Serputinib/Serpatinib (Ruitu) belongs to several generations of targeted anti-cancer drugs

Selpercatinib/Selpercatinib is recognized as a new generation of RET-targeted anti-cancer drugs. It is one of the first targeted drugs in the world specifically developed and approved for marketing against RET gene abnormalities. Unlike traditional multi-target tyrosine kinase inhibitors (such as cabozantinib and vandetanib), seputinib achieves highly selective inhibition of RET kinase based on its molecular structure and hardly affects other signaling pathways. This selectivity not only significantly improves the efficacy of the drug, but also reduces non-target-related side effects, allowing patients to have better tolerance and long-term compliance during treatment.

Early RET inhibitory drugs are often "broad-spectrum targeted drugs", such as sorafenib or cabozantinib. These drugs can act on multiple pathways such as VEGFR, MET, and KIT at the same time. However, due to insufficient selectivity, they lead to many side effects, such as hypertension, hand-foot syndrome, or gastrointestinal discomfort. In contrast, the emergence of seputinib marks the transition of RET inhibition from "non-specific multi-target inhibition" to the era of "high-precision targeted inhibition". It achieves more precise molecular-level intervention by blocking cancer cell growth signals driven by RET fusions or RET mutations.

The research and development concept of Seputinib is also in line with the core trend of today's cancer treatment - from organ-oriented therapy to gene-oriented therapy. Regardless of whether the tumor occurs in the lungs (non-small cell lung cancer), thyroid, or other tissues, as long as RET gene abnormalities are present, seputinib may be an effective option. Because of its precise mechanism and coverage of multiple cancer types, the U.S. FDA granted it "pan-tumor indication" status when it was approved. This move symbolizes the rise of molecular subtyping in the field of tumor treatment.

Compared with other RET inhibitors, seputinib not only achieves a breakthrough in drug selectivity, but also successfully overcomes drug tolerance and brain metastasis control problems common in early drugs. Its molecular design can effectively penetrate the blood-brain barrier and also show significant efficacy in patients with RET-positive brain metastases, which is extremely rare among targeted drugs.

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