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teriflunomide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
	4634	163451-81-8

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: HMR1726 flucyamide aubagio teriflunomide	Teriflunomide, an immunomodulatory agent with anti-inflammatory properties, inhibits dihydroorotate dehydrogenase, a mitochondrial enzyme involved in de novo pyrimidine synthesis. The exact mechanism by which teriflunomide exerts its therapeutic effect in multiple sclerosis is unknown but may involve a reduction in the number of activated lymphocytes in CNS. Molecular weight: 270.21 Formula: C12H9F3N2O2 CLOGP: 2.33 LIPINSKI: 0 HAC: 4 HDO: 2 TPSA: 73.12 ALOGS: -4.34 ROTB: 3 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

HMR1726
flucyamide
aubagio
teriflunomide

Teriflunomide, an immunomodulatory agent with anti-inflammatory properties, inhibits dihydroorotate dehydrogenase, a mitochondrial enzyme involved in de novo pyrimidine synthesis. The exact mechanism by which teriflunomide exerts its therapeutic effect in multiple sclerosis is unknown but may involve a reduction in the number of activated lymphocytes in CNS.

Molecular weight: 270.21
Formula: C12H9F3N2O2
CLOGP: 2.33
LIPINSKI: 0
HAC: 4
HDO: 2
TPSA: 73.12
ALOGS: -4.34
ROTB: 3

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
14	mg	O

ADMET properties:

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Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	4	Hosey CM, Chan R, Benet LZ
t_half (Half-life)	350 hours	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	0.16 L/kg	Lombardo F, Berellini G, Obach RS
S (Water solubility)	0.03 mg/mL	Bocci G, Oprea TI, Benet LZ
CL (Clearance)	0.01 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.01 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Aug. 26, 2013	EMA
Sept. 12, 2012	FDA	SANOFI AVENTIS US

FDA Adverse Event Reporting System (Female)

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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
Multiple sclerosis relapse	5537.79	17.13	1758	35990	46720	63404554
Alopecia	1673.49	17.13	1467	36281	336069	63115205
Hypoaesthesia	853.88	17.13	744	37004	167649	63283625
Paraesthesia	829.11	17.13	710	37038	156256	63295018
Product dose omission issue	604.78	17.13	719	37029	233594	63217680
Balance disorder	446.98	17.13	383	37365	84039	63367235
Product dose omission in error	369.45	17.13	147	37601	7465	63443809
Fall	349.85	17.13	739	37009	391595	63059679
Diarrhoea	328.54	17.13	1049	36699	714317	62736957
Bladder disorder	303.90	17.13	134	37614	8812	63442462

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FDA Adverse Event Reporting System (Male)

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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
Multiple sclerosis relapse	1646.93	27.03	410	7073	12723	34936725
Alopecia	275.12	27.03	124	7359	24231	34925217
Hypoaesthesia	202.96	27.03	139	7344	61305	34888143
Product dose omission issue	171.11	27.03	166	7317	119545	34829903
Paraesthesia	158.97	27.03	122	7361	64050	34885398
Gait disturbance	156.50	27.03	136	7347	85004	34864444
Product dose omission in error	119.50	27.03	36	7447	2238	34947210
Balance disorder	117.81	27.03	85	7398	40569	34908879
Fatigue	97.85	27.03	232	7251	370421	34579027
Multiple sclerosis	88.35	27.03	38	7445	6607	34942841

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FDA Adverse Event Reporting System (Geriatric)

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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
Multiple sclerosis relapse	5307.99	17.61	1572	33499	44961	79664356
Alopecia	1739.22	17.61	1143	33928	230212	79479105
Hypoaesthesia	868.92	17.61	680	34391	178672	79530645
Paraesthesia	765.36	17.61	627	34444	175696	79533621
Product dose omission issue	509.11	17.61	584	34487	246953	79462364
Gait disturbance	403.60	17.61	476	34595	207030	79502287
Balance disorder	383.52	17.61	330	34741	98527	79610790
Fall	322.29	17.61	680	34391	486949	79222368
Diarrhoea	302.66	17.61	959	34112	879530	78829787
Fatigue	298.31	17.61	989	34082	928738	78780579

