tafamidis 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 4192 | 594839-88-0 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
may be effective in treating transthyretin amyloid polyneuropathy
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 20 | mg | O |
ADMET properties:
None
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Sept. 20, 2013 | PMDA | PFIZER | |
| March 5, 2019 | FDA | FOLDRX PHARMS | |
| Nov. 16, 2011 | EMA |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients 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 term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients 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 term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients 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:
| Source | Code | Description |
|---|---|---|
| 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|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| 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 level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 3.55 | acidic |
| pKa2 | 1.19 | Basic |
Orange Book patent data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent 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 strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 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:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA 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:
| ID | Source |
|---|---|
| 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:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| 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 |