg 1 times / day multiple, oral dose: 4 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DESFESOTERODINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
32.8 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022030s000_ClinPharmR.pdf#page=25	8 mg 1 times / day multiple, oral dose: 8 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DESFESOTERODINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED

T_1/2

Value	Dose	Analyte	Population
7.31 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022030s014lbl.pdf	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	5-HYDROXYMETHYL TOLTERODINE plasma	Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN
9.671 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022030s000_ClinPharmR.pdf#page=23	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	DESFESOTERODINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
9.37 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022030s000_ClinPharmR.pdf#page=23	8 mg single, oral dose: 8 mg route of administration: Oral experiment type: SINGLE co-administered:	DESFESOTERODINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
7.58 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022030s000_ClinPharmR.pdf#page=23	16 mg single, oral dose: 16 mg route of administration: Oral experiment type: SINGLE co-administered:	DESFESOTERODINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
8.13 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022030s000_ClinPharmR.pdf#page=25	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	DESFESOTERODINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
6.86 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022030s000_ClinPharmR.pdf#page=25	8 mg 1 times / day single, oral dose: 8 mg route of administration: Oral experiment type: SINGLE co-administered:	DESFESOTERODINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
5.13 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022030s000_ClinPharmR.pdf#page=25	4 mg 1 times / day multiple, oral dose: 4 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DESFESOTERODINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
4.86 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022030s000_ClinPharmR.pdf#page=25	8 mg 1 times / day multiple, oral dose: 8 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DESFESOTERODINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED

F_unbound

Value	Dose	Co-administered	Analyte	Population
50% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022030s014lbl.pdf	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:		5-HYDROXYMETHYL TOLTERODINE plasma	Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN
50% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/022030s019lbl.pdf#page=16			DESFESOTERODINE plasma	Homo sapiens

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inhibitor 2252 inducer 1087 substrate 1946	inhibitor 2438 inducer 440	inhibitor 2507 substrate 1388	inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP1A2 2153 CYP2B6 926 CYP2C8 1057 CYP2C19 2057 CYP2E1 1060 P-gp 1741	P-gp 2052	CYP1A2 832 CYP2B6 669 CYP2C19 329

Drug as perpetrator

Target	Modality	Activity	Metabolite
CYP1A2 2333	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022030s014lbl.pdf#page=12 Page: 12.0	no	SPM 7605 5
CYP1A2 2333	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022030s014lbl.pdf#page=12 Page: 12.0	no	SPM 7605 5
CYP2B6 1160	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022030s014lbl.pdf#page=12 Page: 12.0	no	SPM 7605 5
CYP2B6 1160	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022030s014lbl.pdf#page=12 Page: 12.0	no	SPM 7605 5
CYP2C19 2141	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022030s014lbl.pdf#page=12 Page: 12.0	no	SPM 7605 5
CYP2C19 2141	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022030s014lbl.pdf#page=12 Page: 12.0	no	SPM 7605 5
CYP2C8 1117	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022030s014lbl.pdf#page=12 Page: 12.0	no	SPM 7605 5
CYP2C9 2497	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022030s014lbl.pdf#page=12 Page: 12.0	no	SPM 7605 5
CYP2C9 2497	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022030s014lbl.pdf#page=12 Page: 12.0	no	SPM 7605 5
CYP2D6 2546	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022030s014lbl.pdf#page=12 Page: 12.0	no	SPM 7605 5
CYP2E1 1146	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022030s014lbl.pdf#page=12 Page: 12.0	no	SPM 7605 5
CYP3A4 2633	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022030s014lbl.pdf#page=12 Page: 12.0	no	SPM 7605 5
CYP3A4 2633	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/022030s014lbl.pdf#page=12 Page: 12.0	no	SPM 7605 5
P-gp 1932	inhibitor 4027 Sources: https://www.ema.europa.eu/en/documents/scientific-discussion/toviaz-epar-scientific-discussion_en.pdf#page=18 Page: 18.0	weak
L-type Ca2+ 7	supressor 160 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022030s000_PharmR_P1.pdf#page=58 Page: 58.0	yes [Inhibition 15 uM]

