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	3927.66	17.22	1312	30226	43591	56216938
Alopecia	1434.11	17.22	1233	30305	292225	55968304
Multiple sclerosis	1391.15	17.22	539	30999	27263	56233266
Paraesthesia	687.94	17.22	575	30963	129939	56130590
Hypoaesthesia	669.64	17.22	586	30952	140905	56119624
Product dose omission issue	660.81	17.22	686	30852	204067	56056462
Balance disorder	289.21	17.22	280	31258	76240	56184289
Diarrhoea	285.35	17.22	892	30646	637615	55622914
Gait disturbance	236.88	17.22	368	31170	162953	56097576
Fall	234.99	17.22	576	30962	356934	55903595
Product dose omission in error	221.79	17.22	86	31452	4328	56256201
Memory impairment	189.68	17.22	238	31300	86319	56174210
Bladder disorder	181.32	17.22	89	31449	7935	56252594
Rheumatoid arthritis	168.42	17.22	12	31526	382592	55877937
Off label use	155.44	17.22	59	31479	556121	55704408
Fatigue	155.42	17.22	857	30681	787695	55472834
Depressed mood	152.39	17.22	141	31397	36218	56224311
Depression	145.22	17.22	315	31223	179802	56080727
Muscle spasticity	132.59	17.22	101	31437	19859	56240670
COVID-19	128.49	17.22	183	31355	74875	56185654
Unevaluable event	127.20	17.22	145	31393	47542	56212987
Visual impairment	122.74	17.22	178	31360	74024	56186505
Optic neuritis	112.18	17.22	64	31474	7740	56252789
Mobility decreased	111.04	17.22	199	31339	98792	56161737
Muscular weakness	102.17	17.22	198	31340	104254	56156275
Sensory disturbance	100.31	17.22	71	31467	12472	56248057
Headache	95.50	17.22	586	30952	558458	55702071
Toxicity to various agents	93.29	17.22	9	31529	224555	56035974
Acute kidney injury	91.71	17.22	13	31525	240750	56019779
Contraindicated product administered	87.48	17.22	4	31534	186282	56074247
Limb discomfort	86.77	17.22	90	31448	26532	56233997
Central nervous system lesion	78.88	17.22	56	31482	9882	56250647
Cognitive disorder	75.64	17.22	114	31424	49019	56211510
Therapeutic product effect decreased	75.35	17.22	5	31533	169447	56091082
Synovitis	74.02	17.22	4	31534	161301	56099228
Maternal exposure during pregnancy	68.18	17.22	12	31526	189541	56070988
Throat clearing	67.02	17.22	27	31511	1503	56259026
Decreased interest	66.47	17.22	33	31505	3013	56257516
Drug hypersensitivity	66.04	17.22	36	31502	275169	55985360
JC polyomavirus test positive	65.72	17.22	25	31513	1193	56259336
Systemic lupus erythematosus	65.64	17.22	11	31527	180067	56080462
Joint swelling	65.17	17.22	41	31497	289759	55970770
Completed suicide	62.41	17.22	3	31535	133830	56126699
Burning sensation	61.21	17.22	103	31435	48593	56211936
Condition aggravated	60.85	17.22	365	31173	344533	55915996
Magnetic resonance imaging abnormal	53.66	17.22	28	31510	2838	56257691
Urinary incontinence	51.85	17.22	73	31465	29512	56231017
Hypotension	50.30	17.22	40	31498	250468	56010061
Pericarditis	49.04	17.22	3	31535	108920	56151609
Feeling abnormal	47.79	17.22	174	31364	133428	56127101
Anaemia	47.39	17.22	48	31490	267463	55993066
Micturition urgency	46.68	17.22	39	31499	8742	56251787
Secondary progressive multiple sclerosis	45.91	17.22	20	31518	1355	56259174
Death	45.35	17.22	76	31462	341350	55919179
Drug interaction	45.33	17.22	31	31507	209724	56050805
