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

Stem definitionDrug idCAS RN
4191 286930-02-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • fesoterodine
  • toviaz
  • fesoterodine fumarate
a muscarinic antagonist for treatment of overactive bladder
  • Molecular weight: 411.59
  • Formula: C26H37NO3
  • CLOGP: 4.36
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 1
  • TPSA: 49.77
  • ALOGS: -5.30
  • ROTB: 11

  • Status: OFP

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

Drug dosage:

DoseUnitRoute
4 mg O
3.50 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 256 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 0 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.33 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

Approvals:

DateAgencyCompanyOrphan
Oct. 31, 2008 FDA PFIZER

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
Urinary retention 442.36 32.86 88 949 3579 2353469
Dry mouth 429.79 32.86 99 938 8154 2348894
Drug ineffective 144.62 32.86 84 953 101540 2255508
Multiple fractures 130.02 32.86 24 1013 631 2356417
Brain injury 121.90 32.86 24 1013 895 2356153
Constipation 116.34 32.86 45 992 21584 2335464
Fall 97.08 32.86 50 987 47049 2309999
Urinary incontinence 94.65 32.86 26 1011 4207 2352841
Gait disturbance 80.41 32.86 35 1002 22510 2334538
Pulseless electrical activity 78.76 32.86 17 1020 998 2356050
Electrocardiogram QRS complex prolonged 77.37 32.86 17 1020 1085 2355963
Balance disorder 73.29 32.86 26 1011 9721 2347327
Vision blurred 69.83 32.86 28 1009 14640 2342408
Hypertonic bladder 69.00 32.86 13 1024 381 2356667
Dysuria 68.97 32.86 20 1017 3921 2353127
Bradycardia 68.92 32.86 25 1012 9956 2347092
Dizziness 63.47 32.86 41 996 58624 2298424
Feeling abnormal 63.14 32.86 30 1007 23551 2333497
Drug hypersensitivity 61.54 32.86 37 1000 46606 2310442
Dry eye 60.12 32.86 18 1019 3938 2353110
Hypotension 56.86 32.86 31 1006 32405 2324643
Loss of consciousness 56.79 32.86 26 1011 18741 2338307
Confusional state 53.27 32.86 27 1010 24317 2332731
Overdose 49.22 32.86 24 1013 19883 2337165
Malaise 48.41 32.86 34 1003 55551 2301497
Oedema peripheral 45.20 32.86 24 1013 23739 2333309
Dry throat 41.08 32.86 10 1027 998 2356050
Pollakiuria 39.88 32.86 13 1024 3743 2353305
Rash 39.62 32.86 31 1006 59527 2297521
Dementia 35.58 32.86 11 1026 2670 2354378
Therapeutic product effect incomplete 33.09 32.86 15 1022 10516 2346532

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
Urinary retention 612.21 43.68 119 432 5276 1740954
Dry mouth 150.86 43.68 36 515 3877 1742353
Dysuria 87.32 43.68 23 528 3649 1742581
Constipation 80.35 43.68 30 521 14970 1731260
Fall 69.34 43.68 32 519 27182 1719048
Drug ineffective 53.35 43.68 36 515 63765 1682465
Dizziness 48.08 43.68 27 524 34334 1711896

Pharmacologic Action:

SourceCodeDescription
ATC G04BD11 GENITO URINARY SYSTEM AND SEX HORMONES
UROLOGICALS
UROLOGICALS
Drugs for urinary frequency and incontinence
ATC G04BD13 GENITO URINARY SYSTEM AND SEX HORMONES
UROLOGICALS
UROLOGICALS
Drugs for urinary frequency and incontinence
MeSH PA D018678 Cholinergic Agents
MeSH PA D018680 Cholinergic Antagonists
MeSH PA D018727 Muscarinic Antagonists
MeSH PA D018377 Neurotransmitter Agents
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
Acute nephropathy contraindication 58574008
Hepatic failure contraindication 59927004
Myasthenia gravis contraindication 91637004 DOID:437
Acute constipation contraindication 197119006
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
Poor metabolizer due to cytochrome p450 CYP2D6 variant contraindication 423629005
Aggravated Glaucoma contraindication

