Description of efficacy, effects and side effects of Serputinib/Serpatinib (Ruitu)

Selpercatinib is a highly selective RET kinase inhibitor developed by Eli Lilly and Company of the United States. It is a precision targeted therapy drug that has emerged in recent years. Its main function is to block abnormal signaling caused by RET gene fusion or RET point mutation, thereby inhibiting the growth and spread of tumor cells. The drug has been approved by the US FDA for the treatment of non-small cell lung cancer (NSCLC), medullary thyroid cancer (MTC) and other types of RET fusion-positive solid tumors related to RET gene alterations. It is the world's first highly specific oral inhibitor targeting the RET pathway. Due to its strong precise targeting, significant efficacy, and good tolerability, it is regarded as an important breakthrough in the field of RET-driven cancer treatment.

From the perspective of pharmacological mechanism, seputinib inhibits RET kinase activity and blocks the downstream RAS/MAPK and PI3K/AKT signaling pathways, cutting off the source of signals that promote tumor growth from the root. Compared with early multi-target inhibitors (such as vandetanib and cabozantinib), seputinib is more selective, which means that it targets RET mutations more accurately and reduces interference with other tyrosine kinases, so it has fewer side effects and is better tolerated. Overseas research data shows that the drug has demonstrated significant tumor shrinkage and disease control rates in patients with a variety of RET fusion-positive tumors. It has also shown a certain penetration of the central nervous system in patients with brain metastases, indicating that its molecular design has the potential to cross the blood-brain barrier.

However, like all targeted anti-cancer drugs, seputinib also has potential adverse reactions and needs to be used under the guidance of a doctor. Common side effects include increased blood pressure, increased liver function indicators, diarrhea, tiredness, constipation, dry mouth, and rash. Most of these reactions are mild to moderate and can usually be alleviated by dose adjustment or adjuvant therapy. Increased blood pressure is one of the more typical adverse reactions, so it is recommended to regularly monitor blood pressure in the early stages of medication and take antihypertensive measures as necessary. Abnormal liver function usually manifests as an increase in ALT or AST, which can generally return to normal after stopping or reducing the dose. It is recommended to test liver function every month during the medication period. Some patients may experience minor electrolyte imbalances, such as a decrease in sodium and potassium ions, and doctors will provide supplements based on test results.

It is worth noting that the metabolism of seputinib mainly relies on the hepatic CYP3A4 enzyme system, so caution is required when combined with other drugs. For example, strong CYP3A inhibitors or inducers may affect drug concentration. Patients should proactively report the medications they use, including traditional Chinese medicine and health care products, to their doctors during use to avoid potential interactions. In addition, some patients may experience mild dizziness or prolongation of the QT interval on the ECG during the early stages of treatment, so regular ECG monitoring is recommended. People with underlying heart diseases should use it with caution under the guidance of a doctor.

SeputinibThe overall tolerability is good among targeted drugs. Overseas long-term observation shows that patients can usually maintain a long progression-free survival (PFS), and most of the side effects are reversible and controllable. Doctors usually develop individualized doses based on the patient's weight, age, liver and kidney function, and target status to achieve the best balance. For long-term treatment patients, regular review of blood pressure, liver and kidney function and electrolyte levels is the key to ensuring safety.

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