PharmPK Discussion - In vivo CYPs Inhibition and Pgp

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On 19 May 2004 at 19:46:54, "Makram.B.R" (kimoberg_fr.-a-.yahoo.fr) sent the message

Hi everybody,
I'm searching  for an inhibitor of CYPs  in rats, that I can use in vivo,
and which not interfere with efflux proteins, specially P-gp (neither
substrate, inhibitor nor inducer) .
Thank You in advance ! Will certainly appreciate any response.
Regards,
Makrem,
PhD Student
Pharmacokinetics and Clinical Pharmacy Lab.
Faculty of Pharmacy South Paris - Paris XI - France

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On 20 May 2004 at 20:23:54, "Ansar A. Khan" (ansark.at.glenmarkpharma.com) sent the message

You can use 1-Aminobenzotriazole as an inhibitor of CYP in in vivo,
which does not interfere with Pgp
All the best
Ansar Ali Khan, M.Sc.,
Research Scientist,
Drug Metabolism and Pharmacokinetics,
Glenmark Research Centre,
Plot No.-A-607, TTC, Industrial Area,
Mahape, Navi Mumbai-400 709,
India.
Phone No: 91-22-5590 2491/92 Extn.308
Fax No.: 91-22-5590 2318

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On 20 May 2004 at 20:29:07, "Jean-Pierre Moreau" (jpmoreau.-at-.biopharmacopae.com) sent the message

Due to substrate specificity overlap it might be difficult, cyclosporine is
definitely out as it is a know inhibitor of PGP as well, maybe itraconazole
or ketoconazole but I am less knowledgable of their PGP profile.  One
should consider grapefruit juice if inhibition of 3A4 and 3A5 can be
limited to intestinal metabolism, some suggest that it might induce PGP but
it is less clear, see Kane et al, Mayo Clin Proc 2000;75:933-942.
Jean-Pierre Moreau

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