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

Stem definitionDrug idCAS RN
4634 163451-81-8

Description:

MoleculeDescription

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:

DoseUnitRoute
14 mg O

ADMET properties:

PropertyValueReference
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
S (Water solubility) 0.03 mg/mL Bocci G, Oprea TI, Benet LZ

Approvals:

DateAgencyCompanyOrphan
Aug. 26, 2013 EMA
Sept. 12, 2012 FDA SANOFI AVENTIS US

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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
Gait disturbance 303.18 17.13 453 37295 182725 63268549
Muscle spasticity 235.47 17.13 152 37596 21642 63429632
Fatigue 227.20 17.13 1083 36665 886945 62564329
Memory impairment 220.13 17.13 290 37458 103968 63347306
Off label use 217.42 17.13 66 37682 674396 62776878
Depression 216.43 17.13 405 37343 196087 63255187
Depressed mood 203.65 17.13 178 37570 40013 63411261
Visual impairment 167.63 17.13 228 37520 84218 63367056
Sensory disturbance 164.26 17.13 102 37646 13570 63437704
Mobility decreased 139.83 17.13 255 37493 120904 63330370
COVID-19 136.84 17.13 243 37505 112860 63338414
Multiple sclerosis 127.58 17.13 110 37638 24262 63427012
Headache 119.67 17.13 712 37036 632529 62818745
Muscular weakness 119.60 17.13 240 37508 122113 63329161
Decreased interest 114.57 17.13 50 37698 3204 63448070
Optic neuritis 114.35 17.13 68 37680 8367 63442907
Toxicity to various agents 113.12 17.13 9 37739 247241 63204033
Unevaluable event 113.10 17.13 146 37602 51240 63400034
Contraindicated product administered 111.71 17.13 4 37744 217644 63233630
Limb discomfort 107.12 17.13 109 37639 29607 63421667
Acute kidney injury 104.38 17.13 16 37732 263399 63187875
Cognitive disorder 103.65 17.13 146 37602 55669 63395605
Rheumatoid arthritis 101.53 17.13 15 37733 253804 63197470
Synovitis 93.99 17.13 4 37744 186914 63264360
Glossodynia 92.79 17.13 3 37745 178873 63272401
Systemic lupus erythematosus 86.72 17.13 11 37737 208907 63242367
Maternal exposure during pregnancy 85.73 17.13 14 37734 220048 63231226
Therapeutic product effect decreased 83.09 17.13 9 37739 193178 63258096
Movement disorder 82.74 17.13 82 37666 21579 63429695
Burning sensation 81.91 17.13 129 37619 54278 63396996
Central nervous system lesion 81.37 17.13 60 37688 10575 63440699
Joint swelling 77.09 17.13 50 37698 327616 63123658
Urinary incontinence 76.84 17.13 95 37653 31919 63419355
JC polyomavirus test positive 73.77 17.13 29 37719 1424 63449850
Completed suicide 73.62 17.13 3 37745 145670 63305604
Condition aggravated 69.81 17.13 443 37305 401774 63049500
Throat clearing 68.73 17.13 32 37716 2387 63448887
Drug hypersensitivity 65.78 17.13 53 37695 310634 63140640
Pericarditis 65.52 17.13 3 37745 131576 63319698
Muscle spasms 65.48 17.13 223 37525 155927 63295347
Illness 62.63 17.13 108 37640 48951 63402323
Hypotension 62.21 17.13 43 37705 272561 63178713
Stress 61.13 17.13 128 37620 67039 63384235
Anaemia 60.94 17.13 51 37697 293379 63157895
Feeling abnormal 60.53 17.13 210 37538 148182 63303092
Wound 58.03 17.13 13 37735 163250 63288024
Arthropathy 57.72 17.13 34 37714 234758 63216516
Secondary progressive multiple sclerosis 57.07 17.13 24 37724 1403 63449871
Pneumonia 55.53 17.13 118 37630 456649 62994625
Intentional product use issue 54.87 17.13 6 37742 127886 63323388
Magnetic resonance imaging abnormal 52.90 17.13 29 37719 3056 63448218
Hyponatraemia 51.34 17.13 4 37744 111896 63339378
Death 51.33 17.13 90 37658 374291 63076983
Walking aid user 51.32 17.13 46 37702 10671 63440603
Spinal operation 50.89 17.13 41 37707 8230 63443044
Therapeutic product effect incomplete 50.87 17.13 7 37741 125049 63326225
Overdose 50.39 17.13 5 37743 115073 63336201
Injection site pain 48.90 17.13 9 37739 129791 63321483
Lower respiratory tract infection 48.10 17.13 10 37738 132297 63318977
Incontinence 48.10 17.13 46 37702 11586 63439688
Swelling 47.80 17.13 56 37692 275322 63175952
Micturition urgency 47.51 17.13 42 37706 9569 63441705
Pain in extremity 45.54 17.13 345 37403 331141 63120133
Electric shock sensation 44.53 17.13 17 37731 771 63450503
Drug interaction 43.76 17.13 43 37705 229088 63222186
Dyspnoea 43.54 17.13 224 37524 661089 62790185
Peroneal nerve palsy 43.24 17.13 30 37718 4805 63446469
Onychoclasis 42.93 17.13 33 37715 6189 63445085
Vision blurred 41.81 17.13 135 37613 91789 63359485
Helicobacter infection 40.71 17.13 4 37744 92781 63358493
Tremor 39.06 17.13 169 37579 132070 63319204
Drug intolerance 38.93 17.13 78 37670 308583 63142691
