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Positive Opinion in Europe for Tipranavir

Rio De Janeiro, Brazil and Ingelheim, Germany (ots/PRNewswire)

- New Data Support its Use as Powerful Treatment Against HIV Drug
Resistance
RIO DE JANEIRO, Brazil and INGELHEIM, Germany, July 28 /PRNewswire/
Boehringer Ingelheim announced today that the CHMP (Committee for
Medicinal Products for Human Use) in London has issued a positive
opinion for tipranavir, a non-peptidic protease inhibitor, to treat
HIV-infected patients. The new drug will be indicated for highly
pre-treated adult patients with virus resistant to multiple protease
inhibitors. The positive opinion is seen as a recommendation to the
European Commission that authorization to market the drug should be
granted in the European Union. Marketing authorization, under
exceptional circumstances (comparable to accelerated approval in the
US) is expected in the fourth quarter 2005. If approved, tipranavir
will be marketed by Boehringer Ingelheim also in Europe under the
brand name APTIVUS(R). APTIVUS(R) was approved for use in the U.S. on
22 June 2005 and in Mexico on 19 July 2005 and is currently under
review by further regulatory agencies.
New data presented at the 3rd IAS Conference on HIV Pathogenesis
and Treatment confirmed that APTIVUS(R) (tipranavir), a novel HIV
medication, when boosted with low-dose ritonavir, is a powerful
treatment option for HIV-positive treatment-experienced adults. These
recent data from the RESIST clinical studies indicate that in highly
treatment experienced patients APTIVUS provides superior viral load
reduction and CD4+ cell count increase compared with a genotypically
optimized comparator regimen including lopinavir/r (Kaletra(R)),
ritonavir-boosted amprenavir (Agenerase(R)) or saquinavir
(Invirase(R)) (1)
"The increasing prevalence of HIV drug resistance underscores the
need for medications like APTIVUS that help patients who have become
resistant to current treatment options," said Professor Adriano
Lazzarin of the Clinic of Infectious Diseases, San Raffaele-Vita
Salute University, Milan, Italy. "These data provide additional
evidence that APTIVUS is an effective and much needed HIV therapy."
APTIVUS vs. Commonly Prescribed PIs
The RESIST phase III studies examined the safety and efficacy of
ritonavir-boosted APTIVUS versus established ritonavir-boosted
comparator protease inhibitors (PIs), which included lopinavir/r,
amprenavir/r, saquinavir/r or indinavir/r. PIs represent one of the
four classes of anti-HIV medications and many are commonly taken with
small doses of the PI ritonavir to "boost" their therapeutic levels.
In the RESIST studies conducted in 1483 patients treatment regimen
containing APTIVUS led to greater 24 week decreases of viral load
(amount of virus) in the patients' blood and greater increases in the
amount of immune (CD4+) cells in patients' systems, than regimen
containing lopinavir/r, amprenavir/r or saquinavir/r. (2, 3) Further
sub-analyses found that:
-- Patients receiving APTIVUS/r achieved a more than 2 times
greater  viral load drop and a more than 5 times greater increase in
CD4+ cells  compared to patients receiving lopinavir/r.
-- Patients taking APTIVUS/r achieved a 5 times greater viral load
drop and a more than 3 times greater increase in CD4+ cells compared
to patients taking saquinavir/r.
-- Patients receiving APTIVUS/r achieved a more than 6 times
greater  viral load drop compared to patients receiving amprenavir/r.
Patients taking amprenavir/r did not achieve an increase in CD4+
cells.
+ For detailed figures, please see the notes section.
APTIVUS with Other Active Anti-HIV Medications
APTIVUS was more effective in reducing the amount of virus in a
patient's system and suppressing the virus for a longer period of
time when it was taken with an additional active anti-HIV drug. In a
subset of the RESIST population evaluated at 24 weeks, APTIVUS'
efficacy was further enhanced when combined with enfuvirtide, a drug
to which only limited resistance can be expected at this time. (4)
The majority of patients (70%) who had never taken enfuvirtide before
and who combined the drug with APTIVUS/r, achieved a predefined
treatment response, whereas less than one-third (28%) of patients who
combined enfuvirtide with lopinavir/r, the market leading PI,
achieved this result.
"Boehringer Ingelheim is pleased by these data, which support the
use of APTIVUS in patients who are in need of new treatment options,"
said Dr.  Andreas Barner, Vice-Chairman of the Board of Managing
Directors and Head of Corporate Board Division Pharma Research,
Development and Medicine at Boehringer Ingelheim. "APTIVUS offers a
potent new addition to the HIV treatment armamentarium."
RESIST Study Design
The RESIST (Randomized Evaluation of Strategic Intervention in
Multi-Drug ReSistant Patients with Tipranavir) clinical trial program
is one of the largest study programs undertaken with an
investigational antiretroviral agent in patients previously treated
with multiple combinations of antiretroviral drug regimens.
