BAFIERTAM: the new-generation fumarate

Prodrugs and active drugs: oral fumarate options for patients with relapsing multiple sclerosis (MS)

The introduction of oral agents in the last decade has given patients with relapsing MS new choices for disease-modifying therapies. Tecfidera® (dimethyl fumarate), launched in 2013, was the first fumarate to be developed; it is the most used oral treatment for relapsing MS, and has established efficacy and well-understood safety1-4

Today, there are 3 oral fumarate options, 2 of which are prodrugs. While prodrugs help deliver the pharmacologically active agent to its target, they first require metabolic conversion. Dimethyl fumarate (DMF), for example, requires conversion in the gastrointestinal (GI) tract to the active metabolite monomethyl fumarate (MMF).5-8

The conversion from DMF or diroximel fumarate (DRF), another prodrug, produces metabolites9

There have been no head-to-head studies comparing MMF and DRF.

BAFIERTAM contains the active metabolite of DMF and DRF, both of which require conversion in the duodenum by esterases to MMF.5,7

Unlike DMF, which is converted to MMF in the GI tract, BAFIERTAM achieves a direct therapeutic effect, requiring a lower dosage of administration.5

BAFIERTAM 190 mg was FDA approved by demonstrating that its dose was bioequivalent to DMF 240 mg following oral administration: MMF (380 mg/day) is bioequivalent to DMF (480 mg/day). At the approved dose, it is readily absorbed and produces the same plasma levels of MMF as those ultimately produced by DMF.5

There are no alcohol or dietary restrictions for BAFIERTAM, and no restrictions on administration of BAFIERTAM to patients with renal failure.5

BAFIERTAM is contraindicated in patients currently taking DMF or DRF. BAFIERTAM may be initiated the day following discontinuation of either of these drugs.5

Prescribe BAFIERTAM for your patients with relapsing forms of MS who could benefit from a new-generation fumarate treatment option.


  1. Center for Drug Evaluation and Research. Tecfidera NDA approval. March 27, 2013.
  2. Mills EA, Ogrodnik MA, Plave A, Mao-Draayer Y. Emerging understanding of the mechanism of action for dimethyl fumarate in the treatment of multiple sclerosis. Front Neurol. 2018;9(5):1-8.
  3. Alroughani R, Ahmed SF, Behbehani R, Al-Hashel J. Effectiveness and safety of dimethyl fumarate treatment in relapsing multiple sclerosis patients: real-world evidence. Neurol Ther. 2017;6(2):189-196.
  4. Dubey D, Kieseier BC, Hartung HP, et al. Dimethyl fumarate in relapsing-remitting multiple sclerosis: rationale, mechanisms of action, pharmacokinetics, efficacy and safety. Expert Rev Neurother. 2015;15(4):339-346.
  5. BAFIERTAM. Prescribing information. Banner Life Sciences LLC; 2020.
  6. Tecfidera. Prescribing information. Biogen Inc; 2020.
  7. Vumerity. Prescribing information. Biogen Inc; 2020.
  8. Rautio J, Meanwell NA, Di L, Hageman MJ. The expanding role of prodrugs in contemporary drug design and development. Nat Rev Drug Discov. 2018;17(8):559-587.
  9. Palte MJ, Wehr A, Tawa M, et al. Improving the gastrointestinal tolerability of fumaric acid esters: early findings on gastrointestinal events with diroximel fumarate in patients with relapsing-remitting multiple sclerosis from the phase 3, open-label EVOLVE-MS-1 study. Adv Ther. 2019;36(11):3154-3165.