Molecular underpinnings of enzalutamide resistance

Prostate cancer (PCa) is among the most common adult malignancies, and the second leading cause of cancer-related death in men. As PCa is hormone-dependent, blockade of the androgen receptor (AR) signaling is an effective therapeutic strategy for men with advanced metastatic disease. The discovery of enzalutamide, a compound that effectively blocks the AR axis and its clinical application has led to a significant improvement in survival time. However, the effect of enzalutamide is not permanent, and resistance to treatment ultimately leads to development of lethal disease, for which there currently is no cure. This review will focus on the molecular underpinnings of enzalutamide resistance, bridging the gap between the preclinical and clinical research on novel therapeutic strategies for combating this lethal stage of prostate cancer.

Endocrine-related cancer. 2018 Jul 05 [Epub ahead of print]

Stefan Prekovic, Thomas Van den Broeck, Simon Linder, Martin E van Royen, Adriaan Houtsmuller, Florian Handle, Steven Joniau, Wilbert Zwart, Frank Claessens

S Prekovic, Oncogenomics, Antoni van Leeuwenhoek Nederlands Kanker Instituut, Amsterdam, Netherlands., T Van den Broeck, Development and regeneration, University Hospitals Leuven, Leuven, 3000, Belgium., S Linder, Oncogenomics, Antoni van Leeuwenhoek Nederlands Kanker Instituut, Amsterdam, Netherlands., M van Royen, Department of Pathology, Erasmus MC, Rotterdam, Netherlands., A Houtsmuller, Department of Pathology, Erasmus MC, Rotterdam, Netherlands., F Handle, Laboratory of Molecular Endocrinology, KU Leuven, Leuven, Belgium., S Joniau, Development and Regeneration, University Hospitals Leuven, Leuven, Belgium., W Zwart, Oncogenomics, Antoni van Leeuwenhoek Nederlands Kanker Instituut, Amsterdam, Netherlands., F Claessens, , Laboratory for Molecular Endocrinology, Katholieke Universiteit Leuven, Leuven, Belgium .