Company: Biogen Idec Ltd.
Legal category: Prescription. High tech. Sport permitted.
Active ingredient: Dimethyl fumarate 120mg, 240mg.
Description: Green/white or green gastro-resistant hard capsules marked with BG-12 and strength, respectively.
Presentation: 120mg-14, €283.00; 240mg-56, €1132.00.
Indication: Treatment of relapsing remitting multiple sclerosis.
Pharmacology: The mechanism by which dimethyl fumarate exerts therapeutic effects is not fully understood. Studies indicate that its pharmacodynamic responses are primarily mediated through activation of the Nuclear factor (erythroid-derived 2)-like 2 (Nrf2) transcriptional pathway. It up regulates Nrf2-dependent antioxidant genes in patients (e.g. NAD(P)H dehydrogenase, quinone 1; [NQO1]). Dimethyl fumarate has demonstrated anti-inflammatory and immunomodulatory properties and, along with its primary metabolite (monomethyl fumarate), significantly reduces immune cell activation and subsequent release of pro-inflammatory cytokines in response to inflammatory stimuli.
Dosage: Adult: Do not crush, divide, dissolve, suck or chew. Take with food. Initiate under supervision. Initially, 120mg twice daily. After 7 days, increase to 240mg twice daily. Reduce to 120mg twice daily if flushing and gastrointestinal adverse reactions occur (resume at 240mg twice daily within 1 month). Elderly: As per adults. Children: 10-18 years, not recommended. Under 10 years, no relevant use.
Contraindications: Hypersensitivity to the active substance or to any of the excipients. Pregnancy (only if clearly needed), lactation. Consider non-hormonal contraception.
Special precautions: Resolve serious infections prior to initiation; consider suspending if develop during treatment (assess benefit/risk of re-initiation); patients should report symptoms of infections. Perform complete blood count, including lymphocytes, prior to initiation then every 3 months during treament. Consider suspending if lymphocyte counts <0.5×109/L persist for more than 6 months. Assess renal and hepatic function prior to initiation, 3 and 6 months after initiation, every 6-12 months thereafter and as indicated. Obtain baseline MRI (within 3 months) before initiation; perform immediately if Progressive Multifocal Leukoencephalopathy (PML) suspected. Caution: Severe renal/hepatic impairment, severe gastrointestinal disease, pre-existing low lymphocyte counts. Severe flushing reactions (may require hospitalisation). Severe prolonged lymphopenia (may be risk of opportunistic infection, including PML). Switching from other disease modifying therapies, safety and efficacy not established.
Drug interactions: Do not use live vaccines (assess risk/benefit). Avoid: Other fumaric acid derivatives. Not recommended: Acetylsalicylic acid (long term use for management of flushing). Caution: Anti-neoplastic or immunosuppressive therapies. Nephrotoxic drugs. Large quantities of undiluted strong alcohol (>30% alcohol by volume).
Adverse drug reactions: Gastroenteritis, lymphopenia, leucopenia, burning sensation, flushing, hot flush, gastrointestinal disorders, pruritus, rash, erythema, proteinuria, feeling hot, ketones measured in urine, albumin urine present, increased aspartate aminotransferase, increased alanine aminotransferase, decreased white blood cell count.
Full prescribing information and references available from Biogen Idec Ltd. Telephone: 1800 812 719. Fax: +44 1748 828 801. E-mail: biogen@professionalinformation.co.uk