Serputinib/serpatinib belongs to the first generation of targeted therapy drugs

Selpercatinib is a selective RET (rearranged tyrosine kinase) inhibitor, which belongs to the "new generation" of targeted therapy drugs. Strictly speaking, it is not classified into the traditional "first-generation, second-generation, and third-generation", but represents "RET-specific targeted drugs" developed based on the concept of precision medicine. It was acceleratedly approved by the US FDA in 2020 for the treatment of patients with advanced solid tumors carrying RET gene fusions or mutations, especially in the fields of non-small cell lung cancer (NSCLC) and thyroid cancer.

In RET fusion-positive non-small cell lung cancer, seputinib shows a high objective response rate (ORR) and a durable effect, even in patients who have received multiple lines of therapy. In addition, it also has good efficacy in RET-mutant medullary thyroid cancer, providing new hope for patients who are resistant to conventional treatments. Compared with traditional multi-target tyrosine kinase inhibitors, such as vandetanib or cabozantinib, seputinib has higher target selectivity and therefore milder side effects, especially in terms of hypertension, rash and gastrointestinal reactions. It is better tolerated.

It is worth noting that RET fusion is relatively rare, accounting for about 1%-2% of NSCLC. However, for this population, seputinib is the first-line targeted therapy option currently recommended by international guidelines. Its innovative mechanism represents a new stage of targeted therapy, that is, the precise development of drugs for rare but targetable driver mutations. Under the trend of precise matching treatment at the molecular level, seputinib has become a "representative new target drug" in the treatment of RET fusion-related tumors, which is a milestone. In the future, with the further expansion of its indications and the accumulation of more clinical data, seputinib is expected to occupy a more central position in the field of RET-related tumor treatment.

Reference:https://en.wikipedia.org/wiki/Selpercatinib