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“Borne Out of Necessity and Data”: Conquering Mutations in Leukemia By Jessica Wapner Posted: February 6, 2013

“Borne Out of Necessity and Data”: Conquering Mutations in Leukemia By Jessica Wapner 'A couple of months ago, the FDA approved the latest drug to treat chronic myeloid leukemia (CML). Called ponatinib (brand name Iclusig, made by Ariad), the drug is a third-generation tyrosine kinase inhibitor, the latest in a class of agents founded in 2001 with the approval of imatinib (Gleevec, Novartis). Imatinib, followed by dasatinib and nilotinib, and now ponatinib, are tyrosine kinase inhibitors. These drugs block the activity of a mutant kinase that triggers the growth of white blood cells in an uncontrolled way. By plugging up the site at which the kinase binds with ATP (the energy storehouse of the cell, from which the kinase plucks a single phosphate and then transports that phosphate to the next protein in line on the pathway that leads to white blood cell production), these drugs essentially stop the process that defines CML.

Called ponatinib (brand name Iclusig, made by Ariad), the drug is a third-generation tyrosine kinase inhibitor, the latest in a class of agents founded in 2001 with the approval of imatinib (Gleevec, Novartis). Imatinib, followed by dasatinib and nilotinib, and now ponatinib, are tyrosine kinase inhibitors. These drugs block the activity of a mutant kinase that triggers the growth of white blood cells in an uncontrolled way. By plugging up the site at which the kinase binds with ATP (the energy storehouse of the cell, from which the kinase plucks a single phosphate and then transports that phosphate to the next protein in line on the pathway that leads to white blood cell production), these drugs essentially stop the process that defines CML.

Cheerleading new drugs isn’t always warranted. But there is something truly impressive going on with this particular line of medicines. They work well, often with few side effects, and are among the most successful cancer drugs ever made.'...read full post here:

http://blogs.plos.org/workinprogress/2013/02/06/borne-out-of-necessity-a...