MEK inhibitors: new weapon in the fight against melanoma

Cancer cell signaling has long been an attractive target for oncology drug development. Increased activation of cell survival signaling cascades promotes tumor cell growth and makes cancer cells difficult to kill, notes a new report from intelligence provider GlobalData. Inhibiting proteins that are involved in these survival pathways is one strategy to selectively destroy cancerous cells.

The mitogen activated protein kinase (MAPK) pathway is one such signaling cascade that, when activated, promotes cell survival. Preclinical research has found that this pathway is activated in most melanomas; consequently, one of the key kinases involved in this pathway, MEK, has become the focus of targeted therapies for the treatment of melanoma. MEK, which stands for MAPK/ERK kinase and is also known as MAPKK, has several known structural variants called “isoforms” which play different roles within the cell. Isoforms 1 and 2, referred to as MEK1/2, are the isoforms associated with MEK’s ability to promote cell survival.

Zelboraf already commercialized; others in development