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Fortovase

Saquinavir, with trade name Fortovase® is a protease inhibitor used as a component of highly active antiretroviral therapy (HAART). more...

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Saquinavir mesylate is a different formulation, designed to be combined with another protease inhibitor that increases the bioavailability of the saquinavir.

History

Saquinavir was the first protease inhibitor (and sixth antiretroviral) approved by the Food and Drug Administration (FDA). It was approved on December 6, 1995, as Invirase®, a poorly-absorbed hard gel capsule which quickly led to viral resistance in many of the pioneer patients.

It was approved again on Nov 7, 1997 as Fortovase®, a soft gel capsule reformulated for improved bioavailability. The manufacturer, Roche, is alleged to have rushed Invirase® to market, but the conditions that prevailed at the time were very bad and there was a lot of pressure to produce products quickly.

Method of activity

When given alone, the HIV Protease Inhibitor (HPI) saquinavir has a very low oral bioavailability. In the clinic, it was found that the oral bioavailability of saquinavir significantly increases when patients also receive the HPI ritonavir. For patients, this has the major benefit that they can take less saquinavir, while maintaining sufficient saquinavir blood plasma levels to efficiently suppress the replication of HIV.

The mechanism behind this welcome observation was not directly known, but later it was determined that ritonavir inhibits the enzyme Cytochrome P450 3A4. Normally, this enzyme metabolizes saquinavir to an inactive form, but with the ritonavir inhibiting this enzyme, the saquinavir blood plasma levels increased considerably. Additionally, ritonavir also inhibits multidrug transporters, although to a much lower extent.


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Combo Approved for HIV Treatment
From Nurse Practitioner, 3/1/04

The FDA approved Roche's saquinavir mesylate (Invirase, 1,000 mg) with ritonavir (Abbott's Norvir, 100 mg) for use in combination regimens for HIV infection treatment. The new dosing plan boosts blood levels of saquinavir to enable twice-daily dosing (instead of three times daily).

The organization approved the plan based on data indicating that saquinavir (1,000 mg) with ritonavir (100 mg) twice daily provides levels of saquinavir similar to or greater than those achieved with another formulation of saquinavir (Fortovase, 1,200 mg, three times daily) over a 24-hour period.

Invirase and Fortovase are not bioequivalent and cannot be used interchangeably, Roche notes. Use Invirase only in combination with ritonavir. Fortovase is the recommended formulation when using saquinavir as the sole protease inhibitor in an antiviral regimen.

Consult product labeling for specific information on dosing, adverse events, precautions, and contraindications associated with this drug combination.

Copyright Springhouse Corporation Mar 2004
Provided by ProQuest Information and Learning Company. All rights Reserved

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