fesoterodine ๐Ÿถ Veterinary Use | 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 ยตM/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
Dry mouth 244.88 17.14 131 6852 64074 56221010
Urinary retention 239.89 17.14 100 6883 27974 56257110
Brain injury 98.63 17.14 35 6948 6320 56278764
Fall 98.53 17.14 166 6817 357344 55927740
Urinary incontinence 87.04 17.14 51 6932 29534 56255550
Multiple fractures 79.33 17.14 31 6952 7310 56277774
Pulseless electrical activity 70.08 17.14 28 6955 6996 56278088
Hypertonic bladder 58.62 17.14 20 6963 3212 56281872
Electrocardiogram QRS complex prolonged 55.26 17.14 22 6961 5445 56279639
Dysuria 50.98 17.14 37 6946 30692 56254392
Gait disturbance 44.96 17.14 76 6907 163245 56121839
Constipation 41.72 17.14 83 6900 201860 56083224
Bradycardia 35.81 17.14 43 6940 67461 56217623
Nocturia 34.21 17.14 17 6966 7089 56277995
Micturition urgency 33.60 17.14 18 6965 8763 56276321
Pollakiuria 30.14 17.14 25 6958 25177 56259907
Dry throat 27.68 17.14 14 6969 6060 56279024
Rheumatoid arthritis 27.18 17.14 7 6976 382597 55902487
Loss of consciousness 26.31 17.14 48 6935 109301 56175783
Therapeutic product effect incomplete 26.09 17.14 47 6936 105984 56179100
Bladder spasm 25.76 17.14 9 6974 1550 56283534
Feeling abnormal 22.98 17.14 51 6932 133551 56151533
Overdose 22.41 17.14 44 6939 105786 56179298
Product blister packaging issue 22.19 17.14 5 6978 171 56284913
Vision blurred 20.69 17.14 37 6946 82906 56202178
Multiple sclerosis relapse 19.66 17.14 26 6957 44877 56240207
Balance disorder 18.92 17.14 34 6949 76486 56208598
Dry eye 17.71 17.14 22 6961 35694 56249390
Body height decreased 17.40 17.14 12 6971 9173 56275911

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 440.83 22.00 148 2578 33577 31661041
Dry mouth 117.36 22.00 52 2674 24406 31670212
Dysuria 57.58 22.00 32 2694 24262 31670356
Fall 51.35 22.00 71 2655 186018 31508600
Hypertonic bladder 49.81 22.00 14 2712 1716 31692902
Dementia 36.91 22.00 19 2707 12341 31682277
Benign prostatic hyperplasia 33.03 22.00 18 2708 13107 31681511
Cystitis interstitial 30.09 22.00 6 2720 165 31694453
Constipation 27.82 22.00 43 2683 123948 31570670
Pollakiuria 25.41 22.00 17 2709 17885 31676733
Product substitution issue 23.90 22.00 13 2713 9419 31685199
Urine flow decreased 23.03 22.00 7 2719 1126 31693492

FDA Adverse Event Reporting System (Geriatric)

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 305.19 16.41 139 7949 52381 70867975
Dry mouth 218.72 16.41 122 7966 70335 70850021
Fall 133.78 16.41 205 7883 443891 70476465
Hypertonic bladder 93.52 16.41 29 8059 3754 70916602
Multiple fractures 84.33 16.41 31 8057 6734 70913622
Brain injury 84.03 16.41 35 8053 10582 70909774
Urinary incontinence 67.28 16.41 46 8042 37796 70882560
Pulseless electrical activity 61.29 16.41 30 8058 13185 70907171
Dysuria 59.41 16.41 46 8042 45748 70874608
Gait disturbance 49.26 16.41 81 8007 185025 70735331
Electrocardiogram QRS complex prolonged 41.73 16.41 21 8067 9785 70910571
Micturition urgency 33.41 16.41 19 8069 11295 70909061
Constipation 31.76 16.41 81 8007 252357 70667999
Therapeutic product effect incomplete 31.24 16.41 52 8036 119830 70800526
Urinary tract infection 30.44 16.41 79 8009 248690 70671666
Nocturia 29.49 16.41 18 8070 12186 70908170
Cystitis interstitial 28.75 16.41 9 8079 1200 70919156
Dementia 27.98 16.41 22 8066 22343 70898013
Benign prostatic hyperplasia 26.77 16.41 16 8072 10427 70909929
Loss of consciousness 25.03 16.41 55 8033 155661 70764695
Body height decreased 22.79 16.41 13 8075 7770 70912586
Product blister packaging issue 22.42 16.41 5 8083 178 70920178
Bradycardia 22.31 16.41 46 8042 124569 70795787
Pollakiuria 22.16 16.41 23 8065 33438 70886918
Urine flow decreased 21.58 16.41 7 8081 1047 70919309
Cystitis 20.47 16.41 26 8062 46915 70873441
Bladder spasm 20.27 16.41 8 8080 2105 70918251
Bladder disorder 19.45 16.41 12 8076 8277 70912079
Balance disorder 19.45 16.41 36 8052 90092 70830264
Dizziness 19.34 16.41 104 7984 464037 70456319
Product prescribing error 19.29 16.41 23 8065 38929 70881427
Drug ineffective 18.78 16.41 176 7912 939576 69980780
Colitis ischaemic 17.88 16.41 14 8074 14123 70906233
Mental impairment 17.45 16.41 15 8073 17240 70903116
Fine motor delay 16.90 16.41 4 8084 186 70920170
Completed suicide 16.47 16.41 3 8085 227132 70693224

