Back to the Top
The following message was posted to: PharmPK
Hi All,
Does anybody know Is there a data base or a table that lists the
category of inhibitors (like weak, moderate,etc by using Ki or
IC50,...)
Thanks in advance
Amir Heydari
Back to the Top
The following message was posted to: PharmPK
Amir,
A general guideline for potency is given in the PhRMA
concensus paper on drug-drug interactions;
Bjornsson et al. (2003)
"THE CONDUCT OF IN VITRO AND IN VIVO DRUG-DRUG INTERACTION
STUDIES: A PHARMACEUTICAL RESEARCH AND MANUFACTURERS OF
AMERICA (PhRMA) PERSPECTIVE"
e.g. Drug Metabolism and Disposition 31, 815-832
(simultaneously published in other journals)
There is a summary table within the document giving a
prediction of clinical relevance of competitive P450
inhibition;
Cmax/Ki > 1 "Likely"
1 > Cmax/Ki > 0.1 "Possible"
0.1 > Cmax/Ki "Remote"
For non-competitive inhibition life becomes more
complicated.
There have been recent suggestions that these values
should depend upon which enzyme is actually being inhibited
but I haven't seen solid suggestions for such numbers.
All the very best,
Bernard
Bernard Murray, Ph.D.
Senior Pharmacologist
Drug Metabolism, PCS, PPD, GPRD, Abbott Laboratories, Chicago, USA
Bernard.Murray.at.abbott.com
Back to the Top
Inhibitor of what cyp's, transporters?
PharmPK Discussion List Archive Index page
Copyright 1995-2010 David W. A. Bourne (david@boomer.org)