solifenacin Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
muscarinic receptors antagonists 2457 242478-37-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • YM-67905
  • YM-905
  • solifenacin
  • solifenacin succinate
  • vesicare
A quinuclidine and tetrahydroisoquinoline derivative and selective M3 MUSCARINIC ANTAGONIST. It is used as a UROLOGIC AGENT in the treatment of URINARY INCONTINENCE.
  • Molecular weight: 362.47
  • Formula: C23H26N2O2
  • CLOGP: 4.68
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 0
  • TPSA: 32.78
  • ALOGS: -3.70
  • ROTB: 3

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
5 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 12.50 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.30 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 90 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 8.20 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 2.10 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.02 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 52 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Nov. 19, 2004 FDA ASTELLAS

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Dry mouth 486.39 29.27 122 1677 8131 2348155
Off label use 445.37 29.27 193 1606 73405 2282881
Constipation 223.30 29.27 84 1715 21545 2334741
Vision blurred 203.76 29.27 71 1728 14597 2341689
Drug ineffective 201.87 29.27 127 1672 101497 2254789
Urinary retention 194.31 29.27 50 1749 3617 2352669
Dementia 110.54 29.27 30 1769 2651 2353635
Fall 100.54 29.27 62 1737 47037 2309249
Confusional state 95.82 29.27 48 1751 24296 2331990
Dry eye 90.48 29.27 28 1771 3928 2352358
Inappropriate schedule of product administration 75.71 29.27 33 1766 12171 2344115
Dry throat 74.61 29.27 18 1781 990 2355296
Urinary incontinence 72.29 29.27 24 1775 4209 2352077
Malaise 70.30 29.27 53 1746 55532 2300754
Torsade de pointes 69.12 29.27 20 1779 2226 2354060
Wrong technique in product usage process 66.23 29.27 35 1764 19713 2336573
Dizziness 65.59 29.27 52 1747 58613 2297673
Completed suicide 61.39 29.27 34 1765 21000 2335286
Electrocardiogram QT prolonged 61.36 29.27 25 1774 7789 2348497
Acute kidney injury 54.72 29.27 35 1764 28087 2328199
Urinary tract infection 52.72 29.27 35 1764 29907 2326379
Product use in unapproved indication 49.66 29.27 24 1775 11176 2345110
Somnolence 45.09 29.27 29 1770 23456 2332830
Bladder sphincter atony 44.76 29.27 7 1792 34 2356252
Condition aggravated 41.43 29.27 31 1768 31948 2324338
Hallucination 40.82 29.27 19 1780 8129 2348157
Dyspepsia 40.35 29.27 20 1779 9824 2346462
Orthostatic hypotension 40.03 29.27 14 1785 2865 2353421
Hyperkalaemia 39.99 29.27 17 1782 5876 2350410
Hypertonic bladder 39.49 29.27 9 1790 385 2355901
Dysuria 39.30 29.27 15 1784 3926 2352360
Muscular weakness 37.80 29.27 22 1777 14875 2341411
Hypokalaemia 35.99 29.27 19 1780 10635 2345651
Pyelonephritis 35.97 29.27 12 1787 2129 2354157
Cerebral haematoma 35.92 29.27 9 1790 578 2355708
Liver disorder 35.40 29.27 16 1783 6398 2349888
Syncope 35.27 29.27 22 1777 16853 2339433
Oedema peripheral 35.21 29.27 25 1774 23738 2332548
Sinus node dysfunction 34.43 29.27 9 1790 685 2355601
Palpitations 33.25 29.27 21 1778 16435 2339851
Loss of consciousness 33.13 29.27 22 1777 18745 2337541
Abdominal pain 33.10 29.27 28 1771 34346 2321940
Disorientation 32.35 29.27 15 1784 6357 2349929
Pruritus 31.26 29.27 30 1769 43310 2312976
Language disorder 30.95 29.27 7 1792 289 2355997
Hypomagnesaemia 30.09 29.27 11 1788 2553 2353733
Dysphagia 30.09 29.27 18 1781 12787 2343499
Intentional product misuse 29.45 29.27 16 1783 9473 2346813
Mucosal dryness 29.30 29.27 7 1792 368 2355918

