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Early clinical experience with the novel proteasome inhibitor PS–519 by I. M. Shah; K. R. Lees; C. P. Pien; P. J. Elliott is a Medicine article available to read on EtoBox.

What is Early clinical experience with the novel proteasome inhibitor PS–519 about?

**__Aims__** The main objective of this study was to investigate the safety, tolerability and pharmacodynamics of the novel proteasome inhibitor PS−519 in young male volunteers. Many pro‐inflammatory mediators such as cytokines and cell adhesion molecules that are responsible for the development of the cerebral infarct are under the control of the transcription factor Nuclear Factor kappa‐B (NF‐κB). The activity of NF‐κB is itself tightly regulated through the multicatalytic enzyme known as the proteasome. PS‐519 is a novel and highly selective small molecule that inhibits the proteasome. An __ex vivo__ assay of 20S proteasome activity allows monitoring of the drug effect in blood. PS‐519 is protective in multiple animal models of cerebral ischaemia over a range of doses that achieve 20S inhibition of 40%−80%. **__Methods__** PS‐519 has been administered to healthy male volunteers as single and repeated doses up to 1.6 mg m^−2^. It was given as an intravenous bolus over 20–30 s in a double blind, randomized, placebo‐controlled phase I study, examining vital signs, safety, tolerability and blood 20S proteasome inhibition. **__Results__** Thirty‐nine subjects rec

Who reads Early clinical experience with the novel proteasome inhibitor PS–519?

Author

I. M. Shah; K. R. Lees; C. P. Pien; P. J. Elliott

Publisher

John Wiley and Sons; Wiley (Blackwell Publishing); Blackwell Publishing Inc.; Wiley; Research Square (ISSN 0306-5251)

Published

2002

Language

EN

Field

Medicine (Health Sciences)