As tar­get­ed ther­a­pies get ever more pre­cise, Deer­field un­veils $50M bet on a Har­vard pro­fes­sor's chem­istry in­sights

Be­hind the seem­ing­ly sim­ple con­cept of tar­get­ed can­cer ther­a­pies is the drug de­vel­op­er’s headache that the tar­get is al­ways chang­ing. Each gen­er­a­tion of ki­nase in­hibitors may be os­ten­si­bly hit­ting the same onco­gene, but in ad­di­tion to block­ing the wild­type onco­gene, they must now al­so ad­dress the mu­ta­tions that have de­vel­oped along the way, spurring re­sis­tance to cur­rent drugs.

The more those tar­get ki­nas­es evolve, too, the more they could re­sem­ble off-tar­get ki­nas­es you don’t want to bind. So each it­er­a­tion re­quires more se­lec­tiv­i­ty — some­times down to dif­fer­ences of a few atoms.

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