ligritinib

Ligritinib (AB801) is an orally bioavailable small molecule inhibitor of the AXL receptor tyrosine kinase. AXL is a member of the TAM (TYRO3, AXL, MER) receptor family and is frequently overexpressed in various malignancies, including cholangiocarcinoma and pancreatic adenocarcinoma. Overactivation of AXL is associated with epithelial-to-mesenchymal transition (EMT), tumor progression, metastasis, and resistance to chemotherapy and immunotherapy. By inhibiting AXL, ligritinib aims to sensitize tumor cells to cytotoxic agents and enhance the efficacy of immune checkpoint inhibitors by modulating the tumor microenvironment. It is currently being investigated in Phase 1/1b clinical trials in combination with chemotherapy (e.g., gemcitabine, cisplatin) and PD-1/PD-L1 blockade (e.g., durvalumab, zimberelimab) for the treatment of advanced solid tumors.