瑞普替尼，（Repotrectinib ）40mg
1. Composition:
Repotrectinib is a small-molecule tyrosine kinase inhibitor, with the chemical name N-[4-(4-chlorophenyl)-2-(6-(4-(trifluoromethyl)phenyl)pyrimidin-4-yl)thiazol-5-yl)phenyl]acetamide. Its molecular formula is C23H18ClF3N4S, and the molecular weight is 470.93.
2. Pharmacological Effects:
Repotrectinib is primarily used for the treatment of non-small cell lung cancer (NSCLC) with ROS1 or NTRK gene fusions, as well as certain other tumor types. It works by inhibiting the tyrosine kinase activity of ROS1 and NTRK receptors, interfering with the signaling pathways that mediate cell proliferation and survival, thereby preventing cancer cell growth.
3. Usage Instructions:
Repotrectinib is administered orally in tablet form, with a recommended dosage of 40 mg once daily. The dosage may be adjusted based on the patient's specific condition and tolerance. It should be used under a physician's guidance, and the effects and side effects of the medication should be monitored regularly.
4. Research & Development History:
Repotrectinib was developed by Blueprint Medicines and is primarily indicated for the treatment of cancers that are positive for ROS1 and NTRK gene fusions. It received FDA approval in 2019 for the treatment of ROS1-positive non-small cell lung cancer and has gradually been approved worldwide. The development of Repotrectinib marks a significant advancement in targeted therapies for cancer based on specific gene mutations.
5. Mechanism of Action:
The main mechanism of Repotrectinib is the specific inhibition of the tyrosine kinase activity of ROS1 and NTRK receptors, thereby blocking the signaling pathways mediated by these receptors. This inhibitory action effectively prevents the proliferation and survival of cancer cells caused by ROS1 or NTRK fusion mutations.
6. Summary:
Repotrectinib is a targeted medication primarily used for the treatment of non-small cell lung cancer and other related cancers that contain ROS1 or NTRK gene fusions. It exerts its therapeutic effects by inhibiting relevant tyrosine kinases and blocking the growth signals of cancer cells. The use of Repotrectinib should be in accordance with a physician's guidance and should involve regular monitoring to ensure its safety and efficacy.
