Carfilzomib for the treatment of patients with relapsed and/or refractory multiple myeloma.

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.