Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Toviaz	Tablet, film coated, extended release	8 mg/1	Oral	Avera McKennan Hospital	2015-06-10	Not applicable
Toviaz	Tablet, extended release	4 mg	Oral	Pfizer	2012-04-19	Not applicable
Toviaz	Tablet, extended release	8 mg	Oral	Pfizer Europe Ma Eeig	2007-04-20	Not applicable
Toviaz	Tablet, extended release	4 mg	Oral	Pfizer Europe Ma Eeig	2007-04-20	Not applicable
Toviaz	Tablet, extended release	8 mg	Oral	Pfizer Europe Ma Eeig	2007-04-20	Not applicable
Toviaz	Tablet, film coated, extended release	4 mg/1	Oral	U.S. Pharmaceuticals	2008-10-31	Not applicable
Toviaz	Tablet, extended release	4 mg	Oral	Pfizer Europe Ma Eeig	2007-04-20	Not applicable
Toviaz	Tablet, extended release	8 mg	Oral	Pfizer Europe Ma Eeig	2007-04-20	Not applicable
Toviaz	Tablet, extended release	8 mg	Oral	Pfizer Europe Ma Eeig	2007-04-20	Not applicable
Toviaz	Tablet, film coated, extended release	4 mg/1	Oral	Avera McKennan Hospital	2015-04-01	Not applicable

Generic Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Fesoterodine Fumarate	Tablet, film coated, extended release	4 mg/1	Oral	Cadila Pharnmaceuticals	2017-12-07	Not applicable
Fesoterodine Fumarate	Tablet, film coated, extended release	8 mg/1	Oral	Zydus Pharmaceuticals Usa, Inc.	2017-12-07	Not applicable
Fesoterodine Fumarate	Tablet, film coated, extended release	4 mg/1	Oral	Zydus Pharmaceuticals Usa, Inc.	2017-12-07	Not applicable
Fesoterodine Fumarate	Tablet, film coated, extended release	8 mg/1	Oral	Cadila Pharnmaceuticals	2017-12-07	Not applicable

Categories

UNII

621G617227

CAS number

286930-02-7

Weight

Average: 411.5769
Monoisotopic: 411.277344055

Chemical Formula

C₂₆H₃₇NO₃

InChI Key

DCCSDBARQIPTGU-HSZRJFAPSA-N

InChI

InChI=1S/C26H37NO3/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/h7-13,16,18-20,23,28H,14-15,17H2,1-6H3/t23-/m1/s1

IUPAC Name

2-[(1R)-3-[bis(propan-2-yl)amino]-1-phenylpropyl]-4-(hydroxymethyl)phenyl 2-methylpropanoate

SMILES

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

Pharmacology

Indication

For the treatment of overactive bladder (with symptoms of urinary frequency, urgency, or urge incontinence).

Associated Conditions

Urinary Bladder, Overactive

Pharmacodynamics

Fesoterodine is a prodrug. In-vivo it 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.

Mechanism of action

Fesoterodine, once converted to its active metabolite, 5-hydroxymethyltolterodine, acts as a competitive antagonists at muscarinic receptors. This results in the inhibition of bladder contraction, decrease in detrusor pressure, and an incomplete emptying of the bladder.

Target	Actions	Organism
AMuscarinic acetylcholine receptor M3	antagonist	Humans
UMuscarinic acetylcholine receptor M4	antagonist	Humans
UMuscarinic acetylcholine receptor M1	antagonist	Humans
UMuscarinic acetylcholine receptor M2	antagonist	Humans
UMuscarinic acetylcholine receptor M5	antagonist	Humans

Absorption

Tmax (5-HMT): 5 hours post-adminitration of fesoterodine. AUC (0,∞)= 49.5 ng·h/ ml
Bioavailability, 5-HMT = 52%

Volume of distribution

IV, 5-HMT: 169 L

Protein binding

5-HMT: 50% to albumin and alpha1-acid glycoprotein

Metabolism

Metabolized by ubiquitous, nonspecific esterases to transform fesoterodine into 5-HMT Extensive metabolism via CYP2D6 and CYP3A4 into inactive metabolites

Route of elimination

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

Half life

7-8 hours for the active metabolite 5-hydroxymethyl tolterodine

Clearance

5-HMT, healthy subjects: 14.4 L/h 5-HMT is also secreted into the nephron.

