Use of Multiple Probes to Assess Transporter- and Cytochrome P450-Mediated Drug–Drug Interaction Potential of the Pangenotypic HCV NS5A Inhibitor Velpatasvir

Clinical Pharmacokinetics

Volumn 55, Issue 5, 2016, Pages 605-613

  Mogalian, Erik ^a   German, Polina ^a   Kearney, Brian P ^a   Yang, Cheng Yong ^a   Brainard, Diana ^a   McNally, John ^a   Moorehead, Lisa ^a   Mathias, Anita ^a  

^a GILEAD SCIENCES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CYCLOSPORIN; CYTOCHROME P450; DIGOXIN; KETOCONAZOLE; PRAVASTATIN; RIFAMPICIN; ROSUVASTATIN; VELPATASVIR; ANTIVIRUS AGENT; CARBAMIC ACID DERIVATIVE; CARRIER PROTEIN; FUSED HETEROCYCLIC RINGS;

ADULT; AREA UNDER THE CURVE; ARTICLE; COHORT ANALYSIS; CONTROLLED STUDY; CROSSOVER PROCEDURE; DRUG HALF LIFE; DRUG METABOLISM; DRUG POTENCY; DRUG SAFETY; DRUG TRANSPORT; DRUG WITHDRAWAL; DYSMENORRHEA; DYSPEPSIA; EVALUATION STUDY; FEMALE; HEADACHE; HUMAN; HUMAN EXPERIMENT; IN VITRO STUDY; MALE; MAXIMUM PLASMA CONCENTRATION; NORMAL HUMAN; OPEN STUDY; PHASE 1 CLINICAL TRIAL; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL; SIDE EFFECT; SINGLE DRUG DOSE; ADOLESCENT; CLINICAL TRIAL; DRUG INTERACTION; HEPACIVIRUS; METABOLISM; MIDDLE AGED; YOUNG ADULT;

ADOLESCENT; ADULT; ANTIVIRAL AGENTS; CARBAMATES; CROSS-OVER STUDIES; CYTOCHROME P-450 ENZYME SYSTEM; DRUG INTERACTIONS; FEMALE; HEPACIVIRUS; HETEROCYCLIC COMPOUNDS, 4 OR MORE RINGS; HUMANS; MALE; MEMBRANE TRANSPORT PROTEINS; MIDDLE AGED; YOUNG ADULT;

EID: 84945540112     PISSN: 03125963     EISSN: 11791926     Source Type: Journal    
DOI: 10.1007/s40262-015-0334-7     Document Type: Article

References (33)

