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:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	4	Hosey CM, Chan R, Benet LZ
Vd (Volume of distribution)	0.16 L/kg	Lombardo F, Berellini G, Obach RS
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
t_half (Half-life)	350 hours	Lombardo F, Berellini G, Obach RS

Approvals:

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

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
Multiple sclerosis relapse	2417.44	16.79	875	24059	42089	50538101
Alopecia	1254.93	16.79	1002	23932	244045	50336145
Paraesthesia	524.73	16.79	450	24484	119793	50460397
Hypoaesthesia	500.63	16.79	449	24485	126808	50453382
Product dose omission issue	434.43	16.79	492	24442	183346	50396844
Diarrhoea	234.18	16.79	726	24208	587750	49992440
Gait disturbance	196.63	16.79	301	24633	149704	50430486
Balance disorder	186.94	16.79	201	24733	70389	50509801
Product dose omission in error	165.14	16.79	57	24877	2343	50577847
Fall	153.12	16.79	435	24499	334497	50245693
Unevaluable event	132.25	16.79	137	24797	45929	50534261
Memory impairment	125.23	16.79	174	24760	79186	50501004
Bladder disorder	113.47	16.79	61	24873	7482	50572708
Off label use	112.07	16.79	47	24887	474379	50105811
Depression	108.91	16.79	247	24687	165176	50415014
Fatigue	104.13	16.79	648	24286	706953	49873237
Depressed mood	100.91	16.79	103	24831	33920	50546270
Multiple sclerosis	99.95	16.79	82	24852	20411	50559779
Optic neuritis	98.85	16.79	54	24880	6836	50573354
Muscular weakness	89.96	16.79	165	24769	94848	50485342
COVID-19	80.67	16.79	107	24827	46555	50533635
Toxicity to various agents	73.80	16.79	9	24925	212490	50367700
Acute kidney injury	73.73	16.79	12	24922	228046	50352144
Headache	72.37	16.79	461	24473	506074	50074116
Rheumatoid arthritis	71.78	16.79	8	24926	202542	50377648
Visual impairment	70.27	16.79	123	24811	68152	50512038
Drug hypersensitivity	69.31	16.79	19	24915	250991	50329199
Limb discomfort	69.07	16.79	72	24862	24285	50555905
JC polyomavirus test positive	67.34	16.79	24	24910	1085	50579105
Central nervous system lesion	66.18	16.79	47	24887	9442	50570748
Muscle spasticity	64.06	16.79	59	24875	17125	50563065
Mobility decreased	61.22	16.79	127	24807	79821	50500369
Sensory disturbance	61.19	16.79	49	24885	11780	50568410
Condition aggravated	56.46	16.79	292	24642	296766	50283424
Burning sensation	56.30	16.79	89	24845	45357	50534833
Completed suicide	52.84	16.79	3	24931	131886	50448304
Magnetic resonance imaging abnormal	52.47	16.79	26	24908	2692	50577498
Maternal exposure during pregnancy	50.30	16.79	9	24925	159769	50420421
Therapeutic product effect decreased	49.13	16.79	5	24929	136045	50444145
Synovitis	49.06	16.79	3	24931	123862	50456328
Urinary incontinence	47.68	16.79	64	24870	28144	50552046
Cognitive disorder	44.74	16.79	79	24855	44044	50536146
Throat clearing	40.72	16.79	17	24917	1181	50579009
Injection site pain	40.29	16.79	4	24930	111020	50469170
Joint swelling	40.20	16.79	37	24897	245249	50334941
Decreased interest	39.06	16.79	22	24912	2954	50577236
Feeling abnormal	38.86	16.79	143	24791	125349	50454841
Electric shock sensation	38.76	16.79	11	24923	234	50579956
Systemic lupus erythematosus	38.11	16.79	11	24923	140611	50439579
Micturition urgency	38.06	16.79	32	24902	8232	50571958
Drug interaction	37.87	16.79	26	24908	199595	50380595
Lymphopenia	36.99	16.79	42	24892	15579	50564611
Hypotension	36.86	16.79	37	24897	235432	50344758
Hyponatraemia	36.13	16.79	3	24931	96136	50484054
Death	35.92	16.79	66	24868	325313	50254877
Overdose	35.15	16.79	4	24930	99723	50480467
Exposure during pregnancy	35.06	16.79	135	24799	120880	50459310
Breast cancer	33.83	16.79	69	24865	42821	50537369
Incontinence	32.85	16.79	32	24902	9953	50570237
Anaemia	32.75	16.79	46	24888	252410	50327780
Walking aid user	31.90	16.79	26	24908	6407	50573783
Muscle spasms	30.00	16.79	132	24802	125421	50454769
Peroneal nerve palsy	29.37	16.79	21	24913	4262	50575928
Lower respiratory tract infection	28.60	16.79	6	24928	95195	50484995
Pericarditis	28.12	16.79	3	24931	78686	50501504
Vision blurred	28.11	16.79	94	24840	78553	50501637
Hepatic enzyme increased	28.09	16.79	138	24796	137242	50442948
Onychoclasis	27.89	16.79	22	24912	5174	50575016
Pneumonia	27.56	16.79	95	24839	378306	50201884
Stress	27.51	16.79	73	24861	53720	50526470
Wound	27.36	16.79	9	24925	105785	50474405
Secondary progressive multiple sclerosis	27.11	16.79	13	24921	1253	50578937
Hypertension	25.64	16.79	185	24749	211018	50369172
Therapeutic product effect incomplete	25.08	16.79	7	24927	91508	50488682
Intentional product use issue	24.93	16.79	4	24930	76914	50503276
Lipase increased	23.76	16.79	25	24909	8516	50571674
Paraparesis	23.73	16.79	14	24920	2050	50578140
SARS-CoV-2 test positive	23.46	16.79	19	24915	4640	50575550
Pain in extremity	23.44	16.79	221	24713	272644	50307546
Respiratory failure	23.15	16.79	8	24926	91173	50489017
Hair texture abnormal	22.97	16.79	17	24917	3639	50576551
Heteroplasia	22.42	16.79	4	24930	7	50580183
Arthropathy	22.28	16.79	27	24907	157879	50422311
Pancytopenia	21.99	16.79	7	24927	84023	50496167
Weight decreased	21.98	16.79	185	24749	221060	50359130
Blood pressure increased	21.92	16.79	126	24808	133006	50447184
Haemoglobin decreased	21.04	16.79	19	24915	127197	50452993
Dysstasia	20.83	16.79	34	24900	17785	50562405
Trigeminal neuralgia	20.73	16.79	15	24919	3100	50577090
Hemiparesis	20.45	16.79	36	24898	20012	50560178
Hypokalaemia	20.23	16.79	9	24925	87983	50492207
General physical health deterioration	19.42	16.79	25	24909	142409	50437781
Pleural effusion	19.25	16.79	8	24926	81446	50498744
Paternal exposure timing unspecified	19.15	16.79	4	24930	21	50580169
Temperature intolerance	19.10	16.79	21	24913	7518	50572672
Cardiac failure congestive	18.83	16.79	9	24925	84373	50495817
Dyspnoea	18.80	16.79	176	24758	547432	50032758
Liver function test increased	18.79	16.79	40	24894	25566	50554624
Spinal operation	18.63	16.79	19	24915	6241	50573949
Asthenia	18.46	16.79	239	24695	318803	50261387
Pollakiuria	18.36	16.79	38	24896	23813	50556377
Abortion	18.32	16.79	12	24922	2112	50578078
Neuralgia	18.22	16.79	36	24898	21827	50558363
Neutropenia	18.15	16.79	28	24906	147937	50432253
Band sensation	17.61	16.79	8	24926	682	50579508
Impaired driving ability	17.55	16.79	15	24919	3946	50576244
Swelling	17.03	16.79	47	24887	200825	50379365
Pharyngeal abscess	16.99	16.79	6	24928	264	50579926
Treatment failure	16.93	16.79	26	24908	137611	50442579
Progressive multiple sclerosis	16.92	16.79	8	24926	747	50579443
Hypoglycaemia	16.89	16.79	3	24931	53578	50526612

