Simultaneous population pharmacokinetic model for lopinavir and ritonavir in HIV-infected adults

Clinical Pharmacokinetics

Volumn 47, Issue 10, 2008, Pages 681-692

  Moltó, José ^a,b   Barbanoj, Manuel José ^b,c   Miranda, Cristina ^a   Blanco, Asunción ^a   Santos, José Ramón ^a   Negredo, Eugenia ^a   Costa, Joan ^a   Domingo, Pere ^c   Clotet, Bonaventura ^a,b   Valle, Marta ^b,c  

^a HOSPITAL UNIVERSITARI GERMANS TRIAS I PUJOL   (Spain)

^b UNIVERSITAT AUTÒNOMA DE BARCELONA   (Spain)

^c HOSPITAL DE LA SANTA CREU I SANT PAU   (Spain)

Author keywords

Antiretrovirals, pharmacokinetics; HIV 1 infections; HIV protease inhibitors, pharmacokinetics; Lopinavir, pharmacokinetics; Lopinavir ritonavir, pharmacokinetics; Pharmacokinetic modelling; Population pharmacokinetics; Ritonavir, pharmacokinetics

Indexed keywords

ABACAVIR; DIDANOSINE; LAMIVUDINE; LOPINAVIR; LOPINAVIR PLUS RITONAVIR; RITONAVIR; STAVUDINE; TENOFOVIR; ZIDOVUDINE;

ACCURACY; ADULT; ARTICLE; BLOOD SAMPLING; CAUCASIAN; CLINICAL PRACTICE; COMPARTMENT MODEL; COMPUTER PROGRAM; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG EXPOSURE; FEMALE; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS INFECTED PATIENT; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; LIVER FIBROSIS; MAJOR CLINICAL STUDY; MALE; MONTE CARLO METHOD; NONLINEAR SYSTEM; PHARMACOKINETICS; POPULATION MODEL; POPULATION PHARMACOKINETICS; POPULATION RESEARCH; PRIORITY JOURNAL; VALIDATION STUDY;

ADULT; CROSS-SECTIONAL STUDIES; DRUG COMBINATIONS; FEMALE; HIV INFECTIONS; HIV PROTEASE INHIBITORS; HUMANS; MALE; MODELS, BIOLOGICAL; PYRIMIDINONES; RITONAVIR;

EID: 51649107032     PISSN: 03125963     EISSN: 03125963     Source Type: Journal    
DOI: 10.2165/00003088-200847100-00005     Document Type: Article

References (44)