Drug as victim

Target	Modality	Activity	Metabolite	Clinical evidence
P-gp 2052	substrate 4014 Sources: https://www.ema.europa.eu/en/documents/scientific-discussion/toviaz-epar-scientific-discussion_en.pdf#page=15 Page: 15.0	yes
CYP3A4 1946	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022030s000_ClinPharmR.pdf#page=38 Page: 38.0	yes	SPM 7605 5	yes (co-administration study) Comment: Following blockade of CYP3A4 by coadministration of the potent CYP3A4 inhibitor ketoconazoles, Cmax and AUC of the active metabolite of fesoterodine increased 2.0- and 2.3-fold, respectively, after oral administration of Toviaz to CYP2D6 extensive metabolizers. In CYP2D6 poor metabolizers, Cmax and AUC of the active metabolite of fesoterodine increased 2.1- and 2.5-fold, respectively, during coadministration of ketoconazole. Cmax and AUC were 4.5- and 5.7-fold higher, respectively, in subjects who were CYP2D6 poor metabolizers and taking ketoconazole; Following induction of CYP3A4 by coadministration of rifampicin (inducer), Cmax and AUC of the active metabolite of fesoterodine decreased by approximately 70% and 75%, respectively, after oral administration of Toviaz Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022030s000_ClinPharmR.pdf#page=38 Page: 38.0
CYP2D6 1388	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022030s000_ClinPharmR.pdf#page=38 Page: 38.0	yes	SPM 7605 5	yes (pharmacogenomic study) Comment: CYP2D6 PMs have values for AUC and Cmax that are about 2-fold higher that CYP2D6 EMs Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022030s000_ClinPharmR.pdf#page=38 Page: 38.0

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2263	inhibitor 2237 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022030s000_PharmR_P1.pdf#page=57 Page: 57.0

Sourcing

Vendor/Aggregator	ID	URL
Aaron Chemicals	AR00BFSC	http://www.aaronchem.com/286930-02-7
Achemtek	0102-020049	http://www.achemtek.com/286930-02-7
AK Scientific, Inc. (AKSCI)	X5024	http://www.aksci.com/item_detail.php?cat=X5024
BLD Pharm	BD262927	http://www.bldpharm.com/products/286930-02-7.html
Chem Scene	CS-M2392	http://www.chemscene.com/286930-02-7.html
ChemMol	44025744	http://www.chemmol.com/chemmol/44025744.html
ChemMol	49400560	http://www.chemmol.com/chemmol/49400560.html
ChemMol	49401416	http://www.chemmol.com/chemmol/49401416.html
ChemMol	99063804	http://www.chemmol.com/chemmol/99063804.html
Chemspace	CSSB00020617528	https://chem-space.com/CSSB00020617528
Clearsynth	CS-O-30922	http://www.clearsynth.com/en/CSO30922.html
DC Chemicals	DC23515	http://www.dcchemicals.com/product_show-DC23515.html
eNovation Chemicals	D679729	https://www.enovationchem.com/ProductDetails.asp?ProductID=D679729
eNovation Chemicals	Y1048270	https://www.enovationchem.com/ProductDetails.asp?ProductID=Y1048270
Hairui	HR106732	http://www.hairuichem.com/en/product/250214-44-9.html
MedChem Express	HY-70053	https://www.medchemexpress.com/fesoterodine.html
OChem	26230	http://www.ocheminc.com/index.php?act=psearch&pid=930F027
Smolecule	S623538	https://www.smolecule.com/products/s623538
THE BioTek	bt-337449	https://www.thebiotek.com/product/others/bt-337449
THE BioTek	bt-463777	https://www.thebiotek.com/product/others/bt-463777

