FIELD: pharmaceutical industry.
SUBSTANCE: group of inventions relates to a new gonadotropin-releasing hormone (GnRH) derivative conjugated with palmitic acid and a pharmaceutical composition containing it. The prolonged release palmitic acid-conjugated GnRH derivative is selected from: i) a sodium salt of a GnRH derivative containing the amino acid sequence of SEQ ID NO: 4, ii) an acetate salt of a GnRH derivative containing the amino acid sequence of SEQ ID NO: 5, and iii) an acetate salt of a GnRH derivative containing the amino acid sequence of SEQ ID NO: 6, in which the carboxyl group of palmitic acid is conjugated through a peptide bond to the amino terminus of GnRH. GnRH derivatives exhibit excellent volume of distribution, delayed time to peak concentration after drug administration, enable GnRH to maintain appropriate concentrations for a long period of time in vivo, and have excellent cytotoxic effects.
EFFECT: pharmaceutical composition based on a GnRH derivative is useful for the prevention and treatment of various sex hormone-dependent diseases.
5 cl, 6 dwg, 7tbl, 3 ex
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