Breakthrough in ovarian cancer: Selumetinib

In continuation  of my update on Seumetinab

We know that, Selumetinib (AZD6244) is a drug being investigated for the treatment of various types of cancer, for example non-small cell lung cancer (NSCLC). 

Mode of action : The gene BRAF is part of the MAPK/ERK pathway, a chain of proteins in cells that communicates input from growth factors. Activating mutations in the BRAF gene, primarily V600E (meaning that the amino acid valine in position 600 is replaced by glutamic acid), are associated with lower survival rates in patients with papillary thyroid cancer. Another type of mutation that leads to undue activation of this pathway occurs in the gene KRAS and is found in NSCLC. A possibility of reducing the activity of the MAPK/ERK pathway is to block the enzyme MAPK kinase (MEK), immediately downstream of BRAF, with the drug selumetinib. More specifically, selumetinib blocks the subtypes MEK1 and MEK2 of this enzyme....

The study was initially developed in 2007, with 52 patients enrolled for the Phase II clinical trial between December 2007 and November 2009. Patients were given 50 milligrams of selumetinib orally twice daily. Of those participants, eight had a measurable decrease in tumor size, seven had partial responses and 34 patients saw their tumors stabilize. The findings suggest that inhibitors of the MAPK pathway warrant further investigation in patients with low-grade ovarian cancer.

"There just aren't very good treatments for low-grade ovarian cancer, so this discovery opens up a lot of new exciting possibilities for us," Dr. Farley said. He added that Phase III of this trial is scheduled to begin in the next few weeks, with that trial to be the "definitive test" before the treatment becomes available to the general population.

Ref : http://www.thelancet.com/journals/lanonc/article/PIIS1470-2045(12)70572-7/fulltext



Breakthrough in ovarian cancer: Selumetinib