1.Pharmacology and Clinical Evaluation of Ensartinib Hydrochloride Capsule.
Yang WANG ; Xiaobin YUAN ; Jiayan XIONG ; Zhidong HAO ; Xingzhe PENG ; Wanlin CHEN ; Lingling CUI ; Hua LI ; Xiulan WANG ; Xiangbo HE ; Min YANG ; Congxin LIANG ; Yongbin MA ; Lieming DING ; Li MAO
Chinese Journal of Lung Cancer 2020;23(8):719-729
Lung cancer is one of the most common malignancies with the highest incidence rate and mortality rate worldwide, and non-small cell lung cancer (NSCLC) accounts for about 85%. Only 5% NSCLC patients are anaplastic lymphoma kinase (ALK) rearrangement positive NSCLC, but the prognosis of these patients is poor, and treatment is urgent. Ensartinib (X-396), a next-generation ALK tyrosine kinase inhibitor (ALK-TKI), has shown greater potency on inhibiting ALK activity and controlling brain metastases than crizotinib, which is indicated for the treatment of crizotinib-resistant, ALK-positive NSCLC patients. Several phase I to III clinical trials included both healthy volunteers and NSCLC patients have been conducted both in China and abroad. In this review, we briefly summarized the results of these trials, and preliminary efficacy, safety, pharmacology and pharmacokinetics/pharmacodynamics of ensartinib were discussed.
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