Teriflunomide

What is Teriflunomide

Teriflunomide is an oral pyrimidine synthesis inhibitor, and an active metabolite of leflunomide.

Teriflunomide is indicated for the treatment of relapsing forms of multiple sclerosis, including clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease.

Teriflunomide inhibits dihydroorotate dehydrogenase, which is a mitochondrial enzyme involved in de novo pyrimidine synthesis.

In clinical trials of up to 40 months duration in patients with relapsing forms of multiple sclerosis, teriflunomide consistently demonstrated statistically significant reductions in annual relapse rates and the relative risk of disability progression compared to placebo.

Changes in total lesion volume of T2 and hypointense T1 lesions were also significantly lower with teriflunomide compared to placebo.

The drug labeling carries boxed warnings regarding the risk for hepatotoxicity and a risk for teratogenicity.

Due to the long half-life, an accelerated drug elimination procedure should be used when there is a need to lower the teriflunomide concentration due to potential adverse effects.

Teriflunomide was FDA-approved in 2012

Brand Name

AUBAGIO

Indications

  • multiple sclerosis

For the treatment of relapsing forms of multiple sclerosis (MS), including clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease

Side Effects

  1. abdominal pain
  2. agranulocytosis
  3. alopecia
  4. anaphylactoid reactions
  5. angioedema
  6. arthralgia
  7. back pain
  8. carpal tunnel syndrome
  9. cystitis
  10. diarrhea
  11. dizziness
  12. Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS)
  13. dyspepsia
  14. dyspnea
  15. elevated hepatic enzymes
  16. eosinophilic pneumonia
  17. erythema multiforme
  18. fatigue
  19. fetal death
  20. headache
  21. hepatic failure
  22. hepatotoxicity
  23. hyperbilirubinemia
  24. hyperkalemia
  25. hyperreflexia
  26. hypertension
  27. hyperuricemia
  28. hypoesthesia
  29. hypophosphatemia
  30. immunosuppression
  31. infection
  32. influenza
  33. insomnia
  34. jaundice
  35. lymphopenia
  36. myasthenia
  37. myocardial infarction
  38. nausea
  39. neutropenia
  40. pancreatitis
  41. pancytopenia
  42. paresthesias
  43. peripheral neuropathy
  44. pharyngitis
  45. pneumonitis
  46. pruritus
  47. psoriasis
  48. pulmonary fibrosis
  49. rash
  50. renal failure (unspecified)
  51. Stevens-Johnson syndrome
  52. teratogenesis
  53. thrombocytopenia
  54. toxic epidermal necrolysis
  55. urticaria

Monitoring Parameters

  • CBC with differential
  • LFTs
  • pregnancy testing
  • serum bilirubin
  • tuberculin skin test

Contraindications

  • agranulocytosis
  • alcoholism
  • bone marrow suppression
  • breast-feeding
  • chemotherapy
  • children
  • contraception requirements
  • diabetes mellitus
  • eosinophilic pneumonia
  • geriatric
  • hepatic disease
  • hepatitis
  • hepatotoxicity
  • hypertension
  • immunosuppression
  • infection
  • intrauterine fetal death
  • jaundice
  • male-mediated teratogenicity
  • peripheral neuropathy
  • pneumonitis
  • pregnancy
  • pregnancy testing
  • pulmonary disease
  • pulmonary fibrosis
  • reproductive risk
  • sarcoidosis
  • serious hypersensitivity reactions or anaphylaxis
  • serious rash
  • thrombocytopenia
  • tuberculosis
  • vaccination