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

Affected organisms

Humans and other mammals

Pathways

Not Available

Pharmacogenomic Effects/ADRs

Interacting Gene/Enzyme	Allele name	Genotype(s)	Defining Change(s)	Type(s)	Description	Details
Cytochrome P450 2D6	CYP2D6*3	Not Available	C allele	Effect Inferred	Poor drug metabolizer.	Details
Cytochrome P450 2D6	CYP2D6*4	Not Available	C allele	Effect Inferred	Poor drug metabolizer.	Details
Cytochrome P450 2D6	CYP2D6*5	Not Available	Whole-gene deletion	Effect Inferred	Poor drug metabolizer.	Details
Cytochrome P450 2D6	CYP2D6*6	Not Available	1707delT	Effect Inferred	Poor drug metabolizer.	Details
Cytochrome P450 2D6	CYP2D6*7	Not Available	2935A>C	Effect Inferred	Poor drug metabolizer.	Details
Cytochrome P450 2D6	CYP2D6*8	Not Available	1758G>T	Effect Inferred	Poor drug metabolizer.	Details
Cytochrome P450 2D6	CYP2D6*11	Not Available	883G>C	Effect Inferred	Poor drug metabolizer.	Details
Cytochrome P450 2D6	CYP2D6*12	Not Available	124G>A	Effect Inferred	Poor drug metabolizer.	Details
Cytochrome P450 2D6	CYP2D6*13	Not Available	CYP2D7/2D6 hybrid gene structure	Effect Inferred	Poor drug metabolizer.	Details
Cytochrome P450 2D6	CYP2D6*14A	Not Available	1758G>A	Effect Inferred	Poor drug metabolizer.	Details
Cytochrome P450 2D6	CYP2D6*15	Not Available	137insT, 137_138insT	Effect Inferred	Poor drug metabolizer.	Details
Cytochrome P450 2D6	CYP2D6*19	Not Available	2539_2542delAACT	Effect Inferred	Poor drug metabolizer.	Details
Cytochrome P450 2D6	CYP2D6*20	Not Available	1973_1974insG	Effect Inferred	Poor drug metabolizer.	Details
Cytochrome P450 2D6	CYP2D6*21	Not Available	2573insC	Effect Inferred	Poor drug metabolizer.	Details
Cytochrome P450 2D6	CYP2D6*31	Not Available	-1770G>A / -1584C>G … show all	Effect Inferred	Poor drug metabolizer.	Details
Cytochrome P450 2D6	CYP2D6*36	Not Available	100C>T / -1426C>T … show all	Effect Inferred	Poor drug metabolizer.	Details
Cytochrome P450 2D6	CYP2D6*38	Not Available	2587_2590delGACT	Effect Inferred	Poor drug metabolizer.	Details
Cytochrome P450 2D6	CYP2D6*40	Not Available	1863_1864ins(TTT CGC CCC)2	Effect Inferred	Poor drug metabolizer.	Details
Cytochrome P450 2D6	CYP2D6*42	Not Available	3259_3260insGT	Effect Inferred	Poor drug metabolizer.	Details
Cytochrome P450 2D6	CYP2D6*44	Not Available	2950G>C	Effect Inferred	Poor drug metabolizer.	Details
Cytochrome P450 2D6	CYP2D6*47	Not Available	100C>T / -1426C>T … show all	Effect Inferred	Poor drug metabolizer.	Details
Cytochrome P450 2D6	CYP2D6*51	Not Available	-1584C>G / -1235A>G … show all	Effect Inferred	Poor drug metabolizer.	Details
Cytochrome P450 2D6	CYP2D6*56	Not Available	3201C>T	Effect Inferred	Poor drug metabolizer.	Details
Cytochrome P450 2D6	CYP2D6*57	Not Available	100C>T / 310G>T … show all	Effect Inferred	Poor drug metabolizer.	Details
Cytochrome P450 2D6	CYP2D6*62	Not Available	4044C>T	Effect Inferred	Poor drug metabolizer.	Details
Cytochrome P450 2D6	CYP2D6*68A	Not Available	-1426C>T / -1235A>G … show all	Effect Inferred	Poor drug metabolizer.	Details
Cytochrome P450 2D6	CYP2D6*68B	Not Available	Similar but not identical switch region compared to CYP2D668A. Found in tandem arrangement with CYP2D64.	Effect Inferred	Poor drug metabolizer.	Details
Cytochrome P450 2D6	CYP2D6*69	Not Available	2988G>A / -1426C>T … show all	Effect Inferred	Poor drug metabolizer.	Details
Cytochrome P450 2D6	CYP2D6*92	Not Available	1995delC	Effect Inferred	Poor drug metabolizer.	Details
Cytochrome P450 2D6	CYP2D6*100	Not Available	-1426C>T / -1235A>G … show all	Effect Inferred	Poor drug metabolizer.	Details
Cytochrome P450 2D6	CYP2D6*101	Not Available	-1426C>T / -1235A>G … show all	Effect Inferred	Poor drug metabolizer.	Details

