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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
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

Molecule

Description

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:

Dose	Unit	Route
20	mg	O

ADMET properties:

None

Approvals:

Date	Agency	Company
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	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 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
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 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
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:

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])	Bioact source	MoA source
Transthyretin	Secreted	P02766	TTHY_HUMAN	BINDING AGENT	Kd	6.81	DRUG LABEL	DRUG LABEL
ATP-binding cassette sub-family G member 2	Transporter	Q9UNQ0	ABCG2_HUMAN	INHIBITOR	IC50	5.94	DRUG LABEL
Solute carrier family 22 member 6	Transporter	Q4U2R8	S22A6_HUMAN	INHIBITOR	IC50	5.54	DRUG LABEL
Solute carrier family 22 member 8	Transporter	Q8TCC7	S22A8_HUMAN	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