RESIST-1 and RESIST-2 are randomized, controlled, open-label Phase
III trials designed to study the efficacy and safety of APTIVUS,
boosted with low-dose ritonavir, versus a low-dose ritonavir-boosted
comparator PI in patients who have previously taken other anti-HIV
medications and who have documented PI resistance. The studies
involved 1483 HIV-infected treatment-experienced adults in the US,
Canada, Australia, Latin-America and Europe.
Patients enrolled in the RESIST studies were randomly assigned to
receive an optimized standard of care regimen containing APTIVUS/r
500mg/200mg twice daily or a comparator PI/r at its standard dose.
All patients received resistance testing to aid investigators in the
selection of the comparator PI and background anti-HIV medications.
APTIVUS
APTIVUS, a new non-peptidic protease inhibitor, works by
inhibiting protease, an enzyme needed to complete the HIV replication
process. Based on available clinical and in vitro data, APTIVUS is
active against most strains of HIV-1 that are resistant to
commercially available protease inhibitors. The safety and efficacy
of APTIVUS in pediatric patients or in adult patients who have not
previously taken anti-HIV medications have not been established.
Phase 2 and 3 studies in these populations are fully enrolled and
ongoing.
In studies to date, APTIVUS has been well tolerated by most
patients and has a safety profile similar to other PIs. The most
commonly reported side effects of at least moderate intensity in
patients enrolled in the RESIST studies taking APTIVUS/r are
gastrointestinal, including diarrhea, nausea, vomiting and abdominal
pain. Fever, fatigue, headache, bronchitis, depression and rash also
occurred.
APTIVUS boosted with low-dose ritonavir has been associated with
reports of liver problems, which have included some fatalities. Extra
vigilance is warranted in patients with chronic hepatitis B or
hepatitis C co-infection, as these patients have an increased risk of
liver toxicity. The most common moderate to severe laboratory
abnormalities were elevated liver enzymes and elevated lipid levels.
Most laboratory abnormalities were asymptomatic and most patients
were successfully treated without discontinuation.
APTIVUS does not cure HIV infection/AIDS or prevent the
transmission of HIV to others. Patients may continue to develop
opportunistic infections and other complications associated with HIV
disease.
Boehringer Ingelheim
Boehringer Ingelheim is committed to the research and development
of novel antiretroviral agents. VIRAMUNE(R) (nevirapine) is a product
of original research done at Boehringer Ingelheim. VIRAMUNE was the
first member of the non-nucleoside reverse transcriptase inhibitor
(NNRTI) class of anti-HIV drugs. The company is involved in basic
research and is committed to improving HIV therapy by providing
physicians and patients with innovative antiretrovirals.
For more information on Boehringer Ingelheim, please see
http://www.boehringer-ingelheim.com/hiv.
Notes:
Detailed figures as indicated on page 2:
-- In the lopinavir/r stratum: Patients receiving APTIVUS/r and
those receiving lopinavir/r achieved a viral load drop of -0.71 log10
vs.-0.28 log10, respectively, and a CD4+ cell increase of +31
cells/mm (3) vs. +6 cells/mm (3) (p <0.0012), respectively.
-- In the saquinavir/r stratum: Patients taking APTIVUS/r and
those  taking saquinavir/r achieved a viral load drop of -1.01 log10
vs. -0.20  log10, respectively, and a CD4+ cell increase of +36
cells/mm (3) vs.  +11 cells/mm (3) (p < 0.005), respectively.
-- In the amprenavir/r stratum: Patients receiving APTIVUS/r and
those receiving amprenavir/r achieved a viral load drop of -1.01 vs.
-0.16 log10, respectively, and a CD4+ cell increase of +30 cells/mm
(3) vs. +0 cells/mm (3) (p <0.0001), respectively.
References:
(1) Kaletra, Agenerase and Invirase are registered trademarks of
Abbott Laboratories, GlaxoSmithKline and Hoffmann-La Roche Inc.,
respectively.
(2) Lazzarin et al. Tipranavir/ritonavir (TPV/r) demonstrates
superior treatment response to lopinavir/r (LPV/r), amprenavir/r
(APV/r) or saquinavir/r (SQV/r) in PI-experienced patients from the
TPV RESIST-1 and RESIST-2 trials. 3rd IAS Conference on HIV
Pathogenesis and Treatment, Rio de Janeiro, Brazil. Abstract #:
WePe6.3C07.
(3) Hicks et al. Tipranavir/ritonavir (TPV/r) demonstrates
superior immunologic response to comparator protease inhibitors
(CPIs) in a PI-experienced population with advanced disease. 3rd IAS
Conference on HIV Pathogenesis and Treatment, Rio de Janeiro, Brazil.
Abstract #: WePe16.7B07.
(4) Valdez et al. Tipranavir/ritonavir (TPV/r) 500 mg/200 mg BID
drives week 24 viral load (VL) below 400 copies/mL when combined with
a second active drug (T-20) in highly protease inhibitor experienced
HIV+ patients. 3rd IAS Conference on HIV Pathogenesis and Treatment,
Rio de Janeiro, Brazil. Abstract #: WeOa0205.

Contact:

Judith von Gordon of CD Communications, +49-6132-773582, or fax,
+49-6132-776601

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