[4] Cooper, A.J., Sequist, L.V. & Lin, J.J. Third-generation EGFR and ALK inhibitors: mechanisms of resistance and management. Nat Rev Clin Oncol 19, 499–514 (2022). [5] Ricordel, C., et al. "Molecular mech...
based virtual screening was utilized to screen effective inhibitors targeting wild-type ALK and the gatekeeper mutation L1196M from 3180 approved drugs. Finally, the mechanism of drug resistance was discussed, several novel potential wild-type and L1196M mutant ALK inhibitors were successfully identifie...
22种治疗药物中有20种被批准用于NSCLC作为初始适应症,其中大多数被归类为表皮生长因子受体(EGFR)和间变性淋巴瘤激酶(ALK)抑制剂。 EGFR突变见于约50%的亚洲患者和11~16%的欧洲国家NSCLC患者,FDA已批准6种EGFR酪氨酸激酶抑制剂(TKI),成为携带EGFR突变的NSCLC患者的...
For an examination of the properties of the spine and shell residues and their interactions with low molecular weight inhibitors of important members of the protein kinase superfamily, see the following articles: Refs. [33], [34], [35] for the ALK pleotrophin and midkine receptor protein-...
6、Lipid kinase inhibitor2012一 qzu- SEX0-3 -old =eES p(D>odde jo(DqEnN(CrizotinibJAlectinib;(PazopambCbimetinib ;ib Osimertinib:BlLenvatinibalbocicnib图 3 Small molecular kinase inhibitors approved by FDA in 2001-2016在获批的31中小分子激酶抑制剂类药物中(图3),绝大多数为酪氨酸激酶抑制剂...
[62,63]. The FDA has approved five ALK inhibitors, which have been the first-line standard of care for patients with NSCLC harboringALKrearrangements [17], including the first-generation ALK inhibitor (crizotinib [64,65]), the second-generation ALK inhibitors (ceritinib [66], alectinib [67]...
2022年10月8日,杭州医学院的姜少杰等人,在知名肿瘤学期刊Journal of Hematology & Oncology发表了题为“Small-molecule inhibitors, immune checkpoint inhibitors, and more: FDA-approved novel therapeutic drugs for solid tumors from 1991 to 2021”的综述文章,详细综述了120种实体肿瘤治疗药物的性质,总结了其抗肿...
Cardiac arrhythmias associated with anaplastic lymphoma kinase (ALK) inhibitors: an analysis of the FDA Adverse Event Reporting System (FAERS)Feifei WangGuishui XuXinan Wu
2022年10月8日,杭州医学院的姜少杰等人,在知名肿瘤学期刊Journal of Hematology & Oncology发表了题为“Small-molecule inhibitors, immune checkpoint inhibitors, and more: FDA-approved novel therapeutic drugs for solid tumors from 1991 to 2021”的综述文章,详细综述了120种实体肿瘤治疗药物的性质,总结了其抗肿...
FDA批准了5款ALK抑制剂,目前是ALK重排NSCLC患者的标准一线治疗,包括一代ALK抑制剂克唑替尼,二代TKI塞瑞替尼、阿来替尼和布格替尼,以及三代ALK抑制剂洛拉替尼。ALK抑制剂耐药机制包括靶内机制和靶外机制。20%~36%克唑替尼耐药患者携...