1. Walmsley S. Protease inhibitor-based regimens for HIV therapy: safety and efficacy. J Acquir Immune Defic Syndr 2007; 45 Suppl. 1: S5-S13
2. Sham HL, Kempf DL, Molla A, et al. ABT-378, a highly potent inhibitor of the human immunodeficiency virus protease. Antimicrob Agents Chemother 1998; 42: 3218-24
3. Hicks C, King MS, Gulick RM, et al. Long-term safety and durable antiretroviral activity of lopinavir/ritonavir in treatment-naive patients: 4 year follow-up study. AIDS 2004; 18: 775-9
4. Kempf DJ, Isaacson JD, King MS, et al. Analysis of the virological response with respect to baseline viral phenotype and genotype in protease inhibitor-experienced HIV-1-infected patients receiving lopinavir/ritonavir therapy. Antivir Ther 2002; 7: 165-74
5. Olson DP, Scadden DT, D'Aquila RT, et al. The protease inhibitor ritonavir inhibits the functional activity of the multidrug resistance related-protein (MRP-1). AIDS 2002; 16: 1743-7
6. Cooper CL, van Heeswijk RPG, Gallicano K, et al. A review of low-dose ritonavir in protease inhibitor combination therapy. Clin Infect Dis 2003; 36: 1585-92
7. King JR, Wynn H, Brundage R, et al. Pharmacokinetic enhancement of protease inhibitor therapy. Clin Pharmacokinet 2004; 43: 291-310
8. la Porte C, Back D, Blaschke T, et al. Updated guideline to perform therapeutic drug monitoring for antiretroviral agents. Reviews in Antiviral Therapy 2006; 3: 4-14
9. Moltó J, Blanco A, Miranda C, et al. Variability in non-nucleoside reverse transcriptase and protease inhibitor concentrations among HIV-infected adults in routine clinical practice. Br J Clin Pharmacol 2006; 62: 560-6
10. van der Leur MR, Burger DM, la Porte CJL, et al. A retrospective TDM database analysis of interpatient variability in the pharmacokinetics of lopinavir in HIV- infected adults. Ther Drug Monit 2006; 28: 650-3
11. Masquelier B, Breilh D, Neau D, et al. Human immunodeficiency virus type genotypic and pharmacokinetic determinants of the virological response to lopinavir-ritonavir containing therapy in protease inhibitor-experienced patients. Antimicrob Agents Chemother 2002; 46: 2926-32
12. Boffito M, Arnaudo I, Raiteri R, et al. Clinical use of lopinavir/ritonavir in salvage therapy setting: pharmacokinetics and pharmacodynamics. AIDS 2002; 16: 2081-3
13. Hoefnagel JGM, Koopmans PP, Burger DM, et al. Role of the inhibitory quotient in HIV therapy. Antivir Ther 2005; 10: 879-92
14. Gonzalez de Requena D, Gallego O, Valer L, et al. Prediction of virological response to lopinavir/ritonavir using the genotypic inhibitory quotient. AIDS Research Human Retroviruses 2004; 20: 275-8
15. Castagna A, Gianotti N, Galli L, et al. The NIQ of lopinavir is predictive of 48-week virological response in highly treatment-experienced HIV-1-infected subjects treated with a lopinavir/ritonavir-containing regimen. Antivir Ther 2004; 9: 537-43
16. Marcelin AG, Cohen-Codar I, King MS, et al. Virological and pharmacological parameters predicting the response to lopinavir-ritonavir in heavily protease inhibitors-experienced patients. Antimicrob Agents Chemother 2005; 49: 1720-6
17. Hsu A, Isaacson J, Brun S, et al. Pharmacokinetic-pharmacodynamic analysis of lopinavir-ritonavir in combination with efavirenz and two nucleoside reverse transcriptase inhibitors in extensively pretreated human immunodeficiency virus-infected patients. Antimicrob Agents Chemother 2003; 47: 350-9
18. Best BM, Goicoechea M, Witt MD, et al. A randomized controlled trial of thera-peutic drug monitoring in treatment-naive and -experienced HIV-1-infected patients. J Acquir Immune Defic Syndr 2007; 46: 433-42
19. Kaletra® (lopinavir/ritonavir) [US prescribing information]. North Chicago (IL): Abbott Laboratories, 2003
20. Sterling R, Lissen E, Clumeck N, et al. Development of a simple noninvasive index to predict significant fibrosis in patients with HIV/HCV coinfection. Hepatology 2006; 6: 1317-25
21. Droste JAH, Aarnoutse RE, Koopmans PP, et al. Evaluation of antiretroviral drug measurements by an interlaboratory quality control program. J Acquir Immune Defic Syndr 2003; 32: 287-91
22. Beal SL, Sheiner LB. NONMEM user's guide. Ellicott City (MD): Icon Develop-ment Solutions, 1989-98
23. Jonsson EN, Karlsson MO. Xpose: an S-Plus based population pharmacokinetic/pharmacodynamic model building aid for NONMEM. Comput Methods Programs Biomed 1999; 58: 51-64
