While the activity of enzastaurin was modest in the pre-ARSi era, due to the establishment of ARSi therapies and the prevalence of AR-V7-positive metastatic CRPC, we feel that our in vitro and in vivo work justifies PKCβ1 inhibition in combination with AR antagonists as a viable strategy for further clinical evaluation against AR-V7-positive prostate cancer in an AR-V7 biomarker-selected trial. The gene discussed is AR; the disease is prostate cancer.