tafamidis 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
4192 594839-88-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • Fx-1006A
  • Fx-1006
  • tafamidis meglumine
  • tafamidis
  • vyndaqel
  • FX1006A
  • vynmac
may be effective in treating transthyretin amyloid polyneuropathy
  • Molecular weight: 308.11
  • Formula: C14H7Cl2NO3
  • CLOGP: 5
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 1
  • TPSA: 63.33
  • ALOGS: -3.98
  • ROTB: 2

  • Status: ONP

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

Drug dosage:

DoseUnitRoute
20 mg O

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Sept. 20, 2013 PMDA PFIZER
March 5, 2019 FDA FOLDRX PHARMS
Nov. 16, 2011 EMA

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
Cardiac failure 180.80 35.83 65 976 75975 50528108
Death 81.94 35.83 61 980 325318 50278765
Cardiac amyloidosis 68.27 35.83 12 1029 719 50603364
Cardiac failure chronic 59.70 35.83 14 1027 3549 50600534
Congenital coronary artery malformation 41.65 35.83 6 1035 98 50603985
Pyelonephritis acute 37.93 35.83 10 1031 4073 50600010

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
Cardiac failure 413.47 26.30 211 4199 79076 29491041
Death 334.73 26.30 324 4086 341760 29228357
Cardiac amyloidosis 270.14 26.30 54 4356 849 29569268
Cardiac failure chronic 240.08 26.30 72 4338 6395 29563722
Off label use 105.91 26.30 172 4238 300628 29269489
Atrial fibrillation 83.23 26.30 90 4320 105556 29464561
Product use in unapproved indication 80.96 26.30 81 4329 86794 29483323
Essential hypertension 68.55 26.30 22 4388 2431 29567686
Amyloidosis 60.23 26.30 19 4391 1985 29568132
Amyloidosis senile 54.68 26.30 7 4403 0 29570117
Cardiac failure congestive 54.60 26.30 62 4348 76519 29493598
Chronic left ventricular failure 46.71 26.30 11 4399 380 29569737
Dyspnoea exertional 45.37 26.30 40 4370 36450 29533667
Left ventricular hypertrophy 37.99 26.30 19 4391 6684 29563433
Disease progression 35.72 26.30 52 4358 81864 29488253
Dyspnoea 33.87 26.30 116 4294 326616 29243501
N-terminal prohormone brain natriuretic peptide increased 33.06 26.30 12 4398 1920 29568197
Atrial flutter 29.75 26.30 21 4389 13873 29556244
Acquired haemophilia 29.57 26.30 9 4401 834 29569283
Hyperlipidaemia 29.23 26.30 20 4390 12570 29557547
Cardiac failure acute 27.20 26.30 17 4393 9175 29560942

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
Cardiac failure 582.03 25.34 261 5107 132112 64361252
Death 477.16 25.34 359 5009 482346 64011018
Cardiac failure chronic 299.34 25.34 81 5287 8960 64484404
Cardiac amyloidosis 277.30 25.34 54 5314 1361 64492003
Off label use 129.86 25.34 206 5162 632600 63860764
Atrial fibrillation 100.15 25.34 95 5273 170994 64322370
Essential hypertension 85.13 25.34 27 5341 5167 64488197
Product use in unapproved indication 84.68 25.34 88 5280 176530 64316834
Amyloidosis 80.85 25.34 22 5346 2472 64490892
Cardiac failure congestive 67.87 25.34 68 5300 130512 64362852
Dyspnoea exertional 59.11 25.34 49 5319 73681 64419683
Chronic left ventricular failure 56.59 25.34 13 5355 731 64492633
Amyloidosis senile 56.27 25.34 7 5361 3 64493361
Dyspnoea 52.30 25.34 154 5214 718520 63774844
Left ventricular hypertrophy 51.99 25.34 22 5346 9484 64483880
Cardiac failure acute 43.44 25.34 23 5345 16321 64477043
Atrial flutter 39.78 25.34 23 5345 19357 64474007
Chronic kidney disease 37.32 25.34 34 5334 57885 64435479
Hyperlipidaemia 36.16 25.34 23 5345 22953 64470411
Congenital coronary artery malformation 35.46 25.34 6 5362 66 64493298
Disease progression 32.72 25.34 49 5319 141631 64351733
Drug ineffective 30.61 25.34 16 5352 840231 63653133
Gynaecomastia 26.63 25.34 12 5356 6004 64487360
Bendopnoea 26.58 25.34 4 5364 19 64493345
N-terminal prohormone brain natriuretic peptide increased 25.50 25.34 10 5358 3549 64489815

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N07XX08 NERVOUS SYSTEM
OTHER NERVOUS SYSTEM DRUGS
OTHER NERVOUS SYSTEM DRUGS
Other nervous system drugs
CHEBI has role CHEBI:35470 central nervous system agents

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Wild-type transthyretin cardiac amyloidosis indication 16573007
Amyloidosis indication 17602002 DOID:9120
Transthyretin related familial amyloid cardiomyopathy indication 715655000




