Identification

Summary

Solifenacin is a muscarinic antagonist with antispasmodic properties used to treat urge urinary incontinence, urgency, and urinary frequency associated with an overactive bladder.

Brand Names
Vesicare
Generic Name
Solifenacin
DrugBank Accession Number
DB01591
Background

Solifenacin is a competitive muscarinic receptor antagonist indicated to treat an overactive bladder with urinary incontinence, urgency, and frequency.3 It has a long duration of action as it is usually taken once daily.3

Solifenacin was granted FDA approval on 19 November 2004.3

Type
Small Molecule
Groups
Approved
Structure
Thumb
Weight
Average: 362.473
Monoisotopic: 362.199428085
Chemical Formula
C23H26N2O2
Synonyms
  • Solifenacin
  • Solifenacina
External IDs
  • YM-67905
  • YM-905

Pharmacology

Indication

Solifenacin tablets are indicated to treat an overactive bladder with urinary incontinence, urgency, and frequency.3

Pharmacology
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

Solifenacin antagonizes the M2 and M3 muscarinic receptors in the bladder to treat an overactive bladder.3,2 It has a long duration of action as it is usually taken once daily.3 Patients taking solifenacin should be aware of the risks of angioedema and anaphylaxis.3

Mechanism of action

Solifenacin is a competitive muscarinic receptor antagonist.3 It has the highest affinity for M3, M1, and M2 muscarinic receptors.1 80% of the muscarinic receptors in the bladder are M2, while 20% are M3.2 Solifenacin's antagonism of the M3 receptor prevents contraction of the detrusor muscle, while antagonism of the M2 receptor may prevent contraction of smooth muscle in the bladder.2

TargetActionsOrganism
AMuscarinic acetylcholine receptor M3
antagonist
Humans
UMuscarinic acetylcholine receptor M1
antagonist
Humans
UMuscarinic acetylcholine receptor M2
antagonist
Humans
UMuscarinic acetylcholine receptor M4
antagonist
Humans
UMuscarinic acetylcholine receptor M5
antagonist
Humans
Absorption

Solifenacin is well absorbed in the duodenum, jejunum, and ileum but not the stomach.1 Absorption occurs via passive diffusion and so no transporters are involved.1 The mean oral bioavailability of solifenacin is 88%.1 The Tmax of solifenacin is 3-8 hours with a Css of 32.3ng/mL for a 5mg oral dose and 62.9ng/mL for a 10mg oral dose.3

Volume of distribution

The volume of distribution of solifenacin is 600L.1

Protein binding

Solifenacin is 93-96% protein bound in plasma, mainly to alpha-1-acid glycoprotein.1

Metabolism

Solifenacin undergoes N-oxidation at the quinuclidin ring by cytochrome P450, though the exact enzymes are not revealed in the literature.1 The tetrahydroisoquinolone ring is 4R-hydroxylated by CYP3A4, CYP1A1, and CYP2D6.1 A 4R-hydroxy N-oxide metabolite is also formed by CYP3A4.1 Finally, solifenacin can undergo direct glucuronidation.1 Only solifenacin and the 4R-hydroxy metabolite are pharmacologically active.1

Hover over products below to view reaction partners

Route of elimination

69.2±7.8% of a radiolabelled dose is recovered in the urine, 22.5±3.3% was recovered in feces, and 0.4±7.8% was recovered in exhaled air.1 18% of solifenacin is eliminated as the N-oxide metabolite, 9% is eliminated as the 4R-hydroxy N-oxide metabolite, and 8% is eliminated as the 4R-hydroxy metabolite.1

Half-life

The elimination half life of solifenacin ranges from 33-85 hours.1

Clearance

The clearance of solifenacin is 7-14L/h and a renal clearance of 0.67-1.51L/h.1

Adverse Effects
Adverseeffects
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Toxicity

The LD50 of Solifenacin has yet to be determined.4

Signs of overdose include severe anticholinergic effects, mental status changes, and decreased consciousness.3 In case of overdose, treat patients with gastric lavage and supportive measures.3 Monitor patients with an ECG.3

