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JAIDS Journal of Acquired Immune Deficiency Syndromes:
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Simplifying Protease Inhibitor Therapy with Once-Daily Dosing of Saquinavir Soft-Gelatin Capsules/Ritonavir (1600/100 mg): HIVNAT 001.3 Study.

Cardiello, Peter G.; van Heeswijk, Rolf P.; Hassink, Elly A.; Srasuebkul, Preeyaporn; Mahanontharit, Apicha; Samor, Tarika M.; Worarien, Wassana; Beijnen, Jos H.; Hoetelmans, Richard M.; Ruxrungtham, Kiat; Cooper, David A.; Lange, Joep M.; Phanuphak, Praphan

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Abstract

Objective: To determine the feasibility of switching therapy for HIV-1-infected patients with plasma viral loads of <50 HIV-1 RNA copies/mL who are receiving twice-daily saquinavir soft-gelatin capsules (SQV-SGC) plus dual nucleoside reverse transcriptase inhibitors (NRTIs) to a regimen containing once-daily SQV-SGC/ritonavir (RTV).

Design: Therapy for patients with plasma viral loads of <50 copies/mL after 2 years of treatment with twice-daily SQV-SGC (1400 mg) plus zidovudine/lamivudine or didanosine/stavudine was switched to once-daily SQV-SGC/RTV (1600/100 mg) with continuing NRTI treatment.

Methods: Safety and efficacy (determined by plasma viral load and CD4 cell count) were evaluated (week 24). For 12 patients, steady-state plasma pharmacokinetics of SQV was determined (week 4).

Results: Once-daily SQV-SGC/RTV was well tolerated. No patient changed regimens. After 24 weeks, 64 (93%) of 69 patients had plasma viral loads of <50 copies/mL (the remaining 5 patients had plasma viral loads of <300 copies/mL). The median CD4 cell count increased from 534/mL at the start of once-daily SQV-SGCs/RTV to 695/mL after 24 weeks (p < .001). Compared with the preceding 24 weeks of treatment with twice-daily SQV-SGC, the CD4 cell count improved significantly during once-daily SQV-SGC/RTV therapy (p < .001). All patients maintained SQV trough concentrations (C24h) of >0.05 mg/L. Median values for the area under the plasma concentration-versus-time curve from 0 to 24 hours (AUC0-24h), maximal concentration (Cmax), and C24h for SQV were 48.1 (h.mg)/L, 6.98 mg/L, and 0.17 mg/L, respectively. Body weight was inversely correlated with SQV AUC24h and C24h (p < .01).

Conclusions: Clinical and pharmacokinetic data support once-daily SQV-SGC/RTV (1600/100 mg) with two NRTIs as a convenient and safe therapeutic regimen to maintain viral suppression and immune function in HIV-1-infected patients with plasma viral loads of <50 copies/mL.

(C) 2002 by Lippincott Williams & Wilkins

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