Wound	45.32	17.22	11	31527	138793	56121736
Electric shock sensation	45.08	17.22	15	31523	482	56260047
Muscle spasms	45.05	17.22	174	31364	137197	56123332
Overdose	44.56	17.22	4	31534	105826	56154703
Movement disorder	43.92	17.22	54	31484	19144	56241385
Illness	43.36	17.22	73	31465	34438	56226091
Injection site pain	43.01	17.22	7	31531	117111	56143418
Hyponatraemia	42.63	17.22	4	31534	102135	56158394
Peroneal nerve palsy	42.16	17.22	28	31510	4433	56256096
Lower respiratory tract infection	41.84	17.22	7	31531	114787	56145742
Stress	41.73	17.22	98	31440	58812	56201717
Arthropathy	41.43	17.22	31	31507	200244	56060285
Onychoclasis	40.96	17.22	30	31508	5555	56254974
Walking aid user	39.79	17.22	35	31503	8408	56252121
Pneumonia	39.57	17.22	108	31430	406990	55853539
Incontinence	38.08	17.22	38	31500	10697	56249832
Lymphopenia	38.08	17.22	47	31491	16727	56243802
Therapeutic product effect incomplete	37.48	17.22	7	31531	106024	56154505
Intentional product use issue	36.53	17.22	6	31532	99727	56160802
Dyspnoea	35.17	17.22	192	31346	592385	55668144
Paraparesis	34.59	17.22	19	31519	2134	56258395
Swelling	34.05	17.22	51	31487	239720	56020809
Vision blurred	32.19	17.22	111	31427	82832	56177697
Treatment failure	31.98	17.22	29	31509	170363	56090166
Temperature intolerance	31.40	17.22	30	31508	8010	56252519
Respiratory failure	30.13	17.22	8	31530	95054	56165475
Expanded disability status scale score increased	29.36	17.22	11	31527	503	56260026
Pancytopenia	29.01	17.22	7	31531	88708	56171821
Hair texture abnormal	28.75	17.22	21	31517	3871	56256658
Pain in extremity	28.59	17.22	273	31265	297158	55963371
General physical health deterioration	28.41	17.22	32	31506	169978	56090551
Progressive multiple sclerosis	28.18	17.22	12	31526	769	56259760
Breast cancer	28.03	17.22	75	31463	48758	56211771
Hypokalaemia	28.00	17.22	9	31529	94428	56166101
Spinal operation	27.88	17.22	27	31511	7329	56253200
Helicobacter infection	27.76	17.22	4	31534	73264	56187265
SARS-CoV-2 test positive	27.72	17.22	25	31513	6204	56254325
Haemoglobin decreased	27.42	17.22	21	31517	134116	56126413
Hypertension	26.92	17.22	231	31307	244047	56016482
Neuralgia	25.71	17.22	47	31491	23648	56236881
Oedema peripheral	25.71	17.22	35	31503	171219	56089310
Pleural effusion	25.60	17.22	8	31530	85472	56175057
Dizziness	25.45	17.22	322	31216	375818	55884711
Weight increased	25.36	17.22	57	31481	229646	56030883
Neutropenia	25.11	17.22	31	31507	158136	56102393
Cardiac failure congestive	24.89	17.22	9	31529	87711	56172818
Trigeminal neuralgia	24.30	17.22	18	31520	3389	56257140
Impaired driving ability	23.46	17.22	19	31519	4077	56256452
Intentional overdose	23.02	17.22	5	31533	68112	56192417
Drug intolerance	22.98	17.22	74	31464	264744	55995785
Surgery	22.95	17.22	54	31484	32432	56228097
Asthenia	22.93	17.22	293	31245	342680	55917849
Thrombocytopenia	22.36	17.22	26	31512	136198	56124331
Discomfort	22.27	17.22	28	31510	141733	56118796
Oedema	22.26	17.22	9	31529	81911	56178618
Blood pressure increased	22.00	17.22	148	31390	145028	56115501
Pyrexia	21.96	17.22	141	31397	418632	55841897
Heteroplasia	21.91	17.22	4	31534	7	56260522
Dysstasia	21.78	17.22	39	31499	19315	56241214