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
Multiple sclerosis relapse	902.89	26.35	235	4723	11184	29558385
Alopecia	207.60	26.35	88	4870	18996	29550573
Product dose omission issue	154.34	26.35	128	4830	96255	29473314
Gait disturbance	102.05	26.35	90	4868	73259	29496310
Hypoaesthesia	100.21	26.35	78	4880	53389	29516180
Paraesthesia	97.55	26.35	77	4881	53768	29515801
Multiple sclerosis	82.22	26.35	32	4926	5522	29564047
Diarrhoea	69.86	26.35	164	4794	332534	29237035
Balance disorder	66.02	26.35	52	4906	36118	29533451
Product dose omission in error	63.62	26.35	16	4942	648	29568921
Fatigue	63.01	26.35	153	4805	316668	29252901
Fall	54.08	26.35	102	4856	177076	29392493
Mobility decreased	44.74	26.35	36	4922	25744	29543825
Headache	43.25	26.35	92	4866	173915	29395654
Memory impairment	39.49	26.35	39	4919	36431	29533138
Optic neuritis	35.94	26.35	15	4943	3094	29566475
Visual impairment	34.46	26.35	33	4925	29675	29539894
Unevaluable event	32.45	26.35	32	4926	29819	29539750
Depression	30.95	26.35	53	4905	85094	29484475
Meningoencephalitis herpetic	29.35	26.35	9	4949	760	29568809
Trigeminal neuralgia	26.83	26.35	9	4949	1013	29568556
Acute kidney injury	26.60	26.35	6	4952	265261	29304308

