BETHESDA, MD 13 September 2012—Sanofi and Genzyme on September 12 announced (PDF) the approval of teriflunomide oral tablets for the treatment of patients with relapsing forms of multiple sclerosis (MS).
Teriflunomide is the principal active metabolite of leflunomide, which was approved in 1998 for the treatment of rheumatoid arthritis. Teriflunomide will be marketed under the brand name Aubagio. A launch date for the product has not yet been announced.
As with leflunomide, the labeling (PDF) for teriflunomide includes a boxed warning about teratogenicity and the risk for liver injury in patients who use the drug. Patients treated with teriflunomide should undergo liver-function tests before initiating therapy and monthly for at least six months afterward.
Kidney function should be monitored in patients who show signs of acute renal failure or hyperkalemia.
If teriflunomide-associated liver injury is suspected, the labeling recommends administering cholestyramine or activated charcoal for 11 days to accelerate the elimination of the drug. Without this intervention, teriflunomide persists in plasma for eight months, on average, and can take up to two years to decline to less than 0.02 mg/L in some patients, the labeling states.
Before initiating teriflunomide therapy, patients should be tested for latent tuberculosis and undergo a complete blood count and blood pressure measurement. Patients should be monitored for signs and symptoms of infection and for hypertension during treatment with the drug.
Teriflunomide is contraindicated in pregnant women and women of childbearing age who are not using a reliable method of contraception. The labeling recommends that all women of childbearing potential who discontinue teriflunomide immediately follow an accelerated elimination protocol using cholestyramine or activated charcoal.
Information about the potential risks associated with teriflunomide is included in a medication guide that is part of the drug's labeling.
In placebo-controlled clinical trials, teriflunomide reduced relapse rates and time to disability progression in patients with MS.
The most common adverse events reported in clinical trial participants who received teriflunomide were abnormal liver-function test results, alopecia, nausea, diarrhea, influenza, and paresthesia.
The recommended dosage of teriflunomide is 7 or 14 mg taken once daily with or without food.
The drug will be available as 7- and 14-mg tablets packaged in cartons containing one 5-tablet blister card or two 14-tablet blister cards. Teriflunomide should be stored at controlled room temperature.