Entrectinib/Luoshengquan belongs to the first generation of targeted drugs

Entrectinib (Entrectinib) is a multi-target tyrosine kinase inhibitor (TKI). From the perspective of molecular targeted drug development, it is usually classified as a new generation of precision targeted drugs, rather than a simple first or second generation traditional classification. The reason is that it not only targets a single mutation, but can simultaneously inhibit NTRK fusion genes, ROS1 fusion genes and ALK fusion genes, thus covering a wider range of tumor types. This "broad-spectrum targeting" feature makes entrectinib considered to represent the latest trend in precision medicine in the international medical field.

Compared with early targeted drugs, the biggest feature of entrectinib is that it can penetrate the blood-brain barrier and remain active in the central nervous system. This has important clinical value for patients with non-small cell lung cancer accompanied by brain metastases, as well as patients with solid tumors at risk of brain spread. Traditional targeted drugs are often limited to controlling peripheral lesions, while brain metastasis is always difficult to treat. Entrectinib shows unique advantages in this regard.

Enrectinib can be regarded as a "cross-era" targeted drug. Its significance is that it is no longer limited to organ classification, but is oriented to gene mutations. This gene-driven tumor treatment model is reflected in the approval pathways of the US FDA and the European Medicines Agency. Entrectinib is one of the first drugs approved for "tumor-agnostic" treatment, which means that it can be considered for use as long as a specific gene fusion is detected, regardless of whether the tumor occurs in the lungs, breast, thyroid or elsewhere.

Therefore, strictly speaking, entrectinib is not simply divided into a certain generation like erlotinib and crizotinib, but belongs to a new generation of multi-target broad-spectrum targeted drugs. The improvement of its clinical status lies not only in its efficacy, but also in promoting the popularization of the concept of precision medicine around the world.

Reference materials:https://www.roche.com/products/rozlytrek