Which medications in the drug class Immunomodulators are used in the treatment of Multiple Sclerosis?

Updated: Oct 08, 2019
  • Author: Christopher Luzzio, MD; Chief Editor: Jasvinder Chawla, MD, MBA  more...
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Answer

Immunomodulators

Immunomodulators or receptor modulators are indicated for the treatment of patients with relapsing forms of MS. They help to slow the accumulation of physical disability and decrease the frequency of clinical exacerbations.

Interferon beta-1b (Betaseron, Extavia)

Interferon beta-1b was the first medication approved by the FDA for MS. It is approved for the treatment of relapsing forms of MS to reduce the frequency of clinical exacerbations. It has shown efficacy in patients who have experienced a first clinical episode and have MRI features consistent with MS.

The exact mechanism by which interferon beta-1b exerts its effects is unknown. Interferon beta inhibits the expression of pro-inflammatory cytokines, including interleukin (IL)-1 beta, tumor necrosis factor (TNF)-alpha and TNF-beta, interferon gamma (IFN-γ), and IL-6. IFN-γ is believed to be a major factor responsible for triggering the autoimmune reaction leading to MS.

Interferon beta-1a (Avonex, Rebif)

Interferon beta-1a is approved for the treatment of patients with relapsing forms of MS. It helps to slow the accumulation of physical disability and decrease the frequency of clinical exacerbations.

The exact mechanism by which interferon beta-1a exerts its effects is not fully defined. Interferon beta inhibits the expression of proinflammatory cytokines, including interferon gamma (IFN-γ), which is believed to be a major factor responsible for triggering the autoimmune reaction leading to MS.

Alemtuzumab (Lemtrada)

Alemtuzumab is a recombinant monoclonal antibody against CD52 (lymphocyte antigen). This action promotes antibody-dependent cell lysis. It is indicated for relapsing forms of multiple sclerosis. Because of the risk for severe and lasting autoimmune adverse effects, use is reserved for patients who have an inadequate response to 2 or more other drugs for MS.

Peginterferon beta-1a (Plegridy)

Precise mechanism by which peginterferon beta-1a exerts its effects in patients with multiple sclerosis is unknown. Interferons are thought to alter response to surface antigen and may enhance immune cell activities. It is indicated for treatment of relapsing forms of multiple sclerosis.

Natalizumab (Tysabri)

Natalizumab is indicated as monotherapy for MS to delay the accumulation of physical disability and reduce the frequency of clinical exacerbations. Natalizumab is a recombinant humanized monoclonal antibody that binds with alpha-4 integrins and inhibits their adherence to their counterreceptors. The specific mechanism by which natalizumab exerts its effects in MS has not been defined.

Natalizumab has a black-box warning for progressive multifocal leukoencephalopathy (PML). Because of the risk of PML, natalizumab is available only through a special restricted distribution prescribing program called the Tysabri Outreach Unified Commitment to Health (TOUCH).

Glatiramer acetate (Copaxone, Glatopa)

Glatiramer acetate is approved for the reduction of the frequency of relapses in patients with relapsing-remitting MS, including patients who have experienced a first clinical episode and have MRI features consistent with MS. Glatiramer acetate's mechanism of action is unknown, but this agent is thought to modify immune processes believed to be responsible for the pathogenesis of MS. The recommended dosage is 20 mg/day administered subcutaneously. The sites for injection include the arms, abdomen, hips, and thighs.

Teriflunomide (Aubagio)

Teriflunomide is an oral immunomodulatory agent that elicits anti-inflammatory effects by inhibiting dihydroorotate dehydrogenase, a mitochondrial enzyme involved in pyrimidine synthesis. It is indicated for relapsing forms of MS.

Dimethyl fumarate (Tecfidera)

Dimethyl fumarate (DMF) is an oral Nrf2 pathway activator indicated for relapsing forms of multiple sclerosis. DMF is metabolized rapidly by presystemic hydrolysis by esterases in the GI tract, blood, and tissues (before it reaches systemic circulation) and is converted to its active metabolite, monomethyl fumarate (MMF). MMF activates the nuclear factor (erythroid-derived 2)-like 2 (Nrf2) pathway, a transcription factor encoded by the NFE2L2 gene. The Nrf2 antioxidant response pathway is a cellular defense against oxidative stress. MMF has been identified as a nicotinic acid receptor agonist in vitro.

Ocrelizumab (Ocrevus)

Ocrelizumab is a humanized monoclonal antibody designed to selectively target CD20, a cell surface antigen present on pre-B and mature B lymphocytes. Following cell surface binding to B lymphocytes, ocrelizumab results in antibody-dependent cellular cytolysis and complement-mediated lysis. Following 2 initial IV doses administered 2 weeks apart, subsequent IV doses are administered every 6 months. It is indicated for adults with relapsing or primary progressive forms of multiple sclerosis.


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