Treatment failure 38.41 17.13 37 37711 199006 63252268
Surgery 36.90 17.13 72 37676 35840 63415434
Band sensation 35.98 17.13 15 37733 858 63450416
Pancytopenia 35.91 17.13 7 37741 96926 63354348
Oedema peripheral 35.68 17.13 36 37712 189475 63261799
Lymphopenia 35.58 17.13 49 37699 18278 63432996
Haemoglobin decreased 34.44 17.13 22 37726 145463 63305811
Sexual dysfunction 34.26 17.13 25 37723 4334 63446940
General physical health deterioration 33.82 17.13 42 37706 201360 63249914
Pyrexia 33.42 17.13 155 37593 470323 62980951
Weight increased 32.79 17.13 66 37682 260726 63190548
Paraparesis 32.77 17.13 19 37729 2229 63449045
Respiratory failure 32.58 17.13 10 37738 101848 63349426
Neutropenia 32.09 17.13 34 37714 174971 63276303
Pleural effusion 31.97 17.13 8 37740 93202 63358072
Musculoskeletal stiffness 31.70 17.13 203 37545 184415 63266859
Temperature intolerance 30.70 17.13 32 37716 8932 63442342
Expanded disability status scale score increased 30.62 17.13 12 37736 584 63450690
Oedema 30.49 17.13 10 37738 97612 63353662
Thrombocytopenia 30.46 17.13 27 37721 151130 63300144
Discomfort 30.15 17.13 33 37715 167341 63283933
Speech disorder 29.73 17.13 71 37677 40558 63410716
Trigeminal neuralgia 29.53 17.13 21 37727 3498 63447776
Psoriatic arthropathy 29.25 17.13 9 37739 91511 63359763
Therapy non-responder 29.15 17.13 5 37743 75896 63375378
Stomatitis 28.90 17.13 24 37724 138701 63312573
Neuropathy peripheral 28.89 17.13 139 37609 113528 63337746
Dysstasia 28.86 17.13 48 37700 21118 63430156
Progressive multiple sclerosis 28.64 17.13 14 37734 1164 63450110
Breast cancer 28.60 17.13 78 37670 48305 63402969
Intentional overdose 28.22 17.13 5 37743 74147 63377127
Hair texture abnormal 28.17 17.13 22 37726 4221 63447053
Neuralgia 27.89 17.13 53 37695 25873 63425401
Osteoarthritis 27.68 17.13 11 37737 95332 63355942
Hypertension 27.44 17.13 270 37478 279033 63172241
Fibromyalgia 27.39 17.13 7 37741 80413 63370861
Dizziness 27.30 17.13 382 37366 429543 63021731
Cardiac arrest 26.34 17.13 11 37737 92534 63358740
Arthralgia 25.75 17.13 216 37532 569494 62881780
Impaired driving ability 24.90 17.13 21 37727 4490 63446784
Cerebral disorder 24.84 17.13 21 37727 4505 63446769
SARS-CoV-2 test positive 24.49 17.13 27 37721 8029 63443245
Anal incontinence 24.43 17.13 35 37713 13541 63437733
Asthenia 24.40 17.13 341 37407 383263 63068011
Hypokalaemia 24.15 17.13 16 37732 103788 63347486
Dysgraphia 24.13 17.13 18 37730 3228 63448046
Wheezing 23.25 17.13 14 37734 95581 63355693
Confusional state 23.24 17.13 68 37680 236312 63214962
Cardiac failure congestive 23.24 17.13 13 37735 92420 63358854
Hypoglycaemia 22.97 17.13 4 37744 60061 63391213
Blood creatinine increased 22.60 17.13 12 37736 87832 63363442
Gastrointestinal haemorrhage 22.54 17.13 10 37738 81166 63370108
Disease progression 22.33 17.13 24 37724 122734 63328540
Product use issue 22 17.13 63 37685 220457 63230817
Platelet count decreased 21.91 17.13 22 37726 116100 63335174
Hemiparesis 21.91 17.13 45 37703 23237 63428037
Blood pressure increased 21.82 17.13 168 37580 161894 63289380
Heteroplasia 21.67 17.13 4 37744 7 63451267
Oxygen saturation decreased 21.50 17.13 13 37735 88572 63362702
C-reactive protein increased 21.49 17.13 15 37733 94692 63356582
Drug effect less than expected 21.30 17.13 13 37735 1676 63449598
Type 2 diabetes mellitus 20.92 17.13 6 37742 63862 63387412
Cardio-respiratory arrest 20.84 17.13 5 37743 59954 63391320
Hypoxia 20.76 17.13 5 37743 59787 63391487
Renal failure 20.31 17.13 24 37724 117628 63333646
Needle fatigue 20.28 17.13 6 37742 122 63451152
Disturbance in attention 20.06 17.13 59 37689 38130 63413144
Hyperkalaemia 19.89 17.13 4 37744 54199 63397075
Pollakiuria 19.56 17.13 48 37700 27889 63423385
Deep vein thrombosis 19.38 17.13 13 37735 83787 63367487
Trichorrhexis 19.07 17.13 11 37737 1278 63449996
Vertigo 18.80 17.13 78 37670 59809 63391465
Hip arthroplasty 18.60 17.13 3 37745 47643 63403631
Anaphylactic reaction 18.58 17.13 8 37740 66092 63385182
Migraine 18.56 17.13 115 37633 103231 63348043
Infection 18.39 17.13 72 37676 229101 63222173
Depressed level of consciousness 18.28 17.13 7 37741 62071 63389203
Myelitis 18.21 17.13 11 37737 1392 63449882
Delirium 17.99 17.13 4 37744 50537 63400737
Cardiac failure 17.86 17.13 16 37732 89126 63362148
Dehydration 17.67 17.13 49 37699 173305 63277969
Paternal exposure timing unspecified 17.67 17.13 4 37744 26 63451248
Injury 17.43 17.13 11 37737 73236 63378038
Multiple organ dysfunction syndrome 17.39 17.13 6 37742 56746 63394528
Musculoskeletal disorder 17.23 17.13 38 37710 20606 63430668

