In vitro metabolism of piperaquine is primarily mediated by CYP3A4

Xenobiotica

Volumn 42, Issue 11, 2012, Pages 1088-1095

  Lee, Tina Ming Na ^a   Huang, Liusheng ^a   Johnson, Marla K ^b   Lizak, Patricia ^a   Kroetz, Deanna ^a   Aweeka, Francesca ^a   Parikh, Sunil ^b  

^a UNIVERSITY OF CALIFORNIA   (United States)

^b UNIVERSITY OF CALIFORNIA   (United States)

Author keywords

Antimalarial; CYP3A4; Cytochrome p450; in vitro; Malaria; Metabolism; Piperaquine

Indexed keywords

CYTOCHROME P450 3A4; KETOCONAZOLE; MICONAZOLE; PIPERAQUINE;

ARTICLE; CELL LEVEL; CONTROLLED STUDY; DRUG METABOLISM; HUMAN; HUMAN CELL; IC 50; IN VITRO STUDY; LIVER MICROSOME; METABOLIC RATE; TANDEM MASS SPECTROMETRY; TURNOVER TIME;

ARYL HYDROCARBON HYDROXYLASES; CYTOCHROME P-450 CYP3A; HUMANS; MICROSOMES, LIVER; QUINOLINES;

PLASMODIUM FALCIPARUM;

EID: 84867171279     PISSN: 00498254     EISSN: 13665928     Source Type: Journal    
DOI: 10.3109/00498254.2012.693972     Document Type: Article

References (25)