FDA Adverse Event Reporting System (Pediatric)

None

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 | Suggest Off label Use Form| |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




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

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)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
4MG TOVIAZ PFIZER N022030 Oct. 31, 2008 RX TABLET, EXTENDED RELEASE ORAL June 17, 2024 TREATMENT OF NEUROGENIC DETRUSOR OVERACTIVITY (NDO) IN PEDIATRIC PATIENTS 6 YEARS OF AGE AND OLDER AND WEIGHING GREATER THAN 25 KG
8MG TOVIAZ PFIZER N022030 Oct. 31, 2008 RX TABLET, EXTENDED RELEASE ORAL June 17, 2024 TREATMENT OF NEUROGENIC DETRUSOR OVERACTIVITY (NDO) IN PEDIATRIC PATIENTS 6 YEARS OF AGE AND OLDER AND WEIGHING GREATER THAN 25 KG
4MG TOVIAZ PFIZER N022030 Oct. 31, 2008 RX TABLET, EXTENDED RELEASE ORAL Dec. 17, 2024 PEDIATRIC EXCLUSIVITY
8MG TOVIAZ PFIZER N022030 Oct. 31, 2008 RX TABLET, EXTENDED RELEASE ORAL Dec. 17, 2024 PEDIATRIC EXCLUSIVITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Muscarinic acetylcholine receptor M2 GPCR ANTAGONIST Ki 6.40 WOMBAT-PK CHEMBL
Muscarinic acetylcholine receptor M3 GPCR ANTAGONIST Ki 6.27 WOMBAT-PK CHEMBL
Muscarinic acetylcholine receptor M1 GPCR Ki 6.39 WOMBAT-PK
Muscarinic acetylcholine receptor M4 GPCR Ki 6.19 WOMBAT-PK
Muscarinic acetylcholine receptor M5 GPCR Ki 5.98 WOMBAT-PK

External reference:

IDSource
4028101 VUID
N0000179802 NUI
D07226 KEGG_DRUG
286930-03-8 SECONDARY_CAS_RN
4028101 VANDF
4028102 VANDF
C2343853 UMLSCUI
CHEBI:135920 CHEBI
CHEMBL1201764 ChEMBL_ID
CHEMBL1201765 ChEMBL_ID
DB06702 DRUGBANK_ID
C526675 MESH_SUPPLEMENTAL_RECORD_UI
7473 IUPHAR_LIGAND_ID
8068 INN_ID
621G617227 UNII
6918558 PUBCHEM_CID
DB15578 DRUGBANK_ID
797195 RXNORM
137285 MMSL
25992 MMSL
358891 MMSL
d07162 MMSL
012671 NDDF
012672 NDDF
432254002 SNOMEDCT_US
432255001 SNOMEDCT_US
441469003 SNOMEDCT_US
C4301611 UMLSCUI
CHEMBL3348932 ChEMBL_ID
10020 INN_ID
207679-81-0 SECONDARY_CAS_RN
9819382 PUBCHEM_CID
YU871O78GR UNII

