title: Cabazitaxel: a novel microtubule inhibitor.
abstract: The development of drug resistance is a major obstacle to effective cancer therapy. Several agents are in clinical development with the goal of overcoming resistance. Among them is cabazitaxel, a semisynthetic taxoid that is able to overcome a common mechanism of resistance that limits the efficacy of other chemotherapeutic agents, including the older taxanes. The promise of cabazitaxel as a second-line chemotherapy option for advanced prostate cancer has been confirmed clinically in the phase III TROPIC (Treatment of Hormone-Refractory Metastatic Prostate Cancer Previously Treated with a Taxotere-Containing Regimen) trial. This trial showed that cabazitaxel is the first chemotherapeutic agent to demonstrate a survival benefit in metastatic castration-resistant prostate cancer (mCRPC) since the approval of docetaxel. On this basis, the US FDA and the European Medicines Agency approved cabazitaxel in June 2010 and January 2011, respectively, for the treatment of patients with mCRPC who have previously been treated with docetaxel. The most prevalent toxicity was neutropenia and the use of primary prophylaxis with granulocyte-colony stimulating factor is recommended in high risk patients. This article presents the preliminary antitumour activity, safety, tolerability and pharmacokinetic data of cabazitaxel, and an overview of the current status of clinical development.
authors.affiliation: Department of Medical Oncology, University Hospital, Besançon, France. cvillanueva@chu-besancon.fr
authors.forename: Cristian
authors.initials: C
authors.lastname: Villanueva
authors.forename: Fernando
authors.initials: F
authors.lastname: Bazan
authors.forename: Stefano
authors.initials: S
authors.lastname: Kim
authors.forename: Martin
authors.initials: M
authors.lastname: Demarchi
authors.forename: Loïc
authors.initials: L
authors.lastname: Chaigneau
authors.forename: Antoine
authors.initials: A
authors.lastname: Thiery-Vuillemin
authors.forename: Thierry
authors.initials: T
authors.lastname: Nguyen
authors.forename: Laurent
authors.initials: L
authors.lastname: Cals
authors.forename: Erion
authors.initials: E
authors.lastname: Dobi
authors.forename: Xavier
authors.initials: X
authors.lastname: Pivot
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000009:adverse effects / Q000493:pharmacokinetics / Q000494:pharmacology*; D017277:Drug Approval; D019008:Drug Resistance, Neoplasm; D016179:Granulocyte Colony-Stimulating Factor / Q000627:therapeutic use; D006801:Humans; D008297:Male; D009362:Neoplasm Metastasis; D009503:Neutropenia / Q000139:chemically induced / Q000517:prevention & control; D011471:Prostatic Neoplasms / Q000188:drug therapy* / Q000473:pathology; D013534:Survival; D043823:Taxoids / Q000009:adverse effects / Q000493:pharmacokinetics / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D043823:Taxoids; D016179:Granulocyte Colony-Stimulating Factor; C552428:cabazitaxel