“Docking studies predicted a shift of EVG or COBI binding to the active site of CYP3A4 in the presence of ethanol.”
“Inhibition studies demonstrated that EVG inhibits CYP3A4, and 20 mM ethanol causes a decrease in the IC50 of EVG.”
“Our substrate kinetic results revealed that ethanol mildly decreases the catalytic efficiency for EVG metabolism.”
“Taken together, these results suggest that ethanol interacts with microsomal CYP3A and alters EVG-CYP3A4 interaction thereby altering EVG metabolism and inhibition of CYP3A4 by EVG.”
“Time dependent kinetics data showed that 20mM ethanol decreases the apparent half-life of EVG degradation by ~50% compared to EVG alone.”