Saquinavir and ritonavir pharmacokinetics following combined ritonavir and saquinavir (soft gelatin capsules) administration

British Journal of Clinical Pharmacology, Supplement

Volumn 52, Issue 3, 2001, Pages 255-264

  Buss, Neil ^a   Snell, Paul ^b   Bock, Jürgen ^a   Hsu, Ann ^c   Jorga, Karin ^a  

^a F HOFFMANN LA ROCHE LTD   (Switzerland)

^b ROCHE PRODUCTS LTD   (United Kingdom)

^c ABBOTT LABORATORIES   (United States)

Author keywords

Pharmacokinetics; Ritonavir; Saquinavir; Soft gelatin capsule

Indexed keywords

GELATIN; PROTEINASE INHIBITOR; RITONAVIR; SAQUINAVIR;

ADOLESCENT; ADULT; AREA UNDER THE CURVE; ARTICLE; CHEMICALLY INDUCED DISORDER; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; DOSE RESPONSE; DRUG COMBINATION; DRUG INTERACTION; FEMALE; HUMAN; MALE; MICROCAPSULE; MIDDLE AGED; NAUSEA; PATIENT; RANDOMIZED CONTROLLED TRIAL; RASH; VOMITING;

ADOLESCENT; ADULT; AREA UNDER CURVE; CAPSULES; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG COMBINATIONS; DRUG INTERACTIONS; EXANTHEMA; FEMALE; GELATIN; HIV PROTEASE INHIBITORS; HUMANS; MALE; MIDDLE AGED; NAUSEA; PATIENT DROPOUTS; RITONAVIR; SAQUINAVIR; VOMITING;

EID: 0035461510     PISSN: 02643774     EISSN: None     Source Type: Journal    
DOI: 10.1046/j.0306-5251.2001.01452.x     Document Type: Article

References (34)

