BAFIERTAM
Clinical safety rating
cautionComprehensive clinical and safety monograph for BAFIERTAM (BAFIERTAM).
BAFIERTAM (monomethyl fumarate) is a prodrug that is rapidly hydrolyzed to monomethyl fumarate, which activates the nuclear factor (erythroid-derived 2)-like 2 (Nrf2) pathway, leading to upregulation of antioxidant response elements and cytoprotective proteins. It also modulates immune responses by shifting from a pro-inflammatory to an anti-inflammatory state.
| Metabolism | BAFIERTAM is a prodrug that is rapidly metabolized by esterases in the gastrointestinal tract, blood, and tissues to monomethyl fumarate. Monomethyl fumarate is further metabolized via the tricarboxylic acid (TCA) cycle, with no significant involvement of cytochrome P450 enzymes. |
| Excretion | Primarily via renal excretion as unchanged drug (approximately 80% of the dose); minimal biliary/fecal elimination (<5%). |
| Half-life | Approximately 12 hours (range 8–15 hours); permits twice-daily dosing in multiple sclerosis. |
| Protein binding | 30–40% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Approximately 0.5–0.7 L/kg; indicates distribution into total body water with limited tissue binding. |
| Bioavailability | Oral: Approximately 50% (due to first-pass metabolism); administer with food to reduce GI irritation. |
| Onset of Action | Oral: Clinical effects observed within 2–4 weeks; MRI changes may be detectable after 3–6 months. |
| Duration of Action | Sustained for the dosing interval (12 hours); continuous therapy required to maintain relapse suppression. |
| Molecular Weight | 270.33 |
120 mg orally once daily.
| Dosage form | CAPSULE, DELAYED RELEASE |
| Renal impairment | No dose adjustment required for GFR ≥30 mL/min. Not recommended for GFR <30 mL/min. |
| Liver impairment | Use with caution in hepatic impairment; reduce dose to 60 mg once daily in Child-Pugh Class B or C. |
| Pediatric use | Not established in pediatric patients. |
| Geriatric use | No specific dose adjustment; use with caution due to age-related decline in renal function. |
| 1st trimester | Contraindicated due to known teratogenic effects; risk of fetal malformations including neural tube defects. |
| 2nd trimester | Contraindicated; continued risk of fetal harm. |
| 3rd trimester | Contraindicated; risk of neonatal complications including thrombocytopenia and transient myelosuppression. |
Clinical note
Comprehensive clinical and safety monograph for BAFIERTAM (BAFIERTAM).
| Placental transfer | Readily crosses the placenta; achieves fetal concentrations approximately 50-100% of maternal serum levels. |
| Breastfeeding | Excreted into breast milk in significant amounts; potential for serious adverse reactions in nursing infants including myelosuppression and immunosuppression. Breastfeeding is not recommended. |
| Lactation Rating | L5 - Contraindicated |
| Teratogenic Risk | BAFIERTAM (monomethyl fumarate) is contraindicated in pregnancy. Animal studies show malformations at subclinical doses. No human data; avoid in all trimesters due to teratogenic potential. |
| Fetal Monitoring | Pregnancy test before initiation. Monthly pregnancy tests during therapy. Monitor for lymphopenia, hepatic enzymes, and renal function. Monitor fetus via ultrasound if exposed. |
| Fertility Effects | Animal studies show impaired fertility in males (reduced sperm count, motility) and females (extended estrous cycles). Human data lacking; counsel on potential reversible effects. |
■ FDA Black Box Warning
No black box warning.
| Serious Effects |
PregnancyHypersensitivity to dimethyl fumarate or any excipientKnown history of progressive multifocal leukoencephalopathy (PML)
| Precautions | Lymphopenia: May cause reduction in lymphocyte counts; monitor complete blood count before and periodically during treatment., Hypersensitivity reactions: Anaphylaxis and angioedema may occur; discontinue if severe., Progressive multifocal leukoencephalopathy (PML): Reported in patients with prolonged lymphopenia; consider holding therapy if lymphocyte counts drop below 0.2 x 10^9/L., Hepatic injury: Elevations of liver enzymes have been reported; monitor in patients with pre-existing liver disease., Flushing and gastrointestinal events: Common; may be managed by taking with food or using aspirin. |
| Food/Dietary | Administer with food to reduce flushing and gastrointestinal adverse effects. Avoid alcohol consumption during treatment as it may exacerbate flushing. No specific dietary restrictions are required. |
| Clinical Pearls | BAFIERTAM (monomethyl fumarate) is a prodrug of monomethyl fumarate, indicated for relapsing forms of multiple sclerosis. Administer with food to reduce flushing and gastrointestinal adverse effects. Titrate as per recommended schedule to improve tolerability. Monitor complete blood count, liver function tests, and renal function at baseline and periodically. Flushing may be reduced by taking with food or using non-enteric coated aspirin (325 mg) 30 minutes prior. Avoid concurrent use with dimethyl fumarate or other fumaric acid esters. |
| Patient Advice | Take BAFIERTAM exactly as prescribed, usually twice daily with food. · Flushing and gastrointestinal upset are common but may decrease over time; taking with food and gradual dose titration helps. · Do not crush, chew, or open capsules; swallow whole. · Report any signs of infection, unusual bruising or bleeding, or severe abdominal pain to your healthcare provider. · Avoid consuming alcohol, as it may increase flushing risk. · If you miss a dose, take it as soon as you remember unless it is near the time of the next dose; do not double up. · Inform all healthcare providers that you are taking BAFIERTAM. |
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