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Off label use 267.77 34.01 107 837 38464 1707373
Dry mouth 224.01 34.01 55 889 3858 1741979
Urinary retention 201.70 34.01 54 890 5341 1740496
Confusional state 149.61 34.01 60 884 21218 1724619
Constipation 136.21 34.01 51 893 14949 1730888
Drug ineffective 102.04 34.01 66 878 63735 1682102
Somnolence 64.31 34.01 31 913 16708 1729129
Parkinson's disease 62.74 34.01 17 927 1725 1744112
Vision blurred 59.64 34.01 24 920 8399 1737438
Fall 57.98 34.01 34 910 27180 1718657
Epilepsy 52.88 34.01 18 926 3941 1741896
Hallucination 46.73 34.01 20 924 8150 1737687
Bladder cancer 46.66 34.01 14 930 2042 1743795
Loss of consciousness 40.86 34.01 22 922 14853 1730984
Hyponatraemia 38.55 34.01 18 926 8982 1736855
Overdose 38.48 34.01 22 922 16679 1729158
Obesity 36.36 34.01 10 934 1069 1744768
Dizziness 34.57 34.01 27 917 34334 1711503

Pharmacologic Action:

SourceCodeDescription
ATC G04BD08 GENITO URINARY SYSTEM AND SEX HORMONES
UROLOGICALS
UROLOGICALS
Drugs for urinary frequency and incontinence
ATC G04CA53 GENITO URINARY SYSTEM AND SEX HORMONES
UROLOGICALS
DRUGS USED IN BENIGN PROSTATIC HYPERTROPHY
Alpha-adrenoreceptor antagonists
MeSH PA D018678 Cholinergic Agents
MeSH PA D018680 Cholinergic Antagonists
MeSH PA D018727 Muscarinic Antagonists
MeSH PA D018377 Neurotransmitter Agents
FDA EPC N0000175700 Cholinergic Muscarinic Antagonist
FDA MoA N0000000125 Cholinergic Muscarinic Antagonists
MeSH PA D064804 Urological Agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Urgent desire to urinate indication 75088002
Urge incontinence of urine indication 87557004
Bladder muscle dysfunction - overactive indication 236633002
Increased Urinary Frequency indication
Torsades de pointes contraindication 31722008
Acute nephropathy contraindication 58574008
Hepatic failure contraindication 59927004
Prolonged QT interval contraindication 111975006
Gastrointestinal obstruction contraindication 126765001
Disease of liver contraindication 235856003 DOID:409
Bladder outflow obstruction contraindication 236645006
Retention of urine contraindication 267064002
Gastric retention contraindication 307227006
Angle-closure glaucoma contraindication 392291006 DOID:13550
Gastrointestinal hypomotility contraindication 421807004
Congenital long QT syndrome contraindication 442917000

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.21 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Muscarinic acetylcholine receptor M3 GPCR ANTAGONIST IC50 6.88 CHEMBL CHEMBL
Muscarinic acetylcholine receptor M2 GPCR ANTAGONIST IC50 6.24 CHEMBL CHEMBL
Muscarinic acetylcholine receptor M4 GPCR ANTAGONIST Ki 6.80 IUPHAR
Muscarinic acetylcholine receptor M5 GPCR ANTAGONIST Ki 7.20 IUPHAR
Muscarinic acetylcholine receptor M1 GPCR IC50 7.20 CHEMBL
Muscarinic acetylcholine receptor M1 GPCR Ki 8 CHEMBL
Muscarinic acetylcholine receptor M3 GPCR Ki 8 CHEMBL
Muscarinic acetylcholine receptor M2 GPCR Ki 6.92 CHEMBL

External reference:

