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 247.25 17.74 128 6436 56050 50542510
Urinary retention 232.19 17.74 97 6467 26093 50572467
Brain injury 99.00 17.74 35 6529 5979 50592581
Fall 94.41 17.74 161 6403 334771 50263789
Multiple fractures 81.15 17.74 31 6533 6580 50591980
Pulseless electrical activity 69.59 17.74 28 6536 6813 50591747
Urinary incontinence 64.27 17.74 42 6522 28166 50570394
Electrocardiogram QRS complex prolonged 51.36 17.74 21 6543 5323 50593237
Dysuria 49.71 17.74 36 6528 28468 50570092
Gait disturbance 43.20 17.74 73 6491 149932 50448628
Constipation 41.57 17.74 81 6483 185627 50412933
Bradycardia 35.89 17.74 43 6521 64383 50534177
Therapeutic product effect incomplete 28.27 17.74 46 6518 91469 50507091
Nocturia 25.74 17.74 14 6550 6716 50591844
Dry throat 25.27 17.74 13 6551 5571 50592989
Loss of consciousness 25.13 17.74 47 6517 104306 50494254
Micturition urgency 23.06 17.74 14 6550 8250 50590310
Product blister packaging issue 22.48 17.74 5 6559 154 50598406
Bladder spasm 22.30 17.74 8 6556 1422 50597138
Overdose 21.66 17.74 43 6521 99684 50498876
Feeling abnormal 21.36 17.74 49 6515 125443 50473117
Pollakiuria 20.44 17.74 20 6544 23831 50574729
Balance disorder 19.81 17.74 34 6530 70556 50528004
Multiple sclerosis relapse 19.65 17.74 26 6538 42938 50555622
Vision blurred 19.65 17.74 36 6528 78611 50519949

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 429.10 22.15 144 2470 31754 29540159
Dry mouth 121.81 22.15 52 2562 21732 29550181
Dysuria 56.37 22.15 31 2583 22409 29549504
Fall 49.54 22.15 69 2545 177109 29394804
Dementia 37.47 22.15 19 2595 11639 29560274
Benign prostatic hyperplasia 34.50 22.15 18 2596 11692 29560221
Cystitis interstitial 30.32 22.15 6 2608 154 29571759
Constipation 29.63 22.15 43 2571 114117 29457796
Urine flow decreased 23.02 22.15 7 2607 1097 29570816

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 293.45 16.89 134 7481 49067 64442050
Dry mouth 226.70 16.89 120 7495 60298 64430819
Fall 129.74 16.89 199 7416 416627 64074490
Multiple fractures 86.71 16.89 31 7584 6009 64485108
Brain injury 85 16.89 35 7580 9930 64481187
Dysuria 61.48 16.89 46 7569 42011 64449106
Pulseless electrical activity 61.35 16.89 30 7585 12709 64478408
Urinary incontinence 51.63 16.89 39 7576 36112 64455005
Gait disturbance 46.10 16.89 77 7538 172078 64319039
Electrocardiogram QRS complex prolonged 42.22 16.89 21 7594 9223 64481894
Therapeutic product effect incomplete 35.64 16.89 52 7563 103430 64387687
Constipation 32.85 16.89 79 7536 229258 64261859
Cystitis interstitial 29.03 16.89 9 7606 1123 64489994
Benign prostatic hyperplasia 28.20 16.89 16 7599 9149 64481968
Dementia 26.58 16.89 21 7594 20745 64470372
Nocturia 25.27 16.89 16 7599 11149 64479968
Urinary tract infection 25.19 16.89 72 7543 231524 64259593
Loss of consciousness 24.40 16.89 54 7561 148311 64342806
Micturition urgency 23.84 16.89 15 7600 10344 64480773
Product blister packaging issue 23.04 16.89 5 7610 151 64490966
Body height decreased 22.73 16.89 13 7602 7541 64483576
Bradycardia 21.70 16.89 45 7570 118174 64372943
Urine flow decreased 21.58 16.89 7 7608 1010 64490107
Balance disorder 20.40 16.89 36 7579 83890 64407227
Dizziness 20.09 16.89 102 7513 430061 64061056
Cystitis 18.53 16.89 24 7591 42651 64448466
Drug ineffective 18.44 16.89 165 7450 840082 63651035
Colitis ischaemic 18.10 16.89 14 7601 13400 64477717
Mental impairment 17.70 16.89 15 7600 16328 64474789
Intentional product misuse 17.55 16.89 31 7584 72264 64418853
Fine motor delay 17.39 16.89 4 7611 158 64490959
Bladder disorder 17.25 16.89 11 7604 7756 64483361
Product prescribing error 17.16 16.89 21 7594 35248 64455869
Bladder spasm 17.06 16.89 7 7608 1965 64489152
Toxicity to various agents 17.01 16.89 11 7604 363502 64127615

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 (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
207679-81-0 SECONDARY_CAS_RN
621G617227 UNII
6918558 PUBCHEM_CID
9819382 PUBCHEM_CID
DB15578 DRUGBANK_ID
797195 RXNORM
137285 MMSL
25992 MMSL
d07162 MMSL
012671 NDDF
012672 NDDF
432254002 SNOMEDCT_US
432255001 SNOMEDCT_US
441469003 SNOMEDCT_US
C4301611 UMLSCUI
CHEMBL3348932 ChEMBL_ID
10020 INN_ID
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 0069-0244 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 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 68382-480 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 70771-1169 TABLET, FILM COATED, EXTENDED RELEASE 8 mg ORAL ANDA 1 sections