Saquinavir/ritonavir: Its evolution and current treatment role

AIDS Reader

Volumn 16, Issue 1, 2006, Pages 38-44

  O'Brien III, William A ^a,b  

^a Memphis Pathology Laboratories   (United States)

^b UNIVERSITY OF TEXAS MEDICAL BRANCH   (United States)

Author keywords

Antiretroviral therapy; HIV AIDS; Protease inhibitor, boosted; Ritonavir; Saquinavir

Indexed keywords

ABACAVIR PLUS LAMIVUDINE PLUS ZIDOVUDINE; ANTIRETROVIRUS AGENT; ATAZANAVIR; INDINAVIR; LAMIVUDINE PLUS ZIDOVUDINE; LOPINAVIR; LOPINAVIR PLUS RITONAVIR; PROTEINASE INHIBITOR; PROTON PUMP INHIBITOR; RITONAVIR; SAQUINAVIR;

AREA UNDER THE CURVE; CLINICAL TRIAL; DIARRHEA; DOSE RESPONSE; DRUG ABSORPTION; DRUG BLOOD LEVEL; DRUG CAPSULE; DRUG CONTRAINDICATION; DRUG EFFICACY; DRUG FORMULATION; DRUG SAFETY; DRUG TOLERABILITY; DRUG WITHDRAWAL; DYSLIPIDEMIA; EVOLUTION; FOOD AND DRUG ADMINISTRATION; GASTROINTESTINAL DISEASE; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; HYPERSENSITIVITY; IMMUNE RESPONSE; KIDNEY DISEASE; NAUSEA AND VOMITING; PERIPHERAL NEUROPATHY; PH MEASUREMENT; PHYSICIAN; REVIEW; SKIN DISEASE; TREATMENT FAILURE; TREATMENT OUTCOME; BIOAVAILABILITY; CHEMISTRY; CONTROLLED CLINICAL TRIAL; DRUG COMBINATION; HALF LIFE TIME; MICROCAPSULE; RANDOMIZED CONTROLLED TRIAL;

BIOLOGICAL AVAILABILITY; CAPSULES; CHEMISTRY, PHARMACEUTICAL; DRUG COMBINATIONS; HALF-LIFE; HIV INFECTIONS; HIV PROTEASE INHIBITORS; HUMANS; RANDOMIZED CONTROLLED TRIALS; RITONAVIR; SAQUINAVIR;

EID: 33644843589     PISSN: 10530894     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Review

References (36)