1. Bjornsson TD, Callaghan JT, Einolf HJ, Fischer V, Gan L, Grimm S, Kao J, King SP, Miwa G, Ni L, Kumar G, McLeod J, Obach RS, Roberts S, Roe A, Shah A, Snikeris F, Sullivan JT, Tweedie D, Vega JM, Walsh J, Wrighton SA; Pharmaceutical Research and Manufacturers of America (PhRMA) Drug Metabolism/Clinical Pharmacology Technical Working Group; FDA Center for Drug Evaluation and Research (CDER). (2003). The conduct of in vitro and in vivo drug-drug interaction studies: A Pharmaceutical Research and Manufacturers of America (PhRMA) perspective. Drug Metab Dispos 31:815-832. (Pubitemid 36759050)
2. Davis TM, Hung TY, Sim IK, Karunajeewa HA, Ilett KF. (2005). Piperaquine: A resurgent antimalarial drug. Drugs 65:75-87. (Pubitemid 40143802)
3. Donahue SR, Flockhart DA, Abernethy DR, Ko JW. (1997). Ticlopidine inhibition of phenytoin metabolism mediated by potent inhibition of CYP2C19. Clin Pharmacol Ther 62:572-577. (Pubitemid 28214936)
4. Food and Drug Administration. (2001). Guidance for industry: Bioanalytical method validation. Available at: http://www.fda.gov/downloads/ Drugs/GuidanceComplianceRegulatoryInformation/Guidances/ucm070107.pdf. Accessed on: 28 July, 2009.
5. German P, Parikh S, Lawrence J, Dorsey G, Rosenthal PJ, Havlir D, Charlebois E, Hanpithakpong W, Lindegardh N, Aweeka FT. (2009). Lopinavir/ritonavir affects pharmacokinetic exposure of artemether/lumefantrine in HIV-uninfected healthy volunteers. J Acquir Immune Defic Syndr 51:424-429.
6. Harper TW, Brassil PJ. (2008). Reaction phenotyping: Current industry efforts to identify enzymes responsible for metabolizing drug candidates. AAPS J 10:200-207.
7. Hung TY, Davis TM, Ilett KF, Karunajeewa H, Hewitt S, Denis MB, Lim C, Socheat D. (2004). Population pharmacokinetics of piperaquine in adults and children with uncomplicated falciparum or vivax malaria. Br J Clin Pharmacol 57:253-262. (Pubitemid 38296988)
8. Jancová P, Anzenbacherová E, Papousková B, Lemr K, Luzná P, Veinlichová A, Anzenbacher P, Simánek V. (2007). Silybin is metabolized by cytochrome P450 2C8 in vitro. Drug Metab Dispos 35:2035-2039. (Pubitemid 350005192)
9. Kajosaari LI, Laitila J, Neuvonen PJ, Backman JT. (2005). Metabolism of repaglinide by CYP2C8 and CYP3A4 in vitro: Effect of fibrates and rifampicin. Basic Clin Pharmacol Toxicol 97:249-256. (Pubitemid 41433700)
10. Karunajeewa HA, Ilett KF, Mueller I, Siba P, Law I, Page-Sharp M, Lin E, Lammey J, Batty KT, Davis TM. (2008). Pharmacokinetics and efficacy of piperaquine and chloroquine in Melanesian children with uncomplicated malaria. Antimicrob Agents Chemother 52:237-243.
11. Katrak S, Gasasira A, Arinaitwe E, Kakuru A, Wanzira H, Bigira V, Sandison TG, Homsy J, Tappero JW, Kamya MR, Dorsey G. (2009). Safety and tolerability of artemether-lumefantrine versus dihydroartemisinin-piperaquine for malaria in young HIVinfected and uninfected children. Malar J 8:272.
12. Ko JW, Desta Z, Soukhova NV, Tracy T, Flockhart DA. (2000). In vitro inhibition of the cytochrome P450 (CYP450) system by the antiplatelet drug ticlopidine: Potent effect on CYP2C19 and CYP2D6. Br J Clin Pharmacol 49:343-351. (Pubitemid 30195277)
13. Kunze KL, Trager WF. (1993). Isoform-selective mechanism-based inhibition of human cytochrome P450 1A2 by furafylline. Chem Res Toxicol 6:649-656. (Pubitemid 23290017)
14. Lindegardh N, Annerberg A, White NJ, Day NP. (2008). Development and validation of a liquid chromatographic-tandem mass spectrometric method for determination of piperaquine in plasma stable isotope labeled internal standard does not always compensate for matrix effects. J Chromatogr B Analyt Technol Biomed Life Sci 862:227-236.
15. Myint HY, Ashley EA, Day NP, Nosten F, White NJ. (2007). Efficacy and safety of dihydroartemisinin-piperaquine. Trans R Soc Trop Med Hyg 101:858-866. (Pubitemid 47091464)
16. Rodrigues AD. (2007). Prioritization of clinical drug interaction studies using in vitro cytochrome P450 data: Proposed refinement and expansion of the "rank order" approach. Drug Metab Lett 1:31-35.
17. Röshammar D, Hai TN, Friberg Hietala S, Van Huong N, Ashton M. (2006). Pharmacokinetics of piperaquine after repeated oral administration of the antimalarial combination CV8 in 12 healthy male subjects. Eur J Clin Pharmacol 62:335-341.
18. Singhal P, Gaur A, Gautam A, Varshney B, Paliwal J, Batra V. (2007). Sensitive and rapid liquid chromatography/tandem mass spectrometric assay for the quantification of piperaquine in human plasma. J Chromatogr B Analyt Technol Biomed Life Sci 859:24-29. (Pubitemid 350010923)
19. Slutsker L, Marston BJ. (2007). HIV and malaria: Interactions and implications. Curr Opin Infect Dis 20:3-10. (Pubitemid 46052120)
20. Störmer E, Brockmöller J, Roots I, Schmider J. (2000a). Cytochrome P-450 enzymes and FMO3 contribute to the disposition of the antipsychotic drug perazine in vitro. Psychopharmacology (Berl) 151:312-320.
21. Störmer E, Roots I, Brockmöller J. (2000b). Benzydamine N-oxidation as an index reaction reflecting FMO activity in human liver microsomes and impact of FMO3 polymorphisms on enzyme activity. Br J Clin Pharmacol 50:553-561. (Pubitemid 32010780)
22. Tarning J, Bergqvist Y, Day NP, Bergquist J, Arvidsson B, White NJ, Ashton M, Lindegardh N. (2006). Characterization of human urinary metabolites of the antimalarial piperaquine. Drug Metab Dispos 34:2011-2019. (Pubitemid 44837762)
23. Tarning J, Lindegardh N. (2008). Quantification of the antimalarial piperaquine in plasma. Trans R Soc Trop Med Hyg 102:409-411.
24. World Health Organization. (2010). Guidelines for the treatment of malaria/World Health Organization. Available at: http://whqlibdoc.who.int/ publications/2010/9789241547925-eng.pdf
25. Zhang W, Ramamoorthy Y, Kilicarslan T, Nolte H, Tyndale RF, Sellers EM. (2002). Inhibition of cytochromes P450 by antifungal imidazole derivatives. Drug Metab Dispos 30:314-318. (Pubitemid 34175023)