tafamidis 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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:

PropertyValueReference
S (Water solubility) 0.01 mg/mL Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Bocci G, Oprea TI, Benet LZ
fu (Fraction unbound in plasma) 0.00 % Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR1B,ACVR2A,ACVR2B,ACVRL1,ALK,AURKA,AURKC,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK1,CDK5,CDK9,CSF1R,DDR1,DYRK1B,EGFR,EIF2AK3,ERBB2,FLT3,GRK2,GRK3,GSK3B,IKBKB,ITK,JAK1,JAK2,KDR,KIT,MAP2K6,MAP3K10,MAP3K14,MAP3K21,MAP3K7,MAP4K1,MAP4K3,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MARK4,MTOR,NTRK1,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CA,PIK3CB,PIK3CD,PIK3CG,PIM1,PIM2,PIM3,PRKAA1,PRKCD,PRKDC,SGK1,SIK2,SIK3,STK10,STK33,SYK,TEK,TGFBR1,TTK,UHMK1,ULK1,ULK2,ZAP70 74
kinase-selectivity-class ACVR2A,ACVR2B,AXL,BRAF,CDK9,DYRK1B,EIF2AK3,ERBB2,GRK2,MAPK7,PDK4,PRKDC,SIK2,STK33,TTK 15
pfas-class PFAS structural alert (1 = True, 0 = False) 0

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
Death 495.21 27.38 258 2791 456293 90169105
Cardiac failure 311.02 27.38 122 2927 109374 90516024
Cardiac failure chronic 127.29 27.38 31 3018 5615 90619783
Cardiac amyloidosis 82.14 27.38 16 3033 1020 90624378
Polyneuropathy 66.96 27.38 25 3024 19316 90606082
Congenital coronary artery malformation 65.36 27.38 10 3039 149 90625249
Atrial fibrillation 61.13 27.38 44 3005 133567 90491831
Dyspnoea 53.32 27.38 101 2948 880854 89744544
Sinus arrhythmia 43.30 27.38 10 3039 1439 90623959
Arterial thrombosis 42.32 27.38 10 3039 1590 90623808
Pancreatic steatosis 42.06 27.38 10 3039 1632 90623766
Cardiac failure congestive 39.47 27.38 30 3019 98664 90526734
Drug interaction 35.46 27.38 45 3004 276408 90348990
Acute kidney injury 30.28 27.38 45 3004 320342 90305056
Pyelonephritis acute 30.22 27.38 10 3039 5422 90619976
Rhabdomyolysis 28.37 27.38 19 3030 51237 90574161
Respiratory distress 27.92 27.38 17 3032 38929 90586469

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 1907.09 23.35 1358 11520 469827 42138630
Cardiac failure 1020.74 23.35 539 12339 106317 42502140
Cardiac failure chronic 680.94 23.35 207 12671 9394 42599063
Cardiac amyloidosis 301.76 23.35 78 12800 1927 42606530
Atrial fibrillation 290.59 23.35 278 12600 139315 42469142
Left ventricular hypertrophy 120.40 23.35 58 12820 9261 42599196
Cardiac failure congestive 102.96 23.35 128 12750 85474 42522983
Dyspnoea exertional 102.25 23.35 99 12779 50049 42558408
Dyspnoea 89.89 23.35 315 12563 442306 42166151
Amyloidosis 89.70 23.35 32 12846 2387 42606070
N-terminal prohormone brain natriuretic peptide increased 89.04 23.35 35 12843 3418 42605039
Carpal tunnel syndrome 70.10 23.35 34 12844 5505 42602952
Fluid retention 69.31 23.35 65 12813 31554 42576903
Drug ineffective 67.83 23.35 55 12823 630142 41978315
Chronic left ventricular failure 65.09 23.35 19 12859 743 42607714
Amyloidosis senile 64.88 23.35 13 12865 95 42608362
Atrial flutter 59.45 23.35 46 12832 17205 42591252
Disease progression 57.41 23.35 131 12747 143525 42464932
Pyrexia 52.33 23.35 27 12851 394015 42214442
Oedema peripheral 50.97 23.35 121 12757 135955 42472502
Cardiac disorder 50.66 23.35 68 12810 48864 42559593
Essential hypertension 50.32 23.35 24 12854 3744 42604713
Tricuspid valve incompetence 48.11 23.35 34 12844 11079 42597378
Dysphagia 48.10 23.35 82 12796 72637 42535820
Fatigue 47.20 23.35 257 12621 435384 42173073
Cardiac failure acute 46.20 23.35 36 12842 13597 42594860
Condition aggravated 44.62 23.35 176 12702 260578 42347879
Cardiac pacemaker insertion 44.33 23.35 21 12857 3227 42605230
Toxicity to various agents 44.12 23.35 8 12870 229128 42379329
Dizziness postural 43.70 23.35 28 12850 7767 42600690
Neutropenia 42.93 23.35 5 12873 199426 42409031
Mitral valve incompetence 42.21 23.35 37 12841 16452 42592005
Brain natriuretic peptide increased 42.17 23.35 26 12852 6744 42601713
Diastolic dysfunction 41.43 23.35 26 12852 6957 42601500
Peripheral swelling 39.02 23.35 85 12793 90185 42518272
Dementia 36.33 23.35 34 12844 16446 42592011
Hereditary neuropathic amyloidosis 35.53 23.35 5 12873 0 42608457
Ejection fraction decreased 34.81 23.35 38 12840 22049 42586408
Left atrial dilatation 34.23 23.35 16 12862 2386 42606071
Spinal stenosis 33.43 23.35 22 12856 6384 42602073
Fall 32.84 23.35 149 12729 234371 42374086
Glomerular filtration rate decreased 32.75 23.35 32 12846 16319 42592138
Cerebrovascular accident 32.73 23.35 83 12795 97077 42511380
Thrombocytopenia 31.89 23.35 9 12869 190270 42418187
Bendopnoea 30.38 23.35 5 12873 9 42608448
Therapeutic response unexpected 30.06 23.35 26 12852 11355 42597102
Right ventricular hypertrophy 27.38 23.35 12 12866 1540 42606917
Left ventricular dysfunction 25.87 23.35 24 12854 11477 42596980
Right ventricular dysfunction 25.20 23.35 11 12867 1398 42607059
Pancytopenia 25.20 23.35 3 12875 117740 42490717
Heart rate irregular 24.23 23.35 27 12851 16023 42592434
Hypoacusis 24.10 23.35 29 12849 18673 42589784
Atrioventricular block 23.46 23.35 21 12857 9594 42598863
Sudden death 23.44 23.35 27 12851 16602 42591855

