Fortovase

Generic name:saquinavir
Dosage form: Soft Gelatin Capsules
Drug class:Protease inhibitors

Medically reviewed by Drugs.com. Last updated on Mar 22, 2022.

Product identification in this document includes: INVIRASE® in reference to saquinavir mesylate; Fortovase in reference to saquinavir, and saquinavir in reference to the active base.

Fortovase Description

Fortovase brand of saquinavir is an inhibitor of the human immunodeficiency virus (HIV) protease. Fortovase is available as beige, opaque, soft gelatin capsules for oral administration in a 200-mg strength (as saquinavir free base). Each capsule also contains the inactive ingredients medium chain mono- and diglycerides, povidone and dl-alpha tocopherol. Each capsule shell contains gelatin and glycerol 85% with the following colorants: red iron oxide, yellow iron oxide, and titanium dioxide. The chemical name for saquinavir is N-tert-butyl-decahydro-2-[2(R)-hydroxy-4-phenyl-3(S)-[[N-(2-quinolylcarbonyl)-L-asparaginyl]amino]butyl]-(4aS,8aS)-isoquinoline-3(S)-carboxamide which has a molecular formula C38H50N6O5 and a molecular weight of 670.86. Saquinavir has the following structural formula:

Saquinavir is a white to off-white powder and is insoluble in aqueous medium at 25°C.

MICROBIOLOGY

Mechanism of Action

Saquinavir is an inhibitor of HIV protease. HIV 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 analogue 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.

Antiviral Activity

In vitro antiviral activity of saquinavir was assessed in lymphoblastoid and monocytic cell lines and in peripheral blood lymphocytes. Saquinavir inhibited HIV activity in both acutely and chronically infected cells. IC50 and IC90 values (50% and 90% inhibitory concentrations) were in t...