Improved understanding of prostate cancer biology in recent years has led to the development of new targeted agents for the treatment of castration-resistant prostate cancer, many of which are particularly effective on osseous disease, which is predominant in prostate cancer. We reviewed here some of these promising agents. Data from early Phase I/II trials are promising. In Phase III studies, the RANK ligand inhibitor denosumab was associated with a delay in the occurrence of bone metastasis, and a reduction in the incidence of skeletal-related events. With endothelin receptor antagonists, Phase III results have been disappointing. The results of a Phase III trial with the a-radiation emitter alpharadin are expected soon. The SRC tyrosine kinase inhibitors are also being tested in randomized trials.
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