From Leflunomide to Teriflunomide: Drug Development and Immunosuppressive Oral Drugs in the Treatment of Multiple Sclerosis

Title:From Leflunomide to Teriflunomide: Drug Development and Immunosuppressive Oral Drugs in the Treatment of Multiple Sclerosis

Volume: 15 Issue: 6

Author(s): Lilian Aly, Bernhard Hemmer*Thomas Korn*

Affiliation:

• Department of Neurology, Technische Universität München, Ismaningerstraße 22, 81675 Munich,Germany

• Department of Neurology, Technische Universität München, Ismaningerstraße 22, 81675 Munich,Germany

Keywords: Disease modifying therapy, immunosuppression, leflunomide, multiple sclerosis, oral, teriflunomide.

Abstract: Background: Immunosuppressive drugs have been used in the treatment of multiple sclerosis (MS) for a long time. Today, orally available second generation immunosuppressive agents have been approved or are filed for licensing as MS therapeutics. Due to semi-selective targeting of cellular processes, these second-generation immunosuppressive compounds might rather be immunomodulatory. For example, Teriflunomide inhibits the de novo pyrimidine synthesis and thus only targets rapidly proliferating cells, including lymphocytes. It is used as first line disease modifying therapy (DMT) in relapsing-remitting MS (RRMS).

Methods: Review of online content related to oral immunosuppressants in MS with an emphasis on Teriflunomide.

Results: Teriflunomide and Cladribine are second-generation immunosuppressants that are efficient in the treatment of MS patients. For Teriflunomide, a daily dose of 14 mg reduces the annualized relapse rate (ARR) by more than 30% and disability progression by 30% compared to placebo. Cladribine reduces the ARR by about 50% compared to placebo but has not yet been licensed due to unresolved safety concerns. We also discuss the significance of older immunosuppressive compounds including Azathioprine, Mycophenolate mofetile, and Cyclophosphamide in current MS therapy.

Conclusion: Teriflunomide has shown a favorable safety and efficacy profile in RRMS and is a therapeutic option for a distinct group of adult patients with RRMS.

Cite this article as:

Aly Lilian, Hemmer Bernhard*, Korn Thomas*, From Leflunomide to Teriflunomide: Drug Development and Immunosuppressive Oral Drugs in the Treatment of Multiple Sclerosis, Current Neuropharmacology 2017; 15 (6) . https://dx.doi.org/10.2174/1570159X14666161208151525

DOI https://dx.doi.org/10.2174/1570159X14666161208151525	Print ISSN 1570-159X
Publisher Name Bentham Science Publisher	Online ISSN 1875-6190