molecules of the month


allosteric mutant-EGFR inhibitor

in vivo efficacy in osimertinib-resistant xenograft models

from opt. of prev. disclosed EGFR inhibitor

Nat. Cancer

Dana-Farber Cancer Institute, Boston, MA

JBJ-09-063 chemical structure, allosteric mutant-EGFR inhibitor - Dana-Farber Cancer Institute, Boston, MA
6 mins read

Context. JBJ-09-063 (Dana-Farber Cancer Institute) is an oral allosteric EGFR inhibitor currently in pre-clinical development for the treatment of EGFR L858R-mutant non-small cell lung cancer (NSCLC). Despite the availability of 3 generations of EGFR TKIs for the treatment of EGFR-mutant NSCLC, drug resistance and associated disease relapse are highly prevalent. There is room for improvement in this therapeutic area, even with third-generation agents, such as osimertinib, that have demonstrated superior clinical outcomes. In a space currently dominated by agents targeting EGFR’s ATP-competitive site, JBJ-09-063 instead targets an allosteric site generated by the L858R mutation. Similar to other inhibitors currently being evaluated in preclinical studies, this binding strategy is at the center of a novel fourth generation of EGFR TKIs with…

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