P-glycoprotein effects of cyclic urea HIV protease inhibitor DMP 323 in competitional absorption studies

Martin Richter, Nóra Gyémánt, Joséf Molnár, Andreas Hilgeroth

Research output: Contribution to journalArticle

3 Citations (Scopus)

Abstract

Cyclic ureas form a perspective class of non-peptidic HIV-1 protease inhibitors with major bioavailability problems. Low absorption rates of DMP 323 as one of the first representatives led to investigations whether transport efflux pump P-glycoprotein (P-gp) within the intestine may be partly responsible for the low absorption rates. DMP 323 proved to be a P-gp substrate in competition studies with P-gp inhibitor ritonavir and H17 as a representative of another class of non-peptidic HIV-1 protease inhibitors. Intestinal DMP 323 absorption was mainly increased under co-application of both ritonavir and H17. DMP 323 used as a membrane efflux pump inhibitor itself showed little affinities to P-gp compared to H17 as strong P-gp inhibitor. So P-gp proved to play a decisive role in the low intestinal absorption of the cyclic urea representative DMP 323.

Original languageEnglish
Pages (from-to)625-628
Number of pages4
JournalArchiv der Pharmazie
Volume339
Issue number11
DOIs
Publication statusPublished - Nov 1 2006

Keywords

  • Competition studies
  • HIV-1 protease inhibitor
  • Intestinal absorption
  • P-glycoprotein

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Drug Discovery

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