PubMed

Title	Date	PubMed
Effects of the moderate CYP3A4 inhibitor, fluconazole, on the pharmacokinetics of fesoterodine in healthy subjects.	2011-08	21545485
Efficacy and tolerability of fesoterodine in older and younger subjects with overactive bladder.	2010-12	20974482
Dose escalation improves therapeutic outcome: post hoc analysis of data from a 12-week, multicentre, double-blind, parallel-group trial of trospium chloride in patients with urinary urge incontinence.	2010-09-14	20840754
Fesoterodine in patients with overactive bladder syndrome: can the severity of baseline urgency urinary incontinence predict dosing requirement?	2010-09	20151972
Modeling dose-response relationships of the effects of fesoterodine in patients with overactive bladder.	2010-08-19	20723260
The cost-effectiveness of solifenacin vs fesoterodine, oxybutynin immediate-release, propiverine, tolterodine extended-release and tolterodine immediate-release in the treatment of patients with overactive bladder in the UK National Health Service.	2010-08	20653664
Spinal effects of the fesoterodine metabolite 5-hydroxymethyl tolterodine and/or doxazosin in rats with or without partial urethral obstruction.	2010-08	20639056
The cost-effectiveness of solifenacin vs fesoterodine, oxybutynin immediate-release, propiverine, tolterodine extended-release and tolterodine immediate-release in the treatment of patients with overactive bladder in the UK National Health Service.	2010-08	20132203
Urodynamic evaluation of fesoterodine metabolite, doxazosin and their combination in a rat model of partial urethral obstruction.	2010-07	19888972
Thorough QT study of the effect of fesoterodine on cardiac repolarization.	2010-05	20420787
Efficacy and tolerability of fesoterodine in men with overactive bladder: a pooled analysis of 2 phase III studies.	2010-05	19914702
Response to fesoterodine in patients with an overactive bladder and urgency urinary incontinence is independent of the urodynamic finding of detrusor overactivity.	2010-05	19889062
The overlap of interstitial cystitis/painful bladder syndrome and overactive bladder.	2010-04-24	20412643
Medical management of overactive bladder.	2010-04	20877608
Durability of treatments for overactive bladder.	2010-04	20456203
Long-term safety, tolerability and efficacy of fesoterodine treatment in subjects with overactive bladder symptoms.	2010-04	20201992
Efficacy of fesoterodine over 24 hours in subjects with overactive bladder.	2010-04	20121659
Recent advances in management of bladder overactivity.	2010-02-11	20948824
The pharmacokinetic profile of fesoterodine 8 mg with daytime or nighttime dosing.	2010-02	19915829
Fesoterodine fumarate.	2010-02	20393636
New Drugs2010, PART 1.	2010-02	20083979
Comparison of fesoterodine and tolterodine extended release for the treatment of overactive bladder: a head-to-head placebo-controlled trial.	2010-01	20132103
Randomized, double-blind, placebo-controlled trial of flexible-dose fesoterodine in subjects with overactive bladder.	2010-01	19931895
Bladder dysfunction in diabetes mellitus.	2010	21833175
Determination of fesoterodine in pharmaceutical formulations by using liquid chromatography-tandem mass spectrometry.	2010	21173462
Fesoterodine for the treatment of overactive bladder.	2009-12	19920160
Basic mechanisms of urgency: roles and benefits of pharmacotherapy.	2009-12	19588154
Influence of age, gender, and race on pharmacokinetics, pharmacodynamics, and safety of fesoterodine.	2009-09	19761716
Tolterodine extended-release for overactive bladder.	2009-09	19663610
Fesoterodine for the treatment of overactive bladder.	2009-08	19638887
Practical aspects of lifestyle modifications and behavioural interventions in the treatment of overactive bladder and urgency urinary incontinence.	2009-08	19575724
A meta-analysis of the placebo response in antimuscarinic drug trials for overactive bladder.	2009-07-22	19624824
Efficacy and tolerability of fesoterodine in women with overactive bladder.	2009-07	19495545
New drug information: Toviaz.	2009-06	19601442
Influence of food on the pharmacokinetic profile of fesoterodine.	2009-06	19473600
Evaluation of drug-drug interactions with fesoterodine.	2009-06	19347334
Fesoterodine (toviaz) for overactive bladder.	2009-05-04	19417719
Effects of flexible-dose fesoterodine on overactive bladder symptoms and treatment satisfaction: an open-label study.	2009-04	19348029
Assessment of the effects of renal impairment on the pharmacokinetic profile of fesoterodine.	2009-04	19246724
New drugs: milnacipran hydrochloride, fesoterodine fumarate, and silodosin.	2009-03-18	19289354
The pharmacokinetic profile of fesoterodine: similarities and differences to tolterodine.	2009-03-07	19145494
Fesoterodine: a new agent for treating overactive bladder.	2009-03	19355800
[Anticholinergic treatment of overactive bladder syndrome. Is it all the same?].	2009-03	19145428
Muscarinic receptor antagonists for overactive bladder treatment: does one fit all?	2009-01	19057211
The design and development of fesoterodine as a prodrug of 5-hydroxymethyl tolterodine (5-HMT), the active metabolite of tolterodine.	2009	19835561
Fesoterodine for the treatment of urinary incontinence and overactive bladder.	2009	19956551
The safety and efficacy of tolterodine extended release in the treatment of overactive bladder in the elderly.	2009	19503781
Fesoterodine.	2009	19405552
Antimuscarinic potency and bladder selectivity of PNU-200577, a major metabolite of tolterodine.	1997-10	9353847
Tolterodine--a new bladder selective muscarinic receptor antagonist: preclinical pharmacological and clinical data.	1997	9121357