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.64 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
4MG TOVIAZ PFIZER N022030 Oct. 31, 2008 RX TABLET, EXTENDED RELEASE ORAL 6858650 July 3, 2022 TREATMENT OF OVERACTIVE BLADDER WITH SYMPTOMS OF URGE URINARY INCONTINENCE, URGENCY, AND FREQUENCY
8MG TOVIAZ PFIZER N022030 Oct. 31, 2008 RX TABLET, EXTENDED RELEASE ORAL 6858650 July 3, 2022 TREATMENT OF OVERACTIVE BLADDER WITH SYMPTOMS OF URGE URINARY INCONTINENCE, URGENCY, AND FREQUENCY
4MG TOVIAZ PFIZER N022030 Oct. 31, 2008 RX TABLET, EXTENDED RELEASE ORAL 7807715 June 7, 2027 TREATMENT OF OVERACTIVE BLADDER WITH SYMPTOMS OF URGE URINARY INCONTINENCE, URGENCY, AND FREQUENCY
4MG TOVIAZ PFIZER N022030 Oct. 31, 2008 RX TABLET, EXTENDED RELEASE ORAL 8088398 June 7, 2027 TREATMENT OF OVERACTIVE BLADDER WITH SYMPTOMS OF URGE URINARY INCONTINENCE, URGENCY, AND FREQUENCY
8MG TOVIAZ PFIZER N022030 Oct. 31, 2008 RX TABLET, EXTENDED RELEASE ORAL 7807715 June 7, 2027 TREATMENT OF OVERACTIVE BLADDER WITH SYMPTOMS OF URGE URINARY INCONTINENCE, URGENCY, AND FREQUENCY
8MG TOVIAZ PFIZER N022030 Oct. 31, 2008 RX TABLET, EXTENDED RELEASE ORAL 8088398 June 7, 2027 TREATMENT OF OVERACTIVE BLADDER WITH SYMPTOMS OF URGE URINARY INCONTINENCE, URGENCY, AND FREQUENCY

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 Ki 6.27 WOMBAT-PK CHEMBL
Muscarinic acetylcholine receptor M2 GPCR ANTAGONIST Ki 6.40 WOMBAT-PK CHEMBL
Muscarinic acetylcholine receptor M5 GPCR Ki 5.98 WOMBAT-PK
Muscarinic acetylcholine receptor M4 GPCR Ki 6.19 WOMBAT-PK
Muscarinic acetylcholine receptor M1 GPCR Ki 6.39 WOMBAT-PK

External reference:

IDSource
4028101 VUID
N0000179802 NUI
C2343853 UMLSCUI
D07226 KEGG_DRUG
621G617227 UNII
8068 INN_ID
432254002 SNOMEDCT_US
432255001 SNOMEDCT_US
797195 RXNORM
d07162 MMSL
4028101 VANDF
012671 NDDF
286930-03-8 SECONDARY_CAS_RN
C526675 MESH_SUPPLEMENTAL_RECORD_UI
DB06702 DRUGBANK_ID
CHEBI:135920 CHEBI
CHEMBL1201764 ChEMBL_ID
CHEMBL1201765 ChEMBL_ID
6918558 PUBCHEM_CID
7473 IUPHAR_LIGAND_ID
DB15578 DRUGBANK_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Toviaz HUMAN PRESCRIPTION DRUG LABEL 1 0069-0242 TABLET, FILM COATED, EXTENDED RELEASE 4 mg ORAL NDA 18 sections
Toviaz HUMAN PRESCRIPTION DRUG LABEL 1 0069-0244 TABLET, FILM COATED, EXTENDED RELEASE 8 mg ORAL NDA 18 sections
Toviaz HUMAN PRESCRIPTION DRUG LABEL 1 54868-6156 TABLET, FILM COATED, EXTENDED RELEASE 4 mg ORAL NDA 19 sections
Toviaz HUMAN PRESCRIPTION DRUG LABEL 1 54868-6175 TABLET, FILM COATED, EXTENDED RELEASE 8 mg ORAL NDA 19 sections
Toviaz HUMAN PRESCRIPTION DRUG LABEL 1 55154-2737 TABLET, FILM COATED, EXTENDED RELEASE 4 mg ORAL NDA 18 sections
Toviaz HUMAN PRESCRIPTION DRUG LABEL 1 55154-2738 TABLET, FILM COATED, EXTENDED RELEASE 8 mg ORAL NDA 18 sections
Toviaz HUMAN PRESCRIPTION DRUG LABEL 1 63539-183 TABLET, FILM COATED, EXTENDED RELEASE 8 mg ORAL NDA 19 sections
Toviaz HUMAN PRESCRIPTION DRUG LABEL 1 63539-242 TABLET, FILM COATED, EXTENDED RELEASE 4 mg ORAL NDA 19 sections
fesoterodine fumarate HUMAN PRESCRIPTION DRUG LABEL 1 68382-479 TABLET, FILM COATED, EXTENDED RELEASE 4 mg ORAL ANDA 18 sections
fesoterodine fumarate HUMAN PRESCRIPTION DRUG LABEL 1 68382-480 TABLET, FILM COATED, EXTENDED RELEASE 8 mg ORAL ANDA 18 sections
Toviaz HUMAN PRESCRIPTION DRUG LABEL 1 69189-0242 TABLET, FILM COATED, EXTENDED RELEASE 4 mg ORAL NDA 18 sections
Toviaz HUMAN PRESCRIPTION DRUG LABEL 1 69189-0244 TABLET, FILM COATED, EXTENDED RELEASE 8 mg ORAL NDA 18 sections
fesoterodine fumarate HUMAN PRESCRIPTION DRUG LABEL 1 70771-1168 TABLET, FILM COATED, EXTENDED RELEASE 4 mg ORAL ANDA 18 sections
fesoterodine fumarate HUMAN PRESCRIPTION DRUG LABEL 1 70771-1169 TABLET, FILM COATED, EXTENDED RELEASE 8 mg ORAL ANDA 18 sections