Group 1:

Saquinavir

History of saquinavir
 Was developed by the pharmaceutical company Roche. Saquinavir was the
first protease inhibitor (and sixth antiretroviral) approved by the Food and
Drug Administration (FDA). Within 2 years of its approval, and that of
ritonavir 4 months later, annual deaths from AIDS in the United States fell
from over 50,000 to approximately 18,000.
 HIV protease inhibitors were first invented between 1989 and 1994 by
researchers working for the pharmaceutical companies of Hoffmann- La
Roche Inc. (of Nutley, New Jersey), Abbott Laboratories and Merck & Co.,
Inc. HIV protease inhibitors are used in the treatment of patients with AIDS
and were considered the first breakthrough in over a decade of AIDS
research. HIV protease inhibitors can lower the viral load carried by AIDS
patents.
Mechanism of action:
 Saquinavir is a protease inhibitor. Proteases are enzymes that cleave protein
molecules into smaller fragments. HIV protease is vital for both viral
replication within the cell and release of mature viral particles from an
infected cell.
 Saquinavir binds to the active site of the viral protease and prevents cleavage
of viral polyproteins, preventing maturation of the virus. Saquinavir inhibits
both HIV-1 and HIV-2 proteases.
 Treating HIV infection. Saquinavir must be taken along with ritonavir.
 Saquinavir is a protease inhibitor. It works by blocking the growth of HIV.
 Saquinavir is used together with other medications to treat or prevent
HIV/AIDS. Typically it is used with ritonavir or lopinavir/ritonavir to
increase its effect.

Dosage for HIV Infection

 1000 mg (with ritonavir 100 mg) PO q12hr, or in combination with

ritonavir-enhanced lopinavir

Side effects:

 The most frequent adverse events with saquinavir in either formulation are:
 Mild gastrointestinal symptoms, including diarrhea, nausea, loose
stools & abdominal discomfort. Invirase is better tolerated than
Fortovase.

Availability

 Saquinavir is licensed in Canada for the treatment of HIV infection in

adults, in combination with other anti-HIV drugs.