U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ABSOLUTE
Molecular Formula C23H26N2O2.C4H6O6
Molecular Weight 512.5516
Optical Activity UNSPECIFIED
Defined Stereocenters 4 / 4
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of SOLIFENACIN TARTRATE

SMILES

O[C@H]([C@@H](O)C(O)=O)C(O)=O.O=C(O[C@H]1CN2CCC1CC2)N3CCC4=C(C=CC=C4)[C@@H]3C5=CC=CC=C5

InChI

InChIKey=KTNRTEKPBRTUKA-DWERDEDHSA-N
InChI=1S/C23H26N2O2.C4H6O6/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;5-1(3(7)8)2(6)4(9)10/h1-9,18,21-22H,10-16H2;1-2,5-6H,(H,7,8)(H,9,10)/t21-,22-;1-,2-/m01/s1

HIDE SMILES / InChI

Molecular Formula C4H6O6
Molecular Weight 150.0868
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 2 / 2
E/Z Centers 0
Optical Activity UNSPECIFIED

Molecular Formula C23H26N2O2
Molecular Weight 362.4647
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 2 / 2
E/Z Centers 0
Optical Activity UNSPECIFIED

Description
Curator's Comment: description was created based on several sources, including: http://www.rxlist.com/vesicare-drug.htm https://www.drugs.com/mtm/solifenacin.html http://www.wikidoc.org/index.php/Solifenacin

Solifenacin is a competitive muscarinic acetylcholine receptor antagonist. The binding of acetylcholine to these receptors, particularly the M3 receptor subtype, plays a critical role in the contraction of smooth muscle. By preventing the binding of acetylcholine to these receptors, solifenacin reduces smooth muscle tone in the bladder, allowing the bladder to retain larger volumes of urine. It is FDA approved for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and urinary frequency. Common adverse reactions include constipation, Xerostomia. Inhibitors of CYP3A4 may increase the concentration of Solifenacin. Vice versa, CYP3A4 Inducers decrease concentration.

CNS Activity

Curator's Comment: Known to be CNS penetrant in rat. Human data not available

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
10.0 nM [Ki]
125.0 nM [Ki]
25.0 nM [Ki]
7.73 null [pKi]
7.46 null [pKi]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
VESICARE

Approved Use

VESIcare is a muscarinic antagonist indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and urinary frequency. VESIcare is a muscarinic antagonist indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and urinary frequency (1)

Launch Date

2004
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
14.1 ng/mL
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SOLIFENACIN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
820 ng × h/mL
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SOLIFENACIN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
50.8 h
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SOLIFENACIN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
2%
SOLIFENACIN plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
100 mg single, oral
Highest studied dose
Dose: 100 mg
Route: oral
Route: single
Dose: 100 mg
Sources:
healthy, 19-40
Health Status: healthy
Age Group: 19-40
Sex: M
Sources:
30 mg 1 times / day multiple, oral
Highest studied dose
Dose: 30 mg, 1 times / day
Route: oral
Route: multiple
Dose: 30 mg, 1 times / day
Sources:
healthy, 20-35
Health Status: healthy
Age Group: 20-35
Sex: M
Sources:
10 mg 1 times / day multiple, oral
Recommended
Dose: 10 mg, 1 times / day
Route: oral
Route: multiple
Dose: 10 mg, 1 times / day
Sources:
unhealthy
Disc. AE: Angioedema, Anaphylactic reaction...
AEs leading to
discontinuation/dose reduction:
Angioedema
Anaphylactic reaction (rare)
Sources:
10 mg 1 times / day multiple, oral
Recommended
Dose: 10 mg, 1 times / day
Route: oral
Route: multiple
Dose: 10 mg, 1 times / day
Sources:
unhealthy
Disc. AE: Dry mouth...
AEs leading to
discontinuation/dose reduction:
Dry mouth (1.5%)
Sources:
AEs

AEs

AESignificanceDosePopulation
Angioedema Disc. AE
10 mg 1 times / day multiple, oral
Recommended
Dose: 10 mg, 1 times / day
Route: oral
Route: multiple
Dose: 10 mg, 1 times / day
Sources:
unhealthy
Anaphylactic reaction rare
Disc. AE
10 mg 1 times / day multiple, oral
Recommended
Dose: 10 mg, 1 times / day
Route: oral
Route: multiple
Dose: 10 mg, 1 times / day
Sources:
unhealthy
Dry mouth 1.5%
Disc. AE
10 mg 1 times / day multiple, oral
Recommended
Dose: 10 mg, 1 times / day
Route: oral
Route: multiple
Dose: 10 mg, 1 times / day
Sources:
unhealthy
Overview

OverviewOther

Other InhibitorOther SubstrateOther Inducer







Drug as perpetrator​Drug as victimTox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
Sourcing

