PharmPK Discussion - Human Intestinal Efflux Transporters

• On 28 Jan 2007 at 15:40:10, "Clerk Maxwell" (clerkmaxwell.aaa.hotmail.com) sent the message
  

  
  All,
  
  I have engaged in a great deal of reading on human intestinal efflux
  transporters.  The ones that seem to be "significant" are: BRCP,
  ISBT, LRP, MRP-1, MRP-2, MDR-1 (PGP) and PEPT1.  My question is
  simple.  How does one take a new chemical entity (NCE) and test to
  see if any of these is an active efflux transporter in humans.  Of
  course, PGP is easy to do with CACO-2 cells.  But what about the
  rest.  The literature is replete with references and lots of genetic
  information, but a "synthesis of thought" (e.g., a good review
  article) on practical testing seems to be elusive.  Any help would be
  greatly appreciated.  Thanks, Harold.
  
  Harold Boxenbaum, Ph.D.
  Pharmacokinetic Consultant
  Arishel Inc.
  14621 Settlers Landing Way
  North Potomac, MD 20878-4305
  (P) 301-424-2806
  (C) 240-422-0525
  (F) 301-424-8563
  Email: harold.-a-.arishel.com
  Website: www.arishel.com
  
  

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