1. US Food and Drug Administration. Drugs used in the treatment of HIV infection. Available at: http://www.fda.gov/oashi/aids/virals.html. Accessed December 2, 2005..
2. Invirase (saquinavir mesylate) capsules [package insert]. Nutley, NJ: Hoffman-La Roche Inc; 1995. Available at: http://www.rocheusa.com/products/ invirase/pi.pdf. Accessed December 19, 2005.
3. Fortovase (saquinavir) soft gelatin capsules [prescribing information]. Nutley, NJ: Roche Pharmaceuticals; December 2003. Available at: http://www.rocheusa.com/products/fortovase/. Accessed December 5, 2005.
4. Invirase 500 (saquinavir mesylate) capsules and tablets [prescribing information]. Nutley, NJ: Roche Pharmaceuticals; September 2005. Available at: http://www.rocheusa.com/products/invirase/. Accessed December 5, 2005.
5. US Department of Health and Human Services. Guidelines for the use of antiretroviral agents in HIV-infected adults and adolescents, October 6, 2005. Available at: http://aidsinfo.nih.gov/ContentFiles/AdultandAdolescentGL.pdf. Accessed December 5, 2005.
6. Plosker GL, Scott LJ. Saquinavir: a review of its use in boosted regimens for treating HIV infection. Drugs. 2003;63:1299-1324.
7. Malaty LI, Kuper JJ. Drug interactions of HIV protease inhibitors. Drug Saf. 1999;20:147-169.
8. Hsu A, Granneman GR, Cao G, et al. Pharmacokinetic interactions between two human immunodeficiency virus protease inhibitors, ritonavir and saquinavir. Clin Pharmacol Ther. 1998;63:453-464.
9. 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.
10. Buss N, Snell P, Bock J, et al. Saquinavir and ritonavir pharmacokinetics following combined ritonavir and saquinavir (soft gelatin capsules) administration. Br J Clin Pharmacol. 2001;52:255-264.
11. Staszewski S, Stark T, Knecht G, et al. The QUAD study: a pilot study to assess the efficacy and safety of Trizivir + RTV-boosted saquinavir (TZV + SQVR) compared to Combivir + RTV-boosted saquinavir (CBV + SQVR) in ART-naive patients with high viral load (VL) and low CD4 count - 24 week interim analysis. Presented at the 9th European AIDS Conference; October 25-29, 2003; Warsaw, Poland. Abstract F1/1. Available at: http://www.eacs.ws/conference/index.htm.
12. Ananworanich J, Ruxrungtham K, Siangphoe U, et al. A prospective cohort study of efficacy and safety of 2 NRTIs plus once-daily ritonavir boosted-saquinavir hard gel capsule (SQV-HGC/r) at 24 weeks. Presented at the XV International AIDS Conference; July 11-16, 2004; Bangkok, Thailand. Abstract TuPeB4469. Available at: http://www.iasociety.org/abstract/show.asp?abstract_id= 2170592. Accessed December 5, 2005.
13. Autar RS, Ananworanich J, Apateerapong W, et al. Pharmacokinetic study of saquinavir hard gel caps/ritonavir in HIV-1-infected patients: 1600/100 mg once-daily compared with 2000/100 mg once-daily and 1000/100 mg twice-daily. J Antimicrob Chemother. 2005;54:785-790.
14. Ananworanich J, Sirivichayakul S, Ubolyam S, et al. Different incidence of protease resistance in patients failing treatment on an initial ritonavir-boosted saquinavir (SQV/R) regimen versus those with prior exposure to dual-nucleosides and unboosted saquinavir. Poster presented at the XIV International HIV Drug Resistance Workshop; June 7-11, 2005; Quebec City. Abstract 33.
15. Dragsted UB, Gerstoft J, Pedersen C, et al. Randomized trial to evaluate indinavir/ritonavir versus saquinavir/ritonavir in human immunodeficiency virus type 1-infected patients: the MaxCmin1 Trial. J Infect Dis. 2003;188:635-642.
16. Youle M, Gerstoft J, Fox Z, et al. 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. Presented at the 2nd International AIDS Society Conference on HIV Pathogenesis and Treatment; July 13-16, 2003; Paris. Abstract LB23. Available at: http://www.iasociety.org/ abstract/show.asp?abstract_id=11077. Accessed December 5, 2005.
17. Dragsted UB, Gerstoft J, Youle M, et al; MaxCmin2 Trial Group. A randomized trial to evaluate lopinavir/ritonavir versus saquinavir/ritonavir in HIV-1-infected patients: the MaxCmin2 trial. Antivir Ther. 2005;10:735-743.
18. Durant J, Clevenbergh P, Garraffo R, et al. 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.
19. Baxter JD, Merigan TC, Wentworth DN, et al. 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.
20. Back D, Blaschke T, Boucher C, et al. Optimising TDM in HIV clinical care: a practical guide to performing therapeutic drug monitoring (TDM) for antiretroviral agents. April 2003. Available at: http://www.hivpharmacology.com/ . Accessed December 2, 2005.
21. Boffito M, Maitland D, Dickinson L, et al. Simultaneous administration of saquinavir hard gel (SQV-hg) and ritonavir (RTV) is required for optimal SQV absorption. Poster presented at 44th Interscience Conference on Antimicrobial Agents and Chemotherapy; October 30-November 2, 2004; Washington, DC. Poster A-453.
22. Kurowski M, Sternfeld T, Sawyer A, et al. 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(2):94-100.
23. Luber AD, Garg V, Gharakhanian S, et al. Survey of medications used by HIV-infected patients that affect gastrointestinal (GI) acidity and potential for negative drug interactions with HAART. Poster presented at the 7th international Congress on Drug Therapy in HIV Infection; November 14-18, 2004; Glasgow, Scotland. Abstract P294. Available at: http://www.abstracts2view.com/ icdh. Accessed December 2, 2005.
24. Furfine ES, Baker CT, Hale MR, et al. Preclinical pharmacology and pharmacokinetics of GW433908, a water-soluble prodrug of the human immunodeficiency virus protease inhibitor amprenavir. Antimicrob Agents Chemother. 2004;48:791-798.
25. Burger DM, Hugen PW, Kroon FP, et al. Pharmacokinetic interaction between the proton pump inhibitor omeprazole and the HIV protease inhibitor indinavir. AIDS. 1998;12:2080-2082.
26. Ford SL, Wire MB, Lou Y, et al. Effect of antacids and ranitidine on the single-dose pharmacokinetics of fosamprenavir. Antimicrob Agents Chemother. 2005;49:467-469.
27. Boffito M, Carriero P, Trentini L, et al. Pharmacokinetics of saquinavir co-administered with cimetidine. J Antimicrob Chemother. 2002;50:1081-1084.
28. Gill J, Feinberg J. Saquinavir soft gelatin capsule: a comparative safety review. Drug Saf. 2001;24:223-232.
29. Noble S, Faulds D. Saquinavir: a review of its pharmacology and clinical potential in the management of HIV infection. Drugs. 1996;52:93-112.
30. Grinspoon S, Carr A. Cardiovascular risk and body-fat abnormalities in HIV-infected adults. N Engl J Med. 2005;352:48-62.
31. Walmsley S, Montaner J, Hill A, et al. NRTI treatment as a risk factor for hyperlipidemia: results from the FOCUS trial. Poster presented at the 4th International Workshop on Adverse Drug Reactions and Lipodystrophy in HIV; September 2002; San Diego. Abstract 52.
32. Gallant J, Staszewski S, Pozniak AL, et al. Long-term efficacy and safety of tenofovir disoproxil fumarate (TDF): a 144-week comparison versus stavudine (d4T) in antiretroviral-naive patients. Presented at the XV International AIDS Conference; July 11-16, 2004; Bangkok, Thailand. Abstract TuPeB4538. Available at: http://www.iasociety.org/ejias/show.asp?abstract_id=2169665. Accessed December 2, 2005.
33. Cameron DW, Japour AJ, Xu Y, et al. Ritonavir and saquinavir combination therapy for the treatment of HIV infection. AIDS. 1999;13:213-224.
34. Montaner JS, Saag M, Schwartz R. Pharmacokinetic and safety evaluations of a once daily regimen of saquinavir soft gel capsules (SQV) in HIV infected antiretroviral naive patients. Poster presented at Frontiers in Drug Development for Antiretroviral Therapies (HIV DART 2000); December 17-21, 2000; Isla Verde, Puerto Rico. Abstract 048.
35. Haas DW, Zala C, Schrader S, et al. Therapy with atazanavir plus saquinavir in patients failing highly-active antiretroviral therapy: a randomized comparative pilot trial. AIDS. 2003;17:1339-1349.
36. Johnson LF, DeMeester TR. Development of the 24-hour intraesophageal pH monitoring composite scoring system. J Clin Gastroenterol. 1986;8(suppl 1):52-58.