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
1,2-Benzodiazepine1,2-Benzodiazepine may increase the central nervous system depressant (CNS depressant) activities of Solifenacin.
AbametapirThe serum concentration of Solifenacin can be increased when it is combined with Abametapir.
AbataceptThe metabolism of Solifenacin can be increased when combined with Abatacept.
AbirateroneThe metabolism of Solifenacin can be decreased when combined with Abiraterone.
AcebutololThe metabolism of Solifenacin can be decreased when combined with Acebutolol.
AceclofenacThe risk or severity of hypertension can be increased when Solifenacin is combined with Aceclofenac.
AcemetacinThe risk or severity of hypertension can be increased when Solifenacin is combined with Acemetacin.
AcetaminophenThe metabolism of Solifenacin can be decreased when combined with Acetaminophen.
AcetazolamideAcetazolamide may increase the central nervous system depressant (CNS depressant) activities of Solifenacin.
AcetophenazineAcetophenazine may increase the central nervous system depressant (CNS depressant) activities of Solifenacin.
Interactions
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Food Interactions
  • Take with or without food.

Products

Products2
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Product Ingredients
IngredientUNIICASInChI Key
Solifenacin hydrochlorideNot Available180468-39-7YAUBKMSXTZQZEB-VROPFNGYSA-N
Solifenacin succinateKKA5DLD701242478-38-2RXZMMZZRUPYENV-VROPFNGYSA-N
Product Images
International/Other Brands
Vesikur
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Act SolifenacinTablet10 mgOralActavis Pharma Company2015-09-302018-04-30Canada flag
Act SolifenacinTablet5 mgOralActavis Pharma Company2015-09-302018-04-30Canada flag
Prz-solifenacinTablet10 mgOralPharmaris Canada Inc2020-11-13Not applicableCanada flag
Prz-solifenacinTablet5 mgOralPharmaris Canada Inc2020-11-13Not applicableCanada flag
SolifenacinTablet10 mgOralSanis Health Inc2016-11-03Not applicableCanada flag
SolifenacinTablet5 mgOralPro Doc Limitee2016-10-27Not applicableCanada flag
SolifenacinTablet5 mgOralSanis Health Inc2016-11-03Not applicableCanada flag
SolifenacinTablet10 mgOralPro Doc Limitee2016-10-27Not applicableCanada flag
Solifenacin SuccinateTablet10 mgOralJubilant Generics LimitedNot applicableNot applicableCanada flag
Solifenacin SuccinateTablet5 mgOralJubilant Generics LimitedNot applicableNot applicableCanada flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Ach-solifenacin SuccinateTablet10 mgOralAccord Healthcare IncNot applicableNot applicableCanada flag
Ach-solifenacin SuccinateTablet5 mgOralAccord Healthcare IncNot applicableNot applicableCanada flag
Apo-solifenacinTablet10 mgOralApotex Corporation2018-09-05Not applicableCanada flag
Apo-solifenacinTablet5 mgOralApotex Corporation2018-09-05Not applicableCanada flag
Auro-solifenacinTablet5 mgOralAuro Pharma Inc2016-01-04Not applicableCanada flag
Auro-solifenacinTablet10 mgOralAuro Pharma Inc2016-01-04Not applicableCanada flag
Bio-solifenacinTablet5 mgOralBiomed PharmaNot applicableNot applicableCanada flag
Bio-solifenacinTablet10 mgOralBiomed PharmaNot applicableNot applicableCanada flag
Dom-solifenacinTablet5 mgOralDominion PharmacalNot applicableNot applicableCanada flag
Dom-solifenacinTablet10 mgOralDominion PharmacalNot applicableNot applicableCanada flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
VESOMNİ 6 MG/0.4 MG DEĞİŞTİRİLMİŞ SALIMLI TABLET, 30 ADETSolifenacin succinate (6 mg) + Tamsulosin hydrochloride (0.4 mg)Tablet, delayed releaseOralASTELLAS PHARMA İLAÇ TİC. VE SAN. A.Ş.2020-08-14Not applicableTurkey flag
VESOMNI®Solifenacin succinate (6 mg) + Tamsulosin hydrochloride (0.4 mg)TabletOralASTELLAS FARMA COLOMBIA S.A.S.2017-05-23Not applicableColombia flag

