AXL Inhibitors in Oncology Clinical Trials: A Review

The AXL receptor tyrosine kinase is a transmembrane protein commonly overexpressed in both solid and hematologic malignancies. AXL plays a role in malignant cell growth, survival, proliferation, and adaptive immunity. As such, AXL overexpression is correlated with a worse prognosis. Drugs impairing the function of AXL are currently in development as monotherapies and in combination with other agents and have displayed antitumor efficacy in preclinical models, including tumors with AXL overexpression. AXL inhibitors have demonstrated preliminary antitumor activity in clinical trials and have generally been well tolerated, with the most common side effects including neutropenia, diarrhea, fatigue, nausea, and anemia. This clinical review aims to provide a comprehensive summary of published information from clinical trials investigating AXL inhibitors as monotherapies or in combination regimens.