Kinase Inhibitor Drugs

A comprehensive resource on case studies of marketed kinase drugs and promising drug trials

Since the discovery of protein kinase activity in 1954, the field of protein kinase drug discovery has advanced dramatically. With the ongoing clinical success of the Bcr-Abl kinase inhibitor Gleevec in the treatment of chronic myelogenous leukemia and seven additional marketed kinase inhibitor drugs, researchers have compelling evidence that kinase inhibitors can be highly efficacious in the treatment of diseases caused by aberrant activity of protein kinase. Currently more than 100 protein kinase inhibitors are in clinical development.

In one comprehensive volume, the editors, Dr. Rongshi Li and Dr. Jeffrey Stafford, present timely and important case studies of marketed kinase drugs and several of the most advanced kinase inhibitors in clinical trials. Kinase Inhibitor Drugs includes:

• Case studies from leading investigators and experts in the field that provide firsthand accounts of kinase inhibitor discovery

• Current thinking on kinase structure, biochemistry, and signal transduction pathways

• Information on state-of-the-art technologies and tools such as structure-based and fragment-based drug discovery

• A lineup of clinical-phase growth factor receptor inhibitors

• Inhibitors of cell cycle kinases

• The discovery of allosteric inhibitors of MEK kinase

• Information on pharmacogenomics and its application to kinase inhibitor clinical development

Rongshi Li, PhD, is an Associate Professor in the Drug Discovery Department at H. Lee Moffitt Cancer Center and Research Institute in Tampa, Florida.

Jeffrey A. Stafford, PhD, has led drug discovery research at GlaxoSmithKline, Syrrx, and Takeda. He is a co-inventor of the tyrosine kinase inhibitor, pazopanib (Armala).