Categories

ATC Codes
G04BD08 — SolifenacinG04CA53 — Tamsulosin and solifenacin
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as 1-phenyltetrahydroisoquinolines. These are compounds containing a phenyl group attached to the C1-atom of a tetrahydroisoquinoline moiety.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Tetrahydroisoquinolines
Sub Class
1-phenyltetrahydroisoquinolines
Direct Parent
1-phenyltetrahydroisoquinolines
Alternative Parents
Quinuclidines / Piperidines / Benzene and substituted derivatives / Carbamate esters / Trialkylamines / Organic carbonic acids and derivatives / Azacyclic compounds / Organopnictogen compounds / Organic oxides / Hydrocarbon derivatives
show 1 more
Substituents
1-phenyltetrahydroisoquinoline / Amine / Aromatic heteropolycyclic compound / Azacycle / Benzenoid / Carbamic acid ester / Carbonic acid derivative / Carbonyl group / Hydrocarbon derivative / Monocyclic benzene moiety
show 10 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
Not Available
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
A8910SQJ1U
CAS number
242478-37-1
InChI Key
FBOUYBDGKBSUES-VXKWHMMOSA-N
InChI
InChI=1S/C23H26N2O2/c26-23(27-21-16-24-13-10-18(21)11-14-24)25-15-12-17-6-4-5-9-20(17)22(25)19-7-2-1-3-8-19/h1-9,18,21-22H,10-16H2/t21-,22-/m0/s1
IUPAC Name
(3R)-1-azabicyclo[2.2.2]octan-3-yl (1S)-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate
SMILES
O=C(O[C@H]1CN2CCC1CC2)N1CCC2=CC=CC=C2[C@@H]1C1=CC=CC=C1

References

Synthesis Reference

Katsumi Saito, Masataka Katsuma, "Solifenacin transdermal preparation and method for enhancing transdermal permeation thereof." U.S. Patent US20050181031, issued August 18, 2005.

