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Roche (RHHBY) Release: U.S. FDA Approves New 500 Mg Tablet Formulation Of INVIRASE(R)



10/19/2005 5:12:30 PM

NUTLEY, N.J., Dec. 20 /PRNewswire/ -- Roche today announced U.S. Food and Drug Administration (FDA) approval of a new 500 mg film-coated tablet formulation of its HIV protease inhibitor INVIRASE(R) (saquinavir mesylate), designed for use in combination with a small dose of ritonavir and other anti-HIV drugs for the treatment of HIV infection. The new formulation of INVIRASE, which was approved under a six-month priority FDA review, will reduce pill count for each dose by more than half (from five pills to two, twice-daily) compared to the current formulation of INVIRASE 200 mg capsules.

"It has long been known that patients are better able to adhere to treatments with fewer pills," said Dr. Nick Bellos, President, Southwest Infectious Disease Associates. "This new formulation, combined with the well-established clinical record of potency and tolerability of INVIRASE/ritonavir, makes this treatment an important new option for patients."

Today's approval was based on data that show similar drug levels are achieved with INVIRASE 500 mg tablets and INVIRASE 200 mg capsules when each is administered with low dose ritonavir (100 mg), taken with food. The new 500 mg formulation requires only four INVIRASE tablets daily -- two in the morning and two in the evening, taken with ritonavir.

Originally approved by the FDA in 1995, the introduction of INVIRASE as the first HIV protease inhibitor represented a major milestone in the treatment of HIV/AIDS. When first available, the recommended dose required a total of nine INVIRASE capsules daily -- three capsules in the morning, afternoon and evening. In December 2003, the FDA approved INVIRASE for use in boosted dosing regimens with ritonavir (1000 mg INVIRASE/100 mg ritonavir), which enhances therapeutic blood levels of INVIRASE and allows for twice-daily dosing.

"Today's approval is one in a long line of milestones that illustrate the Roche heritage of innovation in HIV," said Malte Schultz, M.D., Medical Director, Roche. "The new 500 mg tablet formulation makes INVIRASE an attractive option for HIV patients across the treatment spectrum, from those just beginning therapy to those with prior treatment experience."

About INVIRASE

INVIRASE in combination with ritonavir and other antiretroviral agents is indicated for the treatment of HIV infection. The twice-daily administration of INVIRASE in combination with ritonavir is supported by safety data from the MaxCMin 1 study and pharmacokinetic data. The efficacy of INVIRASE with ritonavir or FORTOVASE (with or without ritonavir coadministration) has not been compared against the efficacy of antiretroviral regimens currently considered standard of care.

INVIRASE(R) (saquinavir mesylate) capsules and FORTOVASE(R) (saquinavir) soft gelatin capsules are not bioequivalent and cannot be used interchangeably. INVIRASE may be used only if it is combined with ritonavir, which significantly inhibits saquinavir's metabolism to provide plasma saquinavir levels at least equal to those achieved with FORTOVASE. When using saquinavir as the sole protease inhibitor in an antiviral regimen, FORTOVASE is the recommended formulation.

INVIRASE is contraindicated in patients with clinically significant hypersensitivity to saquinavir or to any of the components contained in the capsule. INVIRASE/ritonavir should not be administered concurrently with terfenadine, cisapride, astemizole, pimozide, triazolam, midazolam or ergot derivatives. Inhibition of CYP3A4 by saquinavir could result in elevated plasma concentrations of these drugs, potentially causing serious or life-threatening reactions, such as cardiac arrhythmias or prolonged sedation.

INVIRASE when administered with ritonavir is contraindicated in patients with severe hepatic impairment. Patients with hepatic impairment have not been studied and caution should be exercised when prescribing saquinavir in this population. Concomitant use of INVIRASE with lovastatin or simvastatin is not recommended. Caution should be exercised if HIV protease inhibitors, including INVIRASE, are used concurrently with other HMG-CoA reductase inhibitors that are also metabolized by the CYP3A4 pathway (eg, atorvastatin).

Concomitant use of INVIRASE and St. John's wort (hypericum perforatum) or products containing St. John's wort is not recommended. Garlic capsules should not be used while taking saquinavir as the sole protease inhibitor, due to the risk of decreased saquinavir plasma concentrations. For a complete list of drugs that should not be taken with saquinavir, please see TABLE 5 in the summary of complete product information.

New-onset diabetes mellitus, exacerbation of preexisting diabetes mellitus and hyperglycemia have been reported during postmarketing surveillance in HIV- infected patients receiving protease-inhibitor therapy. No initial dose adjustment is necessary for patients with renal impairment. However, patients with severe renal impairment have not been studied, and caution should be exercised when prescribing saquinavir in this population. There have been reports of spontaneous bleeding in patients with hemophilia A and B treated with protease inhibitors.

Elevated cholesterol and/or triglyceride levels have been observed in some patients taking saquinavir in combination with ritonavir. Redistribution/accumulation of body fat has been observed in patients receiving antiretroviral therapy. A causal relationship between protease-inhibitor therapy and these events has not been established, and the long-term consequences are currently unknown.

Varying degrees of cross-resistance among protease inhibitors have been observed. In clinical trials with saquinavir (1000 mg) in combination with ritonavir (100 mg) and other antiretrovirals, the grade 2, 3 and 4 adverse events occurring in greater than or equal to 2% of 148 patients (considered at least possibly related to study drug or of unknown relationship): abdominal pain (6.1%), back pain (2%), bronchitis (2.7%), constipation (2%), diarrhea (8.1%), diabetes mellitus/hyperglycemia (2.7%), dry lips/skin (2%), eczema (2%), fatigue (6.1%), fever (3.4%), influenza (2.7%), lipodystrophy (5.4%), nausea (10.8%), pneumonia (5.4%), pruritus (3.4%), rash (3.4%), sinusitis (2.7%) and vomiting (7.4%).

INVIRASE is not a cure for HIV infection or AIDS. INVIRASE does not prevent the transmission of HIV.

About Roche

Hoffmann-La Roche Inc. (Roche), based in Nutley, N.J., is the U.S. prescription drug unit of the Roche Group, a leading research-based health care enterprise that ranks among the world's leaders in pharmaceuticals, diagnostics and vitamins. Roche discovers, develops, manufactures and markets numerous important prescription drugs that enhance people's health, well-being and quality of life. Among the company's areas of therapeutic interest are: dermatology; genitourinary disease; infectious diseases, including influenza; inflammation, including arthritis and osteoporosis; metabolic diseases, including obesity and diabetes; neurology; oncology; transplantation; vascular diseases; and virology, including HIV/AIDS and hepatitis C. For more information on the Roche pharmaceuticals business in the United States, visit the company's web site at: http://www.rocheusa.com/

Ritonavir is manufactured by Abbott Laboratories

Roche

CONTACT: Maureen Byrne of Roche, +1-973-562-2203,maureen.byrne@roche.com; or Noelle Boyd of Manning Selvage & Lee,+1-212-468-4313, noelle.boyd@mslpr.com, for Roche


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