COMPOSITION FOR ATTACHING A RADIOISOTOPE TO POLYPEPTIDES AND A METHOD FOR ATTACHING A RADIOISOTOPE TO POLYPEPTIDES Russian patent published in 2020 - IPC A61K51/08 A61K45/08 A61P35/00 C01G15/00 C07K19/00 

FIELD: pharmacy.

SUBSTANCE: group of inventions relates to a composition for attaching a radioisotope to a polypeptide with a covalently attached chelator and to a method of attaching a radioisotope to a polypeptide with a covalently attached chelator. Composition consists of polypeptide and attached radionuclide, sodium citrate, 4-(2-hydroxyethyl)piperazine-1-ethanesulphonic acid (HEPES), sodium chloride, sodium dodecyl sulphate (SDS) with pH value selected for attachment of radioisotope, which is in range of 4–7.5 units. In the method, a radioisotope is added to a polypeptide with a joined chelator and incubated in a medium containing sodium citrate in range of 1–20 mM, 4-(2-hydroxyethyl)piperazine-1-ethanesulphonic acid (HEPES) concentration of 80 mM, sodium chloride, sodium dodecyl sulphate (SDS) in concentration of 0.02 %, at temperature of 37 °C, at pH in range of 4–7.5 units, after which sodium chloride is added to the physiological concentration of ions in the mixture and sodium hydroxide to pH 7.5.

EFFECT: group of inventions provides a composition which enables to attach radioisotopes which readily form insoluble hydroxides at pH greater than 3–3,5, to polypeptides which are poorly soluble in a weakly acidic medium (pH 3–6).

18 cl, 17 dwg, 19 ex