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21.11.2005 – 10:04

Boehringer Ingelheim

APTIVUS(R) Sustains Convincing Anti-HIV Effect Through 48 Weeks

    Dublin, Ireland, November 21 (ots/PRNewswire)

    - Additional Data Provide Further Guidance on Maximizing Treatment Response with APTIVUS(R)

    New data presented at the 10th European AIDS Conference (EACS) in Dublin demonstrate that through 48 weeks, APTIVUS(R) (tipranavir) provides a convincing and durable benefit, achieving and maintaining a superior treatment response in patients with resistant HIV.(1) The European Commission granted marketing authorization for APTIVUS(R) in the European Union on 25 October 2005 for the combination antiretroviral treatment of HIV-1 in highly pre-treated adult patients with virus resistant to multiple protease inhibitors (PIs), when co-administered with a common boosting agent ritonavir (APTIVUS(R)).

    "Patients with resistance to current therapies have become one of the most challenging populations to treat in recent years," said Professor Pedro Cahn of Buenos Aires University Medical School in Argentina. "The lasting efficacy seen with tipranvir arms physicians with a convincing new treatment for patients whose virus has developed reduced susceptibility to other drugs."

    A combined analysis of the RESIST-1 and RESIST-2 clinical trials demonstrate that APTIVUS(R) continues to outperform a group of ritonavir-boosted comparator protease inhibitors (PIs) that included lopinavir/r (Kaletra(R)), amprenavir/r (Agenerase(R)), saquinavir/r (Invirase(R)) and indinavir/r (Crixivan(R)), through 48 weeks.(2) When compared to these PIs:

      - More than double the percentage of patients in the APTIVUS(R) arm
         responded to treatment
      - More than double the percentage of patients taking APTIVUS(R) were able
         to reduce the amount of HIV present in their blood (viral load) to
         undetectable levels
      - Treatment with APTIVUS(R) more than doubled the amount of patients'
         immune (CD4+) cells.

    Underlining the 48 week trial results, a 24-week sub-analysis of the RESIST studies also presented at EACS shows that for those patients who responded to APTIVUS(R) therapy, the majority were able to reduce the amount of HIV in their blood to undetectable levels. These patients also experienced an improvement in their immune system, having significantly increased their amount of immune cells with APTIVUS(R) therapy.(3)

    Additional sub-analyses of the RESIST studies presented at EACS provide further guidance for HIV-specialists on maximizing treatment response with APTIVUS(R).

    Early Initiation of APTIVUS(R) Leads to Better Treatment Outcomes

    Two separate 24-week sub-analyses within the RESIST patient population provide evidence that patients who initiate APTIVUS(R) treatment earlier have better overall treatment outcomes. These analyses found that:

      - Patients who started treatment with APTIVUS(R) or CPI/r with less PI
         experience achieved better treatment outcomes.(4) However, APTIVUS(R)
         consistently achieved a superior treatment outcome -- measured in viral
         load decreases and immune cell increases -- over the comparator PI/r,
         regardless of the number of PIs patients had taken previously.
      - APTIVUS(R) achieved a consistently superior treatment response and a
         larger decrease in viral load than comparator PIs, regardless of
         patients' viral load and immune cell count when initiating therapy.
         However, the efficacy of APTIVUS(R) was greater in patients with a
         Lower viral load and a higher immune cell count.(5)

    Addition of Active Anti-HIV Medications Improves APTIVUS(R) Treatment Response and Superiority Over Comparator PI

    An additional two 24-week RESIST sub-analyses within the RESIST patient population demonstrate that APTIVUS(R) more effectively reduces the amount of virus in a patient's system and suppresses the virus for a longer period of time with the addition of other active anti-HIV agents. These analyses found that:

      - A greater percentage of patients taking APTIVUS(R) were able to reduce
         their viral load to undetectable levels compared to those taking a
         comparator PI/r, -- regardless of the number of active drugs taken in
         combination with APTIVUS(R) or the comparator PI/r. The magnitude of
         difference in treatment response between APTIVUS(R) and comparator PI/r
         group increased, however, as more active agents were added to the two
         treatment arms.(6)
      - Patients taking APTIVUS(R) in combination with a further active
         anti-HIV drug of/from the non-nucleoside reverse transcriptase
         inhibitor class (NNRTI) achieved larger viral load decreases and immune
         cell increases than patients who received APTIVUS(R) without an


    APTIVUS(R) is a new non-peptidic protease inhibitor which works by inhibiting the viral protease, an enzyme needed to complete the HIV replication process.

