enmd-2076 and danusertib

The Aurora kinase family of kinases (Aurora A, B, and C) are involved in multiple mitotic events, and aberrant expression of these kinases is associated with tumorigenesis. Aurora A and Aurora B are validated anticancer targets, and the development of Aurora kinase inhibitors has progressed from preclinical to clinical studies. A variety of Aurora A, B and pan-Aurora kinase inhibitors have entered the clinic. The main side effects include febrile neutropenia, stomatitis, gastrointestinal toxicity, hypertension, and fatigue. Responses including complete remissions have been described in diverse, advanced malignancies, most notably ovarian cancer and acute myelogenous leukemia. This review highlights the biologic rationale for Aurora kinase as a target, and clinical trials involving Aurora kinase inhibitors, with particular emphasis on published early phase studies, and the observed anti-tumor activity of these agents.

Topics: Antineoplastic Agents; Aurora Kinase A; Aurora Kinase B; Aurora Kinases; Benzamides; Benzazepines; Benzimidazoles; Clinical Trials as Topic; Heterocyclic Compounds, 3-Ring; Humans; Molecular Targeted Therapy; Neoplasms; Norbornanes; Organophosphates; Piperazines; Protein Kinase Inhibitors; Pyrazoles; Pyrimidines; Quinazolines; Urea