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	L04AA31	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS IMMUNOSUPPRESSANTS IMMUNOSUPPRESSANTS Selective immunosuppressants
CHEBI has role	CHEBI:35475	non-steroidal anti-inflammatory agent
CHEBI has role	CHEBI:38637	tyrosine kinase inhibitors
CHEBI has role	CHEBI:49103	drug metabolites
CHEBI has role	CHEBI:50908	agente hepatotoxico
CHEBI has role	CHEBI:68542	DHODH inhibitor
FDA EPC	N0000185502	Pyrimidine Synthesis Inhibitor
FDA MoA	N0000185501	Dihydroorotate Dehydrogenase Inhibitors
MeSH PA	D000700	Analgesics
MeSH PA	D018712	Analgesics, Non-Narcotic

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
Multiple sclerosis	indication	24700007	DOID:2377
Relapsing remitting multiple sclerosis	indication	426373005	DOID:2378
Severe hypoproteinaemia	contraindication	8900005
Nephrotic syndrome	contraindication	52254009	DOID:1184
Significant leucopenia	contraindication	84828003	DOID:615
Severe renal impairment undergoing dialysis	contraindication	105502003
Severe immunodeficiency state	contraindication	234532001	DOID:612
Significant anaemia	contraindication	271737000	DOID:2355
Pregnancy, function	contraindication	289908002
Significant thrombocytopenia	contraindication	302215000	DOID:1588

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	5.59	acidic
pKa2	10.61	acidic

Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
14MG	AUBAGIO	SANOFI AVENTIS US	N202992	Sept. 12, 2012	RX	TABLET	ORAL	6794410	Sept. 12, 2026	TREATMENT OF PATIENTS WITH RELAPSING FORMS OF MULTIPLE SCLEROSIS
14MG	AUBAGIO	SANOFI AVENTIS US	N202992	Sept. 12, 2012	RX	TABLET	ORAL	9186346	Feb. 4, 2034	TREATMENT OF PATIENTS WITH RELAPSING FORMS OF MULTIPLE SCLEROSIS WHILE MANAGING THE RISK OF TERIFLUNOMIDE AND ROSUVASTATIN INTERACTION BY LIMITING THE ROSUVASTATIN DOSE TO NO MORE THAN 10MG AND/OR ADMINISTERING ABOUT HALF THE NORMAL DOSE
7MG	AUBAGIO	SANOFI AVENTIS US	N202992	Sept. 12, 2012	RX	TABLET	ORAL	6794410	Sept. 12, 2026	TREATMENT OF PATIENTS WITH RELAPSING FORMS OF MULTIPLE SCLEROSIS
7MG	AUBAGIO	SANOFI AVENTIS US	N202992	Sept. 12, 2012	RX	TABLET	ORAL	9186346	Feb. 4, 2034	TREATMENT OF PATIENTS WITH RELAPSING FORMS OF MULTIPLE SCLEROSIS WHILE MANAGING THE RISK OF TERIFLUNOMIDE AND ROSUVASTATIN INTERACTION BY LIMITING THE ROSUVASTATIN DOSE TO NO MORE THAN 10MG AND/OR ADMINISTERING ABOUT HALF THE NORMAL DOSE