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 2893.76 23.30 1537 13642 697332 109876788
Cardiac failure 1329.00 23.30 601 14578 187025 110387095
Cardiac failure chronic 858.06 23.30 226 14953 13585 110560535
Atrial fibrillation 405.33 23.30 298 14881 229344 110344776
Cardiac amyloidosis 304.39 23.30 72 15107 2765 110571355
Cardiac failure congestive 154.42 23.30 143 15036 150857 110423263
Left ventricular hypertrophy 151.73 23.30 60 15119 13184 110560936
Dyspnoea exertional 133.26 23.30 112 15067 103948 110470172
Dyspnoea 126.74 23.30 385 14794 1106487 109467633
Amyloidosis 110.20 23.30 33 15146 3148 110570972
N-terminal prohormone brain natriuretic peptide increased 100.16 23.30 36 15143 6085 110568035
Atrial flutter 88.85 23.30 50 15129 24212 110549908
Disease progression 87.01 23.30 135 15044 243899 110330221
Chronic left ventricular failure 74.64 23.30 20 15159 1276 110572844
Drug ineffective 72.17 23.30 62 15117 1520478 109053642
Essential hypertension 70.91 23.30 30 15149 7817 110566303
Cardiac failure acute 70.69 23.30 43 15136 24035 110550085
Carpal tunnel syndrome 67.98 23.30 41 15138 22569 110551551
Oedema peripheral 67.41 23.30 143 15036 328517 110245603
Cardiac disorder 66.09 23.30 66 15113 76214 110497906
Dizziness postural 64.28 23.30 34 15145 14575 110559545
Fluid retention 62.90 23.30 71 15108 94236 110479884
Tricuspid valve incompetence 60.91 23.30 39 15140 23834 110550286
Dysphagia 58.97 23.30 88 15091 153512 110420608
Diastolic dysfunction 57.80 23.30 30 15149 12374 110561746
Brain natriuretic peptide increased 57.72 23.30 29 15150 11180 110562940
Amyloidosis senile 54.98 23.30 10 15169 100 110574020
Congenital coronary artery malformation 53.54 23.30 10 15169 117 110574003
Cardiac pacemaker insertion 53.34 23.30 23 15156 6278 110567842
Fatigue 47.66 23.30 307 14872 1215651 109358469
Glomerular filtration rate decreased 47.34 23.30 36 15143 28920 110545200
Mitral valve incompetence 47.06 23.30 38 15141 33291 110540829
Dementia 46.61 23.30 37 15142 31636 110542484
Therapeutic response unexpected 44.27 23.30 32 15147 23811 110550309
Left atrial dilatation 43.84 23.30 17 15162 3543 110570577
Toxicity to various agents 43.37 23.30 7 15172 480548 110093572
Ejection fraction decreased 42.26 23.30 39 15140 40841 110533279
Polyneuropathy 42.06 23.30 35 15144 31977 110542143
Fall 41.30 23.30 178 15001 603304 109970816
Hereditary neuropathic amyloidosis 40.77 23.30 6 15173 12 110574108
Chronic kidney disease 40.27 23.30 51 15128 76240 110497880
Atrioventricular block complete 39.69 23.30 28 15151 20054 110554066
Condition aggravated 38.80 23.30 201 14978 734635 109839485
Rhabdomyolysis 37.91 23.30 63 15116 120338 110453782
Hypoacusis 37.21 23.30 34 15145 35157 110538963
Sudden death 36.98 23.30 29 15150 24366 110549754
Cerebrovascular accident 36.10 23.30 78 15101 181206 110392914
Right ventricular hypertrophy 35.39 23.30 12 15167 1707 110572413
Neutropenia 34.84 23.30 5 15174 374615 110199505
Gynaecomastia 33.24 23.30 19 15160 9471 110564649
