AZ9814

AZ9814 is a potent and selective small molecule inhibitor of Eg5 (also known as Kinesin Spindle Protein or KSP), a motor protein essential for the formation of a bipolar mitotic spindle. Developed by AstraZeneca, AZ9814 induces mitotic arrest and subsequent apoptosis in rapidly dividing cells. It has been investigated in preclinical models of urothelial cell carcinoma (UCC), where continuous systemic infusion was found to optimize the therapeutic index by balancing anti-tumor efficacy against dose-limiting bone marrow toxicities such as neutropenia and thrombocytopenia. Preclinical studies have compared various dosing routes, including intravesical and systemic administration, concluding that continuous systemic infusion maximizes the therapeutic margin for this class of inhibitors in bladder cancer models.