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Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
14MG	TERIFLUNOMIDE	WATSON LABS TEVA	A209549	July 27, 2018	DISCN	TABLET	ORAL	Sept. 8, 2023	PATENT CHALLENGE
14MG	TERIFLUNOMIDE	APOTEX	A209601	Nov. 2, 2018	RX	TABLET	ORAL	Sept. 8, 2023	PATENT CHALLENGE
14MG	TERIFLUNOMIDE	AMNEAL PHARMS CO	A209613	Sept. 28, 2018	RX	TABLET	ORAL	Sept. 8, 2023	PATENT CHALLENGE
14MG	TERIFLUNOMIDE	AUROBINDO PHARMA	A209638	Oct. 26, 2018	RX	TABLET	ORAL	Sept. 8, 2023	PATENT CHALLENGE
14MG	TERIFLUNOMIDE	GLENMARK PHARMS	A209663	Nov. 15, 2018	RX	TABLET	ORAL	Sept. 8, 2023	PATENT CHALLENGE
14MG	TERIFLUNOMIDE	ZYDUS PHARMS	A209668	Nov. 30, 2018	RX	TABLET	ORAL	Sept. 8, 2023	PATENT CHALLENGE
14MG	TERIFLUNOMIDE	ACCORD HLTHCARE	A209690	Jan. 7, 2019	RX	TABLET	ORAL	Sept. 8, 2023	PATENT CHALLENGE
14MG	TERIFLUNOMIDE	TEVA PHARMS USA	A209700	Sept. 4, 2018	RX	TABLET	ORAL	Sept. 8, 2023	PATENT CHALLENGE
14MG	TERIFLUNOMIDE	SANDOZ	A209710	Jan. 3, 2019	RX	TABLET	ORAL	Sept. 8, 2023	PATENT CHALLENGE
14MG	AUBAGIO	SANOFI AVENTIS US	N202992	Sept. 12, 2012	RX	TABLET	ORAL	April 30, 2024	REVISIONS TO LABELING BASED ON DATA SUBMITTED IN RESPONSE TO PEDIATRIC WRITTEN REQUEST

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Dihydroorotate dehydrogenase (quinone), mitochondrial	Enzyme	Q02127	PYRD_HUMAN	INHIBITOR	Ki	7.52	CHEMBL	CHEMBL
Dihydrofolate reductase	Enzyme	P00374	DYR_HUMAN		IC50	6.41	CHEMBL
Dihydroorotate dehydrogenase (quinone), mitochondrial	Enzyme		PYRD_RAT		IC50	8.05	CHEMBL
Dihydroorotate dehydrogenase (quinone), mitochondrial	Enzyme		PYRD_MOUSE		IC50	7.16	CHEMBL
Dihydroorotate dehydrogenase	Enzyme		Q54A96_PLAFA		Ki	4.66	CHEMBL
Dihydroorotate dehydrogenase	Enzyme		G4VFD7_SCHMA		IC50	4.30	CHEMBL

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External reference:

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ID	Source
014643	NDDF
1310520	RXNORM
193228	MMSL
1C058IKG3B	UNII
28846	MMSL
365635	MMSL
4031717	VANDF
54684141	PUBCHEM_CID
6844	IUPHAR_LIGAND_ID
703785006	SNOMEDCT_US

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Aubagio	HUMAN PRESCRIPTION DRUG LABEL	1	58468-0210	TABLET, FILM COATED	14 mg	ORAL	NDA	32 sections
Aubagio	HUMAN PRESCRIPTION DRUG LABEL	1	58468-0210	TABLET, FILM COATED	14 mg	ORAL	NDA	32 sections
Aubagio	HUMAN PRESCRIPTION DRUG LABEL	1	58468-0210	TABLET, FILM COATED	14 mg	ORAL	NDA	32 sections
Aubagio	HUMAN PRESCRIPTION DRUG LABEL	1	58468-0211	TABLET, FILM COATED	7 mg	ORAL	NDA	32 sections
Aubagio	HUMAN PRESCRIPTION DRUG LABEL	1	58468-0211	TABLET, FILM COATED	7 mg	ORAL	NDA	32 sections
Aubagio	HUMAN PRESCRIPTION DRUG LABEL	1	58468-0211	TABLET, FILM COATED	7 mg	ORAL	NDA	32 sections
Teriflunomide	HUMAN PRESCRIPTION DRUG LABEL	1	0115-1565	TABLET, FILM COATED	14 mg	ORAL	ANDA	20 sections
Teriflunomide	HUMAN PRESCRIPTION DRUG LABEL	1	0378-0627	TABLET, FILM COATED	7 mg	ORAL	ANDA	31 sections
Teriflunomide	HUMAN PRESCRIPTION DRUG LABEL	1	0378-0628	TABLET, FILM COATED	14 mg	ORAL	ANDA	31 sections
Teriflunomide	HUMAN PRESCRIPTION DRUG LABEL	1	0480-3156	TABLET, FILM COATED	14 mg	ORAL	ANDA	28 sections

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