Clinical drug interaction profile of idelalisib in healthy subjects

• Published in: Journal of clinical pharmacology Vol. 55; no. 8; p. 909
• Main Authors: Jin, Feng, Robeson, Michelle, Zhou, Huafeng, Moyer, Candra, Wilbert, Sibylle, Murray, Bernard, Ramanathan, Srini
• Format: Journal Article
• Language: English
• Published: England 01.08.2015
• Subjects: Adult; Antineoplastic Agents - blood; Antineoplastic Agents - pharmacokinetics; Antineoplastic Agents - pharmacology; Class Ia Phosphatidylinositol 3-Kinase - antagonists & inhibitors; Digoxin - blood; Digoxin - pharmacokinetics; Drug Interactions; Female; Healthy Volunteers; Humans; Male; Midazolam - blood; Midazolam - pharmacokinetics; Middle Aged; Purines - blood; Purines - pharmacokinetics; Purines - pharmacology; Quinazolinones - blood; Quinazolinones - pharmacokinetics; Quinazolinones - pharmacology; Rifampin - pharmacology; Rosuvastatin Calcium - blood; Rosuvastatin Calcium - pharmacokinetics; Young Adult; pharmacokinetics; PI3Kδ; idelalisib; drug interaction; safety

Idelalisib, a potent phosphatidylinositol-3-kinase delta (PI3Kδ) inhibitor, is metabolized primarily by aldehyde oxidase to form GS-563117 and to a lesser extent by cytochrome P450 (CYP) 3A and uridine 5'-diphospho-glucuronosyltransferase 1A4. In vitro, idelalisib inhibits P-glycoprotein (P-gp)...