title: Carfilzomib for the treatment of patients with relapsed and/or refractory multiple myeloma.
abstract: Carfilzomib is a proteasome inhibitor that irreversibly binds to its target, resulting in sustained proteasomal inhibition with minimal off-target effects. As a single agent, carfilzomib has demonstrated durable antimyeloma activity with manageable toxicities, which has resulted in its approval in Argentina, Israel, Mexico and the USA for the treatment of patients with relapsed and refractory multiple myeloma. Data from ongoing Phase III studies that are evaluating carfilzomib in earlier lines of therapy may facilitate an expanded indication for this agent, as well as for regulatory approval in the EU. This article summarizes the chemistry, pharmacokinetics, pharmacodynamics and available clinical data for carfilzomib in the treatment of patients with multiple myeloma.
authors.affiliation: Mayo Clinic, 13400 East Shea Blvd, Scottsdale, AZ 85259, USA.
authors.forename: A Keith
authors.initials: AK
authors.lastname: Stewart
mesh_terms: D017326:Clinical Trials, Phase III as Topic; D004305:Dose-Response Relationship, Drug; D064420:Drug-Related Side Effects and Adverse Reactions / Q000473:pathology; D006801:Humans; D009101:Multiple Myeloma / Q000188:drug therapy* / Q000473:pathology; D009364:Neoplasm Recurrence, Local / Q000188:drug therapy* / Q000473:pathology; D009842:Oligopeptides / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D046988:Proteasome Endopeptidase Complex / Q000187:drug effects*; D061988:Proteasome Inhibitors / Q000493:pharmacokinetics / Q000627:therapeutic use
chemical_list: D009842:Oligopeptides; D061988:Proteasome Inhibitors; C524865:carfilzomib; D046988:Proteasome Endopeptidase Complex
keywords: carfilzomib; efficacy; multiple myeloma; proteasome inhibitor; relapsed and/or refractory; safety