Cobicistat versus ritonavir boosting and differences in the drug-drug interaction profiles with co-medications

Journal of Antimicrobial Chemotherapy

Volumn 71, Issue 7, 2016, Pages 1755-1758

  Marzolini, Catia ^a   Gibbons, Sara ^b   Khoo, Saye ^b   Back, David ^b  

^a UNIVERSITY HOSPITAL BASEL   (Switzerland)

^b UNIVERSITY OF LIVERPOOL   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

ACENOCOUMAROL; AGOMELATINE; AMFEBUTAMONE; AMODIAQUINE; ASENAPINE; ATOVAQUONE PLUS PROGUANIL; COBICISTAT; DIAMORPHINE; DIHYDROCODEINE; DULOXETINE; ELTROMBOPAG; GLICLAZIDE; GLIMEPIRIDE; GLIPIZIDE; HYDROMORPHONE; LAMOTRIGINE; MORPHINE; NATEGLINIDE; OLANZAPINE; PETHIDINE; PHENPROCOUMON; PROPOFOL; RITONAVIR; ROSIGLITAZONE; SERTRALINE; SULFADIAZINE; TOLBUTAMIDE; UNINDEXED DRUG; VALPROIC ACID; WARFARIN; ANTI HUMAN IMMUNODEFICIENCY VIRUS AGENT; ATAZANAVIR; CYTOCHROME P450 3A; CYTOCHROME P450 3A INHIBITOR; DARUNAVIR; HUMAN IMMUNODEFICIENCY VIRUS PROTEINASE INHIBITOR;

ARTICLE; DRUG EFFECT; DRUG EXPOSURE; DRUG GLUCURONIDATION; HIGHLY ACTIVE ANTIRETROVIRAL THERAPY; ADVERSE EFFECTS; CHEMISTRY; COMBINATION DRUG THERAPY; DRUG EFFECTS; DRUG INTERACTION; HIV INFECTIONS; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS 1; METABOLISM;

ANTI-HIV AGENTS; ATAZANAVIR SULFATE; COBICISTAT; CYTOCHROME P-450 CYP3A; CYTOCHROME P-450 CYP3A INHIBITORS; DARUNAVIR; DRUG INTERACTIONS; DRUG THERAPY, COMBINATION; HIV INFECTIONS; HIV PROTEASE INHIBITORS; HIV-1; HUMANS; RITONAVIR;

EID: 84979084522     PISSN: 03057453     EISSN: 14602091     Source Type: Journal    
DOI: 10.1093/jac/dkw032     Document Type: Article

References (22)

