| Item |
Information |
|
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 |
| • |
Human Immunodeficiency Virus |
|
| 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 |
| • |
Forestier F, de Renty P, Peytavin G, Dohin E, Farinotti R, Mandelbrot L: Maternal-fetal transfer of saquinavir studied in the ex vivo placental perfusion model. Am J Obstet Gynecol. 2001 Jul;185(1):178-81.
[Pubmed]
|
|
| External Links |
|