FIELD: medicine.
SUBSTANCE: group of inventions relates to compositions and methods of treating cancer using SHP2 protein tyrosine phosphatase inhibitors as monotherapy and in combination with inhibitors of the RAS signaling pathway. A subject who has a cancer carrying certain RAS pathway oncogenic mutations is provided with an SHP2 inhibitor being a compound of formula I-V2.
Also a combination therapy agent and a pharmaceutical composition for the treatment of cancer associated with a mutation of the RAS pathway, containing an inhibitor of the RAS pathway and the specified SHP2 inhibitor is proposed. The RAS pathway mutation is selected from a KRAS mutation, a BRAF class 3 mutation, a MEK1 class I mutation, a MEK1 class II mutation, and an NF1 mutation. The RAS pathway inhibitor is either a MAPK inhibitor, a MEK inhibitor, or an ERK inhibitor.
EFFECT: effective suppression of growth or proliferation of a cell containing a RAS pathway mutation, as well as prevention and slowing down of resistance of tumors carrying RAS pathway mutations to RAS pathway inhibitors.
21 cl, 22 dwg, 5 tbl, 8 ex
Title | Year | Author | Number |
---|---|---|---|
BICYCLIC COMPOUNDS AS ALLOSTERIC SHP2 INHIBITORS | 2018 |
|
RU2776846C2 |
COMPOUND FOR TREATING CANCER | 2014 |
|
RU2708247C2 |
COMBINATION THERAPY | 2018 |
|
RU2815400C2 |
BIOMARKERS FOR PREDICTION OF SENSITIVITY TO ANTITUMOR TREATMENT | 2012 |
|
RU2635193C2 |
COMBINATION OF (A) PHOSPHOINOSITIDE-3-KINASE INHIBITOR AND (B) Ras/Raf/Mek PATHAWAY MODULATOR | 2009 |
|
RU2508110C2 |
SYNERGISTIC COMBINATIONS OF AURISTANE | 2015 |
|
RU2717570C2 |
COMPOUNDS AND COMPOSITIONS AS PROTEINKINASE INHIBITORS | 2006 |
|
RU2411242C2 |
METHODS FOR TREATMENT OF MALIGNANT TUMORS, USING ATR INHIBITOR | 2018 |
|
RU2813966C2 |
COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS | 2006 |
|
RU2383545C2 |
ISOINDOLONES AND METHODS FOR USING THEM | 2009 |
|
RU2495028C2 |
Authors
Dates
2023-10-16—Published
2018-09-06—Filed