Phosphatidylinositol 3-kinases (PI3K) are lipid kinases that play a vital role in cell regulation, including cell survival, proliferation and differentiation. They act as intermediate molecules in PI3K/AKT/mTOR signaling pathway by sending chemical messengers from cell surface to cytoplasm. These signals activate multiple effector kinase pathways, including protein kinase B, bruton's tyrosine kinase and protein kinase C pathway, which result in survival and growth of normal cells. Recent cancer studies have shown that PI3K pathway is mostly targeted either by germline mutation or somatic mutation in human cancers, thus making it one of the most promising targets for therapeutics in cancer.
The activity of PI3K is strictly regulated by PTEN (phosphatase and tensin homolog deleted from chromosome 10) in normal cells. Abnormal activation of PI3K or dysregulated PI3K signaling pathway is mainly observed in tumor angiogenesis and carcinogenesis. Other genetic factors that target PI3K pathway in cancer development include loss of PTEN regulation, gene amplification in PI3Ks and receptor tyrosine kinases (RTKs) mutation activation. Due to all these factors, PI3K has emerged as an attractive target among researchers for novel cancer therapeutics.
Factors such as emerging combination therapies and biomarker identification are driving the growth of the PI3K inhibitors pipeline. Combination therapies are being used to stop further cancer growth and kill the cancerous cells. Also, combining novel drugs against different signaling pathways as well as combination of drugs with biological and biochemical agents may further enhance the treatment quality.
Companies are developing various biomarkers through next-generation sequencing with a single agent strategy at an early stage of development, which can help in avoiding recurrence of cancers. This approach can be applied as combination therapies or as single agent therapies.
Some of the key barriers hindering the growth of the PI3K inhibitors pipeline analysis are complex mechanism of action and alternative targets. The complex mechanism of action of PI3K creates problem in identifying the exact disease etiology. In cancer, mutation in receptor tyrosine kinase activate both PI3K and Raf-mitogen-activated protein kinase pathway that cause cross-inhibitory effect. This leads to the blocking effect on PI3K pathway.
For alternative targets, researchers identified that PI3K pathway is linked to many physiological processes, which results in hampering the clinical outcomes. This has led the researchers to think about several other targets that are associated with the PI3K/mTOR network, that can be successful as anti-cancer therapeutics.
As of March 2017, the PI3K inhibitors pipeline comprises approximately 37 active drug candidates in different stages of development.
NUMBER OF PI3K INHIBITORS DRUG CANDIDATES UNDER DEVELOPMENT (2017)
The major players for PI3K inhibitors pipeline include, but are not limited to, Novartis AG, Genentech, Inc., SignalRX Pharmaceuticals Inc. and others.
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