(2S)-2-amino-3-(4-hydroxyphenyl)propanoic acid;(2S)-2-aminopentanedioic acid;(2S)-2-aminopropanoic acid;(2S)-2,6-diaminohexanoic acid

BeschreibungCopaxone 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.

HistoryCop 1(Copaxone®) was discovered by Arnon and Sela, it was submitted by the TEVA Pharmaceutical Company to the FDA for approval, under the name of Copaxone, on June 14, 1995. In December 1996, following nearly three decades of research, the multiple sclerosis drug copolymer-1 (Copaxone®) became one of the first Israeli medications to receive the approval of the U.S. Food and Drug Administration. Prof. Ruth Arnon, the Institute's Vice President for International Scientific Relations, who, along with Weizmann Institute colleagues Prof. Michael Sela and Dr. Dvora Teitelbaum, originally synthesized and developed copolymer-1, recently documented the drug's dramatic history in the scientific journal Immunology Letters.