Carfilzomib: A Promising Proteasome Inhibitor for the Treatment of Relapsed and Refractory Multiple Myeloma

Shansa Pranami E Jayaweera1, Sacheela Prasadi Wanigasinghe Kanakanamge1, Dharshika Rajalingam1

  • 1Department of Chemistry, Faculty of Science, University of Colombo, Colombo, Sri Lanka.

Frontiers in Oncology
|December 3, 2021
PubMed

Insights

Carfilzomib is a proteasome inhibitor that offers improved treatment options for multiple myeloma by irreversibly targeting proteasomes, potentially overcoming resistance seen with earlier drugs.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Oncology

Background:

  • The proteasome is vital for intracellular protein degradation, regulating cell survival and progression.
  • Cancer cells, particularly multiple myeloma (MM), exhibit heightened dependence on the ubiquitin proteasome pathway (UPP).
  • Proteasome inhibitors represent a key therapeutic strategy for human cancers like MM.

Purpose of the Study:

  • To review the biochemical properties and mechanism of action of carfilzomib.
  • To analyze the toxicity profile and clinical trial data for carfilzomib.
  • To highlight carfilzomib's potential to overcome bortezomib-related toxicities and resistance.

Main Methods:

  • Literature review of biochemical properties.
  • Analysis of preclinical and clinical trial data.
  • Comparison of carfilzomib with other proteasome inhibitors.

Main Results:

  • Carfilzomib is a second-generation proteasome inhibitor with irreversible binding.
  • It demonstrates efficacy in treating relapsed and/or refractory multiple myeloma.
  • Carfilzomib may offer an improved toxicity and resistance profile compared to bortezomib.

Conclusions:

  • Carfilzomib is an important therapeutic option for multiple myeloma patients.
  • Its irreversible binding mechanism addresses limitations of first-generation inhibitors.
  • Further research and clinical application are warranted for carfilzomib in MM treatment.

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