JBJ-09-063

JBJ-09-063 is a fourth-generation, mutant-selective allosteric inhibitor of the epidermal growth factor receptor (EGFR). It was developed to address acquired resistance in non-small cell lung cancer (NSCLC), specifically the C797S mutation that occurs following treatment with third-generation EGFR tyrosine kinase inhibitors (TKIs) like osimertinib. JBJ-09-063 is designed to inhibit EGFR variants harboring the L858R activating mutation, the T790M gatekeeper mutation, and the C797S resistance mutation, while sparing wild-type EGFR to minimize toxicity. It is often studied in combination with other EGFR inhibitors to enhance efficacy and delay the emergence of resistance.