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
Multiple sclerosis relapse	2434.62	18.01	813	23506	40322	64434091
Alopecia	1391.70	18.01	830	23489	164860	64309553
Hypoaesthesia	534.33	18.01	432	23887	138676	64335737
Paraesthesia	510.77	18.01	415	23904	134107	64340306
Product dose omission issue	393.66	18.01	423	23896	194324	64280089
Gait disturbance	266.45	18.01	326	23993	171829	64302584
Diarrhoea	234.82	18.01	698	23621	722006	63752407
Balance disorder	197.29	18.01	198	24121	83728	64390685
Fall	167.66	18.01	436	23883	416390	64058023
Fatigue	159.74	18.01	629	23690	748101	63726312
Unevaluable event	158.68	18.01	140	24179	50349	64424064
Memory impairment	150.02	18.01	173	24146	85509	64388904
Product dose omission in error	132.77	18.01	46	24273	2513	64471900
Headache	129.28	18.01	465	23854	529002	63945411
Multiple sclerosis	122.96	18.01	81	24238	18860	64455553
Acute kidney injury	111.51	18.01	18	24301	449222	64025191
Off label use	109.64	18.01	51	24268	632755	63841658
Optic neuritis	107.00	18.01	55	24264	8061	64466352
Toxicity to various agents	106.68	18.01	8	24311	363505	64110908
Depression	99.71	18.01	216	24103	183075	64291338
Visual impairment	96.52	18.01	129	24190	73948	64400465
Muscular weakness	90.73	18.01	168	24151	127170	64347243
Limb discomfort	90.67	18.01	78	24241	27097	64447316
Depressed mood	84.10	18.01	90	24229	40922	64433491
Bladder disorder	83.66	18.01	46	24273	7721	64466692
Mobility decreased	73.75	18.01	123	24196	85717	64388696
Completed suicide	65.60	18.01	5	24314	224409	64250004
Feeling abnormal	65.35	18.01	151	24168	133451	64340962
Muscle spasticity	64.21	18.01	52	24267	16617	64457796
Central nervous system lesion	63.44	18.01	45	24274	11804	64462609
JC polyomavirus test positive	62.83	18.01	22	24297	1240	64473173
Magnetic resonance imaging abnormal	61.92	18.01	28	24291	3095	64471318
Throat clearing	61.57	18.01	22	24297	1316	64473097
Burning sensation	59.39	18.01	83	24236	49581	64424832
Drug interaction	58.32	18.01	32	24287	362051	64112362
Sensory disturbance	56.88	18.01	44	24275	13164	64461249
Hypotension	56.69	18.01	37	24282	380937	64093476
COVID-19	55.48	18.01	93	24226	65047	64409366
Drug hypersensitivity	49.79	18.01	14	24305	237801	64236612
Pain in extremity	48.28	18.01	234	24085	302851	64171562
Condition aggravated	46.63	18.01	269	24050	372157	64102256
Decreased interest	44.95	18.01	23	24296	3337	64471076
Anaemia	44.87	18.01	46	24273	378634	64095779
Secondary progressive multiple sclerosis	44.52	18.01	17	24302	1226	64473187
Hyponatraemia	44.21	18.01	3	24316	148336	64326077
Muscle spasms	44.10	18.01	135	24184	140888	64333525
Walking aid user	43.54	18.01	28	24291	6253	64468160
Electric shock sensation	42.74	18.01	12	24307	324	64474089
Urinary incontinence	42.60	18.01	60	24259	36091	64438322
Rheumatoid arthritis	42.00	18.01	6	24313	164288	64310125
Hepatic enzyme increased	38.41	18.01	122	24197	129821	64344592
Trigeminal neuralgia	37.92	18.01	20	24299	3089	64471324
Pancytopenia	37.18	18.01	5	24314	143304	64331109
Cognitive disorder	37.09	18.01	71	24248	55016	64419397
Lymphopenia	37.00	18.01	47	24272	25610	64448803
Neutropenia	35.97	18.01	23	24296	239601	64234812
Breast cancer	35.27	18.01	49	24270	29099	64445314
Micturition urgency	35.08	18.01	30	24289	10329	64464084
Death	34.83	18.01	82	24237	482623	63991790
Disease progression	34.35	18.01	6	24313	141674	64332739
Pollakiuria	33.74	18.01	50	24269	31480	64442933
Bradycardia	33.51	18.01	3	24316	118216	64356197
Pain	32.57	18.01	335	23984	553176	63921237
Overdose	32.27	18.01	10	24309	159556	64314857