    Based on available clinical and in vitro data, APTIVUS(R) is active against most strains of HIV-1 that are resistant to commercially available protease inhibitors. The safety and efficacy of APTIVUS(R) in paediatric patients or in adult patients who have not previously taken anti-HIV medications have not yet been established. Currently, phase 2 and 3 studies in these populations are fully enrolled and ongoing.

    In studies to date, APTIVUS(R) 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 diarrhoea, nausea, vomiting and abdominal pain. Fever, fatigue, headache, bronchitis, depression and rash also occurred.

    APTIVUS(R) boosted with low-dose ritonavir has been associated with reports of hepatic adverse events, 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(R) 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.

    Apart from the EU, APTIVUS(R) has received US marketing authorization by the FDA and was launched there in June 2005. Additional marketing authorizations from different countries have been received or are expected.

    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(R) was the first member of the non-nucleoside reverse transcriptase inhibitor (NNRTI) class of anti-HIV drugs on the market. The company is involved in basic research in that area and is committed to improving HIV therapy by providing physicians and patients with innovative antiretroviral treatment options.

    For more information on Boehringer Ingelheim, please see

      In a 48-week meta-analysis of the RESIST-1 and RESIST-2 trials:
      - 33.6% of patients who received APTIVUS(R) achieved a treatment response
         vs. 15.3% in the comparator PI/r arm.
      - A greater proportion of patients achieved a viral load below the level
         of detection in the APTIVUS(R) arm than in the comparator PI/r arm.
         30.4% in the APTIVUS(R) arm and 13.8% in the comparator PI/r arm
         achieved a viral load of less than 400 copies/mL.
      - Patients taking APTIVUS(R) also experienced greater increases in CD4+
         count than those taking a comparator PI/r, with mean CD4+ increases of
         +44.8 cells/mm3 and +21.1 cells/mm3, respectively.
      1. Cahn P. and Hicks C. 48 Week Meta-Analyses Demonstrate Superiority of
          Protease Inhibitor (PI) Tipranavir + Ritonavir (TPV/r) Over an
          Optimized PI (CPI/r) Regimen in Antiretroviral (ARV) Experienced
          Patients. 10th European AIDS Conference, Dublin, Ireland. Abstract
          #PS 3/8.
      2. Kaletra, Agenerase, Invirase and Crixivan are registered trademarks of
          Abbott Laboratories, GlaxoSmithKline, Hoffmann-La Roche Inc. and
          Bristol-Myers Squibb Company, respectively.
      3. Cassetti et al. Most TPV/r Treatment Responders Achieve Large Viral
          Load Reductions, Viral Loads Below Detection, and Substantial CD4+
          Cell Restoration. 10th European AIDS Conference, Dublin, Ireland.
          Abstract # PE2.7/1.
      4. Rockstroh et al. 24-Week Analysis of the Efficacy of Tipranavir
          Boosted With Ritonavir (TPV/r) in HIV Patients Stratified by Previous
          Protease Inhibitor (PI) Use. 10th European AIDS Conference, Dublin,
          Ireland. Abstract # PE7.9/11.
      5. Farthing C. Superior Efficacy of Tipranavir Boosted With Ritonavir
          (TPV/r) vs Comparator Boosted Protease Inhibitors (CPI/r) in Patients
          Stratified by Viral Load (VL) and CD4+ Cell Count. 10th European AIDS
          Conference, Dublin, Ireland. Abstract # PE7.3/22.
      6. Moreno et al. Impact of Including Genotypically Sensitive
          Antiretrovirals in a Tipranavir Boosted With Ritonavir (TPV/r) Regimen
          on Viral Load Response. 10th European AIDS Conference, Dublin,
          Ireland. Abstract # PE3.3/4.
      7. Kohlbrenner at al. Tipranavir Boosted With Ritonavir (TPV/r) Combined
          with an NNRTI Shows Superior Antiviral Activity Than TPV/r Without an
          NNRTI. 10th European AIDS Conference, Dublin, Ireland. Abstract #

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Judith von Gordon, CD Communications, of Boehringer Ingelheim GmbH,
+49-6132-773582, Fax: +49-6132-776601

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