Dozens of multinational pharmaceutical companies are hunting for ntrk kinase inhibitors! Who is the king?

source: | author:webadmin | release time: 2020-06-20 | views:147

Ntrk fusion, widely distributed in different types of cancer, such as salivary gland breast like secretory cancer and congenital fibrosarcoma, can detect 100% ntrk fusion, and the approval of two ntrk inhibitors in 2018 / 2019, the industry has placed great hopes on the production of drugs in this direction, even once considered to be a small molecular anticancer drug compared with PD-1. Through the inquiry, dozens of large pharmaceutical companies around the world have raced in this field, starting from the structure of compounds, summarized as follows.

Ntrk & trka-c introduction
Ntrk, or neurotrophin receptor kinase, is composed of highly homologous kinases trk-a, trk-b and trk-c, which are encoded by ntrk gene.
In 1982, high molecular weight DNA was found in two colon cancer patients, which further identified the kinase trk-a; although Trk was initially identified in tumor transformation, the family was widely distributed in the nervous system and highly related to nerve development; and Trk series was also encoded as trk-a, trk-b and trk-c by ntrk1, NTRK2 and ntrk3.


The endogenous ligands of Trk a-c are slightly different, and the most relevant pathway is to activate PI3K / Akt and RAS / Raf / MAPK (PS: these two important tumor pathways, dozens of drugs have been on the market).