Pneumonia	32.25	18.01	106	24213	559470	63914943
Heteroplasia	31.48	18.01	5	24314	4	64474409
Stress	31.32	18.01	70	24249	60464	64413949
Dysstasia	31.09	18.01	41	24278	23174	64451239
Band sensation	30.78	18.01	11	24308	658	64473755
Impaired driving ability	30.43	18.01	20	24299	4634	64469779
Nausea	30.32	18.01	439	23880	785361	63689052
Renal impairment	30.06	18.01	7	24312	135010	64339403
Weight decreased	29.19	18.01	196	24123	285543	64188870
Haemoglobin decreased	28.89	18.01	19	24300	195044	64279369
Vision blurred	27.78	18.01	86	24233	90230	64384183
Paraparesis	27.77	18.01	17	24302	3485	64470928
Asthenia	27.53	18.01	264	24055	427780	64046633
Incontinence	27.41	18.01	28	24291	12053	64462360
Synovitis	26.82	18.01	3	24316	99087	64375326
Lipase increased	26.72	18.01	30	24289	14372	64460041
Migraine	26.49	18.01	67	24252	62610	64411803
Abdominal discomfort	26.31	18.01	137	24182	182185	64292228
Therapeutic product effect decreased	25.64	18.01	6	24313	115345	64359068
Progressive multiple sclerosis	25.36	18.01	10	24309	786	64473627
Platelet count decreased	25.29	18.01	16	24303	167695	64306718
Lupus vulgaris	25.22	18.01	6	24313	82	64474331
Renal failure	25.19	18.01	19	24300	181669	64292744
Cardiac failure congestive	24.97	18.01	9	24310	130571	64343842
Hair texture abnormal	24.89	18.01	15	24304	2989	64471424
Exposure during pregnancy	24.86	18.01	75	24244	77600	64396813
Hypertension	24.79	18.01	175	24144	259086	64215327
Cardiac arrest	24.21	18.01	14	24305	154050	64320363
Sensory loss	23.86	18.01	24	24295	10145	64464268
Hypoglycaemia	23.64	18.01	3	24316	89889	64384524
Maternal exposure during pregnancy	23.37	18.01	4	24315	95880	64378533
Blood creatinine increased	23.31	18.01	11	24308	135771	64338642
Multiple organ dysfunction syndrome	23.09	18.01	5	24314	101408	64373005
Blood pressure increased	23.09	18.01	127	24192	172425	64301988
Expanded disability status scale score increased	22.59	18.01	8	24311	466	64473947
Treatment failure	22.43	18.01	8	24311	116808	64357605
Thrombocytopenia	22.40	18.01	31	24288	223770	64250643
Hypokalaemia	22.32	18.01	9	24310	121894	64352519
Temperature intolerance	22.21	18.01	21	24298	8234	64466179
Pleural effusion	22.12	18.01	10	24309	126549	64347864
Cardio-respiratory arrest	22.10	18.01	5	24314	98388	64376025
Rhabdomyolysis	21.98	18.01	4	24315	91722	64382691
General physical health deterioration	21.81	18.01	27	24292	204398	64270015
Therapeutic product effect incomplete	21.81	18.01	6	24313	103476	64370937
Neuralgia	21.77	18.01	37	24282	26147	64448266
Peroneal nerve palsy	21.34	18.01	17	24302	5304	64469109
Onychoclasis	21.31	18.01	16	24303	4576	64469837
Respiratory failure	20.91	18.01	18	24301	161165	64313248
Dysgraphia	20.49	18.01	14	24305	3457	64470956
Urinary tract infection	20.22	18.01	153	24166	231443	64242970
Testicular seminoma (pure) stage I	19.91	18.01	4	24315	23	64474390
Dizziness	19.66	18.01	248	24071	429915	64044498
Speech disorder	19.66	18.01	51	24268	48390	64426023
Cardiac failure	19.45	18.01	13	24306	132360	64342053
Gastrointestinal haemorrhage	19.43	18.01	13	24306	132299	64342114
Intentional product use issue	19.23	18.01	6	24313	95358	64379055
Septic shock	18.95	18.01	8	24311	105429	64368984
Wheelchair user	18.89	18.01	15	24304	4657	64469756
Dehydration	18.85	18.01	33	24286	216730	64257683
Depressed level of consciousness	18.57	18.01	4	24315	81432	64392981
Dyspnoea	18.35	18.01	178	24141	718496	63755917
Hemiparesis	18.32	18.01	37	24282	29790	64444623
Oedema peripheral	18.31	18.01	32	24287	210285	64264128
Pyrexia	18.03	18.01	130	24189	558514	63915899

