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
Title | Year | Author | Number |
---|---|---|---|
L718 AND/OR L792 MUTANT INHIBITOR OF TREATMENT-RESISTANT EGFR | 2019 |
|
RU2809621C2 |
SELECTIVE EGFR MUTANT INHIBITOR WITH INSERTION IN EXON 20 | 2017 |
|
RU2774629C2 |
CONJUGATES OF CMET ANTIBODY AND DRUG AND METHODS OF USING | 2017 |
|
RU2740996C2 |
NEOANTIGENS AND THEIR USE | 2019 |
|
RU2813924C2 |
BISPECIFIC ANTIGEN-BINDING PROTEIN EGFR/CD16 | 2019 |
|
RU2792240C2 |
T-CELL RECEPTOR CONSTRUCTS AND THEIR USE | 2019 |
|
RU2785954C2 |
NEW ANTI-C-MET-ANTIBODY AND APPLICATION THEREOF | 2018 |
|
RU2751720C2 |
TGFβR2 MOLECULE WITH TRUNCATED EXTRACELLULAR DOMAIN, FUSION PROTEIN OF TGFβR2 MOLECULE WITH TRUNCATED EXTRACELLULAR DOMAIN, AND ANTI-EGFR ANTIBODIES, AND ANTI-TUMOUR USE OF FUSED PROTEIN | 2021 |
|
RU2824199C1 |
BISPECIFIC FUSION PROTEIN AND ITS USE | 2021 |
|
RU2801528C2 |
MICE CONTAINING MUTATIONS, AS A RESULT OF WHICH FIBRILLIN-1 SHORTENED AT C-TERMINUS IS EXPRESSED | 2017 |
|
RU2721125C1 |
Authors
Dates
2022-12-12—Published
2018-08-31—Filed