Copaxone was launched in Israel and the US for treatment of relapsingremitting
multiple sclerosis. The amino acid polymer is prepared from the Ncarboxyanhydrides
of Tyr, Ala, γ-benzylglutamate and ε,N-trifluoroacetyllysine followed
by deprotection. Structurally, the random polymer, with a residue molar ratio of
6.0:1.9:4.7:1.O=Ala:Glu:Lys:Tyr, simulates myelin basic protein (MBP). This gives it
immunomodulating and immunosuppressive activity (antigen specific so not a general
immunosuppressive). The mechanism involves binding to MHC class Ⅱ (I-A/DR)
molecules which results both in competition with myelin antigens for T-cell activation
and in induction of specific suppressor cells of the Th2 type. Therefore, the antigenspecific
interaction gives rise to a reduced probability of long-term damage to the
immune system. The competition with MBP and other myelin-associated antigens
inhibits T-cell responses to MBP, and the binding occurs with high efficiency, fast rates
and is non-species specific. It resulted in a 29% reduction in relapse rate and is most
effective in patients with less accumulated neurologic disability.
