monomethyl fumarate (Rx)

Brand and Other Names:Bafiertam
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

capsule, delayed-release

  • 95mg
  • 190mg of monomethyl fumarate is bioequivalent to 240mg of the prodrug dimethyl fumarate

Multiple sclerosis

Indicated for relapsing forms of multiple sclerosis (MS), to include clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease

Starting dose: 95 mg PO BID for 7 days

Maintenance dose after 7 days: 190 mg PO BID

Unable to tolerate the maintenance dose

  • Consider temporarily reducing dosage to 95 mg PO BID; within 4 weeks, resume at 190 mg PO BID
  • Unable to tolerate return to the maintenance dose: Consider discontinuing treatment
  • Administration of nonenteric-coated aspirin (up to a 325-mg dose) 30 min before administration may reduce the incidence or severity of flushing

Dosage Modifications

Renal or hepatic impairment

  • No studies have been conducted
  • However, neither condition would be expected to affect plasma exposure to monomethyl fumarate (MMF); therefore, no dosage adjustment is necessary

Dosing Considerations

Laboratory parameters

  • Obtain a CBC count, including lymphocyte count, before initiation, 6 months after initiation, and then every 6-12 months thereafter, as clinically indicated
  • Obtain AST/ALT, alkaline phosphatase, and total bilirubin levels before initiation, during treatment, as clinically indicated

Safety and efficacy not established

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Interactions

Interaction Checker

and monomethyl fumarate

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                • ozanimod

                  ozanimod, monomethyl fumarate. Either increases effects of the other by immunosuppressive effects; risk of infection. Use Caution/Monitor. Coadministration with immunosuppressive therapies may increase the risk of additive immune effects during therapy and in the weeks following administration. When switching from drugs with prolonged immune effects, consider the half-life and mode of action of these drugs in order to avoid unintended additive immunosuppressive effects.

                Minor (0)

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                  Adverse Effects

                  Data obtained from clinical trials of prodrug dimethyl fumarate (DMF), which is metabolized to MMF

                  >10%

                  Flushing (40%)

                  Abdominal pain (18%)

                  Diarrhea (14%)

                  Nausea (12%)

                  1-10%

                  Vomiting (9%)

                  Pruritus (8%)

                  Rash (8%)

                  Albumin urine present (6%)

                  Erythema (5%)

                  Dyspepsia (5%)

                  AST increased (4%)

                  Lymphopenia (2%)

                  Frequency Not Defined

                  A transient increase in mean eosinophil counts during first 2 months of treatment

                  Postmarketing Reports

                  Liver function abnormalities: AST/ALT ≥3x ULN with concomitant elevations in total bilirubin >2x ULN

                  Infections: Herpes zoster infection, other serious opportunistic infections

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                  Warnings

                  Contraindications

                  Hypersensitivity to MMF, DMF, diroximel fumarate, or to any of its excipients

                  Taking DMF or diroximel fumarate

                  Cautions

                  Clinically significant cases of liver injury reported; onset ranges from a few days to several months after initiating; discontinue if clinically significant drug-induced liver injury is suspected

                  May cause flushing (eg, warmth, redness, itching, and/or burning sensation)

                  Anaphylaxis and angioedema

                  • Anaphylaxis and angioedema after initial dose or at any time during treatment may occur
                  • Signs and symptoms have included difficulty breathing, urticaria, and swelling of the throat and tongue

                  Progressive multifocal leukoencephalopathy

                  • Progressive multifocal leukoencephalopathy (PML) has occurred with DMF
                  • Withhold dose at first sign or symptom suggestive of PML and perform diagnostic evaluation
                  • Typical symptoms (eg, progressive weakness on one side of the body or clumsiness of limbs, disturbance of vision, changes in thinking, memory changes, orientation leading to confusion, personality changes) may progress over days to weeks
                  • Monitor with MRI for signs consistent with PML and investigate any suspicious findings to allow for an early diagnosis of PML, if present

