METHOD OF OBTAINING PSMA-TARGET COMPOUND COMPLEX BASED ON UREA Lu-PS-161 AND COMPLEX Russian patent published in 2023 - IPC C07K1/13 A61K51/04 A61K103/30 A61P35/00 

FIELD: medicine, oncology and pharmacology.

SUBSTANCE: invention relates to a method of producing a complex of PSMA-targeting compound PS-161 based on urea, which is a compound of structural formula (1), with a radionuclide label ¹⁷⁷Lu of the general formula ¹⁷⁷Lu-Glu-Urea-Lys-3-chlorobenzyl-ε-Ahx-Suc-L-phenylalanyl-L-phenylalanyl-1,3-diaminopropyl-DOTA-acetamide (2). The method involves adding a solution of PS-161 in dimethyl sulfoxide and ¹⁷⁷Lu in a ratio of 16:(0.1÷3):1, µl, to an ammonium acetate buffer with pH of 5.0÷6.0, after which incubating the resulting mixture for 10–60 min at a temperature of 65–85°C. A complex of general formula ¹⁷⁷Lu-Glu-Urea-Lys-3-chlorobenzyl-ε-Ahx-Suc-L-phenylalanyl-L-phenylalanyl-1,3-diaminopropyl-DOTA-acetamide (2), obtained by the above method is also proposed.

EFFECT: expansion of the arsenal of theranostic agents for selective targeting and penetration into pathogenic tumor tissues expressing PSMA, while simultaneously improving properties: increasing prostate-specific membrane antigen binding activity to 10–29 nmol.

2 cl, 1 dwg, 1 tbl, 19 ex