Analysis of reasons for the impossibility of creating Copaxone generics

Abstract

The characteristics of Copaxone (glatiramer acetate, GA), an immunomodulating drug for the treatment of the serious autoimmune CNS disease multiple sclerosis, were presented. GA is the acetate of a mixture of synthetic polypeptides of various lengths composed of the natural amino acids L-glutamine, L-alanine, L-tyrosine, and L-lysine in stable molecular ratios that are prepared in definite and strictly controlled laboratory and manufacturing conditions. The polymerization reaction is carried out by addition of separate monomers and not whole peptide chains. The average length of the heterogeneous peptides in GA varies from 20 to 200 amino acids. The amino-acid sequence of the GA polypeptides is controlled to a large extent by the polymerization reaction conditions. The average molecular weight of the GA polypeptides varies in the range 5000 – 9000 Da. The majority of GA polypeptides have a molecular-weight distribution of approximately 2,500 – 20,000 Da. An analysis of the materials regarding features of the chemical structure, pharmacological and toxicological properties of GA and its analogs (glatiramoids) indicated that creating GA generics is at present practically impossible.