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 206.03 35.77 76 1268 82017 56208706
Death 175.10 35.77 105 1239 341321 55949402
Cardiac failure chronic 92.17 35.77 21 1323 4046 56286677
Cardiac amyloidosis 71.77 35.77 13 1331 794 56289929
Congenital coronary artery malformation 40.76 35.77 6 1338 98 56290625
Hereditary neuropathic amyloidosis 38.58 35.77 4 1340 0 56290723
Pyelonephritis acute 35.86 35.77 10 1334 4319 56286404

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
Death 680.69 23.38 531 5050 360038 31331725
Cardiac failure 488.45 23.38 256 5325 85697 31606066
Cardiac amyloidosis 378.64 23.38 75 5506 940 31690823
Cardiac failure chronic 377.28 23.38 109 5472 7194 31684569
Off label use 99.92 23.38 200 5381 347074 31344689
Atrial fibrillation 98.10 23.38 110 5471 113673 31578090
Amyloidosis 83.40 23.38 26 5555 2210 31689553
Dyspnoea exertional 66.71 23.38 55 5526 38782 31652981
Essential hypertension 63.47 23.38 22 5559 2605 31689158
Product use in unapproved indication 61.12 23.38 81 5500 99090 31592673
Amyloidosis senile 51.02 23.38 7 5574 3 31691760
Cardiac failure congestive 47.57 23.38 64 5517 79323 31612440
Left ventricular hypertrophy 47.48 23.38 24 5557 7308 31684455
Chronic left ventricular failure 43.50 23.38 11 5570 433 31691330
N-terminal prohormone brain natriuretic peptide increased 40.36 23.38 15 5566 2169 31689594
Disease progression 37.02 23.38 61 5520 90403 31601360
Dyspnoea 36.87 23.38 138 5443 343341 31348422
Atrial flutter 32.15 23.38 24 5557 14631 31677132
Bendopnoea 30.58 23.38 4 5577 0 31691763
Carpal tunnel syndrome 30.37 23.38 15 5566 4346 31687417
Cardiac failure acute 28.44 23.38 19 5562 9722 31682041
Acquired haemophilia 26.94 23.38 9 5572 952 31690811
Hereditary neuropathic amyloidosis 26.92 23.38 4 5577 6 31691757
Drug ineffective 26.20 23.38 19 5562 395554 31296209
Hyperlipidaemia 25.45 23.38 20 5561 13140 31678623

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
Death 1000.59 27.00 608 6152 509453 70412231
Cardiac failure 687.18 27.00 313 6447 143228 70778456
Cardiac failure chronic 478.49 27.00 124 6636 10145 70911539
Cardiac amyloidosis 378.72 27.00 73 6687 1512 70920172
Atrial fibrillation 126.98 27.00 119 6641 184229 70737455
Off label use 125.90 27.00 240 6520 742820 70178864
Amyloidosis 107.51 27.00 29 6731 2750 70918934
Dyspnoea exertional 81.14 27.00 64 6696 78366 70843318
Essential hypertension 80.08 27.00 27 6733 5457 70916227
Cardiac failure congestive 66.65 27.00 73 6687 135384 70786300
Left ventricular hypertrophy 63.77 27.00 27 6733 10175 70911509
Product use in unapproved indication 63.50 27.00 88 6672 207390 70714294
Dyspnoea 54.82 27.00 179 6581 769881 70151803
Amyloidosis senile 54.65 27.00 7 6753 4 70921680
Chronic left ventricular failure 53.65 27.00 13 6747 802 70920882
Cardiac failure acute 44.41 27.00 25 6735 17462 70904222
Atrial flutter 43.50 27.00 26 6734 20301 70901383
Hereditary neuropathic amyloidosis 43.31 27.00 6 6754 11 70921673
Drug ineffective 41.48 27.00 19 6741 939733 69981951
Disease progression 37.14 27.00 59 6701 156613 70765071
N-terminal prohormone brain natriuretic peptide increased 37.10 27.00 14 6746 3910 70917774
Congenital coronary artery malformation 34.65 27.00 6 6754 66 70921618
Bendopnoea 33.45 27.00 5 6755 19 70921665
Hyperlipidaemia 32.52 27.00 23 6737 23840 70897844
Chronic kidney disease 31.90 27.00 34 6726 61023 70860661
Oedema peripheral 28.07 27.00 65 6695 228026 70693658

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