What is the target of larotrectinib?

The main target of Larotrectinib (Larotrectinib) is NTRK gene fusion protein (NTRK fusion protein). NTRK stands for neuronal growth factor receptor (Neurotrophic Tyrosine Kinase Receptor), which is a type of receptor protein related to the neuronal growth factor signaling pathway. The formation of NTRK gene fusion protein results from the abnormal fusion of NTRK gene, usually caused by chromosomal rearrangement events or other gene mutations. This abnormal fusion leads to the production of NTRK gene fusion protein, which is expressed in tumor cells and participates in abnormal cell signaling processes.

The mechanism of action of larotrectinib is to specifically inhibit the activity ofNTRK gene fusion protein, thereby preventing abnormal cell signaling. Specifically, larotrectinib affects theNTRK fusion protein in the following ways:

1.Inhibition of phosphorylation: NTRK gene fusion protein has abnormal tyrosine phosphorylation in its kinase active region, which is an important cell signaling process. Larotrectinib can inhibit this abnormal tyrosine phosphorylation and reduce the activity of the fusion protein.

2.Reduce signaling pathway activity: By inhibiting the activity of the NTRK fusion protein, larotrectinib can interfere with the activity of other proteins related to the NTRK signaling pathway. This further reduces abnormal cell signaling, thereby inhibiting the growth and spread of tumor cells.

Larotrectinib has been launched in China, but it has not been included in medical insurance. Since it has not been launched in China for a long time, it may be difficult to purchase it in China. Please consult the local hospital pharmacy for details. There are original drugs and generic drugs of larotrectinib abroad. The original drugs include German version, American version, European version and Hong Kong version. The price is basically around 20,000 yuan. Generic drugs include Lao and Bangladeshi versions, with prices ranging from two to three thousand. The ingredients of original drugs and generic drugs are basically the same.