PHARMACEUTICAL COMPOSITION AND METHOD OF TREATING GROWTH HORMONE-ASSOCIATED DISEASES IN HUMANS Russian patent published in 2019 - IPC A61K38/27 A61K47/60 C07K14/61 A61P5/06 

FIELD: medicine; pharmaceuticals.

SUBSTANCE: group of inventions relates to pharmaceutics. First invention is a composition containing pharmaceutical excipients and in vivo clinically effective for human amount of conjugate of PEGylated prodrug of recombinant human growth hormone (rhGH), wherein said conjugate has GH activity less than 5 % with respect to native PEG-free growth hormone, and linker self-hydrolysis rate is such that elimination half-life in vivo ranges from 10 to 600 hours, and where the conjugate has a chemical structure (A):

,

where R1, R2, R3, R4 and R5 are independently selected from hydrogen, methyl, ethyl, propyl, isopropyl, butyl, isobutyl and tertiary butyl; n = 1 or 2; and X is selected from C1-C8 alkyl or C1-C12 heteroalkyl. Second invention represents a method of treating hormone-related growth diseases in humans, in which the composition described above is used.

EFFECT: group of inventions provides a low number of cases of lipoatrophy and prolonged rhGH release.

15 cl, 11 dwg, 2 tbl, 27 ex