Patents

Sample Use Guides

In Vivo Use Guide

2-203 nM/kg [0.001-0.1 mg/kg]

Route of Administration: Intravenous

In Vitro Use Guide

In terms of IC50 values (mean of 3-6 experiments), Desfesoterodine was >900 times more potent in blocking bladder muscarinic receptors (IC50 5.7 nM) than calcium channels (papillary muscle: IC50 5.4 uM; atrium: IC50 15 uM, bladder IC50 39 uM), alph-adrenoceptors (portal vein: IC50 100 uM) and histamine receptors (ileum: IC50 6.1 uM).

Substance Class	Chemical Created by `admin` on `Mon Mar 31 22:49:26 GMT 2025` Edited by `admin` on `Mon Mar 31 22:49:26 GMT 2025`
Record UNII	607O3D83YQ
Record Status	`Validated (UNII)`
Record Version

Download

Name

Type

Language

DESFESOTERODINE FUMARATE

Common Name

English

PNU-200577 FUMARATE

Preferred Name

English

(+)-N,N-DIISOPROPYL-3-(2-HYDROXY-5-HYDROXYMETHYLPHENYL)-3-PHENYLPROPYLAMINE FUMARATE

Systematic Name

English

Desfesoterodine fumarate [WHO-DD]

Common Name

English

5-HYDROXYMETHYLTOLTERODINE FUMARATE

Common Name

English

BENZENEMETHANOL, 3-((1R)-3-(BIS(1-METHYLETHYL)AMINO)-1-PHENYLPROPYL)-4-HYDROXY-, (2E)-2-BUTENEDIOATE (1:1) (SALT)

Systematic Name

English

Code System Code Type Description

PUBCHEM

9825360

Created by admin on Mon Mar 31 22:49:26 GMT 2025 , Edited by admin on Mon Mar 31 22:49:26 GMT 2025

PRIMARY

CAS

380636-50-0

Created by admin on Mon Mar 31 22:49:26 GMT 2025 , Edited by admin on Mon Mar 31 22:49:26 GMT 2025

PRIMARY

SMS_ID

300000035003

Created by admin on Mon Mar 31 22:49:26 GMT 2025 , Edited by admin on Mon Mar 31 22:49:26 GMT 2025

PRIMARY

FDA UNII

607O3D83YQ

Created by admin on Mon Mar 31 22:49:26 GMT 2025 , Edited by admin on Mon Mar 31 22:49:26 GMT 2025

PRIMARY

Related Record Type Details


					YU871O78GR

Desfesoterodine

PARENT -> SALT/SOLVATE

Amount:

Related Record Type Details


					YU871O78GR

Desfesoterodine

ACTIVE MOIETY

Amount:

Details

SMILES

InChI

CNS Activity

Originator

Approval Year

Targets

Conditions

Approved Use

Approved Use

Approved Use

Launch Date

Approved Use

Launch Date

Cmax

AUC

T1/2

Funbound

Overview

OverviewOther

Drug as perpetrator​

Drug as victim

Tox targets

Sourcing

PubMed

Patents

Sample Use Guides

C_max

T_1/2

F_unbound

Drug as perpetrator