Exposure during pregnancy	21.27	17.22	140	31398	136202	56124327
Hypoglycaemia	21.25	17.22	3	31535	55812	56204717
Cardiac arrest	21.09	17.22	11	31527	86303	56174226
Needle fatigue	21.02	17.22	6	31532	114	56260415
Disease progression	20.82	17.22	17	31521	105156	56155373
Neuropathy peripheral	20.75	17.22	113	31425	102780	56157749
Renal failure	20.49	17.22	19	31519	110481	56150048
Lipase increased	20.12	17.22	25	31513	8954	56251575
Hemiparesis	20.08	17.22	40	31498	21450	56239079
Blood creatinine increased	19.92	17.22	10	31528	80181	56180348
Stomatitis	19.89	17.22	23	31515	120787	56139742
Therapy non-responder	19.75	17.22	5	31533	61350	56199179
Cerebral disorder	19.63	17.22	17	31521	3999	56256530
Oxygen saturation decreased	19.43	17.22	10	31528	79057	56181472
Pollakiuria	19.02	17.22	43	31495	25159	56235370
Band sensation	18.81	17.22	9	31529	758	56259771
Faeces soft	18.78	17.22	18	31520	4824	56255705
Hyperkalaemia	18.75	17.22	3	31535	50862	56209667
Psoriatic arthropathy	18.73	17.22	9	31529	73999	56186530
Paternal exposure timing unspecified	18.63	17.22	4	31534	21	56260508
Osteoarthritis	18.51	17.22	11	31527	80285	56180244
Arthralgia	18.42	17.22	186	31352	501483	55759046
Anal incontinence	18.16	17.22	28	31510	12270	56248259
Gastrointestinal haemorrhage	18.09	17.22	10	31528	75941	56184588
Speech disorder	18.01	17.22	54	31484	37439	56223090
Platelet count decreased	17.79	17.22	20	31518	106363	56154166
Drug effect less than expected	17.52	17.22	9	31529	883	56259646
Renal impairment	17.32	17.22	12	31526	80701	56179828
Infection	17.32	17.22	56	31482	200150	56060379
Migraine	17.28	17.22	95	31443	86702	56173827

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	1262.42	27.76	321	5970	11726	31679327
Multiple sclerosis	539.49	27.76	151	6140	7886	31683167
Alopecia	220.88	27.76	99	6192	20596	31670457
Product dose omission issue	185.70	27.76	159	6132	105427	31585626
Hypoaesthesia	135.85	27.76	102	6189	55920	31635133
Paraesthesia	118.25	27.76	94	6197	55977	31635076
Gait disturbance	116.60	27.76	107	6184	77388	31613665
Product dose omission in error	101.18	27.76	27	6264	1166	31689887
Fatigue	79.30	27.76	192	6099	335014	31356039
Balance disorder	75.11	27.76	61	6230	37361	31653692
Diarrhoea	69.97	27.76	189	6102	352220	31338833
Fall	67.44	27.76	127	6164	185962	31505091
Mobility decreased	59.84	27.76	47	6244	27422	31663631
Memory impairment	52.12	27.76	50	6241	38080	31652973
Headache	50.64	27.76	112	6179	183540	31507513
Visual impairment	50.47	27.76	45	6246	31234	31659819
Muscle spasticity	47.70	27.76	23	6268	5612	31685441
Depressed mood	40.27	27.76	31	6260	17544	31673509
Muscular weakness	36.07	27.76	54	6237	65394	31625659
Drug ineffective	35.91	27.76	164	6127	395409	31295644
Optic neuritis	35.67	27.76	16	6275	3314	31687739
Off label use	34.49	27.76	13	6278	347261	31343792
Feeling abnormal	34.25	27.76	49	6242	56953	31634100
Acute kidney injury	34.21	27.76	7	6284	279707	31411346
Unevaluable event	32.47	27.76	35	6256	30540	31660513
Trigeminal neuralgia	32.08	27.76	11	6280	1116	31689937
Walking aid user	31.65	27.76	12	6279	1624	31689429
Depression	31.54	27.76	61	6230	90754	31600299
