Carfilzomib: A novel second-generation proteasome inhibitor

Meaghan L. Khan, A. Keith Stewart

Research output: Contribution to journalArticle

47 Scopus citations

Abstract

Carfilzomib (formerly PR-171) is a novel epoxyketone-based irreversible proteasome inhibitor. In preclinical studies, carfilzomib demonstrated irreversible binding to the proteasome and minimal off-target inhibition of other proteases. In clinical studies carfilzomib has demonstrated substantial antitumor activity in hematologic malignancies while exhibiting a well-tolerated side-effect profile. Painful neuropathy was minimally reported, suggesting a possible advantage over other proteasome inhibitors. With single-agent carfilzomib, dose-limiting toxicity was hematologic and included thrombocytopenia and neutropenia. In patients with relapsed or refractory multiple myeloma, twice-weekly consecutive-day single-agent carfilzomib 20 mg/m2 for 3 weeks every 28 days, escalating to 27 mg/m2 the second cycle was associated with a 54% overall response rate in bortezomib-naive patients and a 26% overall response rate in bortezomib and immunomodulatory drug refractory patients.

Original languageEnglish (US)
Pages (from-to)607-612
Number of pages6
JournalFuture Oncology
Volume7
Issue number5
DOIs
StatePublished - May 2011

Keywords

  • PR-171
  • bortezomib
  • carfilzomib
  • chymotrypsin-like
  • multiple myeloma
  • proteasome inhibitor

ASJC Scopus subject areas

  • Oncology
  • Cancer Research

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