Recent clinical advances in PI3K inhibitors on colorectal cancer

被引:13
|
作者
Zhu, Mingliang [1 ]
Jin, Qiuyang [1 ]
Xin, Yizhou [1 ]
机构
[1] Shandong Univ Tradit Chinese Med, Affiliated Hosp, Dept Pharm, Jinan 250014, Peoples R China
来源
PHARMAZIE | 2021年 / 76卷 / 12期
关键词
PHOSPHATIDYLINOSITOL 3-KINASE INHIBITOR; PHASE-II TRIAL; KINASE INHIBITOR; DOSE-ESCALATION; DUAL INHIBITOR; SYNERGISTIC INHIBITION; ANTITUMOR-ACTIVITY; BUPARLISIB BKM120; PIK3CA MUTATION; PX-866;
D O I
10.1691/ph.2021.1820
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The PI3K/Akt/mTOR signaling pathway has the functions of regulating cell cycle, participating in tumor angiogenesis, affecting tumor invasion activity and metastasis, regulating apoptosis and autophagy, and participating in tumor drug resistance. Alpelisib (a PI3K inhibitor) has now been approved by the FDA for the treatment of PIK3CA mutant HR-positive/HER2-negative advanced/metastatic breast cancer in combination with fulvestrant which is the first PI3K inhibitor approved for breast cancer treatment. In some human colorectal cancer cells, the activation of this signal pathway is excessive and the negative regulation is impaired. Inhibitors targeting PI3K, a key protein in the PI3K/Akt/mTOR signaling pathway, have a positive effect on the treatment of colorectal cancer. Based on the role of PI3K/Akt/mTOR in the occurrence and development of colorectal cancer and its clinical application, this article reviews the PI3K inhibitors that have been on the market or are in clinical trials.
引用
收藏
页码:568 / 573
页数:6
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