Pharmacokinetics and safety of apremilast (CC-10004) in subjects with hepatic impairment

Mahmoud S. Assaf, Eric Laille, Liangang Liu, Edward O'Mara, Anfan Wu, Maria Palmisano, Thomas C. Marbury, Richard A. Preston

Research output: Contribution to journalArticle

1 Scopus citations

Abstract

Apremilast (CC-10004), a PDE4 enzyme inhibitor, is under clinical development for the treatment of inflammatory immune-mediated disorders. Since apremilast is extensively metabolised via multiple routes, impact of hepatic impairment on the pharmacokinetics (PK) of apremilast and M12 metabolite was evaluated. Thirty-two subjects were enrolled in a two-centre, open-label, and single-dose study. Subjects with moderate hepatic impairment and their healthy matches received a single 30-mg dose and subjects with severe hepatic impairment and their healthy matches received a single 20-mg dose of apremilast. Plasma concentrations of apremilast and M12 were measured, PK parameters calculated, and statistically compared. During the study, single doses of apremilast were well tolerated, with no clinically meaningful safety findings observed. PK parameters were comparable between hepatic impaired and healthy subjects, and there was no evidence to suggest that the PK of apremilast is affected by moderate and severe hepatic impairment. Therefore, no dose adjustment is required.

Original languageEnglish (US)
Pages (from-to)100-114
Number of pages15
JournalInternational Journal of Medical Engineering and Informatics
Volume6
Issue number2
DOIs
StatePublished - 2014

Keywords

  • Apremilast
  • Hepatic impairment
  • Hepatic metabolism
  • PDE4
  • Pharmacokinetics
  • Phosphodiesterase 4
  • PK

ASJC Scopus subject areas

  • Biomedical Engineering
  • Health Informatics
  • Medicine (miscellaneous)
  • Biomaterials

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