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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:

Property	Value	Reference
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

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	232.00	31.70	86	1513	89056	63398367
Death	225.21	31.70	130	1469	374251	63113172
Cardiac failure chronic	89.30	31.70	21	1578	4397	63483026
Congenital coronary artery malformation	68.98	31.70	10	1589	138	63487285
Cardiac amyloidosis	64.42	31.70	12	1587	810	63486613
Pancreatic steatosis	49.74	31.70	10	1589	1006	63486417
Arterial thrombosis	46.24	31.70	10	1589	1433	63485990
Sinus arrhythmia	46.04	31.70	10	1589	1463	63485960
Polyneuropathy	44.83	31.70	16	1583	14573	63472850
Off label use	37.24	31.70	63	1536	674399	62813024
Pyelonephritis acute	34.64	31.70	10	1589	4631	63482792

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	856.55	23.16	660	6153	397389	34552729
Cardiac failure	565.64	23.16	298	6515	90950	34859168
Cardiac failure chronic	405.60	23.16	120	6693	7759	34942359
Cardiac amyloidosis	259.85	23.16	58	6755	1193	34948925
Atrial fibrillation	125.52	23.16	136	6677	122257	34827861
Off label use	102.07	23.16	240	6573	419284	34530834
Amyloidosis	65.87	23.16	22	6791	2101	34948017
Dyspnoea exertional	62.44	23.16	58	6755	43221	34906897
Essential hypertension	61.73	23.16	23	6790	3025	34947093
Cardiac failure congestive	60.96	23.16	78	6735	83192	34866926
Left ventricular hypertrophy	54.05	23.16	28	6785	8102	34942016
Chronic left ventricular failure	48.66	23.16	13	6800	574	34949544
Product use in unapproved indication	45.76	23.16	82	6731	117417	34832701
Dyspnoea	42.64	23.16	165	6648	376617	34573501
N-terminal prohormone brain natriuretic peptide increased	42.53	23.16	17	6796	2698	34947420
Disease progression	40.25	23.16	74	6739	108003	34842115
Amyloidosis senile	39.48	23.16	7	6806	40	34950078
Atrial flutter	37.29	23.16	28	6785	15546	34934572
Cardiac failure acute	34.59	23.16	23	6790	10547	34939571
Therapeutic response unexpected	31.37	23.16	21	6792	9736	34940382
Fluid retention	31.19	23.16	32	6781	26855	34923263
Carpal tunnel syndrome	30.61	23.16	16	6797	4710	34945408
Dysphagia	30.17	23.16	48	6765	62333	34887785
Toxicity to various agents	28.45	23.16	3	6810	200359	34749759
Bendopnoea	27.94	23.16	4	6809	3	34950115
Drug ineffective	26.65	23.16	30	6783	456721	34493397
Hyperlipidaemia	25.96	23.16	22	6791	14507	34935611
Hypoacusis	25.74	23.16	23	6790	16278	34933840
Acquired haemophilia	25.61	23.16	9	6804	1001	34949117
Drug interaction	24.26	23.16	7	6806	225939	34724179

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	1260.49	24.96	750	7388	565764	79170486
Cardiac failure	788.55	24.96	360	7778	154482	79581768
Cardiac failure chronic	497.85	24.96	132	8006	11003	79725247
Cardiac amyloidosis	274.91	24.96	58	8080	1782	79734468
Atrial fibrillation	163.99	24.96	146	7992	197740	79538510
Off label use	130.35	24.96	285	7853	906930	78829320
Amyloidosis	87.96	24.96	25	8113	2681	79733569
Cardiac failure congestive	83.55	24.96	87	8051	142315	79593935
Essential hypertension	79.45	24.96	28	8110	6025	79730225
Dyspnoea exertional	77.45	24.96	67	8071	87006	79649244
Left ventricular hypertrophy	75.85	24.96	32	8106	11159	79725091
Dyspnoea	62.34	24.96	210	7928	856815	78879435
Chronic left ventricular failure	59.59	24.96	15	8123	1011	79735239
Congenital coronary artery malformation	57.41	24.96	10	8128	106	79736144
Atrial flutter	53.17	24.96	31	8107	21594	79714656
Cardiac failure acute	51.53	24.96	29	8109	18900	79717350
Product use in unapproved indication	47.87	24.96	89	8049	250270	79485980
Disease progression	44.97	24.96	73	8065	184289	79551961
N-terminal prohormone brain natriuretic peptide increased	43.96	24.96	17	8121	4738	79731512
Amyloidosis senile	42.91	24.96	7	8131	48	79736202
Drug ineffective	41.65	24.96	30	8108	1080883	78655367
Therapeutic response unexpected	39.77	24.96	25	8113	19921	79716329
Chronic kidney disease	37.99	24.96	40	8098	66114	79670136
Pancreatic steatosis	34.62	24.96	10	8128	1135	79735115
Hyperlipidaemia	33.68	24.96	25	8113	26068	79710182
Dysphagia	33.41	24.96	51	8087	122085	79614165
Toxicity to various agents	32.13	24.96	3	8135	421537	79314713
Bendopnoea	31.67	24.96	5	8133	27	79736223
Polyneuropathy	30.86	24.96	23	8115	24128	79712122
Hypoacusis	30.48	24.96	25	8113	30125	79706125
Hereditary neuropathic amyloidosis	29.10	24.96	4	8134	6	79736244
Sinus arrhythmia	28.60	24.96	10	8128	2100	79734150
Oedema peripheral	27.92	24.96	72	8066	252216	79484034
Arterial thrombosis	26.29	24.96	10	8128	2664	79733586
Carpal tunnel syndrome	25.85	24.96	19	8119	19509	79716741
Glomerular filtration rate decreased	25.45	24.96	20	8118	22682	79713568

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
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 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
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
Vyndamax	HUMAN PRESCRIPTION DRUG LABEL	1	0069-8730	CAPSULE, LIQUID FILLED	61 mg	ORAL	NDA	27 sections