tafamidis 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
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: OFP

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

Drug dosage:

DoseUnitRoute
20 mg O

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Nov. 16, 2011 EMA
March 5, 2019 FDA FOLDRX PHARMS

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
Pyelonephritis acute 68.13 56.83 9 47 559 2357470
Endocarditis 65.50 56.83 9 47 752 2357277
Staphylococcal sepsis 62.47 56.83 9 47 1056 2356973

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 104.33 37.35 27 159 12575 1734020
Gynaecomastia 51.62 37.35 11 175 2121 1744474

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 drug

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Amyloidosis indication 17602002 DOID:9120
Transthyretin related familial amyloid cardiomyopathy indication 715655000

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

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Vyndaqel HUMAN PRESCRIPTION DRUG LABEL 1 0069-1975 CAPSULE, LIQUID FILLED 20 mg ORAL NDA 17 sections
Vyndaqel HUMAN PRESCRIPTION DRUG LABEL 1 0069-8729 CAPSULE 20 mg ORAL EXPORT ONLY 1 sections
Vyndamax HUMAN PRESCRIPTION DRUG LABEL 1 0069-8730 CAPSULE, LIQUID FILLED 61 mg ORAL NDA 17 sections