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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
Fall 86.47 27.03 155 7328 202730 34746718
Diarrhoea 82.95 27.03 225 7258 389687 34559761
Mobility decreased 73.83 27.03 57 7426 30071 34919377
Muscle spasticity 66.41 27.03 30 7453 5858 34943590
Visual impairment 65.20 27.03 57 7426 35745 34913703
Memory impairment 61.48 27.03 60 7423 43258 34906190
Headache 53.03 27.03 126 7357 200509 34748939
Depressed mood 52.74 27.03 39 7444 19278 34930170
Off label use 50.17 27.03 14 7469 419510 34529938
Muscular weakness 49.37 27.03 69 7414 72828 34876620
Drug ineffective 46.85 27.03 207 7276 456544 34492904
Decreased interest 43.30 27.03 17 7466 2343 34947105
Trigeminal neuralgia 41.92 27.03 14 7469 1215 34948233
Bladder disorder 40.99 27.03 18 7465 3286 34946162
Acute kidney injury 40.71 27.03 8 7475 304980 34644468
Walking aid user 39.35 27.03 15 7468 1909 34947539
Depression 38.42 27.03 72 7411 97026 34852422
Limb discomfort 36.35 27.03 25 7458 11022 34938426
Abdominal discomfort 35.19 27.03 53 7430 59782 34889666
Optic neuritis 33.43 27.03 16 7467 3558 34945890
Musculoskeletal stiffness 32.79 27.03 45 7438 46635 34902813
Band sensation 32.34 27.03 7 7476 112 34949336
Condition aggravated 32.00 27.03 102 7381 192094 34757354
Feeling abnormal 31.62 27.03 52 7431 63183 34886265
Expanded disability status scale score increased 29.75 27.03 8 7475 329 34949119
Illness 29.68 27.03 24 7459 13505 34935943
Central nervous system lesion 29.59 27.03 18 7465 6445 34943003
Pollakiuria 29.29 27.03 28 7455 19646 34929802
Hypotension 29.16 27.03 6 7477 221643 34727805
Unevaluable event 28.48 27.03 35 7448 32555 34916893
Hepatic enzyme increased 27.94 27.03 38 7445 39042 34910406
Toxicity to various agents 27.24 27.03 5 7478 200357 34749091