US20050181031
General References
  1. Doroshyenko O, Fuhr U: Clinical pharmacokinetics and pharmacodynamics of solifenacin. Clin Pharmacokinet. 2009;48(5):281-302. doi: 10.2165/00003088-200948050-00001. [Article]
  2. Kreder KJ: Solifenacin. Urol Clin North Am. 2006 Nov;33(4):483-90, ix. doi: 10.1016/j.ucl.2006.06.008. [Article]
  3. FDA Approved Drug Products: Solifenacin Succinate Tablets [Link]
  4. Cayman Chemicals: Solifenacin MSDS [Link]
KEGG Drug
D08522
PubChem Compound
154059
PubChem Substance
46506006
ChemSpider
135771
BindingDB
50370682
RxNav
322167
ChEBI
135530
ChEMBL
CHEMBL1734
ZINC
ZINC000003936683
Therapeutic Targets Database
DAP001129
PharmGKB
PA164783810
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Solifenacin
FDA label
Download (68.6 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedNot AvailableCognition1
4CompletedNot AvailableOveractive Bladder Syndrome (OABS)1
4CompletedBasic ScienceDetrusor Overactivity / Overactive Bladder Syndrome (OABS)1
4CompletedSupportive CareUrinary Urge Incontinence1
4CompletedTreatmentBenign Prostatic Hyperplasia (BPH) / Benign Prostatic Hypertrophy / Overactive Bladder Syndrome (OABS)1
4CompletedTreatmentBenign Prostatic Hyperplasia (BPH) / Lower Urinary Tract Symptoms (LUTS) / Overactive Bladder Syndrome (OABS)1
4CompletedTreatmentBenign Prostatic Hyperplasia (BPH) / Overactive Bladder Syndrome (OABS) / Photoselective Vaporization Prostatectomy / Transurethral Resection of Prostate1
4CompletedTreatmentFlank Pain / Overactive Bladder Syndrome (OABS)1
4CompletedTreatmentLower Urinary Tract Symptoms (LUTS)1
4CompletedTreatmentMultiple Sclerosis / Neurogenic Bladder Dysfunction / Spinal Cord Diseases1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Astellas Pharma Inc.
  • Bayer Healthcare
  • Cypress Pharmaceutical Inc.
  • Ivax Pharmaceuticals
  • Lake Erie Medical and Surgical Supply
  • MJ Nutritional
  • Murfreesboro Pharmaceutical Nursing Supply
  • Nature's Bounty
  • Novartis AG
  • Pharmics Inc.
  • Physicians Total Care Inc.
  • Redpharm Drug
  • United Research Laboratories Inc.
  • US Pharmaceutical Corp.
Dosage Forms
FormRouteStrength
Tablet, film coatedOral
Tablet, film coatedOral5.00 mg
Tablet, film coatedOral10 MG
Tablet, film coatedOral5 MG
Tablet, orally disintegratingOral10 MG
Tablet, orally disintegratingOral5 MG
Tablet, orally disintegratingOral
Tablet, coatedOral10 mg/1
Tablet, coatedOral5 mg/1
Tablet, film coated, extended releaseOral10 mg/1
SolutionOral1 MG/ML
TabletOral10 mg/1
TabletOral5 mg/1
TabletOral
TabletOral10 mg
TabletOral5 mg
Tablet, film coatedOral10 mg/1
Tablet, film coatedOral5 mg/1
SuspensionOral
SuspensionOral1 mg/1mL
Tablet, delayed releaseOral
TabletOral
Tablet, coatedOral10 mg
Tablet, coatedOral5 mg
Prices
Unit descriptionCostUnit
Fer-In-Sol 75 (15 Fe)mg/ml Solution 50ml Bottle19.0USD bottle
Fergon 100 240 (27 Fe)mg tablet Bottle15.99USD bottle
Fortabs 50-325-40 mg tablet0.4USD tablet
Hemocyte tablet0.33USD tablet
Hemocyte-f tablet0.33USD tablet
Feosol 45 mg tablet0.31USD tablet
Slow fe 142 mg tablet0.27USD tablet
Ferrous fumarate 324 mg tablet0.21USD tablet
Fer-in-sol 15 mg/ml drops0.19USD ml
Feosol 65 mg tablet0.18USD tablet
Ferretts 325 mg tablet0.14USD tablet
Fergon 27 mg tablet0.05USD tablet
Ferretts ips liquid0.05USD ml
Ferrous gluc 246 mg (27 mg) tablet0.04USD tablet
Ferrous gluconate 27 mg tablet0.04USD tablet
Ferrous sulfate 28 mg tablet0.04USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
CA2208839No2006-01-312015-12-27Canada flag
US6017927Yes2000-01-252019-05-19US flag
US9918970No2018-03-202031-05-18US flag

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)134-136https://www.trc-canada.com/product-detail/?S676701
Predicted Properties
PropertyValueSource
Water Solubility0.0729 mg/mLALOGPS
logP3.9ALOGPS
logP3.96ChemAxon
logS-3.7ALOGPS
pKa (Strongest Basic)8.88ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area32.78 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity106.06 m3·mol-1ChemAxon
Polarizability40.13 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.9706
Blood Brain Barrier+0.6159
Caco-2 permeable-0.6679
P-glycoprotein substrateSubstrate0.7801
P-glycoprotein inhibitor IInhibitor0.8572
P-glycoprotein inhibitor IIInhibitor0.8611
Renal organic cation transporterNon-inhibitor0.7498
CYP450 2C9 substrateNon-substrate0.8311
CYP450 2D6 substrateNon-substrate0.7264
CYP450 3A4 substrateSubstrate0.545
CYP450 1A2 substrateNon-inhibitor0.8445
CYP450 2C9 inhibitorNon-inhibitor0.8755
CYP450 2D6 inhibitorNon-inhibitor0.8593
CYP450 2C19 inhibitorNon-inhibitor0.7037
CYP450 3A4 inhibitorNon-inhibitor0.7027
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8748
Ames testNon AMES toxic0.8871
CarcinogenicityNon-carcinogens0.9596
BiodegradationNot ready biodegradable0.9828
Rat acute toxicity2.3839 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8115
hERG inhibition (predictor II)Inhibitor0.727
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Targets

