Bone Targeting Agents in Patients with Metastatic Prostate Cancer: State of the Art

Veronica Mollica, Alessandro Rizzo, Matteo Rosellini, Andrea Marchetti, Angela Dalia Ricci, Alessia Cimadamore, Marina Scarpelli, Chiara Bonucci, Elisa Andrini, Costantino Errani, Matteo Santoni, Rodolfo Montironi, Francesco Massari

Research output: Contribution to journalReview articlepeer-review


Bone health represents a major issue in castration-resistant prostate cancer (CRPC) patients with bone metastases; in fact, the frequently prolonged use of hormonal agents causes important modifications in physiological bone turnover and most of these men will develop skeletal-related events (SREs), including spinal cord compression, pathologic fractures and need for surgery or radiation to bone, which are estimated to occur in almost half of this patient population. In the last decade, several novel therapeutic options have entered into clinical practice of bone metastatic CRPC, with recent approval of enzalutamide and abiraterone acetate, cabazitaxel chemotherapy and radium-223, on the basis of survival benefit suggested by landmark Phase III trials assessing these agents in this setting. Conversely, although bone-targeted agents (BTAs)-such as the bisphosphonate zoledronic acid and the receptor activator of nuclear factor kappa-B (RANK) ligand inhibitor denosumab-are approved for the prevention of SREs, these compounds have not shown benefit in terms of overall survival. However, emerging evidence has suggested that the combination of BTAs and abiraterone acetate, enzalutamide and the radiopharmaceutical radium-223 could result in improved clinical outcomes and prolonged survival in bone metastatic CRPC. In this review, we will provide an overview on bone tropism of prostate cancer and on the role of BTAs in metastatic hormone-sensitive and castration-resistant prostate cancer.

Original languageEnglish
Pages (from-to)1-13
Number of pages13
Issue number3
Publication statusPublished - Feb 1 2021


  • CRPC
  • HSPC
  • bone metastasis
  • bone-targeted agents
  • denosumab
  • prostate cancer
  • zoledronic acid


Dive into the research topics of 'Bone Targeting Agents in Patients with Metastatic Prostate Cancer: State of the Art'. Together they form a unique fingerprint.

Cite this