Pharmacokinetics of once-daily saquinavir/ritonavir in HIV-infected subjects: Comparison with the standard twice-daily regimen

Antiviral Therapy

Volumn 9, Issue 3, 2004, Pages 423-429

  Boffito, Marta ^a   Dickinson, Laura ^b   Hill, Andrew ^c   Back, David ^b   Moyle, Graeme ^a   Nelson, Mark ^a   Higgs, Chris ^a   Fletcher, Carl ^a   Mandalia, Sundhiya ^a   Gazzard, Brian ^a   Pozniak, Anton ^a  

^a CHELSEA AND WESTMINSTER HOSPITAL   (United Kingdom)

^b UNIVERSITY OF LIVERPOOL   (United Kingdom)

^c NONE

Author keywords

[No Author keywords available]

Indexed keywords

ABACAVIR; CHOLESTEROL; DIDANOSINE; GLUCOSE; LAMIVUDINE; PROTEINASE INHIBITOR; RITONAVIR; RNA DIRECTED DNA POLYMERASE INHIBITOR; SAQUINAVIR; STAVUDINE; TENOFOVIR; TRIACYLGLYCEROL; ZIDOVUDINE;

ABDOMINAL PAIN; ACQUIRED IMMUNE DEFICIENCY SYNDROME; ADULT; AGED; ARTICLE; CHOLESTEROL BLOOD LEVEL; CLINICAL ARTICLE; CLINICAL TRIAL; CONSTIPATION; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; CROSSOVER PROCEDURE; DIARRHEA; DOSE RESPONSE; DRUG BLOOD LEVEL; DRUG DOSE REGIMEN; DRUG EFFICACY; DRUG SAFETY; DRUG TOLERABILITY; FEMALE; GASTROINTESTINAL SYMPTOM; GLUCOSE BLOOD LEVEL; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HIGHLY ACTIVE ANTIRETROVIRAL THERAPY; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; LIVER FUNCTION TEST; MALE; MATHEMATICAL MODEL; PRIORITY JOURNAL; STEADY STATE; TANDEM MASS SPECTROMETRY; TRIACYLGLYCEROL BLOOD LEVEL;

ADULT; AGED; CROSS-OVER STUDIES; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG ADMINISTRATION SCHEDULE; DRUG COMBINATIONS; FEMALE; GASTROINTESTINAL DISEASES; GREAT BRITAIN; HIV PROTEASE INHIBITORS; HIV SEROPOSITIVITY; HUMANS; MALE; MIDDLE AGED; RITONAVIR; SAQUINAVIR;

EID: 3042775727     PISSN: 13596535     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (25)