1. Boffito M, Back D, Gatell JM. Twenty years of boosting antiretroviral agents: where are we today? AIDS 2015; 29: 2229-33
2. Hsu A, Granneman GR, Bertz RJ. Ritonavir. Clinical pharmacokinetics and interactions with other anti-HIV agents. Clin Pharmacokinet 1998; 35: 275-91
3. Xu L, Liu H, Hong A et al. Structure-activity relationships of diamine inhibitors of cytochrome P450 (CYP) 3A as novel pharmacoenhancers. Part II:P2/P3 region and discovery of cobicistat (GS-9350). Bioorg Med Chem Lett 2014; 24: 995-9
4. Xu L, Liu H, Murray BP et al. Cobicistat (GS-9350): a potent and selective inhibitor of human CYP3A as a novel pharmacoenhancer. ACS Med Chem Lett 2010; 1: 209-13
5. Mathias AA, German P, Murray BP et al. Pharmacokinetics and pharmacodynamics of GS-9350: a novel pharmacokinetic enhancer without anti-HIV activity. Clin Pharmacol Ther 2010; 87: 322-9
6. Elion R, Cohen C, Gathe J et al. Phase 2 study of cobicistat versus ritonavir each with once-daily atazanavir and fixed-dose emtricitabine/tenofovir df in the initial treatment of HIV infection. AIDS 2011; 25: 1881-6
7. Kakuda TN, Opsomer M, Timmers M et al. Pharmacokinetics of darunavir in fixed-dose combination with cobicistat compared with coadministration of darunavir and ritonavir as single agents in healthy volunteers. J Clin Pharmacol 2014; 54: 949-57
8. German P, Warren D, West S et al. Pharmacokinetics and bioavailability of an integrase and novel pharmacoenhancer-containing single-tablet fixed-dose combination regimen for the treatment of HIV. J Acquir Immune Defic Syndr 2010; 55: 323-9
9. Renjifo B, van Wyk J, Salem AH et al. Pharmacokinetic enhancement in HIV antiretroviral therapy: a comparison of ritonavir and cobicistat. AIDS Rev 2015; 17: 39-49
10. FDA Antiviral Drug Advisory Meeting-May 2012. http://www.fda.gov/AdvisoryCommittees/CommitteesMeetingMaterials/Drugs/AntiviralDrugsAdvisoryCommittee/ucm303394.htm
11. Lepist EI, Phan TK, Roy A et al. Cobicistat boosts the intestinal absorption of transport substrates, including HIV protease inhibitors and GS-7340, in vitro. Antimicrob Agents Chemother 2012; 56: 5409-13
12. Lepist EI, Zhang X, Hao J et al. Contribution of the organic anion transporter OAT2 to the renal active tubular secretion of creatinine and mechanism for serum creatinine elevations caused by cobicistat. Kidney Int 2014; 86: 350-7
13. German P, Liu HC, Szwarcberg J et al. Effect of cobicistat on glomerular filtration rate in subjects with normal and impaired renal function. J Acquir Immune Defic Syndr 2012; 61: 32-40
14. Gallant JE, Koenig E, Andrade-Villanueva JF et al. Brief report: cobicistat compared with ritonavir as a pharmacoenhancer for atazanavir in combination with emtricitabine/tenofovir disoproxil fumarate: week 144 results. J Acquir Immune Defic Syndr 2015; 69: 338-40
15. Tolson AH, Wang H. Regulation of drug-metabolizing enzymes by xenobiotic receptors: PXR and CAR. Adv Drug Deliv Rev 2010; 62: 1238-49
16. Yeh RF, Gaver VE, Patterson KB et al. Lopinavir/ritonavir induces the hepatic activity of cytochrome P450 enzymes CYP2C9, CYP2C19, and CYP1A2 but inhibits the hepatic and intestinal activity of CYP3A as measured by a phenotyping drug cocktail in healthy volunteers. J Acquir Immune Defic Syndr 2006; 42: 52-60
17. Kirby BJ, Collier AC, Kharasch ED et al. Complex drug interactions of HIV protease inhibitors 2: in vivo induction and in vitro to in vivo correlation of induction of cytochrome P450 1A2, 2B6, and 2C9 by ritonavir and nelfinavir. Drug Metab Dispos 2011; 39: 2329-37
18. Park J, Vousden M, Brittain C et al. Dose-related reduction in bupropion plasma concentrations by ritonavir. J Clin Pharmacol 2010; 50: 1180-7
19. Van der Lee MJ, Dawood L, ter Hofstede HJ et al. Lopinavir/ritonavir reduces lamotrigine plasma concentrations in healthy subjects. Clin Pharmacol Ther 2006; 80: 159-8
20. Liverpool HIV Drug Interactions. http://www.hiv-druginteractions.org
21. Ageno W, Gallus AS, Wittkowsky A et al. Oral anticoagulant therapy: Antithrombotic Therapy and Prevention of Thrombosis, 9th ed: American College of Chest Physicians Evidence-Based Clinical Practice Guidelines. Chest 2012; 141 (2 Suppl): e44S-88S
22. Good BL, Gomes DC, Fulco PP. An unexpected interaction between warfarin and cobicistat-boosted elvitegravir. AIDS 2015; 29: 986-7