67DHB Grapefruit Inhibitor

Case ID:
96-387

The invention comprises a composition and methods for inhibiting cytochrome P450 enzyme activity and, in particular, inhibiting the activity of the cytochrome P450 3A sub-family of enzymes, specifically, CYP3A4.  It is believed that 6',7'-dihydroxybergamottin, a furanocoumarin, is the compound primarily responsible for the inhibitory effects of grapefruit juice on cytochrome P450 enzyme activity.  The compound is potentially useful as an inhibitor of cytochrome P450 by incorporating 67DHB into the formulation of a drug for the purpose of improving the bioavailability of the drug.  It may also be useful by itself as a chemopreventive agent to reduce cancer risk.
 

References:
Issued Patent: 6,160,006
 
1997 "Synthesis and biological evaluation of 6',7'-dihydroxybergamottin (6,7-DHB), a naturally occurring inhibitor of cytochrome P450 3A4"
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS  Vol 7 (20) pp2593-2598
 
Patent Information:
For Information, Contact:
Nicole Grynaviski
Commercialization Principal
Wayne State University
nicole.grynaviski@wayne.edu
Inventors:
Patrick Woster
David Edwards
Keywords: