SELECTIVE INHIBITOR OF EGFR HAVING MUTATION IN EXON 18 AND/OR EXON 21 Russian patent published in 2022 - IPC A61K31/519 C12Q1/6869 G01N33/574 A61P35/00 

Abstract RU 2785657 C2

FIELD: biotechnology.

SUBSTANCE: group of inventions relates to a selective inhibitor of EGFR with mutation in exon 18 and/or 21. The use of (S)-N-(4-amino-6-methyl-5-(quinoline-3-yl)-8,9-dihydropyrimido[5,4-b]indolysine-8-yl)acrylamide or its pharmaceutically acceptable salt in methods for the treatment of a patient with malignant tumor and prediction of therapeutic effects of chemotherapy, using an antitumor agent in a patient with malignant tumor, is proposed, where tumor has mutation of EGFR gene, selected from a group consisting of G719X mutation in exon 18, E709X mutation in exon 18, and L861X mutation in exon 21, where X is a random amino acid residue.

EFFECT: inventions provide excellent selectivity and effects of tumor growth inhibition relatively to EGFR with mutation in exon 18 and/or exon 21, without causing inhibition of EGFR of a wild type.

20 cl, 4 dwg, 4 tbl, 5 ex

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RU 2 785 657 C2

Authors

Abe, Naomi

Hasako, Shinichi

Dates

2022-12-12Published

2018-08-31Filed