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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
Product dose omission in error 289.18 17.61 114 34957 7674 79701643
Memory impairment 241.56 17.61 271 34800 111463 79597854
Bladder disorder 228.50 17.61 101 34970 9064 79700253
Off label use 208.71 17.61 70 35001 907145 78802172
Muscle spasticity 207.50 17.61 125 34946 21350 79687967
Visual impairment 200.01 17.61 224 34847 91907 79617410
Headache 176.26 17.61 658 34413 653114 79056203
Depression 169.66 17.61 325 34746 216465 79492852
Depressed mood 164.20 17.61 150 34921 48330 79660987
Multiple sclerosis 158.72 17.61 107 34964 22175 79687142
Acute kidney injury 157.93 17.61 21 35050 519383 79189934
Toxicity to various agents 152.70 17.61 8 35063 421532 79287785
Mobility decreased 151.37 17.61 225 34846 121950 79587367
Unevaluable event 141.37 17.61 147 34924 55438 79653879
Sensory disturbance 138.55 17.61 85 34986 14992 79694325
Muscular weakness 133.16 17.61 247 34824 160482 79548835
Limb discomfort 129.91 17.61 111 34960 32739 79676578
Optic neuritis 117.50 17.61 65 35006 9455 79699862
Decreased interest 116.14 17.61 48 35023 3649 79705668
COVID-19 96.80 17.61 214 34857 157460 79551857
Feeling abnormal 92.07 17.61 211 34860 158988 79550329
Hypotension 89.33 17.61 41 35030 440276 79269041
Throat clearing 88.63 17.61 36 35035 2618 79706699
Completed suicide 87.87 17.61 5 35066 245762 79463555
Burning sensation 84.34 17.61 116 34955 58516 79650801
Secondary progressive multiple sclerosis 83.40 17.61 29 35042 1368 79707949
Pain in extremity 83.32 17.61 349 34722 364189 79345128
Central nervous system lesion 82.98 17.61 59 35012 13309 79696008
Cognitive disorder 79.77 17.61 124 34947 69802 79639515
Urinary incontinence 79.49 17.61 94 34977 40815 79668502
Muscle spasms 76.21 17.61 208 34863 174522 79534795
Anaemia 75.09 17.61 52 35019 444963 79264354
Walking aid user 68.14 17.61 47 35024 10101 79699216
Movement disorder 67.33 17.61 71 35000 27188 79682129
Drug interaction 64.28 17.61 53 35018 415130 79294187
Magnetic resonance imaging abnormal 63.98 17.61 31 35040 3428 79705889
Condition aggravated 63.55 17.61 407 34664 500717 79208600
Stress 62.93 17.61 120 34951 79492 79629825
Hyponatraemia 62.40 17.61 4 35067 177844 79531473
JC polyomavirus test positive 61.39 17.61 24 35047 1578 79707739
Trigeminal neuralgia 59.78 17.61 30 35041 3579 79705738
Pneumonia 57.90 17.61 128 34943 660118 79049199
Band sensation 57.43 17.61 19 35052 769 79708548
Neutropenia 56.44 17.61 28 35043 287682 79421635
Pancytopenia 54.56 17.61 5 35066 165740 79543577
Contraindicated product administered 53.94 17.61 4 35067 157534 79551783
Pain 52.78 17.61 506 34565 703296 79006021
Synovitis 51.12 17.61 4 35067 150730 79558587
Illness 49.61 17.61 80 34991 46431 79662886
Death 49.49 17.61 110 34961 566404 79142913
Drug hypersensitivity 48.96 17.61 36 35035 298880 79410437
Micturition urgency 48.51 17.61 42 35029 12599 79696718
Overdose 48.12 17.61 11 35060 184195 79525122
Electric shock sensation 48.10 17.61 17 35054 842 79708475
