Effectiveness and Tolerability of Colesevelam HCl for Accelerated Elimination of Teriflunomide in Healthy Participants

Teriflunomide, a once-daily oral immunomodulator approved for the treatment of relapsing-remitting multiple sclerosis, demonstrated efficacy on clinical and magnetic resonance imaging measures of disease activity and a consistent and manageable safety profile in clinical trials.1–5 Teriflunomide is contraindicated in pregnancy because data from animal studies (observed in rats and rabbits) suggest the potential for embryotoxic and teratogenic effects5; however, to date, there has been no human signal of teratogenticity.6 Teriflunomide undergoes enterohepatic recycling in which it is excreted into bile and transported to the small intestine, where it is reabsorbed.7,8 Because the mean elimination half-life of teriflunomide is approximately 19 days, it may take an average of 8 months (up to 2 years owing to individual variation in substance clearance) once dosing is halted for plasma concentrations to decrease to <0.02 μg/mL, a concentration expected to confer minimal embryo-fetal risk to humans based on animal data.5 The following accelerated elimination procedure (AEP) is available for patients taking teriflunomide who become pregnant or who are planning a pregnancy, or in any case in which it is medically desirable to rapidly reduce the plasma concentrations of teriflunomide5: