tafamidis 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 |
|---|---|---|---|
| Nov. 16, 2011 | EMA | ||
| March 5, 2019 | FDA | FOLDRX PHARMS |
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 |
|---|---|---|---|---|---|---|
| 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 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 | 104.33 | 37.35 | 27 | 159 | 12575 | 1734020 |
| Gynaecomastia | 51.62 | 37.35 | 11 | 175 | 2121 | 1744474 |
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 drug |
Drug Use (View source of the data)
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Amyloidosis | indication | 17602002 | DOID:9120 |
| Transthyretin related familial amyloid cardiomyopathy | indication | 715655000 |
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 |
|---|---|
| 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:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| 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 |