Overview
11 DESCRIPTION BAFIERTAM contains the active ingredient monomethyl fumarate, which is an unsaturated monomethyl ester. It is also known by its chemical name, fumaric acid monomethyl ester, (C 5 H 6 O 4 ). It has the following structure: Monomethyl fumarate is a white to off-white powder that is highly soluble in water with a molecular mass of 130.10.
Mechanism of Action
12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action The mechanism by which monomethyl fumarate (MMF) exerts its therapeutic effect in multiple sclerosis is unknown. MMF has been shown to activate the Nuclear factor (erythroid-derived 2) like 2 (Nrf2) pathway in vitro and in vivo in animals and humans. The Nrf2 pathway is involved in the cellular response to oxidative stress. MMF has been identified as a nicotinic acid receptor agonist in vitro . 12.2 Pharmacodynamics Potential to prolong the QT interval In a placebo controlled thorough QT study performed in healthy subjects with dimethyl fumarate [the prodrug of BAFIERTAM], there was no evidence that dimethyl fumarate caused QT interval prolongation of clinical significance (i.e.
Indications
- 1 INDICATIONS AND USAGE BAFIERTAM is indicated for the treatment of relapsing forms of multiple sclerosis (MS), to include clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease, in adults. BAFIERTAM is indicated for the treatment of relapsing forms of multiple sclerosis (MS), to include clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease, in adults. ( 1 )
Common Doses
- 95 mg
- 190 mg
- 325 mg
Dosage
2 DOSAGE AND ADMINISTRATION Blood tests are required prior to initiation of BAFIERTAM. ( 2.1 ) Starting dose: 95 mg twice a day, orally, for 7 days ( 2.2 ) Maintenance dose after 7 days: 190 mg (administered as two 95 mg capsules) twice a day, orally ( 2.2 ) Swallow BAFIERTAM capsules whole and intact. Do not crush, chew, or mix contents with food. ( 2.3 ) Take BAFIERTAM with or without food. ( 2.3 ) 2.1 Blood Tests Prior to Initiation of BAFIERTAM Obtain the following prior to treatment with BAFIERTAM: A complete blood cell count (CBC), including lymphocyte count [see Warnings and...
Contraindications
- 4 CONTRAINDICATIONS BAFIERTAM is contraindicated in patients: with known hypersensitivity to monomethyl fumarate, dimethyl fumarate, diroximel fumarate, or to any of the excipients of BAFIERTAM. Reactions may include anaphylaxis or angioedema [see Warnings and Precautions ( 5.1 )]. taking dimethyl fumarate or diroximel fumarate [see Drug Interactions ( 7.1 )]. Known hypersensitivity to monomethyl fumarate, dimethyl fumarate, diroximel fumarate, or any of the excipients of BAFIERTAM Co-administration with dimethyl fumarate or diroximel fumarate ( 4 )
Side Effects
- 6 ADVERSE REACTIONS The following clinically significant adverse reactions are described elsewhere in the labeling: Anaphylaxis and Angioedema [see Warnings and Precautions ( 5.1 )] Progressive Multifocal Leukoencephalopathy [see Warnings and Precautions ( 5.2 ) ] Herpes Zoster and Other Serious Opportunistic Infections [see Warnings and Precautions ( 5.3 ) ] Lymphopenia [see Warnings and Precautions ( 5.4 )] Liver Injury [see Warnings and Precautions ( 5.5 )] Flushing [see Warnings and Precautions ( 5.6 )] Serious Gastrointestinal Reactions [see Warnings and Precautions ( 5.
Interactions
- 7 DRUG INTERACTIONS 7.1 Concomitant Dimethyl Fumarate or Diroximel Fumarates Both dimethyl fumarate and diroximel fumarate are metabolized to monomethyl fumarate. Therefore, BAFIERTAM is contraindicated in patients currently taking dimethyl fumarate or diroximel fumarate. BAFIERTAM may be initiated the day following discontinuation of either of these drugs.