Clinical drug interaction profile of idelalisib in healthy subjects

Journal of Clinical Pharmacology

Volumn 55, Issue 8, 2015, Pages 909-919

  Jin, Feng ^a   Robeson, Michelle ^b   Zhou, Huafeng ^b   Moyer, Candra ^a   Wilbert, Sibylle ^b   Murray, Bernard ^a   Ramanathan, Srini ^a  

^a GILEAD SCIENCES   (United States)

^b GILEAD SCIENCES INC   (United States)

Author keywords

drug interaction; idelalisib; pharmacokinetics; PI3K ; safety

Indexed keywords

1 HYDROXY MIDAZOLAM; ALANINE AMINOTRANSFERASE; ASPARTATE AMINOTRANSFERASE; BILIRUBIN; CORTICOSTEROID; CYTOCHROME P450 3A; DIGOXIN; GS 563117; IDELALISIB; MIDAZOLAM; RIFAMPICIN; ROSUVASTATIN; UNCLASSIFIED DRUG; ANTINEOPLASTIC AGENT; PHOSPHATIDYLINOSITOL 4,5 BISPHOSPHATE 3 KINASE; PURINE DERIVATIVE; QUINAZOLINONE DERIVATIVE;

ADULT; ALANINE AMINOTRANSFERASE BLOOD LEVEL; AREA UNDER THE CURVE; ARTICLE; ASPARTATE AMINOTRANSFERASE BLOOD LEVEL; BILIRUBIN BLOOD LEVEL; BLOOD SAMPLING; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; CORTICOSTEROID THERAPY; DISEASE SEVERITY; DRUG BLOOD LEVEL; DRUG EXPOSURE; DRUG FEVER; DRUG HALF LIFE; DRUG INDUCED HEADACHE; DRUG INHIBITION; DRUG METABOLISM; DRUG SAFETY; ELIMINATION HALF-LIFE; ELIMINATION RATE CONSTANT; FEMALE; FOLLOW UP; HUMAN; HYPERTRANSAMINASEMIA; HYPERURICEMIA; IN VITRO STUDY; LIMIT OF QUANTITATION; MALAISE; MALE; MAXIMUM PLASMA CONCENTRATION; MULTIPLE DRUG DOSE; NORMAL HUMAN; OPEN STUDY; PARALLEL DESIGN; PHASE 1 CLINICAL TRIAL; POSITIVE ION ELECTROSPRAY; SIDE EFFECT; SINGLE DRUG DOSE; TIME TO MAXIMUM PLASMA CONCENTRATION; TOXIC HEPATITIS; ANTAGONISTS AND INHIBITORS; BLOOD; CLINICAL TRIAL; DRUG INTERACTION; MIDDLE AGED; YOUNG ADULT;

ADULT; ANTINEOPLASTIC AGENTS; CLASS IA PHOSPHATIDYLINOSITOL 3-KINASE; DIGOXIN; DRUG INTERACTIONS; FEMALE; HEALTHY VOLUNTEERS; HUMANS; MALE; MIDAZOLAM; MIDDLE AGED; PURINES; QUINAZOLINONES; RIFAMPIN; ROSUVASTATIN CALCIUM; YOUNG ADULT;

EID: 84936098546     PISSN: 00912700     EISSN: 15524604     Source Type: Journal    
DOI: 10.1002/jcph.495     Document Type: Article

References (23)