Condition aggravated	30.33	27.76	86	6205	163923	31527130
Limb discomfort	30.09	27.76	21	6270	10228	31680825
Decreased interest	28.29	27.76	12	6279	2173	31688880
Hepatic enzyme increased	27.89	27.76	35	6256	35873	31655180

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	3787.94	18.31	1180	28724	41837	70856703
Alopecia	1528.58	18.31	980	28924	197510	70701030
Multiple sclerosis	1434.86	18.31	499	29405	24786	70873754
Hypoaesthesia	679.83	18.31	543	29361	153196	70745344
Paraesthesia	647.59	18.31	516	29388	145021	70753519
Product dose omission issue	537.82	18.31	554	29350	216914	70681626
Gait disturbance	328.55	18.31	397	29507	184709	70713831
Balance disorder	271.15	18.31	256	29648	89872	70808668
Diarrhoea	263.78	18.31	824	29080	782517	70116023
Fall	234.30	18.31	552	29352	443544	70454996
Fatigue	213.78	18.31	795	29109	823524	70075016
Memory impairment	205.12	18.31	223	29681	92418	70806122
Product dose omission in error	179.23	18.31	69	29835	4547	70893993
Headache	157.62	18.31	569	29335	579836	70318704
Unevaluable event	154.76	18.31	147	29757	51916	70846624
Off label use	151.91	18.31	62	29842	742998	70155542
Visual impairment	148.40	18.31	176	29728	80074	70818466
Bladder disorder	143.38	18.31	70	29834	8219	70890321
Acute kidney injury	136.92	18.31	19	29885	474605	70423935
Toxicity to various agents	129.50	18.31	8	29896	382164	70516376
Mobility decreased	126.89	18.31	185	29719	102814	70795726
Depressed mood	121.31	18.31	119	29785	43701	70854839
Depression	118.52	18.31	260	29644	198714	70699826
Optic neuritis	115.70	18.31	62	29842	8838	70889702
Muscular weakness	111.37	18.31	205	29699	138131	70760409
Muscle spasticity	109.64	18.31	80	29824	19609	70878931
Limb discomfort	106.09	18.31	93	29811	29612	70868928
Rheumatoid arthritis	88.14	18.31	10	29894	291795	70606745
COVID-19	87.97	18.31	159	29745	105598	70792942
Throat clearing	86.32	18.31	31	29873	1680	70896860
Sensory disturbance	85.74	18.31	60	29844	13772	70884768
Feeling abnormal	81.32	18.31	183	29721	142136	70756404
Central nervous system lesion	77.15	18.31	54	29850	12399	70886141
Completed suicide	76.14	18.31	5	29899	227130	70671410
Secondary progressive multiple sclerosis	73.63	18.31	26	29878	1341	70897199
Decreased interest	71.57	18.31	33	29871	3408	70895132
Hypotension	71.34	18.31	41	29863	404340	70494200
Drug interaction	69.71	18.31	37	29867	381404	70517136
Magnetic resonance imaging abnormal	64.42	18.31	30	29874	3170	70895370
Burning sensation	63.66	18.31	94	29810	52776	70845764
Anaemia	61.61	18.31	48	29856	403375	70495165
JC polyomavirus test positive	59.72	18.31	22	29882	1282	70897258
Pain in extremity	59.71	18.31	285	29619	327797	70570743
Muscle spasms	59.68	18.31	171	29733	153875	70744665
Cognitive disorder	58.96	18.31	98	29806	60858	70837682
Walking aid user	57.51	18.31	38	29866	7943	70890597
Condition aggravated	56.41	18.31	340	29564	427295	70471245
Urinary incontinence	54.02	18.31	73	29831	37769	70860771
Hyponatraemia	52.26	18.31	4	29900	160083	70738457
Trigeminal neuralgia	47.77	18.31	25	29879	3396	70895144
Electric shock sensation	46.52	18.31	15	29889	584	70897956
Pancytopenia	46.04	18.31	5	29899	151102	70747438
