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Background: Lopinavir is
a novel HIV protease inhibitor (PI) that is co-formulated with ritonavir, an
inhibitor of cytochrome P450 3A, as Kaletra™.
Superior efficacy was demonstrated in a 48-week Phase III trial of
antiretroviral (ARV) naïve patients (pts) comparing Kaletra (n=326) to
nelfinavir (n=327). Antiviral
activity has been maintained through 108 weeks in ARV-naïve pts (n= 100) and
through 96 and 48 weeks in single (n=70) and multiple PI-experienced (MPIE) pts
(n=57), respectively.
Methods: The safety and
tolerability of Kaletra were examined in Phase II/III trials through adverse
events (AE) with severity/relationship assessed by investigator, and laboratory
test results obtained without regard to fasting.
Results: Kaletra has
been well tolerated with study drug-related discontinuations (DC) occurring in
3% of ARV-naïve subjects and 5–6% of PI-experienced pts. Diarrhea (16%) and nausea (7%) were the most common AE
reported but resulted in interruption in 2% and DC in <1% of pts in Phase
III. Similar rates of GI AE were reported in Phase I. Grade 3/4 elevations of
cholesterol (>300 mg/dL) and triglycerides (>750 mg/dL) were each reported
in 9% of Kaletra-treated subjects in Phase III.
Elevations tended to be intermittent, non-progressive after 12 weeks, and
rarely associated with study drug interruptions or DC.
Increases occurred more frequently in MPIE pts and pts with higher
baseline values. No statistically
significant increase in LDL/HDL ratio was seen through 24 weeks of therapy.
AE consistent with body composition changes were seen in 4% of Phase III
pts. AST/ALT elevations were more
common in pts with baseline positive hepatitis B/C serologies, but the
elevations rarely led to interruption or DC.
Conclusions: Clinical trials demonstrate that Kaletra is well tolerated, as shown by the low rate of study drug-related DC. AE incidence rates are similar to or lower than those of other PIs; AE rarely resulted in drug interruption or discontinuation.
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