METHODS AND COMBINATIONS OF KAT6 INHIBITORS FOR TREATING CANCER Russian patent published in 2025 - IPC A61K31/18 A61K31/423 A61K31/506 A61K31/519 A61K31/7064 A61K45/06 A61P35/00 

Abstract RU 2833058 C1

FIELD: medicine.

SUBSTANCE: group of inventions relates to the treatment of breast cancer. Disclosed is a method of treating breast cancer, comprising administering lysine acetyltransferase 6 (KAT6) inhibitor to a patient in need thereof and a) an amount of cyclin-dependent kinase 4 (CDK4) inhibitor, or b) an amount of an antioestrogen, or c) an amount of a CDK4 inhibitor and an amount of an antioestrogen, where the amounts are combined therapeutically effective in treating cancer. CAT6 inhibitor is 2-methoxy-N-{4-methoxy-6-[(1H-pyrazol-1-yl)methyl]-1,2-benzoxazol-3-yl}benzene-1-sulphonamide or a pharmaceutically acceptable salt thereof, and the CDK4 inhibitor is 1,5-anhydro-3-({5-chloro-4-[4-fluoro-2-(2-hydroxypropan-2-yl)-1-(propan-2-yl)-1H-benzimidazol-6-yl]pyrimidin-2-yl}amino)-2,3-dideoxy-D-threo-pentite or its pharmaceutically acceptable salt or palbociclib or its pharmaceutically acceptable salt. Group of inventions also relates to a method of overcoming clinical resistance to endocrine therapy, comprising administering to a patient in need thereof, an amount of said KAT6 inhibitor and an amount of said CDK4 inhibitor, wherein said amounts together are therapeutically effective in overcoming clinical resistance to endocrine therapy.

EFFECT: invention provides a synergistic effect against ER+ breast cancer cells and enables to overcome clinically significant resistance to endocrine therapy.

9 cl, 18 dwg, 14 tbl, 18 ex

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RU 2 833 058 C1

Authors

Stappl, Pol Entoni

Mazurek, Entoni

Arndt, Kim Timoti

Chen, Lej

Folletti, Maksimillian Todd

Fruling, Devid Skott

Kung, Pej-Pej

Chzhun, Venyan

Tedeski, Filip Majkl

Dates

2025-01-14Published

2021-07-15Filed