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Summary of Phase Ⅰ data for MEK inhibitors approved |
GUO Yuying TIAN Hongqi |
Peking Union Medical College Institute of Radiation Medicine, Chinese Academy of Medical Sciences Tianjin Key Laboratory of Radiation Medicine and Molecular Nuclear Medicine, Tianjin 300192, China |
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Abstract The mitogen-activated extracellular signal-regulated kinase (MEK) is a dual specificity kinase that selectively phosphorylates serine/threonine and tyrosine residues on target protein. MEK has become an attractive target because inhibiting its activity can prevent cell proliferation and induce cell apoptosis. Phase Ⅰ clinical trials of new anti-tumor drugs have great risk, high fatality rate and is one of the key factors that affect the launch of the drug. Four MEK inhibitors have been approved by the U.S. Food and Drug Administration (FDA), including Trametinib, Cobimetinib, Binimetinib and Selumetinib. In this review, phase Ⅰ clinical trial data of these drugs are summarized to provide some references for other MEK inhibitors that are going to conduct phase Ⅰ clinical trials or are in clinical trials.
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