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	L04AA31	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS IMMUNOSUPPRESSANTS IMMUNOSUPPRESSANTS Selective immunosuppressants
MeSH PA	D000700	Analgesics
MeSH PA	D018712	Analgesics, Non-Narcotic
MeSH PA	D000893	Anti-Inflammatory Agents
MeSH PA	D000894	Anti-Inflammatory Agents, Non-Steroidal
MeSH PA	D018501	Antirheumatic Agents
MeSH PA	D007155	Immunologic Factors
MeSH PA	D007166	Immunosuppressive Agents
MeSH PA	D018373	Peripheral Nervous System Agents
MeSH PA	D018689	Sensory System Agents
FDA MoA	N0000185501	Dihydroorotate Dehydrogenase Inhibitors
FDA EPC	N0000185502	Pyrimidine Synthesis Inhibitor
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

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

Disease	Relation	SNOMED_ID	DOID
Multiple sclerosis	indication	24700007	DOID:2377

🐶 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)

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
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
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	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

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
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
7MG	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
14MG	AUBAGIO	SANOFI AVENTIS US	N202992	Sept. 12, 2012	RX	TABLET	ORAL	Oct. 30, 2024	PEDIATRIC EXCLUSIVITY
7MG	AUBAGIO	SANOFI AVENTIS US	N202992	Sept. 12, 2012	RX	TABLET	ORAL	Oct. 30, 2024	PEDIATRIC EXCLUSIVITY

Bioactivity Summary:

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

External reference:

ID	Source
D10172	KEGG_DRUG
4031717	VANDF
CHEBI:68540	CHEBI
A26	PDB_CHEM_ID
CHEMBL973	ChEMBL_ID
C527525	MESH_SUPPLEMENTAL_RECORD_UI
6844	IUPHAR_LIGAND_ID
7761	INN_ID
DB08880	DRUGBANK_ID
1C058IKG3B	UNII
54684141	PUBCHEM_CID
1310520	RXNORM
193228	MMSL
28846	MMSL
d07905	MMSL
014643	NDDF
703785006	SNOMEDCT_US
703786007	SNOMEDCT_US
C1718383	UMLSCUI

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Teriflunomide	HUMAN PRESCRIPTION DRUG LABEL	1	0115-1565	TABLET, FILM COATED	14 mg	ORAL	ANDA	20 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
teriflunomide	HUMAN PRESCRIPTION DRUG LABEL	1	68462-311	TABLET, FILM COATED	7 mg	ORAL	ANDA	29 sections
teriflunomide	HUMAN PRESCRIPTION DRUG LABEL	1	68462-312	TABLET, FILM COATED	14 mg	ORAL	ANDA	29 sections
Teriflunomide	HUMAN PRESCRIPTION DRUG LABEL	1	69238-1303	TABLET, FILM COATED	7 mg	ORAL	ANDA	23 sections
Teriflunomide	HUMAN PRESCRIPTION DRUG LABEL	1	69238-1304	TABLET, FILM COATED	14 mg	ORAL	ANDA	23 sections
Teriflunomide	Human Prescription Drug Label	1	69539-032	TABLET, FILM COATED	7 mg	ORAL	ANDA	27 sections
Teriflunomide	Human Prescription Drug Label	1	69539-033	TABLET, FILM COATED	14 mg	ORAL	ANDA	27 sections