General Description:
Fortovase is a protease inhibitor developed by Roche Laboratories designed for the clinical treatment of the human immunodeficiency virus (HIV).  It is available in a 200-mg strength soft gelatin capsule.

Mechanism:
Molecular Formula: C38H50N6O5
Molecular Weight: 670.86
See below for Molecular Structure
 
 

Saquinavir is an inhibitor of HIV protease.  The protease is an enzyme required for "the proteolytic cleavage of viral polyprotein precursors into individual functional proteins found in infectious HIV.  Saquinavir is a peptide-like substrate that binds to the protease active site and inhibits the activity of the enzyme".  Saquinavir inhibition prevents cleavage of the viral polyproteins resulting in the formation of immature noninfectious virus particles.

Indications and usage:
Fortovase is indicated for use in combination with other anti-retroviral drugs for the treatment of HIV infection.  This indication is based on clinical data that showed a reduction in both mortality and AIDS-related disease for patients who recieved fortovase in combination with zalcitabine, and/or other drug regiments.

The recommended dosage is three 200 mg capsules daily.  Fortovase should be taken within two hours of completing a meal.  Lower dosages have shown little or no therapeutic effect.

Precautions:
New cases of diabetes mellitus, worsening of pre-existing diabetes mellitus and hyperglycemia have been reported during posmarketing surveillance in HIV infected patients recieving protease-inhibitor treatment.  In some severe cases, diabetic ketacidosis has occured.

Contraindications:
Fortovase is contrainicated for patients with known hypersensitivity to saquinavir or its components.  It should NOT be administered concomitantly with terfenadine, casapride, astmiazole, triazolam, midazolam, or ergot derivatives.

Potential Adverse Effects:
The most frequently reported treatment emergent adverse events among patients receiving fortovase in combination with other antiretroviral agents were diarrhea, nausea, abdominal discomfort, and dyspepsia.
 
 

Back