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Review
. 2010 Nov;19(11):1355-66.
doi: 10.1517/13543784.2010.520701. Epub 2010 Sep 16.

Akt inhibitors in clinical development for the treatment of cancer

Sumanta Kumar Pal  1 , Karen Reckamp, Hua Yu, Robert A Figlin
Affiliations
Review

Akt inhibitors in clinical development for the treatment of cancer

Sumanta Kumar Pal et al. Expert Opin Investig Drugs. 2010 Nov.

Abstract

Importance of the field: The evolution of _targeted therapies is dependent upon identification of cellular moieties that can be pharmacologically modulated. As one such example, the serine-threonine kinase Akt was identified nearly two decades ago. Since then, its role in mediating multiple signaling cascades (ultimately leading to cell growth and proliferation) has since been identified. More recently, several agents have been developed that antagonize Akt--these agents are in various stages of clinical testing.

Areas covered in this review: Herein, we outline development of several promising Akt inhibitors, including perifosine, MK-2206, RX-0201, PBI-05204, GSK2141795 and others.

What the reader will gain: The reader will gain insight into the current pipeline of Akt inhibitors, and the degree to which these agents have been examined both clinically and preclinically.

Take home message: With an emerging pipeline of agents _targeting Akt, it will be critical to decipher which amongst them holds the greatest promise. Herein, we explore this drug pipeline and provide strategies for determining the future clinical application of these agents.

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Figures

Figure 1
Figure 1
Signal transduction cascades relevant to Akt-mediated cell growth and proliferation.
Figure 2
Figure 2
Suggested designs for clinical trials evaluating biomarkers. (Adapted from Pal SK, Figlin RA: Renal Cell Carcinoma in 2010: Many Options with Little Comparative Data Clin Adv Hem Onc 8(3):1–7.)
See this image and copyright information in PMC

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