Laquinimod (ABR-215062)

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Background

ABR-215062 is an orally active immunoregulator. Experimental autoimmune encephalomyelitis (EAE) is an inflammatory autoimmune disease of the CNS that can be elicited in rodents and represents the major animal model for the study of multiple sclerosis (MS).
In vitro: ABR-215062 was shown to completely inhibit the development of murine acute experimental autoimmune encephalomyelitis (EAE) [1].
In vivo: ABR-215062 dose-dependently inhibited disease and showed better disease inhibitory effects as compared to roquinimex (Linomide). Furthermore, ABR-215062 inhibited the inflammation of both CD4+ T cells and macrophages into central nervous tissues [2].
Clinical trial: Randomized, controlled clinical trials in relapsing MS demonstrate a dose–response effect of ABR-215062 on disease activities, indicated by reduced clinical relapse rate, number of brain MRI active lesions, and sustained disability and brain atrophy [3].

[1] Brunmark C, Runström A, Ohlsson L, Sparre B, Brodin T, Aström M, Hedlund G. The new orally active immunoregulator laquinimod (ABR-215062) effectively inhibits development and relapses of experimental autoimmune encephalomyelitis. J Neuroimmunol. 2002 Sep;130(1-2):163-72.
[2] Yang JS, Xu LY, Xiao BG, Hedlund G, Link H. Laquinimod (ABR-215062) suppresses the development of experimental autoimmune encephalomyelitis, modulates the Th1/Th2 balance and induces the Th3 cytokine TGF-beta in Lewis rats. J Neuroimmunol. 2004 Nov;156(1-2):3-9.
[3] Haggiag S, Ruggieri S, Gasperini C. Efficacy and safety of laquinimod in multiple sclerosis: current status. Ther Adv Neurol Disord. 2013 Nov;6(6):343-52.