                  Herpes zoster and other serious opportunistic infections

                  • Serious cases of herpes zoster reported; these events may occur at any time during treatment
                  • Monitor for signs and symptoms of herpes zoster
                  • If herpes zoster occurs, administer appropriate treatment
                  • Other serious opportunistic infections reported, including serious viral (herpes simplex virus, West Nile virus, cytomegalovirus), fungal (Candida and Aspergillus), and bacterial (Nocardia, Listeria monocytogenes, Mycobacterium tuberculosis) infections
                  • Consider withholding treatment in patients with herpes zoster or other serious infections until the infection has resolved

                  Lymphopenia

                  • May decrease lymphocyte counts
                  • Consider interrupting dose in patients with lymphocyte counts <0.5 x 109/L persisting for >6 months
                  • Continue to monitor CBC count until their recovery if therapy is discontinued or interrupted because of lymphopenia
                  • Consider withholding treatment from patients with serious infections until resolution
                  • Decide whether or not to restart treatment based on clinical circumstances

                  Drug interaction overview

                  • DMF or diroximel fumarate
                    • Both DMF and diroximel fumarate are metabolized to MMF
                    • Therefore, coadministration of MMF with DMF or diroximel fumarate is contraindicated
                    • MMF may initiate the day following discontinuation of either of these drugs
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                  Pregnancy & Lactation

                  Pregnancy

                  No adequate data available on the use of MMF or its prodrug in pregnant females

                  Animal data

                  • In animals, adverse effects on offspring survival, growth, sexual maturation, and neurobehavioral function were observed when DMF was administered during pregnancy and lactation at clinically relevant doses

                  Lactation

                  No data available on presence of DMF or MMF in human milk

                  Effects on breastfed infants and on milk production are unknown

                  Consider the mother’s clinical need and any potential adverse effects on the breastfed infants from the drug or from the underlying maternal condition

                  Pregnancy Categories

                  A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

                  B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

                  C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

                  D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

                  X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

                  NA: Information not available.

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                  Pharmacology

                  Mechanism of Action

                  Monomethyl fumarate (MMF) is the active moiety of dimethyl fumarate (DMF) and diroximel fumarate

                  Mechanism by which MMF exerts its therapeutic effect in MS is unknown

                  Activates 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

                  Absorption

                  Peak plasma time: 4.03 hr (MMF)

                  Effects of food

                  • Administration with high-fat, high-calorie meal: No significant change at AUC; decreased peak plasma concentration by 20%; delayed peak plasma time by 7 hr

                  Distribution

                  Protein bound: 27-45% (MMF)

                  Vd: 53-73 L (MMF)

                  Metabolism

                  In humans, metabolism of MMF occurs through the tricarboxylic acid cycle, with no involvement of the CYP450 system

                  Major metabolites in plasma: MMF, fumaric and citric acid, and glucose

                  Elimination

                  Half-life: ~0.5 hr

                  Excretion

                  • Exhalation of CO2: ~ 60%
                  • Renal: 16%
                  • Feces: 1%
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                  Administration

                  Oral Administration

                  May take with or without food

                  Swallow capsules whole and intact; do not crush, chew or mix contents with food

                  Administration of nonenteric-coated aspirin (up to a 325-mg dose) 30 min before administration may reduce the incidence or severity of flushing

                  Storage

                  Unopened bottle

                  • Refrigerate at 2-8ºC (35-46ºF); do not freeze

                  Opened bottle

                  • Store at 20-25ºC (68-77ºF); excursions permitted at 15-30ºC (59-86ºF) for up to 3 months
                  • Protect from light
                  • Store in original container
                  • Capsules may become deformed if kept at high temperatures
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                  Patient Handout

                  A Patient Handout is not currently available for this monograph.
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                  Formulary

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                  Tier Description
                  1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
                  2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
                  3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
                  4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                  5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                  6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                  NC NOT COVERED – Drugs that are not covered by the plan.
                  Code Definition
                  PA Prior Authorization
                  Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
                  QL Quantity Limits
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                  Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.