DISCONTINUOUS INTRODUCTION OF MDM2 INHIBITOR Russian patent published in 2019 - IPC A61K31/506 A61K31/496 A61P35/00 A61K45/00 

Abstract RU 2695228 C2

FIELD: medicine.

SUBSTANCE: group of inventions relates to oncology and pharmacology. Disclosed is the use of MDM2 inhibitor (MDM2i) for treating cancer, where MDM2i should be administered once every 3 weeks (q3w), where MDM2i is (S)-5-(5-chloro-1-methyl-2-oxo-1,2-dihydro-pyridin-3-yl)-6-(4-chlorophenyl)-2-(2,4-dimethoxy-pyrimidin-5-yl)-1-isopropyl-5,6-dihydro-1H-pyrrolo[3,4-d] imidazol-4-one or (S)-1-(4-chlorophenyl)-7-isopropoxy-6-methoxy-2-(4-{methyl-[4-(4-methyl-3-oxo-piperazin-1-yl)-trans-cyclohexylmethyl]amino}phenyl)-1,4-dihydro-2H-isoquinolin-3-one; use of the first MDM2i, which is administered in dose of 100 to 800 mg once every 3 weeks per os; use of the second MDM2i, which is administered in dose of 500 to 4,000 mg once every 3 weeks per os (versions). Treatment with intermittent Mdm2 inhibitor introduction schedule can be combined with daily administration of Mdm2i or other pharmaceutically acceptable ingredient.

EFFECT: technical result: inventions provide an antineoplastic effect by triggering substantially longer-lasting antiproliferative mechanisms in cells, duration of which is maintained for several weeks after administration of one dose, which enables to introduce declared MDM2i in intermittent mode.

11 cl, 22 dwg, 4 tbl, 10 ex

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RU 2 695 228 C2

Authors

Ferretti, Stephane

Jeay, Sebastien

Dates

2019-07-22Published

2015-06-25Filed