Drugtargets2
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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
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
  3. Ito Y, Oyunzul L, Yoshida A, Fujino T, Noguchi Y, Yuyama H, Ohtake A, Suzuki M, Sasamata M, Matsui M, Yamada S: Comparison of muscarinic receptor selectivity of solifenacin and oxybutynin in the bladder and submandibular gland of muscarinic receptor knockout mice. Eur J Pharmacol. 2009 Aug 1;615(1-3):201-6. doi: 10.1016/j.ejphar.2009.04.068. Epub 2009 May 13. [Article]
  4. Sinha S, Gupta S, Malhotra S, Krishna NS, Meru AV, Babu V, Bansal V, Garg M, Kumar N, Chugh A, Ray A: AE9C90CB: a novel, bladder-selective muscarinic receptor antagonist for the treatment of overactive bladder. Br J Pharmacol. 2010 Jul;160(5):1119-27. doi: 10.1111/j.1476-5381.2010.00752.x. [Article]
  5. 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. [Article]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
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
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
  3. Sinha S, Gupta S, Malhotra S, Krishna NS, Meru AV, Babu V, Bansal V, Garg M, Kumar N, Chugh A, Ray A: AE9C90CB: a novel, bladder-selective muscarinic receptor antagonist for the treatment of overactive bladder. Br J Pharmacol. 2010 Jul;160(5):1119-27. doi: 10.1111/j.1476-5381.2010.00752.x. [Article]
  4. 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. [Article]
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
  1. Sinha S, Gupta S, Malhotra S, Krishna NS, Meru AV, Babu V, Bansal V, Garg M, Kumar N, Chugh A, Ray A: AE9C90CB: a novel, bladder-selective muscarinic receptor antagonist for the treatment of overactive bladder. Br J Pharmacol. 2010 Jul;160(5):1119-27. doi: 10.1111/j.1476-5381.2010.00752.x. [Article]
  2. 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. [Article]
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
  1. 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. [Article]
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
  1. 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. [Article]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
No
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
  1. Doroshyenko O, Fuhr U: Clinical pharmacokinetics and pharmacodynamics of solifenacin. Clin Pharmacokinet. 2009;48(5):281-302. doi: 10.2165/00003088-200948050-00001. [Article]
  2. Swart PJ, Krauwinkel WJ, Smulders RA, Smith NN: Pharmacokinetic effect of ketoconazole on solifenacin in healthy volunteers. Basic Clin Pharmacol Toxicol. 2006 Jul;99(1):33-6. doi: 10.1111/j.1742-7843.2006.pto_285.x. [Article]
  3. FDA Approved Drug Products: Solifenacin Succinate Tablets [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Vitamin d 24-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 oxidizes a variety of structurally un...
Gene Name
CYP1A1
Uniprot ID
P04798
Uniprot Name
Cytochrome P450 1A1
Molecular Weight
58164.815 Da
References
  1. Doroshyenko O, Fuhr U: Clinical pharmacokinetics and pharmacodynamics of solifenacin. Clin Pharmacokinet. 2009;48(5):281-302. doi: 10.2165/00003088-200948050-00001. [Article]
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
  1. Doroshyenko O, Fuhr U: Clinical pharmacokinetics and pharmacodynamics of solifenacin. Clin Pharmacokinet. 2009;48(5):281-302. doi: 10.2165/00003088-200948050-00001. [Article]

Carriers

Kind
Protein group
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
General Function
Not Available
Specific Function
Functions as transport protein in the blood stream. Binds various ligands in the interior of its beta-barrel domain. Also binds synthetic drugs and influences their distribution and availability in...

Components:
References
  1. Doroshyenko O, Fuhr U: Clinical pharmacokinetics and pharmacodynamics of solifenacin. Clin Pharmacokinet. 2009;48(5):281-302. doi: 10.2165/00003088-200948050-00001. [Article]
  2. FDA Approved Drug Products: Solifenacin Succinate Tablets [Link]

Drug created at June 13, 2005 13:24 / Updated at November 28, 2021 11:56