Interactions

Drug Interactions

Drug	Interaction
(R)-warfarin	The metabolism of (R)-warfarin can be decreased when combined with Fesoterodine.
(S)-Warfarin	The metabolism of (S)-Warfarin can be decreased when combined with Fesoterodine.
1,10-Phenanthroline	The therapeutic efficacy of Fesoterodine can be decreased when used in combination with 1,10-Phenanthroline.
2,5-Dimethoxy-4-ethylamphetamine	The risk or severity of Tachycardia can be increased when 2,5-Dimethoxy-4-ethylamphetamine is combined with Fesoterodine.
2,5-Dimethoxy-4-ethylthioamphetamine	The risk or severity of Tachycardia can be increased when Fesoterodine is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
3,4-Methylenedioxyamphetamine	The risk or severity of Tachycardia can be increased when 3,4-Methylenedioxyamphetamine is combined with Fesoterodine.
3,5-diiodothyropropionic acid	The metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Fesoterodine.
4-Bromo-2,5-dimethoxyamphetamine	The risk or severity of Tachycardia can be increased when 4-Bromo-2,5-dimethoxyamphetamine is combined with Fesoterodine.
4-hydroxycoumarin	The metabolism of 4-hydroxycoumarin can be decreased when combined with Fesoterodine.
4-Methoxyamphetamine	4-Methoxyamphetamine may increase the central nervous system depressant (CNS depressant) activities of Fesoterodine.

Food Interactions

Take with or without food.

References

Synthesis Reference

Claus Meese, "CHIRAL INTERMEDIATE, PROCESS FOR PRODUCING THE SAME AND ITS USE IN THE MANUFACTURE OF TOLTERODINE, FESOTERODINE, OR THE ACTIVE METABOLITE THEREOF." U.S. Patent US20090192224, issued July 30, 2009.

US20090192224

General References

Malhotra B, Dickins M, Alvey C, Jumadilova Z, Li X, Duczynski G, Gandelman K: Effects of the moderate CYP3A4 inhibitor, fluconazole, on the pharmacokinetics of fesoterodine in healthy subjects. Br J Clin Pharmacol. 2011 Aug;72(2):263-9. doi: 10.1111/j.1365-2125.2011.04007.x. [PubMed:21545485]
Malhotra B, Gandelman K, Sachse R, Wood N, Michel MC: The design and development of fesoterodine as a prodrug of 5-hydroxymethyl tolterodine (5-HMT), the active metabolite of tolterodine. Curr Med Chem. 2009;16(33):4481-9. [PubMed:19835561]

External Links

Human Metabolome Database: HMDB0015648
KEGG Drug: D07226
PubChem Compound: 6918558
PubChem Substance: 99443256
ChemSpider: 5293755
ChEBI: 135920
ChEMBL: CHEMBL1201764
PharmGKB: PA165958376
RxList: RxList Drug Page
Drugs.com: Drugs.com Drug Page
Wikipedia: Fesoterodine

ATC Codes

G04BD11 — Fesoterodine

AHFS Codes

86:12.04 — Antimuscarinics

FDA label

Download (430 KB)

MSDS

Download (102 KB)