Off label use 33.04 23.30 332 14847 1499853 109074267
Product use complaint 32.58 23.30 14 15165 3789 110570331
Bendopnoea 31.91 23.30 6 15173 73 110574047
Headache 31.75 23.30 45 15134 882332 109691788
Left ventricular dysfunction 31.51 23.30 26 15153 23467 110550653
Right ventricular dysfunction 31.01 23.30 13 15166 3310 110570810
Gout 30.49 23.30 31 15148 36535 110537585
Pyrexia 30.20 23.30 48 15131 898217 109675903
Pain 29.38 23.30 54 15125 954901 109619219
Pleural effusion 29.32 23.30 71 15108 177638 110396482
Neuropathy peripheral 28.91 23.30 71 15108 179206 110394914
Orthopnoea 28.10 23.30 18 15161 11003 110563117
Cerebral infarction 27.90 23.30 35 15144 51803 110522317
Rheumatoid arthritis 27.85 23.30 4 15175 299609 110274511
Atrioventricular block 27.62 23.30 21 15158 16856 110557264
Atrial enlargement 27.54 23.30 9 15170 1142 110572978
Drug hypersensitivity 27.50 23.30 14 15165 454076 110120044
Spinal stenosis 27.48 23.30 22 15157 19034 110555086
Alopecia 27.45 23.30 8 15171 364745 110209375
Hyperlipidaemia 27.38 23.30 29 15150 35819 110538301
Nasopharyngitis 27.31 23.30 10 15169 394351 110179769
Pancreatic steatosis 27.14 23.30 10 15169 1812 110572308
Drug intolerance 27 23.30 11 15168 406501 110167619
Heart rate irregular 26.67 23.30 28 15151 34246 110539874
Cardiorenal syndrome 26.64 23.30 10 15169 1908 110572212
Nausea 26.12 23.30 85 15094 1235605 109338515
Cardiac dysfunction 26.01 23.30 14 15165 6209 110567911
Sinus arrhythmia 25.44 23.30 10 15169 2160 110571960
Ventricular hypokinesia 25.38 23.30 17 15162 11197 110562923
Dizziness 25.22 23.30 173 15006 698020 109876100
Aortic dilatation 25.11 23.30 10 15169 2236 110571884
Vomiting 25.01 23.30 55 15124 910620 109663500
Renal impairment 24.63 23.30 69 15110 188376 110385744
Cardiac resynchronisation therapy 24.61 23.30 5 15174 93 110574027
Heart transplant 24.49 23.30 9 15170 1619 110572501
Hypervolaemia 24.43 23.30 32 15147 49428 110524692
Foreign body in throat 24.18 23.30 8 15171 1055 110573065
Body height decreased 23.88 23.30 16 15163 10547 110563573
Exeresis 23.68 23.30 3 15176 0 110574120
Sinus node dysfunction 23.62 23.30 15 15164 9032 110565088
Therapeutic product effect decreased 23.32 23.30 3 15176 244313 110329807

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 drug

Related Drugs by ATC class:

N07XX Other nervous system drugs 23 drugs
amifampridinearimoclomoldeutetrabenazinedextromethorphanedaravoneeplontersenfampridineinotersen laquinimodlevacetylleucineomaveloxolonepatisiran show all 23 →

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
Amyloid polyneuropathy type I indication 398229007
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 DISCN CAPSULE ORAL 7214696 Dec. 19, 2026 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, 2026 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 DISCN 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
8FG9H9D31J INXIGHT DRUGS

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