IDSource
D000069464 MESH_DESCRIPTOR_UI
4024390 VUID
N0000022393 NUI
C1099677 UMLSCUI
D01269 KEGG_DRUG
407031006 SNOMEDCT_US
407030007 SNOMEDCT_US
322167 RXNORM
d05413 MMSL
4024390 VANDF
008712 NDDF
A8910SQJ1U UNII
8155 INN_ID
CHEMBL1734 ChEMBL_ID
CHEMBL1200803 ChEMBL_ID
242478-38-2 SECONDARY_CAS_RN
DB01591 DRUGBANK_ID
CHEBI:135530 CHEBI
154059 PUBCHEM_CID
7483 IUPHAR_LIGAND_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Solifenacin Succinate HUMAN PRESCRIPTION DRUG LABEL 1 0093-5263 TABLET, FILM COATED 5 mg ORAL ANDA 17 sections
Solifenacin Succinate HUMAN PRESCRIPTION DRUG LABEL 1 0093-5264 TABLET, FILM COATED 10 mg ORAL ANDA 17 sections
solifenacin succinate HUMAN PRESCRIPTION DRUG LABEL 1 27241-037 TABLET, FILM COATED 5 mg ORAL ANDA 16 sections
solifenacin succinate HUMAN PRESCRIPTION DRUG LABEL 1 27241-038 TABLET, FILM COATED 10 mg ORAL ANDA 16 sections
Solifenacin Succinate HUMAN PRESCRIPTION DRUG LABEL 1 29300-328 TABLET, FILM COATED 5 mg ORAL ANDA 17 sections
Solifenacin Succinate HUMAN PRESCRIPTION DRUG LABEL 1 29300-329 TABLET, FILM COATED 10 mg ORAL ANDA 17 sections
Solifenacin Succinate HUMAN PRESCRIPTION DRUG LABEL 1 35561-285 TABLET, FILM COATED 5 mg ORAL ANDA 17 sections
Solifenacin Succinate HUMAN PRESCRIPTION DRUG LABEL 1 35561-286 TABLET, FILM COATED 10 mg ORAL ANDA 17 sections
Solifenacin Succinate HUMAN PRESCRIPTION DRUG LABEL 1 46708-192 TABLET, COATED 5 mg ORAL ANDA 17 sections
Solifenacin Succinate HUMAN PRESCRIPTION DRUG LABEL 1 46708-193 TABLET, COATED 10 mg ORAL ANDA 17 sections
solifenacin succinate HUMAN PRESCRIPTION DRUG LABEL 1 48792-7909 TABLET, FILM COATED 5 mg ORAL ANDA 17 sections
solifenacin succinate HUMAN PRESCRIPTION DRUG LABEL 1 48792-7910 TABLET, FILM COATED 10 mg ORAL ANDA 17 sections
SOLIFENACIN SUCCINATE HUMAN PRESCRIPTION DRUG LABEL 1 50228-427 TABLET, FILM COATED 5 mg ORAL ANDA 17 sections
SOLIFENACIN SUCCINATE HUMAN PRESCRIPTION DRUG LABEL 1 50228-428 TABLET, FILM COATED 10 mg ORAL ANDA 17 sections
VESIcare HUMAN PRESCRIPTION DRUG LABEL 1 51248-150 TABLET, FILM COATED 5 mg ORAL NDA 17 sections
VESIcare HUMAN PRESCRIPTION DRUG LABEL 1 51248-151 TABLET, FILM COATED 10 mg ORAL NDA 17 sections
Solifenacin Succinate HUMAN PRESCRIPTION DRUG LABEL 1 51407-227 TABLET, FILM COATED 5 mg ORAL ANDA 17 sections
Solifenacin Succinate HUMAN PRESCRIPTION DRUG LABEL 1 51407-228 TABLET, FILM COATED 10 mg ORAL ANDA 17 sections
SOLIFENACIN SUCCINATE HUMAN PRESCRIPTION DRUG LABEL 1 51407-254 TABLET, FILM COATED 5 mg ORAL ANDA 17 sections
SOLIFENACIN SUCCINATE HUMAN PRESCRIPTION DRUG LABEL 1 51407-255 TABLET, FILM COATED 10 mg ORAL ANDA 17 sections
VESIcare HUMAN PRESCRIPTION DRUG LABEL 1 54868-4705 TABLET, FILM COATED 10 mg ORAL NDA 16 sections
VESIcare HUMAN PRESCRIPTION DRUG LABEL 1 54868-5398 TABLET, FILM COATED 5 mg ORAL NDA 16 sections
VESIcare HUMAN PRESCRIPTION DRUG LABEL 1 55154-3877 TABLET, FILM COATED 5 mg ORAL NDA 17 sections
VESIcare HUMAN PRESCRIPTION DRUG LABEL 1 55154-3878 TABLET, FILM COATED 10 mg ORAL NDA 17 sections
Solifenacin Succinate HUMAN PRESCRIPTION DRUG LABEL 1 60505-4702 TABLET, FILM COATED 5 mg ORAL ANDA 17 sections
Solifenacin Succinate HUMAN PRESCRIPTION DRUG LABEL 1 60505-4703 TABLET, FILM COATED 10 mg ORAL ANDA 17 sections
Solifenacin Succinate HUMAN PRESCRIPTION DRUG LABEL 1 60687-499 TABLET, COATED 5 mg ORAL ANDA 18 sections
Solifenacin Succinate HUMAN PRESCRIPTION DRUG LABEL 1 62332-192 TABLET, COATED 5 mg ORAL ANDA 17 sections
Solifenacin Succinate HUMAN PRESCRIPTION DRUG LABEL 1 62332-193 TABLET, COATED 10 mg ORAL ANDA 17 sections
solifenacin succinate HUMAN PRESCRIPTION DRUG LABEL 1 64380-941 TABLET, FILM COATED 5 mg ORAL ANDA 17 sections