奥希替尼
生产厂家：孟加拉珠峰制药（Everest）
功能主治：一线治疗非小细胞肺癌EGFR抑制剂，改善生存且耐受良好
用法用量： 用法用量 本品的推荐剂量为每日80mg，直至疾病进展或出现无法耐受的毒性。 如果漏服本品1次，则应补服本品，除非下次服药时间在12小时以内。 本品应在每日相同的时间服用，进餐或空腹时服用均可。 剂量调整根据患者个体的安全性和耐受性，可暂停用药或减量。 如果需要减量，则剂量应减至40mg，每日1次。
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Osimertinib, also known as AZD9291, is a third-generation small molecule tyrosine kinase inhibitor (TKI) that has shown great promise in the treatment of non-small cell lung cancer (NSCLC). Specifically, it has been approved by the FDA for the treatment of patients with metastatic EGFR T790M mutation-positive NSCLC who have progressed on or after EGFR TKI therapy.
The EGFR gene is commonly mutated in NSCLC, leading to the activation of signaling pathways that promote tumor growth and survival. While first-generation EGFR TKIs, such as gefitinib and erlotinib, showed significant clinical benefit in patients with EGFR-mutated NSCLC, many patients eventually developed resistance to these drugs. This resistance is often due to the emergence of the T790M mutation, which confers resistance to first-generation TKIs, but remains sensitive to osimertinib.Osimertinib selectively targets mutated forms of EGFR, including the T790M mutation, while sparing wild-type EGFR, which reduces toxicity compared to earlier EGFR TKIs. In clinical trials, osimertinib has shown high response rates in patients with the T790M mutation, with a median duration of response of 12.4 months.
In addition to its efficacy against the T790M mutation, osimertinib has also demonstrated activity against the EGFR C797S mutation, which is another mechanism of resistance to EGFR TKIs. Early preclinical data suggest that osimertinib could also have activity against other oncogenic drivers in NSCLC, such as the ALK and ROS1 rearrangements.
Osimertinib is administered orally, once daily, at a dose of 80 mg. Common side effects include diarrhea, rash, and nail toxicity, but these are generally manageable and rarely lead to treatment discontinuation.
Overall, osimertinib represents an exciting development in the treatment of EGFR-mutated NSCLC, particularly for patients with the T790M mutation who have limited treatment options. Ongoing research is investigating osimertinib in combination with other agents, as well as in earlier lines of therapy, which could further expand its utility in the management of lung cancer.
