What type of anti-cancer drug is Serputinib/Serpatinib (Ruitu)?

Selpercatinib is a highly selective oral targeted anti-cancer drug specifically targeting tumors driven by RET gene fusions or RET mutations. RET (REarranged during Transfection) gene abnormalities exist in a variety of solid tumors, including non-small cell lung cancer (NSCLC), medullary thyroid carcinoma (MTC) and some other RET fusion-positive solid tumors. By inhibiting RET kinase activity, Seputinib blocks downstream signaling pathways from the source and inhibits the proliferation and metastasis of tumor cells, providing a precise treatment option for RET-driven cancers.

Abnormal activation of RET will promote the abnormal operation of signaling pathways such as RAS/MAPK and PI3K/AKT, leading to rapid tumor growth and metastasis. Although traditional multi-target tyrosine kinase inhibitors (such as vandetanib or cabozantinib) can also inhibit RET, their effects are not specific enough and are often accompanied by more non-specific toxicity. In contrast, serpatinib inhibits RET with high selectivity and precision, reducing interference with non-target tyrosine kinases, making the treatment effect more clear and tolerable. Overseas clinical data show that after using seputinib in RET-positive patients, most tumors show significant shrinkage and disease control, and patients with central nervous system metastases may also benefit. This reflects the high penetration and targeting advantages of the drug's molecular design.

In terms of its mechanism of action, seputinib inhibits its phosphorylation activity by directly binding to the ATP binding site of RET kinase, thereby blocking the cell proliferation signaling chain and inducing tumor cell apoptosis. Compared with traditional chemotherapy, it does not depend on the tumor's proliferation rate, so it is equally effective in some chronic or low-proliferative RET tumors. Clinically, seputinib is usually used for RET-positive patients who have failed or are resistant to previous treatments, and can also be used as a first-line option. It is convenient for oral administration, reduces the inconvenience caused by long-term intravenous chemotherapy, and significantly improves patients' quality of life.

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