1. Moyle GJ & Back D. Principles and practice of HIV-protease inhibitor pharmacoenhancement. HIV Medicine 2001; 2:105-113.
2. British HIV Association (BHIVA) guidelines for the treatment of HIV-infected adults with antiretroviral therapy. HIV Medicine 2003; 4 (Suppl.1):1-41.
3. Kurowski M, Sternfeld T, Sawyer A, Hill A & Mocklinghoff C. Pharmacokinetic and tolerability profile of twice-daily saquinavir hard gelatin capsules and saquinavir soft gelatin capsules boosted with ritonavir in healthy volunteers. HIV Medicine 2003; 4:94-100
4. Plosker GL & Scott LJ. Saquinavir: a review of its use in boosted regimens for treating HIV infection. Drugs 2003; 63:1299-1324.
5. Gerstoft J, Bak Dragsted U, Cahn P, Castagna A, Duran A, Hill A, Pedersen C, Peters B, Vernazza P, Youle M & Lundgren JD; on behalf of the MaxCmin1 Trial Group. Final analysis of a randomised trial to evaluate safety and efficacy of indinavir/ritonavir versus saquinavir/ritonavir in adult HIV-1 infection: the MaxCmin1 trial. 6th International Congress on Drug Therapy in HIV Infection. Glasgow, UK, 8-12 November 2002. Abstract P29.
6. Youle M, Gerstoft J, Fox Z, Losso M, Jayaweera DT, Riger A, Bruun JN, Castagna A, Walmsley S, Hill A, Dragsted UB & Lundgren JD for the MaxCmin2 Trial Group. The final Week 48 analysis of a phase IV, randomised, open-label, multi-centre trial to evaluate safety and efficacy of lopinavir/ritonavir (400/100 mg bid) versus saquinavir/ritonavir (1000/100 mg bid) in adult HIV-1 infection: The MaxCmin2 trial. 2nd IAS Conference on HIV Pathogenesis & Treatment. Paris, France, 12-16 July 2003. Abstract LB23.
7. Casado JL, Sabido R, Perez-Elias MJ, Antela A, Oliva J, Dronda F, Mejia B & Fortun J. Percentage of adherence correlates with the risk of protease inhibitor (PI) treatment failure in HIV-infected patients. Antiviral Therapy 1999; 4:157-161.
8. D'Arminio MA, Lepri AC, Rezza G, Pezzotti P, Antinori A, Phillips AN, Angarano G, Colangeli V, De Luca A, Ippolito G, Caggese L, Soscia F, Filice G, Gritti F, Narciso P, Tirelli U & Moroni M. Insights into the reasons for discontinuation of the first highly active antiretroviral therapy (HAART) regimen in a cohort of antiretroviral naive patients. Italian Cohort of Antiretroviral-Naive Patients (I.CO.N.A) Study Group. AIDS 2000; 14:499-507.
9. Moyle G. The Assessing Patient's Preferred Treatments (APPT-1) study. International Journal of STD & AIDS 2003; 14(Suppl.1):34-36.
10. Leenen FH, Wilson TW, Bolli P, Larochelle P, Myers M, Handa SP, Boileau G & Tanner J. Patterns of compliance with once versus twice daily antihypertensive drug therapy in primary care: a randomized clinical trial using electronic monitoring. Canadian Journal of Cardiology 1997; 13:914-920.
11. Mounier-Vehier C, Bernaud C, Carre A, Lequeuche B, Hotton JM & Charpentier JC. Compliance and antihypertensive efficacy of amlodipine compared with nifedipine slow-release. American Journal of Hypertension 1998; 11:478-486.
12. Montaner JSG, Saag M.S., Barylski C & Siemon-Hryczyk P. FOCUS Study: Saquinavir qd regimen versus efavirenz qd regimen week 48 analysis in HIV infected patients. 42nd Interscience Conference on Antimicrobial Agents & Chemotherapy. San Diego, Calif., USA, 27-30 September 2002; Abstract H-167.
13. Back D, Blaschke T, Boucher C, Burger D, Fletcher C, Flexner C, Gerber J & Schapiro J. Optimising TDM in HIV clinical care: a practical guide to performing therapeutic drug monitoring (TDM) for antiretroviral agents. Version 1.0. 2003. Available at: http://www.hivpharmacology.com/ (accessed 21-11-2003).
14. Cardiello PG, van Heeswijk RP, Hassink EA, Srasubkul P, Mahanontharit A, Samor TM, Worarien W, Beijnen JH et al. Simplifying protease inhibitor therapy with once-daily dosing of saquinavir soft-gelatin capsules/ritonavir (1600/100 mg): HIVNAT 001.3 Study. Journal of Acquired Immune Deficiency Syndromes 2002; 29:464-470.
15. Back DJ, Gatti G, Fletcher C, Garaffo R, Haubrich R, Hoetelmans R, Kurowski M, Luber A, Merry C & Perno CF. Therapeutic drug monitoring in HIV infection: current status and future directions. AIDS 2002; 16:S5-S37.
16. Durant J, Clevenbergh P, Garraffo R, Halfon P, Icard S, Del Giudice P, Montagne N, Schapiro JM & Dellamonica P. Importance of protease inhibitor plasma levels in HIV-infected patients treated with genotypic-guided therapy: pharmacological data from the Viradapt Study. AIDS 2000; 14:1333-1339.
17. Veldkamp AI, van Heeswijk RP, Mulder JW, Meenhorst PL, Schreij G, van der GS, Lange JM, Beijnen JH & Hoetelmans RM. Steady-state pharmacokinetics of twice-daily dosing of saquinavir plus ritonavir in HIV-1-infected individuals. Journal of Acquired Immune Deficiency Syndromes 2001; 27:344-349.
18. Gerber JG. Using pharmacokinetics to optimize antiretroviral drug-drug interactions in the treatment of human immunodeficiency virus infection. Clinical Infectious Diseases 2000; 30(Suppl 2):S123-S129.
19. Hsu A, Granneman GR, Cao G, Carothers L, El-Shourbagy T, Baroldi P, Erdman K, Brown F, Sun E & Leonard JM. Pharmacokinetic interactions between two human immunodeficiency virus protease inhibitors, ritonavir and saquinavir. Clinical Pharmacology & Therapeutics. 1998; 63:453-464.
20. Saag MS, Kilby M., Ehrensing E, Gizzi NA, Siemon-Hryczyk P, Buss N & Oo CY. Saquinavir systemic exposure and safety of once daily administration of Fortovase™ (saquinavir) soft gel capsule (FTV) in combination with low dose ritonavir (RTV). 39th Interscience Conference on Antimicrobial Agents & Chemotherapy. San Francisco, Calif., USA, 26-29 September 1999. Abstract 330.
21. Hoetelmans RM, Reijers MH, Weverling GJ, ten Kate RW, Wit FW, Mulder JW, Weigel HM, Frissen PH, Roos M, Jurriaans S, Schuitemaker H, de Wolf F, Beijnen JH & Lange JM. The effect of plasma drug concentrations on HIV-1 clearance rate during quadruple drug therapy. AIDS 1998; 12:F111-F115.
22. Gieschke R, Fotteler B, Buss N & Steimer JL. Relationships between exposure to saquinavir monotherapy and antiviral response in HIV-positive patients. Clinical Pharmacokinetics 2003; 37:75-86.
23. Schapiro JM, Winters MA, Stewart F, Efron B, Norris J, Kozal MJ & Merigan TC. The effect of high-dose saquinavir on viral load and CD4+ T-cell counts in HIV-infected patients. Annals of Internal Medicine 1996; 124:1039-1050.
24. Baxter JD, Merigan TC, Wentworth DN, Neaton JD, Hoover ML, Hoetelmans RM, Piscitelli SC, Verbiest WH & Mayers DL. Both baseline HIV-1 drug resistance and antiretroviral drug levels are associated with short-term virologic responses to salvage therapy. AIDS 2002; 16:1131-1138.
25. Valer L, De Mendoza C, De Requena DG, Labarga P, Garcia-Henarejos A, Barreiro P, Guerrero F, Vergara A, Soriano V & Fortogene Spanish Study Group. Impact of HIV genotyping and drug levels on the response to salvage therapy with saquinavir/ritonavir. AIDS 2002; 16:1964-1969.