24. Sheiner LB, Beal SL. Some suggestions for measuring predictive performance. J Pharmacokinet Biopharm 1981; 9: 503-12
25. Sale M, Sadler BM, Stein DS. Pharmacokinetic modeling and simulations of interaction of amprenavir and ritonavir. Antimicrob Agents Chemother 2002; 46: 746-54
26. Lu JF, Blaschke TF, Flexner C, et al. Model-based analysis of the pharmacokinetic interactions between ritonavir, nelfinavir, and saquinavir after simultaneous and staggered oral administration. Drug Metab Dispos 2002; 30: 1455-61
27. Kappelhoff BS, Huitema AD, Crommentuyn KM, et al. Development and validation of a population pharmacokinetic model for ritonavir used as a booster or as an antiviral agent in HIV-1-infected patients. Br J Clin Pharmacol 2004; 59: 174-84
28. Moltó J, Valle M, Blanco A, et al. Lopinavir/ritonavir pharmacokinetics in HIV and hepatitis C virus co-infected patients without liver function impairment: influence of liver fibrosis. Clin Pharmacokinet 2007; 46: 85-92
29. Vrijens B, Tousset E, Rode R, et al. Successful projection of the time course of drug concentration in plasma during a 1-year period from electronically compiled dosing-time data used as input to individually parametrized pharmacokinetic models. J Clin Pharmacol 2005; 45: 461-7
30. Dailly E, Gagnieu MC, Allavena C, et al. No significant influence of saquinavir hard-gel capsule administration on pharmacokinetics of lopinavir in combination with ritonavir: a population approach. Ther Drug Monit 2005; 27: 782-4
31. Dailly E, Allavena C, Raffi F, et al. Pharmacokinetic evidence of the induction of lopinavir metabolism by efavirenz. Br J Clin Pharmacol 2005; 60: 32-4
32. Crommentuyn KML, Kappelhoff BS, Mulder JW, et al. Population pharmaco-kinetics of lopinavir in combination with ritonavir in HIV-1-infected patients. Br J Clin Pharmacol 2005; 60: 378-89
33. Boffito M, Hoggard PG, Lindup WE, et al. Lopinavir protein binding in vivo through the 12-hour dosing interval. Ther Drug Monit 2004; 26: 35-9
34. Boffito M, Sciole K, Raitieri R, et al. α-1 acid glycoprotein levels in human immunodeficiency virus-infected subjects on antiretroviral regimens. Drug Metab Dispos 2002; 30: 859-60
35. Oie S, Jacobson MA, Abrams DI. Alpha-1-acid glycoprotein levels in AIDS patients before and after short-term treatment with zidovudine (ZDV). J Acquir Immune Defic Syndr 1993; 5: 531-3
36. Jones K, Hoggard PG, Khoo S, et al. Effect of alpha1-acid glycoprotein on the intracellular accumulation of the HIV protease inhibitors saquinavir, ritonavir and indinavir in vitro. Br J Clin Pharmacol 2001; 51: 99-102
37. Holladay JW, Dewey MJ, Michniak BB, et al. Elevated alpha-1-acid glycoprotein reduces the volume of distribution and systemic clearance of saquinavir. Drug Metab Dispos 2001; 29: 299-303
38. Colombo S, Buclin T, Décosterd LA, et al. Orosomucoid (alpha1-acid glycoprotein) plasma concentrations and genetic variants: effects on human immunodeficiency virus protease inhibitor clearance and cellular accumulation. Clin Pharmacol Ther 2006; 80: 307-18
39. Hoggard PG, Owen A. The mechanisms that control intracellular penetration of the HIV protease inhibitors. J Antimicrob Chemother 2003; 51: 493-6
40. Kumar GN, Jayanti VK, Johnson MK, et al. Metabolism and disposition of the HIV-1 protease inhibitor lopinavir (ABT-378) given in combination with ritonavir in rats, dogs, and humans. Pharm Res 2004; 21: 1622-30
41. Eron J, Feinberg J, Kessler HA, et al. Once-daily versus twice-daily lopinavir/ritonavir in antiretroviral-naive HIV-positive patients: a 48-week randomized clinical trial. J Infect Dis 2004; 189: 265-72
42. van Heeswijk RPG, Bourbeau M, Seguin I, et al. Absence of circadian variation in the pharmacokinetics of lopinavir/ritonavir given as a once daily dosing regimen in HIV-1 infected patients. Br J Clin Pharmacol 2005; 59: 398-404
43. Barrett JS, Labbe L, Pfister M. Application and impact of population pharmacokinetics in the assessment of antiretroviral pharmacotherapy. Clin Pharmacokinet 2005; 44: 591-625
44. Klein CE, Chiu YL, Awni W, et al. The tablet formulation of lopinavir/ritonavir provides similar bioavailability to the soft-gelatin capsule formulation with less pharmacokinetic variability and diminished food effect. J Acquir Immune Defic Syndr 2007; 44: 401-10