Spinal operation 46.97 17.61 34 35037 7883 79701434
Disease progression 46.22 17.61 12 35059 184350 79524967
Rheumatoid arthritis 46.12 17.61 17 35054 208453 79500864
Surgery 45.87 17.61 64 35007 32702 79676615
Bradycardia 44.86 17.61 4 35067 135553 79573764
Therapeutic product effect decreased 44.40 17.61 9 35062 163854 79545463
Musculoskeletal stiffness 44.21 17.61 173 34898 174835 79534482
Peroneal nerve palsy 42.98 17.61 29 35042 6013 79703304
Haemoglobin decreased 42.97 17.61 22 35049 222097 79487220
Therapeutic product effect incomplete 42.30 17.61 6 35065 141639 79567678
Intentional product use issue 41.96 17.61 8 35063 152104 79557213
Treatment failure 41.05 17.61 12 35059 170474 79538843
Expanded disability status scale score increased 40.54 17.61 14 35057 647 79708670
Maternal exposure during pregnancy 40.27 17.61 6 35065 136532 79572785
Vision blurred 40.23 17.61 120 34951 105778 79603539
Injection site pain 39.96 17.61 5 35066 129833 79579484
Thrombocytopenia 39.62 17.61 35 35036 265224 79444093
Hyperkalaemia 38.88 17.61 3 35068 114395 79594922
Impaired driving ability 38.54 17.61 26 35045 5389 79703928
Dyspnoea 38.28 17.61 221 34850 856804 78852513
Pollakiuria 38.19 17.61 63 35008 37254 79672063
Migraine 37.95 17.61 104 34967 87389 79621928
Pyrexia 37.75 17.61 162 34909 678547 79030770
Platelet count decreased 36.59 17.61 20 35051 194644 79514673
Sexual dysfunction 36.47 17.61 29 35042 7734 79701583
Renal impairment 36.38 17.61 12 35059 157771 79551546
Paraparesis 36.37 17.61 22 35049 3781 79705536
Abdominal discomfort 36.34 17.61 211 34860 250516 79458801
Breast cancer 35.88 17.61 58 35013 33723 79675594
Progressive multiple sclerosis 35.54 17.61 15 35056 1202 79708115
Pleural effusion 35.38 17.61 10 35061 145252 79564065
Tremor 35.05 17.61 158 34913 169925 79539392
Pericarditis 34.69 17.61 3 35068 104233 79605084
General physical health deterioration 34.68 17.61 42 35029 275196 79434121
Hand deformity 34.56 17.61 3 35068 103916 79605401
Glossodynia 34.32 17.61 3 35068 103334 79605983
Dysstasia 34.16 17.61 51 35020 27695 79681622
Multiple organ dysfunction syndrome 33.86 17.61 6 35065 120240 79589077
Blood creatinine increased 33.69 17.61 13 35058 155044 79554273
Hypoglycaemia 33.60 17.61 3 35068 101591 79607726
Incontinence 33.40 17.61 36 35035 14128 79695189
Lymphopenia 33.19 17.61 53 35018 30504 79678813
Hair texture abnormal 32.65 17.61 20 35051 3514 79705803
Cardiac failure congestive 32.53 17.61 11 35060 142391 79566926
Speech disorder 32.35 17.61 73 34998 54372 79654945
Respiratory failure 32.00 17.61 20 35051 180891 79528426
Cardiac arrest 31.88 17.61 18 35053 172078 79537239
Rhabdomyolysis 31.67 17.61 4 35067 103127 79606190
Cardio-respiratory arrest 31.47 17.61 5 35066 108505 79600812
Lower respiratory tract infection 31.28 17.61 9 35062 129211 79580106
Oedema peripheral 31.25 17.61 39 35032 252249 79457068
Asthenia 31.19 17.61 353 34718 511336 79197981
Onychoclasis 30.94 17.61 23 35048 5555 79703762
Temperature intolerance 30.84 17.61 29 35042 9676 79699641
Renal failure 30.63 17.61 26 35045 200942 79508375
