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QuickView for Saquinavir (compound)


PubChem
Name: Saquinavir
PubChem Compound ID: 10604536
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.
Molecular formula: C38H50N6O5
Molecular weight: 674.866 g/mol
DrugBank
Identification
Name: Saquinavir
Name (isomeric): DB01232
Drug Type: small molecule
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.
Synonyms:
SQV; Saquinavir Mesylate
Brand: Invirase, ROC, Fortovase
Category: HIV Protease Inhibitors, Anti-HIV Agents
CAS number: 127779-20-8
Pharmacology
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 ...
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Mechanism of Action: Saquinavir inhibits the HIV viral proteinase enzyme which prevents cleavage of the gag-pol polyprotein, resulting in noninfectious, immature viral particles.
Absorption: Absolute bioavailability averages 4%
Protein binding: 98%
Biotransformation: Hepatic
Route of 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.
Clearance: 1.14 L/h/kg [Healthy volunteers receiving IV doses of 6, 36, and 72 mg]
Toxicity: Probably experience pain in the throat
Affected organisms: Human Immunodeficiency Virus
Interactions
Food interaction:
Take after a full meal.
Drug interaction:
ErlotinibThis CYP3A4 inhibitor increases levels/toxicity of erlotinib
DihydroergotamineThe protease inhibitor, saquinavir, may increase the effect and toxicity of the ergot derivative, dihydroergotamine.
TemsirolimusSaquinavir may inhibit the metabolism and clearance of Temsirolimus. Concomitant therapy should be avoided.
EfavirenzEfavirenz decreases the effect of saquinavir
TadalafilSaquinavir may reduce the metabolism of Tadalafil. Concomitant therapy should be avoided if possible due to high risk of Tadalafil toxicity.
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