FESOTERODINE FUMARATE

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C26H37NO3.C4H4O4
Molecular Weight	527.649
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=CC(CO)=CC=C2OC(=O)C(C)C)C(C)C

InChI

InChIKey=MWHXMIASLKXGBU-RNCYCKTQSA-N

InChI=1S/C26H37NO3.C4H4O4/c1-18(2)26(29)30-25-13-12-21(17-28)16-24(25)23(22-10-8-7-9-11-22)14-15-27(19(3)4)20(5)6;5-3(6)1-2-4(7)8/h7-13,16,18-20,23,28H,14-15,17H2,1-6H3;1-2H,(H,5,6)(H,7,8)/b;2-1+/t23-;/m1./s1

HIDE SMILES / InChI

Molecular Formula	C26H37NO3
Molecular Weight	411.5769
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
Tolterodine--a new bladder selective muscarinic receptor antagonist: preclinical pharmacological and clinical data.	1997	9121357
Gateways to clinical trials.	2006 Dec	17235418
Gateways to clinical trials.	2006 Jul-Aug	16894408
Treatment of the overactive bladder syndrome with muscarinic receptor antagonists: a matter of metabolites?	2006 Nov	17021853
Toviaz approved for overactive bladder.	2008 Dec 1	19020177
Pharmacokinetic profile of fesoterodine.	2008 Nov	19000553
Comparison of fesoterodine and tolterodine in patients with overactive bladder.	2008 Nov	18647298
The effects of antimuscarinic treatments in overactive bladder: an update of a systematic review and meta-analysis.	2008 Sep	18599186
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
Assessment of the effects of renal impairment on the pharmacokinetic profile of fesoterodine.	2009 Apr	19246724
Fesoterodine for the treatment of overactive bladder.	2009 Aug	19638887
Practical aspects of lifestyle modifications and behavioural interventions in the treatment of overactive bladder and urgency urinary incontinence.	2009 Aug	19575724
Fesoterodine for the treatment of overactive bladder.	2009 Dec	19920160
Basic mechanisms of urgency: roles and benefits of pharmacotherapy.	2009 Dec	19588154
Muscarinic receptor antagonists for overactive bladder treatment: does one fit all?	2009 Jan	19057211
Efficacy and tolerability of fesoterodine in women with overactive bladder.	2009 Jul	19495545
A meta-analysis of the placebo response in antimuscarinic drug trials for overactive bladder.	2009 Jul 22	19624824
New drug information: Toviaz.	2009 Jun	19601442
Influence of food on the pharmacokinetic profile of fesoterodine.	2009 Jun	19473600
Fesoterodine: a new agent for treating overactive bladder.	2009 Mar	19355800
[Anticholinergic treatment of overactive bladder syndrome. Is it all the same?].	2009 Mar	19145428
Comparison of receptor binding characteristics of commonly used muscarinic antagonists in human bladder detrusor and mucosa.	2009 Mar	19029429
The pharmacokinetic profile of fesoterodine: similarities and differences to tolterodine.	2009 Mar 7	19145494
Fesoterodine (toviaz) for overactive bladder.	2009 May 4	19417719
Influence of age, gender, and race on pharmacokinetics, pharmacodynamics, and safety of fesoterodine.	2009 Sep	19761716
Tolterodine extended-release for overactive bladder.	2009 Sep	19663610
Bladder dysfunction in diabetes mellitus.	2010	21833175
Determination of fesoterodine in pharmaceutical formulations by using liquid chromatography-tandem mass spectrometry.	2010	21173462
Long-term safety, tolerability and efficacy of fesoterodine treatment in subjects with overactive bladder symptoms.	2010 Apr	20201992
Efficacy of fesoterodine over 24 hours in subjects with overactive bladder.	2010 Apr	20121659
Efficacy and tolerability of fesoterodine in older and younger subjects with overactive bladder.	2010 Dec	20974482
The pharmacokinetic profile of fesoterodine 8 mg with daytime or nighttime dosing.	2010 Feb	19915829
Fesoterodine fumarate.	2010 Feb	20393636
New Drugs2010, PART 1.	2010 Feb	20083979
The overlap of interstitial cystitis/painful bladder syndrome and overactive bladder.	2010 Jan-Mar	20412643
Urodynamic evaluation of fesoterodine metabolite, doxazosin and their combination in a rat model of partial urethral obstruction.	2010 Jul	19888972
Thorough QT study of the effect of fesoterodine on cardiac repolarization.	2010 May	20420787
Efficacy and tolerability of fesoterodine in men with overactive bladder: a pooled analysis of 2 phase III studies.	2010 May	19914702
Response to fesoterodine in patients with an overactive bladder and urgency urinary incontinence is independent of the urodynamic finding of detrusor overactivity.	2010 May	19889062
Fesoterodine in patients with overactive bladder syndrome: can the severity of baseline urgency urinary incontinence predict dosing requirement?	2010 Sep	20151972
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 Sep 14	20840754
Effects of the moderate CYP3A4 inhibitor, fluconazole, on the pharmacokinetics of fesoterodine in healthy subjects.	2011 Aug	21545485

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 18:00:57 GMT 2025` Edited by `admin` on `Mon Mar 31 18:00:57 GMT 2025`
Record UNII	EOS72165S7
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

FESOTERODINE FUMARATE

Official Name

English

TOVIAZ

Preferred Name

English

FESOTERODINE FUMARATE [MI]

Common Name

English

2-((1R)-3-(BIS(1-METHYLETHYL)AMINO)-1-PHENYLPROPYL)-4-(HYDROXYMETHYL)PHENYL 2-METHYLPROPANOATE HYDROGEN(2E)-BUTENEDIOATE (SALT)

Common Name

English

SPM 907

Code

English

FESOTERODINE FUMARATE [JAN]

Common Name

English

FESOTERODINE FUMARATE [VANDF]

Common Name

English

FESOTERODINE FUMARATE [MART.]

Common Name

English

FESOTERODINE FUMARATE [ORANGE BOOK]

Common Name

English

SPM-907

Code

English

SPM-8272

Code

English

FESOTERODINE FUMARATE [EMA EPAR]

Common Name

English

SPM 8272

Code

English

FESOTERODINE FUMARATE [USAN]

Common Name

English

Fesoterodine Fumarate [WHO-DD]

Common Name

English

PROPANOIC ACID,2-METHYL ,2-((1R)-3-(BIS(1-METHYLETHYL)AMINO)-1-PHENYLPROPYL)-4-(HYDROXYMETHYL)PHENYL ESTER,(2E)-2-BUTENEDIOATE (1:1)(SALT)

Common Name

English

Classification Tree Code System Code

EMA ASSESSMENT REPORTS

TOVIAZ (AUTHORIZED: URINARY BLADDER, OVERACTIVE)