PharmPK Discussion - Arishel Newsletter: No 3, September 23, 2007

• On 28 Sep 2007 at 17:04:56, Clerk Maxwell (clerkmaxwell.aaa.hotmail.com) sent the message
  

  
  Topotecan oral bioavailability increased dramatically by inhibiting BCRP
  
  Topotecan, an anti-cancer drug, is being administered IV, since its
  oral absolute bioavailability (F) is 42 +/- 13 %.  This relatively
  low value for F is primary due to the effect of the gut efflux
  transporter breast cancer resistance protein (BCRP).  By blocking the
  effect of BCRP with elacridar, the oral absolute bioavailability of
  topotecan increases to 100%.  The reference cited below deals with
  this phenomenon:
  
  A phase I, randomized, open-label, parallel-cohort, dose-finding
  study of elacridar (GF120918) and oral topotecan in cancer patients.
  Clin Cancer Res, 2007 Jun 1;13(11):3276-85.
  Kuppens IE, Witteveen EO, Jewell RC, Radema SA, Paul EM, Mangum SG,
  Beijnen JH, Voest EE, Schellens JH.
  
  Harold Boxenbaum, Ph.D.
  Pharmacokinetics Consultant
  Arishel Inc.
  14621 Settlers Landing Way
  North Potomac, MD 20878-4305
  (P) 301-424-2806
  (F) 301-424-8563
  harold.-at-.arishel.com
  www.arishel.com
  
  

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