tipifarnib + osimertinib

Tipifarnib + osimertinib is an investigational combination therapy comprising **tipifarnib**, a selective farnesyltransferase inhibitor, and **osimertinib**, a third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor. The combination is primarily being studied for the treatment of advanced or metastatic EGFR-mutated non-small cell lung cancer (NSCLC). Tipifarnib inhibits farnesyltransferase, thereby disrupting the post-translational modification and function of key proteins, including RAS family members, which are implicated in tumor resistance; osimertinib selectively inhibits both sensitizing and resistance EGFR mutations, including T790M. Preclinical and emerging clinical data suggest the combination may delay or prevent the development of acquired resistance to EGFR-targeted therapy by targeting complementary resistance pathways[1][4][5][6].