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 3.55 acidic
pKa2 1.19 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
20MG VYNDAQEL FOLDRX PHARMS N211996 May 3, 2019 RX CAPSULE ORAL 7214696 Dec. 19, 2023 TREATMENT OF THE CARDIOMYOPATHY OF WILD TYPE OR HEREDITARY TRANSTHYRETIN-MEDIATED AMYLOIDOSIS (ATTR-CM)
61MG VYNDAMAX FOLDRX PHARMS N212161 May 3, 2019 RX CAPSULE ORAL 7214696 Dec. 19, 2023 TREATMENT OF THE CARDIOMYOPATHY OF WILD TYPE OR HEREDITARY TRANSTHYRETIN-MEDIATED AMYLOIDOSIS (ATTR-CM)
20MG VYNDAQEL FOLDRX PHARMS N211996 May 3, 2019 RX CAPSULE ORAL 8653119 Jan. 28, 2024 TREATMENT OF THE CARDIOMYOPATHY OF WILD TYPE OR HEREDITARY TRANSTHYRETIN-MEDIATED AMYLOIDOSIS (ATTR-CM)
61MG VYNDAMAX FOLDRX PHARMS N212161 May 3, 2019 RX CAPSULE ORAL 9770441 Aug. 31, 2035 TREATMENT OF THE CARDIOMYOPATHY OF WILD TYPE OR HEREDITARY TRANSTHYRETIN-MEDIATED AMYLOIDOSIS (ATTR-CM)

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
20MG VYNDAQEL FOLDRX PHARMS N211996 May 3, 2019 RX CAPSULE ORAL May 3, 2024 NEW CHEMICAL ENTITY
61MG VYNDAMAX FOLDRX PHARMS N212161 May 3, 2019 RX CAPSULE ORAL May 3, 2024 NEW CHEMICAL ENTITY
20MG VYNDAQEL FOLDRX PHARMS N211996 May 3, 2019 RX CAPSULE ORAL May 3, 2026 TREATMENT OF THE CARDIOMYOPATHY OF WILD TYPE OR HEREDITARY TRANSTHYRETIN-MEDIATED AMYLOIDOSIS (ATTR-CM) IN ADULTS TO REDUCE CARDIOVASCULAR MORTALITY AND CARDIOVASCULAR-RELATED HOSPITALIZATION
61MG VYNDAMAX FOLDRX PHARMS N212161 May 3, 2019 RX CAPSULE ORAL May 3, 2026 TREATMENT OF THE CARDIOMYOPATHY OF WILD TYPE OR HEREDITARY TRANSTHYRETIN-MEDIATED AMYLOIDOSIS (ATTR-CM) IN ADULTS TO REDUCE CARDIOVASCULAR MORTALITY AND CARDIOVASCULAR-RELATED HOSPITALIZATION

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Transthyretin Secreted BINDING AGENT Kd 6.81 DRUG LABEL DRUG LABEL
ATP-binding cassette sub-family G member 2 Transporter INHIBITOR IC50 5.94 DRUG LABEL
Solute carrier family 22 member 6 Transporter INHIBITOR IC50 5.54 DRUG LABEL
Solute carrier family 22 member 8 Transporter INHIBITOR IC50 5.63 DRUG LABEL

External reference:

IDSource
D09673 KEGG_DRUG
951395-08-7 SECONDARY_CAS_RN
4038378 VANDF
4038379 VANDF
C2745274 UMLSCUI
CHEBI:78538 CHEBI
3MI PDB_CHEM_ID
CHEMBL2103837 ChEMBL_ID
CHEMBL2105675 ChEMBL_ID
DB11644 DRUGBANK_ID
C547076 MESH_SUPPLEMENTAL_RECORD_UI
8378 IUPHAR_LIGAND_ID
9094 INN_ID
8FG9H9D31J UNII
11001318 PUBCHEM_CID
DB05352 DRUGBANK_ID
1545063 RXNORM
199417 MMSL
29344 MMSL
37371 MMSL
d08073 MMSL
015816 NDDF
015819 NDDF
703348000 SNOMEDCT_US
703349008 SNOMEDCT_US
703810000 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Vyndaqel HUMAN PRESCRIPTION DRUG LABEL 1 0069-1975 CAPSULE, LIQUID FILLED 20 mg ORAL NDA 27 sections
Vyndaqel HUMAN PRESCRIPTION DRUG LABEL 1 0069-1975 CAPSULE, LIQUID FILLED 20 mg ORAL NDA 27 sections
Vyndamax HUMAN PRESCRIPTION DRUG LABEL 1 0069-8730 CAPSULE, LIQUID FILLED 61 mg ORAL NDA 27 sections
Vyndamax HUMAN PRESCRIPTION DRUG LABEL 1 0069-8730 CAPSULE, LIQUID FILLED 61 mg ORAL NDA 27 sections