Interactions

  • Abacavir; Lamivudine, 3TC; Zidovudine, ZDV
  • Acetaminophen; Aspirin, ASA; Caffeine
  • Acetaminophen; Butalbital; Caffeine
  • Acetaminophen; Butalbital; Caffeine; Codeine
  • Acetaminophen; Caffeine
  • Acetaminophen; Caffeine; Dihydrocodeine
  • Acetaminophen; Caffeine; Magnesium Salicylate; Phenyltoloxamine
  • Acetaminophen; Caffeine; Phenyltoloxamine; Salicylamide
  • Alogliptin; Pioglitazone
  • Alosetron
  • Alpelisib
  • Amlodipine; Atorvastatin
  • Anagrelide
  • Aspirin, ASA; Butalbital; Caffeine
  • Aspirin, ASA; Butalbital; Caffeine; Codeine
  • Aspirin, ASA; Caffeine; Dihydrocodeine
  • Aspirin, ASA; Caffeine; Orphenadrine
  • Aspirin, ASA; Pravastatin
  • Atorvastatin
  • Atorvastatin; Ezetimibe
  • Bacillus Calmette-Guerin Vaccine, BCG
  • Baricitinib
  • Bosentan
  • Bupivacaine; Lidocaine
  • Caffeine
  • Caffeine; Ergotamine
  • Cefaclor
  • Charcoal
  • Cholestyramine
  • Cimetidine
  • Cinacalcet
  • Ciprofloxacin
  • Clofarabine
  • Clozapine
  • Cycloserine
  • Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir
  • Dichlorphenamide
  • Dienogest; Estradiol valerate
  • Diphenhydramine; Naproxen
  • Drospirenone
  • Drospirenone; Estradiol
  • Drospirenone; Ethinyl Estradiol
  • Drospirenone; Ethinyl Estradiol; Levomefolate
  • Duloxetine
  • Elagolix
  • Elagolix; Estradiol; Norethindrone acetate
  • Elbasvir; Grazoprevir
  • Eltrombopag
  • Eluxadoline
  • Esomeprazole; Naproxen
  • Estradiol; Levonorgestrel
  • Estradiol; Norethindrone
  • Estradiol; Norgestimate
  • Ethinyl Estradiol
  • Ethinyl Estradiol; Desogestrel
  • Ethinyl Estradiol; Ethynodiol Diacetate
  • Ethinyl Estradiol; Etonogestrel
  • Ethinyl Estradiol; Levonorgestrel
  • Ethinyl Estradiol; Levonorgestrel; Ferrous bisglycinate
  • Ethinyl Estradiol; Levonorgestrel; Folic Acid; Levomefolate
  • Ethinyl Estradiol; Norelgestromin
  • Ethinyl Estradiol; Norethindrone
  • Ethinyl Estradiol; Norethindrone Acetate
  • Ethinyl Estradiol; Norethindrone Acetate; Ferrous fumarate
  • Ethinyl Estradiol; Norethindrone; Ferrous fumarate
  • Ethinyl Estradiol; Norgestimate
  • Ethinyl Estradiol; Norgestrel
  • Ezetimibe; Simvastatin
  • Fluvastatin
  • Furosemide
  • Glecaprevir; Pibrentasvir
  • Glimepiride; Pioglitazone
  • Glimepiride; Rosiglitazone
  • HMG-CoA reductase inhibitors
  • Influenza Virus Vaccine
  • Intranasal Influenza Vaccine
  • Isoniazid, INH; Pyrazinamide, PZA; Rifampin
  • Isoniazid, INH; Rifampin
  • Ketoprofen
  • Lamivudine, 3TC; Zidovudine, ZDV
  • Lansoprazole; Naproxen
  • Leflunomide
  • Letermovir
  • Leuprolide; Norethindrone
  • Levonorgestrel
  • Lidocaine
  • Lidocaine; Prilocaine
  • Live Vaccines
  • Loperamide
  • Loperamide; Simethicone
  • Lovastatin
  • Lovastatin; Niacin
  • Maraviroc
  • Measles Virus; Mumps Virus; Rubella Virus; Varicella Virus Vaccine, Live
  • Measles/Mumps/Rubella Vaccines, MMR
  • Mestranol; Norethindrone
  • Metformin; Pioglitazone
  • Metformin; Repaglinide
  • Metformin; Rosiglitazone
  • Methotrexate
  • Mexiletine
  • Mitoxantrone
  • Nanoparticle Albumin-Bound Paclitaxel
  • Naproxen
  • Naproxen; Pseudoephedrine
  • Naproxen; Sumatriptan
  • Nateglinide
  • Niacin; Simvastatin
  • Norethindrone
  • Norgestrel
  • Ocrelizumab
  • Ombitasvir; Paritaprevir; Ritonavir
  • Oral Contraceptives
  • Ozanimod
  • Paclitaxel
  • Penicillin G
  • Penicillin G Benzathine
  • Penicillin G Benzathine; Penicillin G Procaine
  • Penicillin G Procaine
  • Pioglitazone
  • Pitavastatin
  • Pravastatin
  • Propafenone
  • Quinine
  • Rasagiline
  • Repaglinide
  • Revefenacin
  • Rifampin
  • Rifaximin
  • Riluzole
  • Rimegepant
  • Ropinirole
  • Rosiglitazone
  • Rosuvastatin
  • Rotavirus Vaccine
  • Rubella Virus Vaccine Live
  • Segesterone Acetate; Ethinyl Estradiol
  • Selegiline
  • Selexipag
  • Simeprevir
  • Simvastatin
  • Simvastatin; Sitagliptin
  • Smallpox and Monkeypox Vaccine, Live, Nonreplicating
  • Smallpox Vaccine, Vaccinia Vaccine
  • Sofosbuvir; Velpatasvir
  • Sofosbuvir; Velpatasvir; Voxilaprevir
  • Talazoparib
  • Terbinafine
  • Theophylline, Aminophylline
  • Tizanidine
  • Topotecan
  • Tucatinib
  • Typhoid Vaccine
  • Ubrogepant
  • Varicella-Zoster Virus Vaccine, Live
  • Warfarin
  • Yellow Fever Vaccine, Live
  • Zidovudine, ZDV
15585

Sign up to receive the trending updates and tons of Health Tips

Join SeekhealthZ and never miss the latest health information

15856
Scroll to Top