TOLL-LIKE RECEPTOR 7 OR 8 AGONIST AND CHOLESTEROL COMPLEX AND ITS USE Russian patent published in 2023 - IPC A61K31/4745 A61K39/39 A61K47/54 A61K47/69 A61P35/00 

FIELD: pharmaceuticals.

SUBSTANCE: present invention relates to a complex agent of a 7 or 8 toll-like receptor agonist and cholesterol, in which cholesterol is linked to the amino group (NH₂) of the active site of the 7/8 toll-like receptor agonist, where the bond is cleavable, and the use of the complex agent. A toll-like 7 or 8 receptor agonist containing cholesterol chemically bound to it is not absorbed into the blood vessels and thus reduces the adverse side effects of the original toll-like 7 or 8 receptor. In particular, since the complex agent is designed in such a way that the immune activation function of the toll-like receptor agonist 7 or 8 is inhibited due to chemical bonding with cholesterol, and then the immune activation function is restored in the tumour microenvironment or in immune target cells, the complex agent demonstrates dynamic characteristics that can modulate the effectiveness of immune activation over time and minimize the induction of non-specific immune responses.

EFFECT: in addition, the complex of a toll-like receptor 7 or 8 agonist and cholesterol can be easily prepared in various nanoparticle formulations and thus can be widely used in drug compositions for various purposes, such as the activation of therapeutic immune cells in the tumour microenvironment, as well as the control of immunosuppressive cells and environment.

13 cl, 24 dwg, 6 ex