Saquinavir: profile and news

International Approvals: Invirase and Remicade May 15, 2006
May 15, 2006 — Health Canada has approved a 500-mg tablet formulation of saquinavir mesylate that significantly reduces the daily pill count for patients ... - Medscape (subscription)

HIV-positive people with higher viral load have increased risk of ... Apr 23, 2006
Individuals who took unboosted saquinavir, a component of an antiretroviral regimen which would now be considered suboptimal, also had an increased risk of ... - Aidsmap,

Roche Women Honored as 2006 TWIN Awardees Apr 28, 2006
She led the FDA filings for the early AIDS drugs HIVID® (zalcitabine) and Invirase® (saquinavir mesylate), which positively affected the lives of countless ... - Yahoo! News (press release)

Other information

Indication
HIV-1 with advanced immunodeficiency together with antiretroviral nucleoside analogues

Pharmacology
Saquinavir is a protease inhibitor with activity against Human Immunodeficiency Virus Type 1 (HIV-1). Protease inhibitors block the part of HIV called protease. HIV-1 protease is an enzyme required for the proteolytic cleavage of the viral polyprotein precursors into the individual functional proteins found in infectious HIV-1. Saquinavir binds to the protease active site and inhibits the activity of the enzyme. This inhibition prevents cleavage of the viral polyproteins resulting in the formation of immature non-infectious viral particles. Protease inhibitors are almost always used in combination with at least two other anti-HIV drugs.

Mechanism Of Action
Saquinavir inhibits the HIV viral proteinase enzyme which prevents cleavage of the gag-pol polyprotein, resulting in noninfectious, immature viral particles.

Drug Category
Anti-HIV Agents; Anti-HIV Agents; ATC:J05AE01

Brand Names/Synonyms
Fortovase; Invirase; ROC; SAQUINAVIR; SQV; Saquinavir; Saquinavir Mesylate; Saquinavir [Usan]

Dosage Forms
INVIRASE (saquinavir mesylate) capsules and FORTOVASE (saquinavir) soft gelatin capsules

Absorption
Absolute bioavailability of saquinavir administered as INVIRASE averaged 4%

Interactions