Which generation of targeted drugs does larotrectinib belong to?

Larotrectinib is a new type of targeted drug specifically used to treat tumor patients carrying NTRK (neurotrophic tyrosine receptor kinase) gene fusions. It ushered in the era of targeted drugs based on gene drive therapy, but it was not clearly classified in the traditional generational division of targeted drugs. From the perspective of the field of TRK inhibitors, larotrectinib can be considered the first generation TRK inhibitor.

Larotrectinib blocks tumor cell proliferation and metastasis caused by NTRK gene fusion by selectively inhibiting TRK protein activity. This mechanism makes it suitable for a variety of cancers, including lung cancer, sarcoma, thyroid cancer, breast cancer, colorectal cancer, etc., and is not limited by the tissue source of the tumor. As the world's first TRK inhibitor, it marks a major breakthrough in the field of precision medicine, which is in sharp contrast to the "cancer species-oriented " treatment of traditional targeted drugs.

Targeted drugs are traditionally divided into generations based on their targets and development time, such as first-, second- and third-generation drugs for EGFR and ALK inhibitors. However, the target of larotrectinib TRK is a new area of u200bu200bexploration, and a similar generation system has not yet been formed. As the first approved TRK Inhibitors, which are "groundbreaking", and subsequently developed drugs (such as entrectinib) can be regarded as "second-generation " due to their stronger function against drug-resistant mutations.

Larotinib has significant efficacy, especially in patients carrying NTRK fusion, showing a high response rate. However, its long-term effects and drug resistance management are still under study. With the development and competition of similar drugs, TRK inhibitors may form a more complete generational classification in the future.

Larotrectinib can be regarded as the first generation TRK inhibitor, which promoted the transformation of tumor treatment from "cancer type classification" to "gene target" and created a new treatment concept.

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Reference materials:

1.FDADrug Description:https://www.fda.gov

2.PubMedLiterature:https://pubmed.ncbi.nlm.nih.gov/

3.NMPADrug information:https://www.nmpa.gov.cn