Drug hypersensitivity	45.69	18.31	27	29877	262432	70636108
Micturition urgency	45.65	18.31	38	29866	11276	70887264
Neutropenia	45.41	18.31	26	29878	257130	70641410
Stress	45.21	18.31	93	29811	67873	70830667
Death	44.34	18.31	93	29811	509968	70388572
Pneumonia	42.93	18.31	120	29784	596112	70302428
Contraindicated product administered	42.19	18.31	4	29900	134608	70763932
Overdose	41.95	18.31	10	29894	169735	70728805
Disease progression	41.22	18.31	8	29896	156664	70741876
Therapeutic product effect decreased	40.50	18.31	6	29898	143012	70755528
Band sensation	40.10	18.31	14	29890	698	70897842
Synovitis	40.08	18.31	4	29900	129224	70769316
Bradycardia	38.28	18.31	4	29900	124611	70773929
Injection site pain	38.21	18.31	3	29901	117616	70780924
Paraparesis	38.18	18.31	22	29882	3607	70894933
Pollakiuria	38.14	18.31	58	29846	33403	70865137
Pain	37.37	18.31	417	29487	628399	70270141
Impaired driving ability	37.13	18.31	24	29880	4833	70893707
Migraine	36.95	18.31	89	29815	72149	70826391
Peroneal nerve palsy	36.49	18.31	25	29879	5545	70892995
Movement disorder	35.13	18.31	47	29857	24082	70874458
Lymphopenia	34.89	18.31	50	29854	27309	70871231
Expanded disability status scale score increased	34.81	18.31	12	29892	576	70897964
Illness	34.68	18.31	54	29850	31737	70866803
Renal impairment	34.55	18.31	9	29895	143928	70754612
Haemoglobin decreased	34.45	18.31	22	29882	205137	70693403
Progressive multiple sclerosis	34.41	18.31	13	29891	813	70897727
Breast cancer	33.86	18.31	55	29849	33494	70865046
Treatment failure	32.77	18.31	10	29894	144132	70754408
Hair texture abnormal	32.72	18.31	19	29885	3161	70895379
Vision blurred	32.54	18.31	101	29803	94883	70803657
Temperature intolerance	32.53	18.31	28	29876	8695	70889845
Therapeutic product effect incomplete	31.79	18.31	6	29898	119876	70778664
Dyspnoea	31.58	18.31	193	29711	769867	70128673
Cardiac failure congestive	31.52	18.31	9	29895	135448	70763092
Asthenia	31.12	18.31	312	29592	457354	70441186
Thrombocytopenia	31.04	18.31	33	29871	239077	70659463
Heteroplasia	30.92	18.31	5	29899	4	70898536
Renal failure	30.76	18.31	21	29883	189049	70709491
Dysstasia	30.63	18.31	45	29859	25134	70873406
Blood creatinine increased	30.62	18.31	11	29893	142990	70755550
Maternal exposure during pregnancy	30.11	18.31	6	29898	115339	70783201
Platelet count decreased	30.07	18.31	19	29885	178203	70720337
Hypokalaemia	30.00	18.31	9	29895	131179	70767361
Nausea	29.77	18.31	514	29390	851574	70046966
Multiple organ dysfunction syndrome	29.71	18.31	5	29899	108510	70790030
Onychoclasis	29.45	18.31	21	29883	4963	70893577
Hypoglycaemia	29.05	18.31	3	29901	94361	70804179
Dizziness	28.99	18.31	311	29593	463830	70434710
Pleural effusion	28.82	18.31	10	29894	132854	70765686
Wheelchair user	28.60	18.31	21	29883	5193	70893347
Respiratory failure	28.45	18.31	18	29886	168717	70729823
Cardiac arrest	28.43	18.31	16	29888	159818	70738722
Hepatic enzyme increased	28.21	18.31	136	29768	156854	70741686
Incontinence	28.15	18.31	31	29873	12997	70885543
General physical health deterioration	28.01	18.31	35	29869	235996	70662544
Intentional product use issue	27.92	18.31	8	29896	120134	70778406