1. Ghany MG, Strader DB, Thomas DL, Seeff LB. Diagnosis, management, and treatment of hepatitis C: an update. Hepatology. 2009;49(4):1335–74.
2. Naggie S, Patel K, McHutchison J. Hepatitis C virus directly acting antivirals: current development with NS3/4A HCV serine protease inhibitors. J Antimicrob Chemother. 2010;65(10):2063–9.
3. Negro F, Alberti A. The global health burden of hepatitis C virus infection. Liver Int. 2011;31(Suppl 2):1–3.
4. Cornberg M, Razavi HA, Alberti A, Bernasconi E, Buti M, Cooper C, et al. A systematic review of hepatitis C virus epidemiology in Europe, Canada, and Israel. Liver Int. 2011;31(Suppl 2):30–60.
5. Sievert W, Altraif I, Razavi HA, Abdo A, Ahmed EA, Alomair A, et al. A systematic review of hepatitis C virus epidemiology in Asia, Australia, and Egypt. Liver Int. 2011;31(Suppl 2):61–80.
6. Pietschmann T, Lohmann V, Rutter G, Kurpanek K, Bartenschlager R. Characterization of cell lines carrying self-replicating hepatitis C virus RNAs. J Virol. 2001;75(3):1252–64.
7. Tellinghuisen TL, Foss KL, Treadaway J. Regulation of hepatitis C virion production via phosphorylation of the NS5A protein. PLoS Pathog. 2008;4(3):e1000032.
8. Gale MJ Jr, Korth MJ, Tang NM, Tan SL, Hopkins DA, Dever TE, et al. Evidence that hepatitis C virus resistance to interferon is mediated through repression of the PKR protein kinase by the nonstructural 5A protein. Virology. 1997;230(2):217–27.
9. Cheng G, Yu M, Peng B, Lee Y, Trejo-Martin A, Gong R, et al. GS-5816, a second generation HCV HS5A inhibitor with potent antiviral activity, broad genotypic coverage and a high resistance barrier. J Hepatol. 2013;58:S484–5.
10. Tucker GT, Houston JB, Huang SH. Optimizing drug development: strategies to assess drug metabolism/transporter interaction potential-toward a consensus. Clin Pharm Ther. 2001;70(2):103–14.
11. Fuhr U, Jetter A, Kirchheiner J. Appropriate phenotyping procedures for drug metabolizing enzymes and transporters in humans and their simultaneous use in “cocktail” approach. Clin Pharm Ther. 2007;81(2):270–83.
12. Saari TI, Laine K, Leino K, Valtonen M, Neuvonen PJ, et al. Effect of voriconazole on the pharmacokinetics and pharmacodynamics of intravenous and oral midazolam. Clin Pharmacol Ther. 2006;79(4):362–70.
13. Katzenmaier S, Markert C, Riedel KD, Burhenne J, Haefeli WE, Mikus G. Determining the time course of CYP3A inhibition by potent reversible and irreversible CYP3A inhibitors using a limited sampling strategy. Clin Pharmacol Ther. 2011;90(5):666–73.
14. Thummel KE, O’Shea D, Paine MF, Shen DD, Kunze KL, Perkins JD, et al. Oral first-pass elimination of midazolam involves both gastrointestinal and hepatic CYP3A-mediated metabolism. Clin Pharmacol Ther. 1996;59(5):491–502.
15. Schellens JH, van der Wart JH, Brugman M, Breimer DD. Influence of enzyme induction and inhibition on the oxidation of nifedipine, sparteine, mephenytoin, and antipyrine in humans as assessed by a “cocktail” study design. J Pharmacol Exp Ther. 1989;249:638–45.
16. Schellens JH, Ghabrial H, van der Wart HH, Bakker EN, Wilkinson GR, Breimer DD. Differential effects of quinidine on the disposition of nifedipine, sparteine, and mephenytoin in humans. Clin Pharm Ther. 1991;50:520–8.
17. Maeda K, Ikeda Y, Fujita K, Azuma Y, Haruyama Y, Yamane N, Kumagai Y, Sugiyama Y. Identification of rate-determining process in the hepatic clearance of atorvastatin in a clinical cassette microdosing study. Clin Pharm Ther. 2011;90(4):575–81.
18. White RE, Manitpisitkul P. Pharmacokinetic theory of cassette dosing in drug delivery screening. Drug Metab Dispos. 2001;29(7):957–66.
19. Olah TV, McLoughlin SA, Gilbert JD. The simultaneous determination of mixtures of drug candidates by liquid chromatography/atmospheric pressure chemical ionization mass spectrometry as an in vivo drug screening procedure. Rapid Commun Mass Spectrom. 1997;11:17–23.
20. Allen MC, Shah TS, Day WW. Rapid determination of oral pharmacokinetics and plasma free fraction using cocktail approaches: methods and application. Pharm Res. 1998;15:93–7.
21. Frick LW, Adkinson KL, Wells-Knecht KJ, Woolard P, Higton DM. Cassette dosing: rapid in vivo assessment of pharmacokinetics. Pharm Sci Technol Today. 1998;1:12–8.
22. Shaffer JE, Adkison KK, Halm K, Hedeen K, Berman J. Use of “N-in-one” dosing to create an in vivo pharmacokinetic database for use in developing structure-pharmacokinetic relationships. J Pharm Sci. 1999;88:313–8.
23. Wu JT, Zeng H, Qian M, Brogdon BL, Unger SE. Direct plasma sample injection in multiple-component LC-MS-MS assays for high-throughput pharmacokinetic screening. Anal Chem. 2000;72:61–7.
24. United States Food and Drug Administration. Guidance for industry: drug interaction Studies: study design, data analysis, implications for dosing, and labeling recommendations. Draft. 2012.
25. Giacomini KM, Huang SM, Tweedie DJ, Benet LZ, Brouwer KL, Chu X, et al. Membrane transporters in drug development. Nat Rev Drug Discov. 2010;9(3):216–36.
26. Huang SM, Woodcock J. Transporters in drug development: advancing on the critical path. Nat Rev Drug Discov. 2010;9(3):175–6.
27. Benet LZ, Cummins CL. The drug efflux-metabolism alliance: biochemical aspects. Adv Drug Deliv Rev. 2001;50:S3–11.
28. Luo G, Cunningham M, Kim S, Burn T, Lin J, Sinz M, Hamilton G, et al. CYP3A4 induction by drugs: correlation between a pregnane X receptor reporter gene assay and CYP3A4 expression in human hepatocytes. Drug Metab Dispos. 2002;30(7):795–804.
29. Xu C, Li CYT, Kong ANT. Induction of phase I, II, and III drug metabolism/transport by xenobiotics. Arch Pharm Res. 2005;28(3):249–68.
30. German P, Mathias A, Pang PS, Han L, Link JO, McNally J, Kearney BP. Healthy volunteer first-in-human evaluation of GS-5816, a novel second generation broad-genotypic NS5A inhibitor with potential for once-daily dosing. In: Poster #1195 presented at: European Association for the Study of the Liver, Amsterdam, Netherlands. 2013.
31. U.S. 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 label recommendations. 2012.
32. Obach RS, Walsky RL, Venkatakrishnan K, Houston JB, Tremaine LM. In vitro cytochrome P450 inhibition data and the prediction of drug-drug interactions: qualitative relationships, quantitative predications, and the rank-order approach. Clin Pharm Ther. 2005;78(6):582–92.
33. Mogalian E, Yang C, Stamm LM, Shen G, Hernandez M, Mathias A. Metabolism and excretion of pangenotypic HCV NS5A inhibitor GS-5816 in humans. In: 16th International workshop on clinical pharmacology of HIV and hepatitis therapy. Washington; 2015. p. 72.