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Toviaz HUMAN PRESCRIPTION DRUG LABEL 1 0069-0242 TABLET, FILM COATED, EXTENDED RELEASE 4 mg ORAL NDA 32 sections
Toviaz HUMAN PRESCRIPTION DRUG LABEL 1 0069-0242 TABLET, FILM COATED, EXTENDED RELEASE 4 mg ORAL NDA 32 sections
Toviaz HUMAN PRESCRIPTION DRUG LABEL 1 0069-0242 TABLET, FILM COATED, EXTENDED RELEASE 4 mg ORAL NDA 32 sections
Toviaz HUMAN PRESCRIPTION DRUG LABEL 1 0069-0244 TABLET, FILM COATED, EXTENDED RELEASE 8 mg ORAL NDA 32 sections
Toviaz HUMAN PRESCRIPTION DRUG LABEL 1 0069-0244 TABLET, FILM COATED, EXTENDED RELEASE 8 mg ORAL NDA 32 sections
Toviaz HUMAN PRESCRIPTION DRUG LABEL 1 0069-0244 TABLET, FILM COATED, EXTENDED RELEASE 8 mg ORAL NDA 32 sections
Fesoterodine fumarate HUMAN PRESCRIPTION DRUG LABEL 1 43598-247 TABLET, EXTENDED RELEASE 4 mg ORAL ANDA 26 sections
Fesoterodine fumarate HUMAN PRESCRIPTION DRUG LABEL 1 43598-248 TABLET, EXTENDED RELEASE 8 mg ORAL ANDA 26 sections
Fesoterodine fumarate HUMAN PRESCRIPTION DRUG LABEL 1 51407-661 TABLET, EXTENDED RELEASE 4 mg ORAL ANDA 26 sections
Fesoterodine fumarate HUMAN PRESCRIPTION DRUG LABEL 1 51407-662 TABLET, EXTENDED RELEASE 8 mg ORAL ANDA 26 sections
Toviaz HUMAN PRESCRIPTION DRUG LABEL 1 54868-6156 TABLET, FILM COATED, EXTENDED RELEASE 4 mg ORAL NDA 29 sections
Toviaz HUMAN PRESCRIPTION DRUG LABEL 1 54868-6175 TABLET, FILM COATED, EXTENDED RELEASE 8 mg ORAL NDA 29 sections
Toviaz HUMAN PRESCRIPTION DRUG LABEL 1 63539-183 TABLET, FILM COATED, EXTENDED RELEASE 8 mg ORAL NDA 32 sections
Toviaz HUMAN PRESCRIPTION DRUG LABEL 1 63539-183 TABLET, FILM COATED, EXTENDED RELEASE 8 mg ORAL NDA 32 sections
Toviaz HUMAN PRESCRIPTION DRUG LABEL 1 63539-242 TABLET, FILM COATED, EXTENDED RELEASE 4 mg ORAL NDA 32 sections
Toviaz HUMAN PRESCRIPTION DRUG LABEL 1 63539-242 TABLET, FILM COATED, EXTENDED RELEASE 4 mg ORAL NDA 32 sections
FESOTERODINE FUMARATE Human Prescription Drug Label 1 65862-766 TABLET, FILM COATED, EXTENDED RELEASE 4 mg ORAL ANDA 27 sections
FESOTERODINE FUMARATE Human Prescription Drug Label 1 65862-767 TABLET, FILM COATED, EXTENDED RELEASE 8 mg ORAL ANDA 27 sections
Fesoterodine Fumarate Human Prescription Drug Label 1 67877-064 TABLET, EXTENDED RELEASE 4 mg ORAL ANDA 26 sections
Fesoterodine Fumarate Human Prescription Drug Label 1 67877-068 TABLET, EXTENDED RELEASE 8 mg ORAL ANDA 26 sections
fesoterodine fumarate HUMAN PRESCRIPTION DRUG LABEL 1 68382-479 TABLET, FILM COATED, EXTENDED RELEASE 4 mg ORAL ANDA 26 sections
fesoterodine fumarate HUMAN PRESCRIPTION DRUG LABEL 1 68382-479 TABLET, FILM COATED, EXTENDED RELEASE 4 mg ORAL ANDA 26 sections
fesoterodine fumarate HUMAN PRESCRIPTION DRUG LABEL 1 68382-479 TABLET, FILM COATED, EXTENDED RELEASE 4 mg ORAL ANDA 26 sections
fesoterodine fumarate HUMAN PRESCRIPTION DRUG LABEL 1 68382-480 TABLET, FILM COATED, EXTENDED RELEASE 8 mg ORAL ANDA 26 sections
fesoterodine fumarate HUMAN PRESCRIPTION DRUG LABEL 1 68382-480 TABLET, FILM COATED, EXTENDED RELEASE 8 mg ORAL ANDA 26 sections
fesoterodine fumarate HUMAN PRESCRIPTION DRUG LABEL 1 68382-480 TABLET, FILM COATED, EXTENDED RELEASE 8 mg ORAL ANDA 26 sections
Toviaz HUMAN PRESCRIPTION DRUG LABEL 1 69189-0242 TABLET, FILM COATED, EXTENDED RELEASE 4 mg ORAL NDA 28 sections
Toviaz HUMAN PRESCRIPTION DRUG LABEL 1 69189-0244 TABLET, FILM COATED, EXTENDED RELEASE 8 mg ORAL NDA 28 sections
fesoterodine fumarate HUMAN PRESCRIPTION DRUG LABEL 1 70771-1168 TABLET, FILM COATED, EXTENDED RELEASE 4 mg ORAL ANDA 1 sections
fesoterodine fumarate HUMAN PRESCRIPTION DRUG LABEL 1 70771-1168 TABLET, FILM COATED, EXTENDED RELEASE 4 mg ORAL ANDA 1 sections