New phosphatidylinositol 3-kinase inhibitors for cancer

被引：64

作者：

Bowles, Daniel W. ^{[1
]}

Jimeno, Antonio ^{[1
,2
]}

机构：

[1] Univ Colorado, Ctr Comprehens Canc, Aurora, CO 80045 USA

[2] Univ Colorado, Charles C Gates Ctr Stem Cell Biol, Aurora, CO 80045 USA

来源：

EXPERT OPINION ON INVESTIGATIONAL DRUGS | 2011年 / 20卷 / 04期

关键词：

BEZ235; CAL-101; GDC-0941; PI3K; PIK3CA; PTEN; PX-866; SF1126; XL147; XL765; PHOSPHOINOSITIDE; 3-KINASE; ANTITUMOR-ACTIVITY; PI3K PATHWAY; LUNG-CANCER; PIK3CA AMPLIFICATION; ACQUIRED-RESISTANCE; GENE AMPLIFICATION; TUMOR-SUPPRESSOR; STEM-CELLS; DE-NOVO;

D O I：

10.1517/13543784.2011.562192

中图分类号：

R9 [药学];

学科分类号：

100702 [药剂学];

摘要：

Areas covered: This article reviews current literature and recent conference proceedings to analyze the rationale for targeting PI3K and its downstream effectors in cancer. Preclinical and clinical results of several PI3K and PI3K--mammalian target of rapamycin (mTOR) inhibitors in early clinical trials, as single agents and in combination with other drugs, are discussed. Thus far, clinical results have been mixed. Expert opinion: The clinical utility of PI3K and PI3K--mTOR inhibitors will depend on appropriate selection of patients. Mutations in the PI3K pathway may predict sensitivity to PI3K inhibition but they are not reliable biomarkers at this point. Efforts to define predictive biomarkers will probably be the key to finding therapeutic uses for this novel class of anticancer agents.

引用

页码：507 / 518

页数：12

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