Magdalena Zaborowska-Szmi, Sebastian Szmit, Maciej Krzakowski, Dariusz M Kowalski
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引用次数: 3
摘要
Savolitinib是一种高选择性的MET酪氨酸激酶抑制剂。MET参与了许多细胞过程,如增殖、分化和远处转移的形成。MET扩增和MET过表达在许多癌症中都很常见,但MET外显子14跳变在非小细胞肺癌(NSCLC)中最常见。MET信号作为旁路通路在EGFR基因突变的癌症患者对酪氨酸激酶抑制剂(TKI)表皮生长因子受体(EGFR)治疗的获得性耐药发展中的作用被记录。savolitinib治疗的潜在受益者是初始诊断为MET ex 14跳跃突变的非小细胞肺癌患者。Savolitinib治疗对EGFR-TKI一线治疗期间进展的egfr -突变MET NSCLC患者有效。savolitinib联合osimertinib的抗肿瘤活性非常有希望作为晚期egfr突变的NSCLC患者的一线治疗,最初是MET表达。在所有可用的研究中,savolitinib作为单一疗法和与奥西替尼或吉非替尼联合使用的安全性非常有利,因此该药物已成为一种非常有前途的治疗选择,正在进行的临床试验中进行深入研究。
Savolitinib is a highly selective MET tyrosine kinase inhibitor. MET is involved in numerous cellular processes such as proliferation, differentiation and the formation of distant metastases. MET amplification and MET overexpression are quite common in many cancers, but MET exon 14 skipping alteration is most common in non-small cell lung cancer (NSCLC). The role of MET signaling as a bypass pathway in the development of acquired resistance to tyrosine kinase inhibitor (TKI) epidermal growth factor receptor (EGFR) therapy in cancer patients with EGFR gene mutation was documented. Potential beneficiaries of savolitinib therapy are patients with NSCLC and initial diagnosis of MET ex 14 skipping mutation. Savolitinib therapy can be effective in NSCLC patients with EGFR-mutant MET with progression during first-line treatment with an EGFR-TKI. Antitumor activity of savolitinib in combination with osimertinib is very promising as first-line therapy of patients with advanced EGFR-mutated NSCLC, initially with MET expression. The safety profile of savolitinib as monotherapy and in combination with osimertinib or gefitinib is so favorable in all available studies that this drug has become a very promising therapeutic option and is being intensively investigated in ongoing clinical trials.
期刊介绍:
An international, peer-reviewed journal publishing monographs on new products entering the market and review articles.
Since its inception in 1965, Drugs of Today has established a reputation for excellence in providing physicians and other key healthcare professionals with practical, up-to-date monographs on recently approved and launched drugs.