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. 2013 Feb 26;5:37–47. doi: 10.2147/DHPS.S28822

Table 1.

Oral agents in RRMS: Overview of mechanisms of action and efficiency.

Drug MOA MRI Outcome Clinical outcome
Laquinimod – Induction of type ii myeloid cells.
– Induction of Th2 cytokine balance.
– Increase of BDNF and suppression of TH17 responses.
– Attenuation of astrocytic NF-κB activation.
– Reduction of enlarging or new T2 hyperintense lesions.
– Reduction of gadolinium enhancing lesions.
– Reduction in the loss of brain volume.
– Reduction of ARR.
– Modest reduction in the risk of confirmed disability progression.
Fingolimod – Modulation of S1PR 1, 3–5.
– Inhibits egress of lymphocytes. from lymph nodes towards CNS.
– Retains Th17 cells.
– May reduce astrogliosis and favor remyelination.
– Reduction of enlarging or new T2 hyperintense lesions.
– Reduction of gadolinium enhancing lesions.
– Reduction of brain atrophy.
– Reduction of ARR.
– Reduces the risk of disability progression.
– Superior efficacy with respect to ARR compared to IFN-β-1a.
Teriflunomide – Downregulation of T- and B-cell proliferation by suppression of pyrimidine synthesis. – Reduction of enlarging or new T2 hyperintense lesions.
– Reduction of gadolinium enhancing lesions.
– Reduction of ARR.
– Reduces the risk of disability progression.
Cladribine – Induction of DNA damage via accumulation in monocytes and lymphocytes. – Reduction of active T2 lesions.
– Reduction of gadolinium enhancing lesions.
– Reduction of ARR.
– Reduces the risk for disability progression.
BG-12 – Induction of Th2-like cytokines and apoptosis in activated T cell.
– Activation of Nrf2 pathway and antioxidant response elements.
– Decrease of vascular and intracellular adhesion molecules.
– Reduction of enlarging or new T2 hyperintense lesions.
– Reduction of gadolinium enhancing lesions.
– Reduction of brain atrophy.
– Reduces the number of newhypointense T1-lesions.
– Reduction of ARR and the proportion of patients relapsing.
– Reduces the risk of disability progression.
– Superior efficacy with respect to ARR compared to GA.

Abbreviations: ARR, annual relapse rate; GA, glatiramer acetate; Ian; interferon, MOA; mechanisms of action, MRI; magnetic resonance imaging.