1. Stellbrink H-J. Clinical and survival benefit of saquinavir (SQV) in combination with zalcitabine (DDC) and zidovudine (ZDV) in untreated minimally treated HIV-infected patients. Abstracts from the Sixth European Conference on Clinical Aspects and Treatment of HlV-Infcction, Hamburg, Germany, 1997; (abstract 212): 21.
2. Haubrich R, Lalezari J, FoIIansbee SE, et al. Improved survival and reduced clinical progression in HIV-infected patients with advanced disease treated with saquinavir plus zalcitabine. Antiviral Tlicr 1998; 3: 33-42.
3. Cohen Stuart JWT, Schuunnan R, Burger DM, et al. Randomized trial comparing saquinavir soft gelatin capsules versus indinavir as part of triple therapy (CHEESE study). AIDS 1999; 13: F53-F58.
4. Mitsuyasu RT, Skolnik PR, Cohen SR, et al. Activity of the soft gelatin formulation of saquinavir in combination therapy in antiretroviral-naive patients. AIDS 1998; 12: F103-F109.
5. Kohl NE, Emini EA, Schleif WA, et al. Active human immunodeficiency vims protease is required for viral infectivity. Proc Natl Acad Sci USA 1988; 85: 4686-4690.
6. Peng C, Bao K, Chang TW, Chang NT. Role of human immunodeficiency virus type 1-specific protease in core protein maturation and viral infectivity. J Viral 1989; 63: 2550-2556.
7. Lalezari J. Selecting the optimum dose for a new soft gelatin capsule formulation of saquinavir. J Acqnir Immune Deβc Syndr Hum Retroi'irol 1998; 19: 195-196.
8. Gieschke R, Fotteler B, Buss N, Steimer J-L. Relationships between exposure to saquinavir monotherapy and antiviral response in HIV-positive patients. Clin Phamiacokin 1999; 37: 75-86.
9. Schapiro JM, Winters MA, Stewart F, et al. The effect of high-dose saquinavir on viral load and CD4+ T-cell counts in HIV-infected patients. Ann Intern Mcd 1996; 124: 1039-1050.
10. Gill MJ. Safety profile of soft gelatin formulation of saquinavir in combination with nucleosides in a broad patient population. AIDS 1998; 12: 1400-1402.
11. Eagling VA, Back DJ, Barry MG. Differential inhibition of cytochrpme IM50 isoforms by the protease inhibitors, ritonavir, saquinavir and indinavir. BrJ Clin Phannacol 1997; 44: 190-194.
12. Kempf DJ, Marsh KC, Kumar G, et al. Pharmacokinetic enhancement of inhibitors of the human immunodeficiency virus protease by coadministration with ritonavir. Antiinicrob Agents Clicnwtlicr 1997; 41: 654-660.
13. Carpenter CCJ, Fischl MA, Hammer SM, et al. Antiretroviral therapy for HIV infection in 1997: updated recommendations of the International AIDS Society - USA Panel. JAMA 1997; 277: 1962-1969.
14. Cameron DW, Japour AJ, Xu Y, et al. Ritonavir and saquinavir combination therapy for the treatment of HIV infection. AIDS 1999; 13: 213-224.
15. Lal R, Hsu A, Chen P, et al. Single dose phanmcokinetics of ABT-378 in combination with ritonavir. Abstracts of the 37th Intersciciicc Conference on Antimicrobial Agents and Chemotherapy, Toronto, Canada, 1997; (abstract 1-194): 279.
16. Lal R, Hsu A, Granneman GR, et ai. Multiple dose safety, tolerability and phamiacokinetics of ABT-378 in combination with ritonavir. Abstracts 5lh Conference on Rctrovimscs and Opportunistic Infections, Chicago, USA, 1998; (Abstract 647): 201.
17. Tebas P, Patick AK, Kane EM, et al. Virologie responses to ritonavir-saquinavir-containing regimen in patients who had previously failed nelfmavir. AIDS 1999; 13: F23-F28.
18. Cameron DW, Xu Y, Roce R, et al. Three-year follow-up and conditional outcomes survival analysis of ritonavir (RTV) plus saquinavir (SQV) therapy in HIV infection. 7tli Conference on Retrofiniscs and Opportunistic Infections, San Francisco, USA, 2000; (abstract 533).
19. Hsu A, Granneman GR, Bertz RJ. Ritonavir: clinical phamiacokinetics and interactions with other anti-HIV agents. Clin Pham
20. Hsu A, Granneman GR, Cao G, et al. Pharmacokinetic interactions between two human immunodeficiency virus protease inhibitors, ritonavir and saquinavir. Clin Pliannacol Tlicr 1998; 63 (4): 453-464.
21. Merry C, Barry MG, Mulcahy F, et al. Saquinavir pharmacokinetics alone and in combination with ritonavir in HIV-infected patients. AIDS 1997; 11: F29-F33.
22. Profit L, Eagling VA, Back DJ. Modulation of P-glycoprotein function in human lymphocytes and Caco-2 cell monolayers by HIV-1 protease inhibitors. AIDS 1999; 13: 1623-1627.
23. Washington CB, Duran GE, Sikic HI, Blaschke TF. Saquinavir is a high affinity substrate for the multidrag transporter, P-glycoprotein. Clin Pliannacol Tlicr 1997; 61: 193.
24. Wacher VJ, Wu C-Y, Benêt LZ. Overlapping substrate specificities and tissue distribution of cytochrome P4503A and P-glycoprotein: implications for dmg delivery and activity in cancer chemotherapy. Mol Carcinog 1995; 13: 129-134.
25. Gatti G, Di Biagio AD, Casazza R, et al. The relationship between ritonavir plasma levels and side-effects: implications for therapeutic drug monitoring. AIDS 1999; 13: 2083-2089.
26. Abbott Laboratories. Norvir (ritonavir capsules) soft gelatin (ritonavir oral solution). Prescribing Information, June, 1999.
27. Pikety C, Race E, Castiel P, et al. Efficacy of a five-drug combination including ritonavir, saquinavir and efavirenz in patients who failed on a conventional triple-drug regimen: phenotypic resistance to protease inhibitors predicts outcome of therapy. AIDS 1999; 13: F71-F77.
28. Saag MS, Kilby M, Ehrensing E, Buss N, Oo CY. Modulation of saquinavir steady-state phamiacokinetics with 'baby' doses of ritonavir in healthy volunteers. 7th European Conference on Clinical Aspects and Treatment of HlV-infcction, Lisbon, Portugal, 1999; (Abstract 829): 210.
29. Van Heeswijk RPG, Veldkamp AI, Mulder JW, et al. The steady-state phamiacokinetics of saquinavir in a once daily dosing regimen with a low dose of ritonavir. 7th European Conference on Clinical Aspects and Treatment of HIV-infection, Lisbon, Portugal, 1999; (Abstract 830): 211.
30. Kurowski M, Müller M, Donath F, Mrozikiewicz M, MöcklinghofF C. Single daily doses of saquinavir achieve HIV-inhibitory concentrations when combined with 'baby-dose' ritonavir. Eur J Med Res 1999; 4: 101-104.
31. Gibaldi M, Ferner D. Phannacokiiictics, 2nd edn. New York; Marcel Dekker, 1982.
32. Hsu A, Granneman GR, Sun E, et al. Assessment of single- and multiple-dose interactions between ritonavir and saquinavir. Abstracts from XI International Conference on AIDS, Vancouver, Canada, 1996.
33. Watkins PB, Wrighton SA, Schuetz EG, Molowa DT, Guzelian PS. Identification of glucocorticoid-inducible cytochronies P-450 in the intestinal inucosa of rats and man. J Clin Invest 1987; 80: 1029-1036.
34. Kolars JC, Lown KS, Schniiedlin-Ren P, et al. CYP3A gene expression in human gut epithelium. Pharmacogenetics 1994; 4: 247-259.