Pharmacology differences among proteasome inhibitors: Implications for their use in clinical practice

Preclinical and clinical investigation on proteasome as a druggable target in cancer has led to the development of proteasome inhibitors (PIs) with different pharmacodynamic and pharmacokinetic properties. For example, carfilzomib has a better safety profile and a lower risk of clinically relevant drug-drug interactions than bortezomib, whereas ixazomib can be orally administered on a weekly basis due to a very long elimination half-life and high systemic exposure. The purpose of this review article is to elucidate the quantitative and qualitative differences in potency, selectivity, pharmacokinetics, safety and drug-drug interactions of clinically validated PIs to provide useful information for their clinical use in real life setting.

Automated summary

This review article explores the differences in potency, selectivity, pharmacokinetics, safety, and drug-drug interactions of clinically validated proteasome inhibitors, aiming to provide useful information for their clinical use in real life settings.