Sourcing

Vendor/AggregatorIDURL
PubMed

PubMed

TitleDatePubMed
An unusual cause of postoperative detrusor overactivity.
2007-10
Comparison of the efficacy and tolerability of solifenacin succinate with or without previous use of trospium chloride.
2007-09
Nocturnal polyuria and nocturia relief in patients treated with solifenacin for overactive bladder symptoms.
2007-07
Solifenacin for overactive bladder with incontinence: symptom bother and health-related quality of life outcomes.
2007-03
Effect of antimuscarinic drugs used for overactive bladder on learning in a rat passive avoidance response test.
2007-02-28
Pharmacokinetics, safety, and tolerability of solifenacin in patients with renal insufficiency.
2007-01
Redefining response in overactive bladder syndrome.
2007-01
Pharmacological characterization of a new antimuscarinic agent, solifenacin succinate, in comparison with other antimuscarinic agents.
2007-01
Newer agents for the management of overactive bladder.
2006-12-15
New developments in the treatment of urinary incontinence.
2006-12
Solifenacin succinate (VESIcare): overactive bladder therapy.
2006-12
Open-label study of the safety and pharmacokinetics of solifenacin in subjects with hepatic impairment.
2006-12
[Pharmacological and clinical profile of solifenacin succinate (Vesicare) developed as a new therapeutic agent for overactive bladder].
2006-12
Pharmacoeconomic evaluation of antimuscarinic agents for the treatment of overactive bladder.
2006-12
Solifenacin provides effective antimuscarinic therapy for the complete management of overactive bladder.
2006-12
Symptom bother and health-related quality of life outcomes following solifenacin treatment for overactive bladder: the VESIcare Open-Label Trial (VOLT).
2006-11
Gateways to clinical trials.
2006-11
Treatment of the overactive bladder syndrome with muscarinic receptor antagonists: a matter of metabolites?
2006-11
Solifenacin.
2006-11
Anticholinergic drugs versus placebo for overactive bladder syndrome in adults.
2006-10-18
Efficacy and tolerability of solifenacin in elderly subjects with overactive bladder syndrome: A pooled analysis.
2006-09
Solifenacin succinate for the treatment of symptoms of overactive bladder.
2006-09
Reductions in overactive bladder-related incontinence from pooled analysis of phase III trials evaluating treatment with solifenacin.
2006-09
Gateways to clinical trials.
2006-08-09
Patient-reported outcomes in overactive bladder: importance for determining clinical effectiveness of treatment.
2006-08
Solifenacin significantly improves all symptoms of overactive bladder syndrome.
2006-08
Multiple doses of the antimuscarinic agent solifenacin do not affect the pharmacodynamics or pharmacokinetics of warfarin or the steady-state pharmacokinetics of digoxin in healthy subjects.
2006-08
Pharmacokinetic effect of ketoconazole on solifenacin in healthy volunteers.
2006-07
Comparative evaluation of exocrine muscarinic receptor binding characteristics and inhibition of salivation of solifenacin in mice.
2006-07
[Comment on the STAR study: Comparison of the efficacy and tolerance of solifenacin and tolterodine retard in the treatment of overactive bladder].
2006-07
[Oral anticholinergics in overactive bladder].
2006-07
Short- and long-term efficacy of solifenacin treatment in patients with symptoms of mixed urinary incontinence.
2006-06
Gateways to clinical trials.
2006-05
Gateways to clinical trials.
2006-04
The causes and consequences of overactive bladder.
2006-04
Efficacy and tolerability of solifenacin in elderly subjects with overactive bladder syndrome: a pooled analysis.
2006-03
The emergence of new drugs for overactive bladder.
2006-03
Management of overactive bladder and urge urinary incontinence in the elderly patient.
2006-03
Pharmacologic management of overactive bladder: practical options for the primary care physician.
2006-03
Using anticholinergics to treat overactive bladder: the issue of treatment tolerability.
2006-03
Muscarinic receptors in the bladder: from basic research to therapeutics.
2006-02
New drugs 06, part I.
2006-02
Efficacy of solifenacin in patients with severe symptoms of overactive bladder: a pooled analysis.
2006-01
Solifenacin in overactive bladder syndrome.
2006
[Drug discovery in the fields of urology: tamsulosin and solifenacin].
2005-11
Solifenacin in overactive bladder: a viewpoint by Hashim Hashim.
2005
Solifenacin in overactive bladder syndrome: a viewpoint by Scott Serels.
2005
Solifenacin in overactive bladder syndrome.
2005
Overactive bladder in the elderly: a guide to pharmacological management.
2005
Drug forecast--solifenacin: an investigational anticholinergic for overactive bladder.
2004-05
Patents

Sample Use Guides

5 mg tablet taken once daily, and if well tolerated may be increased to 10 mg once daily.
Route of Administration: Oral
The inhibitory effect of solifenacin (dose range: 10^-10 - 10^-6 M) for bladder smooth muscle cells (pK(i)=8.12) was 3.6-fold more potent than that for salivary gland cells (pK(i)=7.57).
Substance Class Chemical
Created
by admin
on Wed Apr 02 02:53:35 GMT 2025
Edited
by admin
on Wed Apr 02 02:53:35 GMT 2025
Record UNII
CCM244AP8R
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
SOLIFENACIN TARTRATE
Common Name English
SOLIFENACIN BITARTRATE
Preferred Name English
Solifenacin tartrate [WHO-DD]
Common Name English
SOLIFENACIN HYDROGEN TARTRATE
Common Name English
2(1H)-ISOQUINOLINECARBOXYLIC ACID, 3,4-DIHYDRO-1-PHENYL-, (3R)-1-AZABICYCLO(2.2.2)OCT-3-YL ESTER, (1S)-, (2R,3R)-2,3-DIHYDROXYBUTANEDIOATE (1:1)
Systematic Name English
Code System Code Type Description
FDA UNII
CCM244AP8R
Created by admin on Wed Apr 02 02:53:35 GMT 2025 , Edited by admin on Wed Apr 02 02:53:35 GMT 2025
PRIMARY
CAS
1035547-81-9
Created by admin on Wed Apr 02 02:53:35 GMT 2025 , Edited by admin on Wed Apr 02 02:53:35 GMT 2025
PRIMARY
PUBCHEM
154731572
Created by admin on Wed Apr 02 02:53:35 GMT 2025 , Edited by admin on Wed Apr 02 02:53:35 GMT 2025
PRIMARY
Related Record Type Details
PARENT -> SALT/SOLVATE
Related Record Type Details
ACTIVE MOIETY