Dysgraphia 30.24 17.61 20 35051 4012 79705305
Neuralgia 29.74 17.61 53 35018 33331 79675986
Gastrointestinal haemorrhage 29.52 17.61 14 35057 147705 79561612
Dehydration 29.07 17.61 40 35031 248147 79461170
Cardiac failure 28.96 17.61 16 35055 154826 79554491
Dizziness 28.48 17.61 355 34716 526086 79183231
Systemic lupus erythematosus 28.30 17.61 9 35062 121140 79588177
Heteroplasia 28.16 17.61 5 35066 10 79709307
Pulmonary oedema 28.15 17.61 3 35068 88251 79621066
Hemiparesis 28.08 17.61 52 35019 33681 79675636
Joint swelling 27.73 17.61 53 35018 288593 79420724
Hypoxia 27.28 17.61 6 35065 103237 79606080
Septic shock 27.17 17.61 10 35061 122791 79586526
Sensory loss 27.15 17.61 31 35040 12960 79696357
Back pain 26.93 17.61 227 34844 303953 79405364
Hypokalaemia 26.77 17.61 15 35056 144025 79565292
Delirium 26.68 17.61 3 35068 84624 79624693
Wheezing 26.67 17.61 9 35062 116655 79592662
Intentional overdose 26.35 17.61 7 35064 105953 79603364
Urinary tract infection 25.99 17.61 208 34863 274304 79435013
Interstitial lung disease 25.20 17.61 9 35062 112591 79596726
Wheelchair user 24.80 17.61 21 35050 6111 79703206
Blood pressure increased 24.47 17.61 168 34903 211192 79498125
Oedema 24.40 17.61 11 35060 119569 79589748
Electrocardiogram QT prolonged 24.40 17.61 5 35066 90381 79618936
Hypertension 24.21 17.61 237 34834 330755 79378562
Drug intolerance 24.07 17.61 50 35021 264069 79445248
Trichorrhexis 23.55 17.61 10 35061 813 79708504
Nausea 23.43 17.61 568 34503 956628 78752689
Influenza like illness 23.30 17.61 77 34994 71630 79637687
Oxygen saturation decreased 23.19 17.61 14 35057 129033 79580284
Ascites 23.03 17.61 3 35068 75559 79633758
Hepatic enzyme increased 22.85 17.61 148 34923 182462 79526855
Anaphylactic reaction 21.86 17.61 5 35066 83738 79625579
Depressed level of consciousness 21.16 17.61 8 35063 96644 79612673
Stomatitis 21.14 17.61 20 35051 146737 79562580
Bladder discomfort 21.02 17.61 9 35062 747 79708570
Confusional state 20.79 17.61 71 35000 317926 79391391
Gait inability 20.71 17.61 65 35006 58852 79650465
Hallucination 20.70 17.61 6 35065 85739 79623578
Helicobacter infection 20.69 17.61 3 35068 69701 79639616
Deep vein thrombosis 20.52 17.61 14 35057 120905 79588412
Cerebral disorder 20.44 17.61 18 35053 5520 79703797
Syncope 19.94 17.61 30 35041 179419 79529898
Lipase increased 19.89 17.61 30 35041 16436 79692881
Weight decreased 19.81 17.61 241 34830 354957 79354360
Testicular seminoma (pure) stage I 19.29 17.61 4 35067 23 79709294
Intervertebral disc protrusion 19.14 17.61 36 35035 23585 79685732
Heavy menstrual bleeding 19.06 17.61 27 35044 13984 79695333
Sepsis 18.40 17.61 59 35012 269369 79439948
Intentional dose omission 18.36 17.61 21 35050 8796 79700521
Hospitalisation 18.25 17.61 86 34985 94150 79615167
Vertigo 18.00 17.61 69 35002 69013 79640304
Osteoarthritis 17.86 17.61 8 35063 87301 79622016
Wound 17.73 17.61 15 35056 116164 79593153
Meningoencephalitis herpetic 17.73 17.61 11 35060 1978 79707339
Anal incontinence 17.69 17.61 30 35041 18138 79691179

