A phase I study evaluating the effect of everolimus on the pharmacokinetics of midazolam in healthy subjects

• Published in: Journal of clinical pharmacology Vol. 53; no. 4; p. 444
• Main Authors: Urva, Shweta, Bouillaud, Emmanuel, Delaney, Rosemary, Jappe, Annette, Cheung, Wing
• Format: Journal Article
• Language: English
• Published: England 01.04.2013
• Subjects: Adult; Anti-Anxiety Agents - adverse effects; Anti-Anxiety Agents - blood; Anti-Anxiety Agents - pharmacokinetics; Drug Interactions; Everolimus; Humans; Hypnotics and Sedatives - adverse effects; Hypnotics and Sedatives - blood; Hypnotics and Sedatives - pharmacokinetics; Immunosuppressive Agents - administration & dosage; Immunosuppressive Agents - adverse effects; Male; Midazolam - adverse effects; Midazolam - analogs & derivatives; Midazolam - blood; Midazolam - pharmacokinetics; Middle Aged; Sirolimus - administration & dosage; Sirolimus - adverse effects; Sirolimus - analogs & derivatives; Young Adult

The selective mammalian target of rapamycin (mTOR) inhibitor everolimus has demonstrated competitive inhibition of cytochrome P450 enzyme (CYP) 3A4 in vitro; however, its influence on CYP3A4 activity in humans is unknown. This study examined the influence of everolimus on the pharmacokinetics of mid...