[WePe3.2C08] Safety of Lopinavir Pharmakokinetics in Combination with Efavirenz or Nevirapine in a Nuke-free regimen

3rd International AIDS Society Conference on HIV Pathogenesis and Treatment

Rio de Janeiro - July 24 - 27, 2005

SAFETY OF LOPINAVIR PHARMAKOKINETICS IN COMBINATION WITH EFAVIRENZ OR NEVIRAPINE IN A NUKE-FREE REGIMEN

IAS Conf HIV Pathog Treat 2005 Jul 24-27;3rd: Abstract No. WePe3.2C08

Langmann P.¹, Trein A.², Zilly M.¹, Klinker H.¹, Schnaitmann E.²
¹Medizinische Klinik II, Wuerzburg, Germany, ²HIV Schwerpunktpraxis, Stuttgart, Germany

INTRODUCTION: To avoid mitochondrial toxicity nuke free regimens are a promising concept. PI in combination with NNRTI requires dose adjustment of the PI because of inducing effects of Efavirenz (EFV) or Nevirapine (NVP).

METHODS: In this pilot study pharmacokinetics of 16 patients treated with Lopinavir (533/133mg bid) (LPV) and EFV (600mg qd) (n=5) or NVP (200mg bid) (n=13) were evaluated by detecting trough plasma levels or random timed drug levels. After 4, 12, 24 and 36 weeks plasma samples of drug levels were taken. Clinical data concerning safety and efficacy were also evaluated. A HPLC method with UV detection was used. Data were shown as MW ± SD (min; max).

RESULTS: In n=5 patients EFV C12 was 1906 ± 988 (720; 5062) ng/ml; trough level (C_min) of NVP (n=8) was 4986 ± 3312 (1234; 19412)ng/ml and the trough level (C_min) of LPV (n=16) was 5400 ± 3063 (187; 13532) ng/ml. LPV trough levels during 36 weeks of therapy were above the required limit in patients taking the recommended dosage. Only in one patient with temporary adherence problems a single LPV level was 187 ng/ml. There was no difference in LPV trough levels between coadministration of NVP (5272 ± 3394 (187; 13077) ng/ml or EFV (4637 ± 2345 (1248; 8031) ng/ml. No changes of LPV or NNRTI plasmalevels were found during 36 weeks on combination therapy. High levels for one of the drugs were not associated with mentionable adverse events. The virological response in ITT analysis at 36 weeks showed 11/16 (68%) had VL <50 c/ml. The median increase from baseline CD4 count at week 36 was +243 (range 70 – 850) cells/µL. The LPV/r NNRTI combination was well tolerated over 36 weeks of treatment.

CONCLUSIONS: Pharmacokinetics of LPV in a nuke free treatment regimen consisting of NVP or EFV required dose adjustment of LPV to 533/133mg bid. Trough plasma levels of LPV and the coadministered NNRTI were save over 36 weeks.

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Clinical | WePe3.2C08 | Peter Langmann
Pharmacological Monitoring of ARV Therapy

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