RADIOPHARMACEUTICALS TARGETING GRPR AND THEIR USE Russian patent published in 2023 - IPC A61K51/08 A61K47/10 A61K47/14 A61K47/32 A61K9/00 A61K9/08 A61P35/00 

Abstract RU 2798978 C2

FIELD: radiopharmaceuticals.

SUBSTANCE: invention relates to gastrin-releasing peptide (GRPR) receptor-targeted pharmaceutical composition containing a radioactively labeled GRPR antagonist and a surfactant containing polyethylene glycol-15-hydroxystearate. The antagonist has the following formula: MС-S-P, where M is a radioactive metal and C is a chelator that binds M; S is an optional spacer covalently linked between the C and N-terminus of P; P is a peptide GRP receptor antagonist with the general formula: Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Xaa6-Xaa7-Z, where Xaa1 is the D-isomer of Phe; Xaa2 is Gln; Xaa3 is Trp; Xaa4 is Ala; Xaa5 is Val; Xaa6 is Gly; Xaa7 is His; Z is -NH-alkyl or Z is, where X is NH, and R1 and R2 are the same or different and are selected from proton or optionally substituted alkyl. The invention also relates to the use of the said pharmaceutical composition, a method for treating or preventing cancer, and a method for imaging a tumor.

EFFECT: invention makes it possible to obtain a stable pharmaceutical composition by preventing peptide adhesion.

13 cl, 8 dwg, 3 tbl, 2 ex

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RU 2 798 978 C2

Authors

Orlandi, Francesca

Fugazza, Lorenza

Barbato, Donato

Tedesco, Mattia

Sacchetti, Lorenzo

Dates

2023-06-30Published

2019-10-11Filed