Predicting intestinal absorption of raltegravir using a population-based ADME simulation

Journal of Antimicrobial Chemotherapy

Volumn 68, Issue 7, 2013, Pages 1627-1634

  Moss, Darren M ^a   Siccardi, Marco ^b   Back, David J ^b   Owen, Andrew ^b  

^a LIVERPOOL SCHOOL OF TROPICAL MEDICINE   (United Kingdom)

^b UNIVERSITY OF LIVERPOOL   (United Kingdom)

Author keywords

HIV; Integrase inhibitors; IVIVE; Permeability; Pharmacokinetics

Indexed keywords

MAGNESIUM; RALTEGRAVIR;

ADULT; AREA UNDER THE CURVE; ARTICLE; DRUG ABSORPTION; DRUG DISPOSITION; DRUG DISTRIBUTION; DRUG EXCRETION; DRUG METABOLISM; DRUG SOLUBILITY; FEMALE; GASTROINTESTINAL TRACT; HUMAN; HUMAN EXPERIMENT; IN VITRO STUDY; INTESTINE ABSORPTION; MAXIMUM PLASMA CONCENTRATION; PREDICTION; SINGLE DRUG DOSE; STOMACH PH;

EID: 84879477892     PISSN: 03057453     EISSN: 14602091     Source Type: Journal    
DOI: 10.1093/jac/dkt084     Document Type: Article

References (43)