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
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|

DiseaseRelationSNOMED_IDDOID
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 levelDissociation constantType (acidic/basic)
pKa1 5.59 acidic
pKa2 10.61 acidic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent 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 strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
14MG TERIFLUNOMIDE WATSON LABS TEVA A209549 July 27, 2018 DISCN TABLET ORAL Sept. 8, 2023 PATENT CHALLENGE
7MG 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
7MG 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
7MG 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
7MG 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
7MG 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
7MG 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
7MG 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
7MG 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
7MG 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
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:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Dihydroorotate dehydrogenase (quinone), mitochondrial Enzyme INHIBITOR Ki 7.52 CHEMBL CHEMBL
Dihydrofolate reductase Enzyme IC50 6.41 CHEMBL
Dihydroorotate dehydrogenase (quinone), mitochondrial Enzyme IC50 8.05 CHEMBL
Dihydroorotate dehydrogenase (quinone), mitochondrial Enzyme IC50 7.16 CHEMBL
Dihydroorotate dehydrogenase Enzyme Ki 4.66 CHEMBL
Dihydroorotate dehydrogenase Enzyme IC50 4.30 CHEMBL

External reference:

IDSource
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
365635 MMSL
d07905 MMSL
014643 NDDF
703785006 SNOMEDCT_US
703786007 SNOMEDCT_US
C1718383 UMLSCUI
54684141 PUBCHEM_CID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
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
Teriflunomide HUMAN PRESCRIPTION DRUG LABEL 1 0480-3157 TABLET, FILM COATED 7 mg ORAL ANDA 28 sections
Teriflunomide HUMAN PRESCRIPTION DRUG LABEL 1 0781-5747 TABLET, FILM COATED 7 mg ORAL ANDA 29 sections
Teriflunomide HUMAN PRESCRIPTION DRUG LABEL 1 0781-5755 TABLET, FILM COATED 14 mg ORAL ANDA 29 sections
Teriflunomide HUMAN PRESCRIPTION DRUG LABEL 1 16729-399 TABLET, FILM COATED 7 mg ORAL ANDA 30 sections
Teriflunomide HUMAN PRESCRIPTION DRUG LABEL 1 16729-400 TABLET, FILM COATED 14 mg ORAL ANDA 30 sections
Teriflunomide HUMAN PRESCRIPTION DRUG LABEL 1 31722-246 TABLET, FILM COATED 7 mg ORAL ANDA 28 sections
Teriflunomide HUMAN PRESCRIPTION DRUG LABEL 1 31722-247 TABLET, FILM COATED 14 mg ORAL ANDA 28 sections
Teriflunomide HUMAN PRESCRIPTION DRUG LABEL 1 42291-830 TABLET, FILM COATED 7 mg ORAL ANDA 28 sections
Teriflunomide HUMAN PRESCRIPTION DRUG LABEL 1 42291-831 TABLET, FILM COATED 14 mg ORAL ANDA 28 sections
Teriflunomide HUMAN PRESCRIPTION DRUG LABEL 1 43598-281 TABLET, FILM COATED 14 mg ORAL ANDA 26 sections
Teriflunomide HUMAN PRESCRIPTION DRUG LABEL 1 43598-282 TABLET, FILM COATED 7 mg ORAL ANDA 26 sections
TERIFLUNOMIDE Human Prescription Drug Label 1 46708-313 TABLET, FILM COATED 7 mg ORAL ANDA 29 sections
TERIFLUNOMIDE Human Prescription Drug Label 1 46708-314 TABLET, FILM COATED 14 mg ORAL ANDA 29 sections
Teriflunomide HUMAN PRESCRIPTION DRUG LABEL 1 51991-881 TABLET 7 mg ORAL ANDA 33 sections
Teriflunomide HUMAN PRESCRIPTION DRUG LABEL 1 51991-882 TABLET 14 mg ORAL ANDA 33 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 58468-0210 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 59651-054 TABLET 7 mg ORAL ANDA 28 sections
Teriflunomide Human Prescription Drug Label 1 59651-055 TABLET 14 mg ORAL ANDA 28 sections
teriflunomide HUMAN PRESCRIPTION DRUG LABEL 1 60505-4477 TABLET, FILM COATED 7 mg ORAL ANDA 29 sections
teriflunomide HUMAN PRESCRIPTION DRUG LABEL 1 60505-4478 TABLET, FILM COATED 14 mg ORAL ANDA 29 sections
TERIFLUNOMIDE Human Prescription Drug Label 1 62332-313 TABLET, FILM COATED 7 mg ORAL ANDA 29 sections