PROMISE FOR ONCE-A-DAY DOSING OF FORTOVASE, STUDY SHOWS
Major Advance in Convenience
SAN FRANCISCO, 26 September 1999 Preliminary data presented here today indicate
that a new once-a-day regimen of the protease inhibitor FORTOVASE®
(saquinavir), when combined with a low dose of ritonavir (another protease inhibitor),
maintains saquinavir trough blood levels above those achieved by the currently licensed
three-times-a-day regimen of FORTOVASE throughout the entire 24-hour dosing interval.
The once-a-day FORTOVASE regimen could simplify the treatment schedule and
significantly reduce the number of anti-HIV pills a patient must take while maintaining
high saquinavir concentrations in patients blood. As people with HIV live longer,
convenient dosing and tolerability have been shown to be critical factors in helping
patients adhere to treatment regimens an important component of long-term treatment
Higher trough blood levels may give patients more flexibility in when they take their
dose during the course of a given day an important advantage as people with HIV
remain healthy longer and lead busy lives. This pharmacokinetic study is the first step in
establishing FORTOVASE + ritonavir once-a-day as a treatment option. Past studies of
saquinavir at high blood levels have found that the compound remains well-tolerated, even
with the higher exposure.
Further studies of the once-a-day combination in people with HIV are ongoing.This study is important because its a
preliminary demonstration that we can further optimize the convenience of treatment while
maintaining the power of protease inhibitors giving physicians and patients options
that are convenient and well-tolerated," said Michael Saag, M.D., director of the
AIDS Outpatient Clinic at the University of Alabama at Birmingham and lead investigator of
"Weve been very encouraged by how positive the saquinavir plus ritonavir
once-a-day dose looks so far. Were eager to continue studying this exciting
The pharmacokinetic study in healthy volunteers found that FORTOVASE 1600-mg once a day
(or QD) + ritonavir 100-mg QD resulted in trough blood levels that were roughly five times
higher than those achieved in the study arm using FORTOVASE 1200-mg dosed three times a
day (or TID), its current standard dose. The trough blood level is the concentration of
the drug in patients blood immediately before the next dose of drug is taken and is
believed to be important in maintaining suppression of the virus. The FORTOVASE 1600-mg QD
+ ritonavir 100-mg QD regimen was generally well-tolerated over the course of the
Further information on this study is available in the accompanying FORTOVASE
backgrounder; all FORTOVASE press materials and the abstract by Dr. Saag and colleagues
may also be found on the Roche HIV web site at www.roche-hiv.com.
Twice-Daily Dosing Continues to Provide Benefit in Large, Longer-Term Study
In addition to preliminary data on once-daily FORTOVASE dosing, the body of data on
twice-daily (or BID) FORTOVASE dosing continues to grow. In a large, prospective,
intent-to-treat 24-week analysis presented here, 838 patients were studied in three
groups: those receiving FORTOVASE 1600-mg BID + 2 nucleoside analogues (NAs), FORTOVASE
1200-mg BID + VIRACEPT® (nelfinavir mesylate) 1250-mg BID + 1 NA or FORTOVASE
1200-mg TID + 2 NAs.
The study looked at the results of these regimens through both an on-treatment analysis
and the more stringent intent-to-treat analysis, a type of analysis that includes patients
who discontinue treatment during the study in its final results. Both analyses found that
FORTOVASE taken twice a day + 2 nucleoside analogs (NAs) suppresses viral load similarly
to its current standard dose, FORTOVASE taken three times a day + 2 NAs at 24 weeks. In
addition, the FORTOVASE BID regimen supports the sustained increase in CD4 cells as seen
in other FORTOVASE trials.
Furthermore, preliminary data from a 48-week on-treatment analysis continue to show
durability of response in both the BID and TID treatment arms.
FORTOVASE is available in North America, Europe and Australia. It continues to be
introduced in other countries.
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