Clinical and pharmacokinetic evaluation of satraplatin

Introduction: The toxicities of cisplatin, that is, nephrotoxicity, neurotoxicity and emesis, provided the impetus for the development of more tolerable platinum analogs. Satraplatin is an investigational third-generation orally available lipophilic platinum, which has demonstrated safety and antitumor activity in multiple settings. Areas covered: The clinical activity of satraplatin in metastatic castrate-resistant prostate cancer (mCRPC), breast, lung and other advanced solid tumors is discussed with a focus on its pharmacokinetic properties. The article was formulated using publications found through PubMed search in addition to presentations given at major conferences. Expert opinion: Satraplatin was associated with dose-limiting myelosuppression, but no significant ototoxicity, neurotoxicity or nephrotoxicity. Despite the activity of satraplatin in mCRPC, survival was not extended in an unselected population included in a Phase III trial. While further development of satraplatin in large Phase III trials is not planned at this time, efforts are ongoing to develop tailored therapy in mCRPC based on excision repair cross-complementing group 1 expression or BRCAness. Moreover, based on potentially better central nervous system penetration due to lipophilicity, evaluation in patients with brain tumors is ongoing. Given the favorable toxicity profile and convenient oral administration, satraplatin may warrant development in settings that preclude cisplatin, for example, underlying renal dysfunction, elderly age and poor performance status.