STABLE LOCAL DRUG LEVELS FOR INNATE IMMUNITY AGONISTS Russian patent published in 2024 - IPC A61K31/4745 A61K47/60 A61P35/00 

FIELD: medicine; pharmaceutics.

SUBSTANCE: group of inventions refers to pharmaceutics and can be used for treating cell proliferation disorders. Disclosed is a water-insoluble controlled-release pattern recognition receptor (PRRA) agonist or a pharmaceutically acceptable salt thereof, wherein said water-insoluble controlled-release PRRA releases one or more PRRAs, and at least 25% of the amount of PRRA remains locally in such tissue 3 days after interstitial administration, wherein the water-insoluble PRRA contains a carrier moiety Z, with which one or more fragments -L2-L1-D are conjugated, where: each -L2- is individually a C1-20 alkyl chain, which is optionally interrupted by one or more groups independently selected from -O-, -T- and -C(O)N(Ry1)-; each -L1- is individually a linker fragment with which -D is reversibly and covalently conjugated; each D is resiquimod; Z is a water-insoluble PEG hydrogel. Also disclosed is a pharmaceutical composition containing said water-insoluble PRRA and at least one excipient.

EFFECT: group of inventions provides effective treatment regimens with TLR agonists, higher local concentrations of PRRA for an extended period of time while maintaining low systemic concentrations of PRRA, which minimizes side effects.

11 cl, 17 ex