1. Siccardi M, D'Avolio A, Rodriguez-Novoa S et al. Intrapatient and interpatient pharmacokinetic variability of raltegravir in the clinical setting. Ther Drug Monit 2012; 34: 232-5.
2. Cattaneo D, Gervasoni C, Meraviglia P, et al. Inter- and intra-patient variability of raltegravir pharmacokinetics in HIV-1-infected subjects. J Antimicrob Chemother 2012; 67: 460-4.
3. Kassahun K, McIntosh I, Cui D, et al. Metabolism and disposition in humans of raltegravir (MK-0518), an anti-AIDS drug targeting the human immunodeficiency virus 1 integrase enzyme. Drug Metab Dispos 2007; 35: 1657-63.
4. Iwamoto M, Kassahun K, Troyer MD, et al. Lack of a pharmacokinetic effect of raltegravir on midazolam: in vitro/in vivo correlation. J Clin Pharmacol 2008; 48: 209-14.
5. Cattaneo D, Ripamonti D, Baldelli S, et al. Exposure-related effects of atazanavir on the pharmacokinetics of raltegravir in HIV-1-infected patients. Ther Drug Monit 2010; 32: 782-6.
6. Wenning LA, Hanley WD, Brainard DM, et al. Effect of rifampin, a potent inducer of drug-metabolizing enzymes, on the pharmacokinetics of raltegravir. Antimicrob Agents Chemother 2009; 53: 2852-6.
7. Moss DM, Kwan WS, Liptrott NJ, et al. Raltegravir is a substrate for SLC22A6: a putative mechanism for the interaction between raltegravir and tenofovir. Antimicrob Agents Chemother 2011; 55: 879-87.
8. Croteau D, Letendre S, Best BM, et al. Total raltegravir concentrations in cerebrospinal fluid exceed the 50-percent inhibitory concentration for wild-type HIV-1. Antimicrob Agents Chemother 2010; 54: 5156-60.
9. Clavel C, Peytavin G, Tubiana R, et al. Raltegravir concentrations in the genital tract of HIV-1-infected women treated with araltegravir-containing regimen (DIVA 01 study). Antimicrob Agents Chemother 2011; 55: 3018-21.
10. Arab-Alameddine M, Fayet-Mello A, Lubomirov R, et al. Population pharmacokinetic analysis and pharmacogenetics of raltegravir in HIV-positive and healthy individuals. Antimicrob Agents Chemother 2012; 56: 2959-66.
11. Iwamoto M, Wenning LA, Nguyen BY, et al. Effects of omeprazole on plasma levels of raltegravir. Clin Infect Dis 2009; 48: 489-92.
12. Moss DM, Siccardi M, Khoo SH, et al. The interplay between raltegravir solubility, tablet dissolution, metal binding, charge state and cell permeability. In: Abstracts of the Thirteenth International Workshop on Clinical Pharmacology of HIV Therapy, Barcelona, Spain, 2012. Abstract P-27. Virology Education, Utrecht, The Netherlands.
13. Brainard DM, Friedman EJ, Jin B, et al. Effect of low-, moderate-, and high-fat meals on raltegravir pharmacokinetics. J Clin Pharmacol 2011; 51: 422-7.
14. Kiser JJ, Bumpass JB, Meditz AL, et al. Effect of antacids on the pharmacokinetics of raltegravir in human immunodeficiency virus-seronegative volunteers. Antimicrob Agents Chemother 2010; 54: 4999-5003.
15. da Silva D, Van Wesenbeeck L, Breilh D, et al. HIV-1 resistance patterns to integrase inhibitors in antiretroviral-experienced patients with virological failure on raltegravir-containing regimens. J Antimicrob Chemother 2010; 65: 1262-9.
16. Kozal MJ, Lupo S, DeJesus E, et al. A nucleoside- and ritonavir-sparing regimen containing atazanavir plus raltegravir in antiretroviral treatment-naive HIV-infected patients: SPARTAN study results. HIV Clin Trials 2012; 13: 119-30.
17. Rizk ML, Hang Y, Luo WL, et al. Pharmacokinetics and pharmacodynamics of once-daily versus twice-daily raltegravir in treatment-naive HIV-infected patients. Antimicrob Agents Chemother 2012; 56: 3101-6.
18. Wang L, Soon GH, Seng KY, et al. Pharmacokinetic modeling of plasma and intracellular concentrations of raltegravir in healthy volunteers. Antimicrob Agents Chemother 2011; 55: 4090-5.
19. Moss DM, Siccardi M, Murphy M, et al. Divalent metals and pH alter raltegravir disposition in vitro. Antimicrob Agents Chemother 2012; 56: 3020-6.
20. Soldin OP, Chung SH, Mattison DR. Sex differences in drug disposition. J Biomed Biotechnol 2011; 2011: 187103.
21. Perloff MD, von Moltke LL, Greenblatt DJ. Fexofenadine transport in Caco-2 cells: inhibition with verapamil and ritonavir. J Clin Pharmacol 2002; 42: 1269-74.
22. Storch CH, Theile D, Lindenmaier H, et al. Comparison of the inhibitory activity of anti-HIV drugs on P-glycoprotein. Biochem Pharmacol 2007; 73: 1573-81.
23. Sharma M, Saravolatz LD. Rilpivirine: a new non-nucleoside reverse transcriptase inhibitor. J Antimicrob Chemother 2013; 68: 250-6.
24. Azijn H, Tirry I, Vingerhoets J, et al. TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. Antimicrob Agents Chemother 2010; 54: 718-27.
25. Darwich AS, Neuhoff S, Jamei M, et al. Interplay of metabolism and transport in determining oral drug absorption and gut wall metabolism: a simulation assessment using the 'Advanced Dissolution, Absorption, Metabolism (ADAM)' model. Curr Drug Metab 2010; 11: 716-29.
26. Poulin P, Theil FP. Prediction of pharmacokinetics prior to in vivo studies. 1. Mechanism-based prediction of volume of distribution. J Pharm Sci 2002; 91: 129-56.
27. Jamei M, Marciniak S, Feng K, et al. The Simcyp population-based ADME simulator. Expert Opin Drug Metab Toxicol 2009; 5: 211-23.
28. Charman WN, Porter CJ, Mithani S, et al. Physiochemical and physiological mechanisms for the effects of food on drug absorption: the role of lipids and pH. J Pharm Sci 1997; 86: 269-82.
29. McCloy RF, Greenberg GR, Baron JH. Duodenal pH in health and duodenal ulcer disease: effect of a meal, Coca-Cola, smoking, and cimetidine. Gut 1984; 25: 386-92.
30. Rune SJ, Viskum K. Duodenal pH values in normal controls and in patients with duodenal ulcer. Gut 1969; 10: 569-71.
31. Yuasa H, Soga N, Kimura Y, et al. Effect of aging on the intestinal transport of hydrophilic drugs in the rat small intestine. Biol Pharm Bull 1997; 20: 1188-92.
32. Iwamoto M, Wenning LA, Petry AS, et al. Safety, tolerability, and pharmacokinetics of raltegravir after single and multiple doses in healthy subjects. Clin Pharmacol Ther 2008; 83: 293-9.
33. Ibekwe VC, Fadda HM, McConnell EL, et al. Interplay between intestinal pH, transit time and feed status on the in vivo performance of pH responsive ileo-colonic release systems. Pharm Res 2008; 25: 1828-35.
34. McConnell EL, Fadda HM, Basit AW. Gut instincts: explorations in intestinal physiology and drug delivery. Int J Pharm 2008; 364: 213-26.
35. Shelton MJ, Akbari B, Hewitt RG, et al. Eradication of Helicobacter pylori is associated with increased exposure to delavirdine in hypochlorhydric HIV-positive patients. J Acquir Immune Defic Syndr 2000; 24: 79-82.
36. Chave JP, Thorens J, Frohlich F, et al. Gastric and duodenal bacterial colonization in HIV-infected patients without gastrointestinal symptoms. Am J Gastroenterol 1994; 89: 2168-71.
37. Rhame F, Matson M, Wood D et al. Effects of famotidine and omeprazole on raltegravir pharmacokinetics in HIV-infected individuals. In: Abstracts of the Twelfth European AIDS Conference, Cologne,Germany, 2009. Abstract PE4.1/1.
38. Cohen CJ, Andrade-Villanueva J, Clotet B et al. Rilpivirine versus efavirenz with two background nucleoside or nucleotide reverse transcriptase inhibitors in treatment-naive adults infected with HIV-1(THRIVE): a phase 3, randomised, non-inferiority trial. Lancet 2011; 378: 229-37.
39. Molina JM, Cahn P, Grinsztejn B, et al. Rilpivirine versus efavirenz with tenofovir and emtricitabine in treatment-naive adults infected with HIV-1 (ECHO): a phase 3 randomised double-blind active-controlled trial. Lancet 2011; 378: 238-46.
40. van Lunzen J, Maggiolo F, Arribas JR, et al. Once daily dolutegravir (S/GSK1349572) in combination therapy in antiretroviral-naive adults with HIV: planned interim 48 week results from SPRING-1, a doseranging, randomised, phase 2b trial. Lancet Infect Dis 2012; 12: 111-8.
41. Shimura K, Kodama EN. Elvitegravir: a new HIV integrase inhibitor. Antivir Chem Chemother 2009; 20: 79-85.
42. Summa V, Petrocchi A, Bonelli F, et al. Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection. J Med Chem 2008; 51: 5843-55.
43. Laufer R, Paz OG, Di Marco A, et al. Quantitative prediction of human clearance guiding the development of raltegravir (MK-0518, Isentress) and related HIV integrase inhibitors. Drug Metab Dispos 2009; 37: 873-83.