Clinical Trials

Clinical Trials

Phase	Status	Purpose	Conditions	Count
0	Withdrawn	Diagnostic	Bladder Dysfunction / Urinary Incontinence (UI)	1
1	Completed	Not Available	Healthy Volunteers	1
1	Completed	Not Available	Overactive Bladder (OAB) With Symptoms of Frequency, Urgency, and Urgency	1
1	Completed	Not Available	Urinary Bladder, Overactive	1
1	Completed	Basic Science	Healthy Volunteers	1
1	Completed	Basic Science	Urinary Bladder, Overactive	1
1	Completed	Other	Treatment of Overactive Bladder	2
1	Completed	Treatment	Food / Therapeutic Equivalency	1
1	Completed	Treatment	Healthy Volunteers	1
1	Completed	Treatment	Overactive Bladder With Symptoms of Frequency, Urgency, and Urge Urinary Incontinence	1
1	Terminated	Treatment	Healthy Volunteers	1
2	Completed	Treatment	Neurogenic Detrusor Overactivity / Urinary Bladder, Overactive	1
2	Completed	Treatment	Stress Urinary Incontinence (SUI)	1
2	Completed	Treatment	Urinary Bladder, Overactive	1
2	Recruiting	Other	Mild Cognitive Impairment (MCI) / Urinary Bladder, Overactive	1
2	Recruiting	Treatment	Autonomic Dysreflexia	1
2, 3	Terminated	Treatment	Nocturia	1
3	Completed	Treatment	Urge Urinary Incontinence	1
3	Completed	Treatment	Urinary Bladder, Overactive	8
4	Active Not Recruiting	Treatment	Adenocarcinoma, Prostate	1
4	Completed	Treatment	Bladder Outlet Obstruction	1
4	Completed	Treatment	Urge Urinary Incontinence / Urinary Bladder, Overactive	1
4	Completed	Treatment	Urinary Bladder, Overactive	8
4	Recruiting	Treatment	Parkinson's Disease (PD) / Urinary Bladder, Overactive	1
4	Recruiting	Treatment	Urinary Bladder, Overactive	1
4	Terminated	Treatment	Urinary Bladder, Overactive	1
Not Available	Active Not Recruiting	Not Available	Urinary Bladder, Overactive	1
Not Available	Completed	Not Available	Urinary Bladder Diseases / Urinary Bladder, Overactive / Urologic Diseases	1
Not Available	Completed	Not Available	Urinary Bladder, Overactive	5
Not Available	Completed	Not Available	Urinary Bladder, Overactive / Urinary Incontinence (UI)	1
Not Available	Recruiting	Not Available	Urinary Bladder, Overactive	1
Not Available	Unknown Status	Not Available	Urinary Bladder, Overactive	1
Not Available	Unknown Status	Treatment	Urinary Bladder, Overactive	1

Pharmacoeconomics

Manufacturers

Not Available

Packagers

Not Available

Dosage forms

Form	Route	Strength
Tablet, extended release	Oral	4 mg
Tablet, extended release	Oral	8 mg
Tablet, film coated, extended release	Oral	4 mg/1
Tablet, film coated, extended release	Oral	8 mg/1

Prices

Not Available

Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)
US6858650	No	2005-02-22	2022-07-03
US7384980	No	2008-06-10	2019-05-11
US7807715	No	2010-10-05	2027-06-07
US7855230	No	2010-12-21	2019-05-11
US7985772	No	2011-07-26	2019-05-11
US8088398	No	2012-01-03	2027-06-07
US8338478	No	2012-12-25	2019-05-11
US8501723	No	2013-08-06	2027-06-07

Properties

State

Solid

Experimental Properties

Property	Value	Source
water solubility	Highly soluble	MSDS

Predicted Properties

Property	Value	Source
Water Solubility	0.00205 mg/mL	ALOGPS
logP	5.45	ALOGPS
logP	5.7	ChemAxon
logS	-5.3	ALOGPS
pKa (Strongest Acidic)	14.98	ChemAxon
pKa (Strongest Basic)	10.64	ChemAxon
Physiological Charge	1	ChemAxon
Hydrogen Acceptor Count	3	ChemAxon
Hydrogen Donor Count	1	ChemAxon
Polar Surface Area	49.77 Å²	ChemAxon
Rotatable Bond Count	11	ChemAxon
Refractivity	124.08 m³·mol^-1	ChemAxon
Polarizability	48.29 Å³	ChemAxon
Number of Rings	2	ChemAxon
Bioavailability	0	ChemAxon
Rule of Five	No	ChemAxon
Ghose Filter	No	ChemAxon
Veber's Rule	No	ChemAxon
MDDR-like Rule	No	ChemAxon

Predicted ADMET features

Property	Value	Probability
Human Intestinal Absorption	+	0.9535
Blood Brain Barrier	+	0.5648
Caco-2 permeable	+	0.7699
P-glycoprotein substrate	Substrate	0.5268
P-glycoprotein inhibitor I	Non-inhibitor	0.5556
P-glycoprotein inhibitor II	Non-inhibitor	0.625
Renal organic cation transporter	Inhibitor	0.6025
CYP450 2C9 substrate	Non-substrate	0.6853
CYP450 2D6 substrate	Non-substrate	0.5151
CYP450 3A4 substrate	Substrate	0.5939
CYP450 1A2 substrate	Inhibitor	0.6306
CYP450 2C9 inhibitor	Non-inhibitor	0.7227
CYP450 2D6 inhibitor	Inhibitor	0.6255
CYP450 2C19 inhibitor	Non-inhibitor	0.7334
CYP450 3A4 inhibitor	Non-inhibitor	0.5718
CYP450 inhibitory promiscuity	Low CYP Inhibitory Promiscuity	0.6144
Ames test	Non AMES toxic	0.646
Carcinogenicity	Non-carcinogens	0.7213
Biodegradation	Not ready biodegradable	0.9385
Rat acute toxicity	2.4003 LD50, mol/kg	Not applicable
hERG inhibition (predictor I)	Weak inhibitor	0.9196
hERG inhibition (predictor II)	Inhibitor	0.5602

ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)

Not Available

Spectra

Spectrum	Spectrum Type	Splash Key
Predicted GC-MS Spectrum - GC-MS	Predicted GC-MS	Not Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)	Predicted LC-MS/MS	Not Available

Taxonomy

Description: This compound belongs to the class of organic compounds known as diphenylmethanes. These are compounds containing a diphenylmethane moiety, which consists of a methane wherein two hydrogen atoms are replaced by two phenyl groups.
Kingdom: Organic compounds
Super Class: Benzenoids
Class: Benzene and substituted derivatives
Sub Class: Diphenylmethanes
Direct Parent: Diphenylmethanes
Alternative Parents: Phenol esters / Phenoxy compounds / Benzyl alcohols / Aralkylamines / Trialkylamines / Carboxylic acid esters / Amino acids and derivatives / Monocarboxylic acids and derivatives / Primary alcohols / Organopnictogen compounds
show 4 more
Substituents: Diphenylmethane / Phenol ester / Phenoxy compound / Benzyl alcohol / Aralkylamine / Amino acid or derivatives / Carboxylic acid ester / Tertiary amine / Tertiary aliphatic amine / Carboxylic acid derivative
show 14 more
Molecular Framework: Aromatic homomonocyclic compounds
External Descriptors: Not Available

Targets

Details1. Muscarinic acetylcholine receptor M3

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Antagonist

General Function: Receptor activity
Specific Function: The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name: CHRM3
Uniprot ID: P20309
Uniprot Name: Muscarinic acetylcholine receptor M3
Molecular Weight: 66127.445 Da

References

Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Nilvebrant L: Tolterodine and its active 5-hydroxymethyl metabolite: pure muscarinic receptor antagonists. Pharmacol Toxicol. 2002 May;90(5):260-7. [PubMed:12076307]

Details2. Muscarinic acetylcholine receptor M4

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Antagonist

General Function: Guanyl-nucleotide exchange factor activity
Specific Function: The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name: CHRM4
Uniprot ID: P08173
Uniprot Name: Muscarinic acetylcholine receptor M4
Molecular Weight: 53048.65 Da

References

Mansfield KJ, Chandran JJ, Vaux KJ, Millard RJ, Christopoulos A, Mitchelson FJ, Burcher E: Comparison of receptor binding characteristics of commonly used muscarinic antagonists in human bladder detrusor and mucosa. J Pharmacol Exp Ther. 2009 Mar;328(3):893-9. doi: 10.1124/jpet.108.145508. Epub 2008 Nov 24. [PubMed:19029429]

Details3. Muscarinic acetylcholine receptor M1

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Antagonist

General Function: Phosphatidylinositol phospholipase c activity
Specific Function: The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name: CHRM1
Uniprot ID: P11229
Uniprot Name: Muscarinic acetylcholine receptor M1
Molecular Weight: 51420.375 Da

References

Nilvebrant L: Tolterodine and its active 5-hydroxymethyl metabolite: pure muscarinic receptor antagonists. Pharmacol Toxicol. 2002 May;90(5):260-7. [PubMed:12076307]

Details4. Muscarinic acetylcholine receptor M2

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Antagonist

General Function: G-protein coupled acetylcholine receptor activity
Specific Function: The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name: CHRM2
Uniprot ID: P08172
Uniprot Name: Muscarinic acetylcholine receptor M2
Molecular Weight: 51714.605 Da

References

Mansfield KJ, Chandran JJ, Vaux KJ, Millard RJ, Christopoulos A, Mitchelson FJ, Burcher E: Comparison of receptor binding characteristics of commonly used muscarinic antagonists in human bladder detrusor and mucosa. J Pharmacol Exp Ther. 2009 Mar;328(3):893-9. doi: 10.1124/jpet.108.145508. Epub 2008 Nov 24. [PubMed:19029429]