Neuralgia	27.66	18.31	46	29858	28557	70869983
Pyrexia	27.61	18.31	147	29757	606805	70291735
Abdominal discomfort	27.15	18.31	169	29735	214489	70684051
Rhabdomyolysis	27.15	18.31	4	29900	95756	70802784
Cardio-respiratory arrest	26.78	18.31	5	29899	100672	70797868
Sensory loss	26.12	18.31	28	29876	11391	70887149
Surgery	26.07	18.31	46	29858	29943	70868597
Cardiac failure	26.06	18.31	14	29890	143527	70755013
Hand deformity	25.99	18.31	3	29901	86479	70812061
Oedema peripheral	25.85	18.31	35	29869	228056	70670484
Musculoskeletal stiffness	25.83	18.31	127	29777	147633	70750907
Pericarditis	25.30	18.31	3	29901	84702	70813838
Septic shock	25.13	18.31	8	29896	112250	70786290
Spinal operation	25.08	18.31	22	29882	7006	70891534
Lower respiratory tract infection	25.01	18.31	8	29896	111905	70786635
Joint swelling	24.72	18.31	43	29861	253168	70645372
Pulmonary oedema	24.36	18.31	3	29901	82275	70816265
Blood pressure increased	24.20	18.31	149	29755	188368	70710172
Gastrointestinal haemorrhage	24.08	18.31	14	29890	137394	70761146
Dehydration	23.38	18.31	37	29867	226105	70672435
Dysgraphia	23.08	18.31	16	29888	3616	70894924
Lipase increased	22.65	18.31	30	29874	15216	70883324
Hypertension	22.65	18.31	207	29697	295826	70602714
Back pain	22.50	18.31	193	29711	270959	70627581
Interstitial lung disease	22.50	18.31	8	29896	104677	70793863
Speech disorder	22.39	18.31	59	29845	50521	70848019
Relapsing multiple sclerosis	22.14	18.31	6	29898	126	70898414
Hypoxia	22.09	18.31	6	29898	93338	70805202
Intentional overdose	22.06	18.31	7	29897	98428	70800112
Depressed level of consciousness	21.89	18.31	5	29899	87426	70811114
Oxygen saturation decreased	21.66	18.31	11	29893	116418	70782122
Delirium	21.42	18.31	3	29901	74611	70823929
Weight decreased	21.22	18.31	212	29692	310276	70588264
Influenza like illness	21.02	18.31	68	29836	65263	70833277
Gait inability	20.85	18.31	55	29849	47120	70851420
Hemiparesis	20.85	18.31	43	29861	31426	70867114
Urinary tract infection	20.60	18.31	177	29727	248592	70649948
Electrocardiogram QT prolonged	20.47	18.31	5	29899	83512	70815028
Systemic lupus erythematosus	19.91	18.31	9	29895	101893	70796647
Faeces soft	19.55	18.31	19	29885	6891	70891649
Testicular seminoma (pure) stage I	19.46	18.31	4	29900	23	70898517
Meningoencephalitis herpetic	18.95	18.31	11	29893	1828	70896712
Oedema	18.95	18.31	10	29894	103571	70794969
Ascites	18.74	18.31	3	29901	67544	70830996
Epistaxis	18.64	18.31	10	29894	102617	70795923
Cerebral disorder	18.54	18.31	16	29888	4983	70893557
Deep vein thrombosis	18.50	18.31	12	29892	111030	70787510

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
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
Significant neutropenia	contraindication	303011007	DOID:1227
Breastfeeding (mother)	contraindication	413712001
Severe hepatic impairment	contraindication	710067001
Severe active infection	contraindication

🐶 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
1310520	RXNORM
193228	MMSL
28846	MMSL
d07905	MMSL
014643	NDDF
703785006	SNOMEDCT_US
703786007	SNOMEDCT_US
C1718383	UMLSCUI
54684141	PUBCHEM_CID

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