Drug Groups

approved; investigational

Description

An HIV protease inhibitor which acts as an analog of an HIV protease cleavage site. It is a highly specific inhibitor of HIV-1 and HIV-2 proteases. [PubChem]

Indication

For the treatment of 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.

Toxicity

Probably experience pain in the throat

Affected Organisms

Biotransformation

Hepatic

Absorption

Absolute bioavailability averages 4%

Protein Binding

98%

Elimination

In vitro studies using human liver microsomes have shown that the metabolism of saquinavir is cytochrome P450 mediated with the specific isoenzyme, CYP3A4, responsible for more than 90% of the hepatic metabolism. Only 1% of saquinavir is excreted in the urine, so the impact of renal impairment on saquinavir elimination should be minimal.

Distribution

* 700 L

Clearance

* 1.14 L/h/kg [Healthy volunteers receiving IV doses of 6, 36, and 72 mg]

References

External Links