Details5. Muscarinic acetylcholine receptor M5

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Antagonist

General Function: Phosphatidylinositol phospholipase c activity
Specific Function: The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name: CHRM5
Uniprot ID: P08912
Uniprot Name: Muscarinic acetylcholine receptor M5
Molecular Weight: 60073.205 Da

References

Mansfield KJ, Chandran JJ, Vaux KJ, Millard RJ, Christopoulos A, Mitchelson FJ, Burcher E: Comparison of receptor binding characteristics of commonly used muscarinic antagonists in human bladder detrusor and mucosa. J Pharmacol Exp Ther. 2009 Mar;328(3):893-9. doi: 10.1124/jpet.108.145508. Epub 2008 Nov 24. [PubMed:19029429]

Enzymes

Details1. Cytochrome P450 3A4

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate

General Function: Vitamin d3 25-hydroxylase activity
Specific Function: Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name: CYP3A4
Uniprot ID: P08684
Uniprot Name: Cytochrome P450 3A4
Molecular Weight: 57342.67 Da

References

Malhotra B, Guan Z, Wood N, Gandelman K: Pharmacokinetic profile of fesoterodine. Int J Clin Pharmacol Ther. 2008 Nov;46(11):556-63. [PubMed:19000553]
Malhotra B, Dickins M, Alvey C, Jumadilova Z, Li X, Duczynski G, Gandelman K: Effects of the moderate CYP3A4 inhibitor, fluconazole, on the pharmacokinetics of fesoterodine in healthy subjects. Br J Clin Pharmacol. 2011 Aug;72(2):263-9. doi: 10.1111/j.1365-2125.2011.04007.x. [PubMed:21545485]
Malhotra B, Sachse R, Wood N: Evaluation of drug-drug interactions with fesoterodine. Eur J Clin Pharmacol. 2009 Jun;65(6):551-60. doi: 10.1007/s00228-009-0648-1. Epub 2009 Apr 4. [PubMed:19347334]
Malhotra BK, Wood N, Sachse R: Influence of age, gender, and race on pharmacokinetics, pharmacodynamics, and safety of fesoterodine. Int J Clin Pharmacol Ther. 2009 Sep;47(9):570-8. [PubMed:19761716]

Details2. Cytochrome P450 2D6

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate

General Function: Steroid hydroxylase activity
Specific Function: Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name: CYP2D6
Uniprot ID: P10635
Uniprot Name: Cytochrome P450 2D6
Molecular Weight: 55768.94 Da

References

Malhotra B, Guan Z, Wood N, Gandelman K: Pharmacokinetic profile of fesoterodine. Int J Clin Pharmacol Ther. 2008 Nov;46(11):556-63. [PubMed:19000553]
Malhotra B, Dickins M, Alvey C, Jumadilova Z, Li X, Duczynski G, Gandelman K: Effects of the moderate CYP3A4 inhibitor, fluconazole, on the pharmacokinetics of fesoterodine in healthy subjects. Br J Clin Pharmacol. 2011 Aug;72(2):263-9. doi: 10.1111/j.1365-2125.2011.04007.x. [PubMed:21545485]
Malhotra B, Sachse R, Wood N: Evaluation of drug-drug interactions with fesoterodine. Eur J Clin Pharmacol. 2009 Jun;65(6):551-60. doi: 10.1007/s00228-009-0648-1. Epub 2009 Apr 4. [PubMed:19347334]
Malhotra BK, Wood N, Sachse R: Influence of age, gender, and race on pharmacokinetics, pharmacodynamics, and safety of fesoterodine. Int J Clin Pharmacol Ther. 2009 Sep;47(9):570-8. [PubMed:19761716]

Transporters

Details1. Multidrug resistance protein 1

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate

General Function: Xenobiotic-transporting atpase activity
Specific Function: Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name: ABCB1
Uniprot ID: P08183
Uniprot Name: Multidrug resistance protein 1
Molecular Weight: 141477.255 Da

References

Chancellor MB, Staskin DR, Kay GG, Sandage BW, Oefelein MG, Tsao JW: Blood-brain barrier permeation and efflux exclusion of anticholinergics used in the treatment of overactive bladder. Drugs Aging. 2012 Apr 1;29(4):259-73. doi: 10.2165/11597530-000000000-00000. [PubMed:22390261]

Drug created on May 06, 2010 10:47 / Updated on February 16, 2019 05:57

Fesoterodine

Identification

Structure for Fesoterodine (DB06702)

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Enzymes

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