Cytochromes P450 (P450s) 3A, 2C, and 1A2 constitute the major “pieces” of the human
liver P450 “pie” and account, on average, for 40, 25, and 18%, respectively, of total …

Cytochrome P450 3A (CYP3A) metabolizes a diverse array of clinically important drugs. For
some of these (eg, cyclosporine, verapamil, midazolam), CYP3A in the intestinal mucosa …

Objective To determine in humans the relative roles of intestinal and hepatic metabolism in
the oral first‐pass elimination of a CYP3A substrate using midazolam as a model compound. …

The in vivo intestinal metabolism of the CYP3A probe midazolam to its principal metabolite,
1′‐hydroxymidazolam, was investigated during surgery in 10 liver transplant recipients. …

At present, the methods and enzymology of the UDP-glucuronosyltransferases (UGTs) lag
behind that of the cytochromes P450 (CYPs). About 15 human UGTs have been identified, …

The human colon carcinoma cell line, Caco-2, is widely used as a model for oral absorption
of xenobiotics. The usefulness of Caco-2 cells has been limited, however, because they do …

The synthetic opioid fentanyl undergoes extensive metabolism in humans. Systemic
elimination occurs primarily by hepatic metabolism. When administered as a lozenge for oral …

Purpose. The contribution of the efflux transporter P-glycoprotein (P-gp) as a barrier to drug
absorption may depend on its level of expression at the site of absorption. Accordingly, the …

… Paine PhD… Mary F. Paine PhD …

This is a report of a symposium held at the March 1997 meeting of the American Society for
Pharmacology and Therapeutics in San Diego. Our understanding of the events that control …