1. Okkenhaug K, Vanhaesebroeck B,. PI3K in lymphocyte development, differentiation and activation. Nat Rev Immunol. 2003; 3 (4): 317-330.
2. Vanhaesebroeck B, Ali K, Bilancio A, Geering B, Foukas LC,. Signalling by PI3K isoforms: insights from gene-targeted mice. Trends Biochem Sci. 2005; 30 (4): 194-204.
3. Herman SE, Lapalombella R, Gordon AL, et al., The role of phosphatidylinositol 3-kinase-δ in the immunomodulatory effects of lenalidomide in chronic lymphocytic leukemia. Blood. 2011; 117 (16): 4323-4327.
4. Bernal A, Pastore RD, Asgary Z, et al., Survival of leukemic B cells promoted by engagement of the antigen receptor. Blood. 2001; 98 (10): 3050-3057.
5. Lannutti BJ, Meadows SA, Herman SE, et al., CAL-101, a p110delta selective phosphatidylinositol-3-kinase inhibitor for the treatment of B-cell malignancies, inhibits PI3K signaling and cellular viability. Blood. 2011; 117 (2): 591-594.
6. Hoellenriegel J, Meadows SA, Sivina M, et al., The phosphoinositide 3′-kinase delta inhibitor, CAL-101, inhibits B-cell receptor signaling and chemokine networks in chronic lymphocytic leukemia. Blood. 2011; 118 (13): 3603-3612.
7. Gopal AK, Kahl BS, de Vos S, et al., PI3Kδ inhibition by idelalisib in patients with relapsed indolent lymphoma. N Engl J Med. 2014; 370 (11): 1008-1018.
8. Furman RR, Sharman JP, Coutre SE, et al., Idelalisib and rituximab in relapsed chronic lymphocytic leukemia. N Engl J Med. 2014; 370 (11): 997-1007.
9. Jin F, Robeson M, Zhou H, Kwan E, Ramananthan S,. Pharmacokinetics, metabolism and excretion of idelalisib [ASH abstract]. Blood. 2013; 122 (21): 5570.
10. Kirby B, Kharasch ED, Thummel KT, Narang VS, Hoffer CJ, Unadkat JD,. Simultaneous measurement of in vivo P-glycoprotein and cytochrome P450 3A activities. J Clin Pharmacol. 2006; 46 (11): 1313-1319.
11. Penzak SR, Shen JM, Alfaro RM, Remaley AT, Natarajan V, Falloon J,. Ritonavir decreases the nonrenal clearance of digoxin in healthy volunteers with known MDR1 genotypes. Ther Drug Monit. 2004; 26 (3): 322-330.
12. Chen M, Nafziger AN,., Bertino JS Jr,. Drug-metabolizing enzyme inhibition by ketoconazole does not reduce interindividual variability of CYP3A activity as measured by oral midazolam. Drug Metab Dispos. 2006; 34 (12): 2079-2082.
13. Busti AJ, Bain AM, RG Hall, II, et al., Effects of atazanavir/ritonavir or fosamprenavir/ritonavir on the pharmacokinetics of rosuvastatin. J Cardiovasc Pharmacol. 2008; 51 (6): 605-610.
14. Perucca E, Grimaldi R, Frigo GM, Sardi A, Mönig H, Ohnhaus EE,. Comparative effects of rifabutin and rifampicin on hepatic microsomal enzyme activity in normal subjects. Eur J Clin Pharmacol. 1988; 34 (6): 595-599.
15. Webb HK, Chen H, Yu AS, et al., Clinical pharmacokinetics of CAL-101, a p110δ isoform-selective PI3K inhibitor, following single- and multiple-dose administration in healthy volunteers and patients with hematological malignancies [ASH abstract]. Blood. 2010; 116 (21): 1774.
16. US Department of Health and Human Services/Food and Drug Administration/Center for Drug Evaluation and Research. Drug interaction studies-study design, data analysis, implications for dosing, and labeling recommendations [draft]. February 2012. http://www.fda.gov/downloads/Drugs/GuidanceComplianceRegulatoryInformation/Guidances/ucm292362.pdf. Accessed September 25, 2014.
17. Simonson SG, Raza A, Martin PD, et al., Rosuvastatin pharmacokinetics in heart transplant recipients administered an antirejection regimen including cyclosporine. Clin Pharmacol Ther. 2004; 76 (2): 167-177.
18. Nader AM, Foster DR,. Suitability of digoxin as a P-glycoprotein probe: implications of other transporters on sensitivity and specificity. J Clin Pharmacol. 2014; 54 (1): 3-13.
19. Kaminsky LS, Zhang ZY,. Human P450 metabolism of warfarin [abstract]. Pharmacol Ther. 1997; 73 (1): 67-74.
20. Abernethy DR, Kaminsky LS, Dickinson TH,. Selective inhibition of warfarin metabolism by diltiazem in humans. J Pharmacol Exp Ther. 1991; 257 (1): 411-415.
21. Savi P, Pereillo JM, Uzabiaga MF, et al., Identification and biological activity of the active metabolite of clopidogrel. Thromb Haemost. 2000; 84 (5): 891-896.
22. Blech S, Ebner T, Ludwig-Schwellinger E, Stangier J, Roth W,. The metabolism and disposition of the oral direct thrombin inhibitor, dabigatran, in humans. Drug Metab Dispos. 2008; 36 (2): 386-399.
23. Dixit V, Hariparsad N, Li F, Desai P, Thummel KE, Unadkat JD,. Cytochrome P450 enzymes and transporters induced by anti-human immunodeficiency virus protease inhibitors in human hepatocytes: implications for predicting clinical drug interactions. Drug Metab Dispos. 2007; 35 (10): 1853-1859.