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
- abdominal pain
- agranulocytosis
- alopecia
- anaphylactoid reactions
- angioedema
- arthralgia
- back pain
- carpal tunnel syndrome
- cystitis
- diarrhea
- dizziness
- Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS)
- dyspepsia
- dyspnea
- elevated hepatic enzymes
- eosinophilic pneumonia
- erythema multiforme
- fatigue
- fetal death
- headache
- hepatic failure
- hepatotoxicity
- hyperbilirubinemia
- hyperkalemia
- hyperreflexia
- hypertension
- hyperuricemia
- hypoesthesia
- hypophosphatemia
- immunosuppression
- infection
- influenza
- insomnia
- jaundice
- lymphopenia
- myasthenia
- myocardial infarction
- nausea
- neutropenia
- pancreatitis
- pancytopenia
- paresthesias
- peripheral neuropathy
- pharyngitis
- pneumonitis
- pruritus
- psoriasis
- pulmonary fibrosis
- rash
- renal failure (unspecified)
- Stevens-Johnson syndrome
- teratogenesis
- thrombocytopenia
- toxic epidermal necrolysis
- 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
