erlotinib + gilteritinib

This drug is a combination of two targeted small molecule inhibitors used in cancer therapy. Erlotinib is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor primarily indicated for metastatic non-small cell lung cancer (NSCLC) with specific EGFR mutations and locally advanced or metastatic pancreatic cancer in combination with gemcitabine. Gilteritinib is a potent selective inhibitor of FLT3 receptor tyrosine kinase mutations (internal tandem duplication ITD and tyrosine kinase domain TKD), also inhibiting AXL and ALK kinases, approved for relapsed or refractory acute myeloid leukemia (AML) with FLT3 mutation. The combination has been noted to increase the risk or severity of QTc prolongation, indicating potential cardiac safety concerns when used together. Mechanistically, erlotinib blocks EGFR signaling pathways involved in tumor cell proliferation, while gilteritinib inhibits FLT3-driven leukemic cell growth and survival pathways. The combined use may be explored to overcome resistance mechanisms in cancers involving these pathways.

Other names

erlotinib + gilteritinib