Name: | Saquinavir |
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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 |
Name: | Saquinavir |
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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
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Brand: | Invirase, ROC, Fortovase |
Category: | HIV Protease Inhibitors, Anti-HIV Agents |
CAS number: | 127779-20-8 |
Indication: | For the treatment of HIV-1 with advanced immunodeficiency together with antiretroviral nucleoside analogues. |
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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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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.
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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 |
Food interaction: |
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Drug interaction: |
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UniProt ID: | O90777 | |||||||
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Gene: | HIV-1 protease | |||||||
Actions: | inhibitor | |||||||
References: |
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UniProt ID: | P24462 | |
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Gene: | CYP3A7 | |
Actions: | substrate, inhibitor | |
References: |
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UniProt ID: | P20815 | ||
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Gene: | CYP3A5 | ||
Actions: | substrate, inhibitor | ||
References: |
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UniProt ID: | P08684 | ||||
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Gene: | CYP3A4 | ||||
Actions: | substrate, inhibitor | ||||
References: |
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UniProt ID: | P05108 | |
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Gene: | CYP11A1 | |
Actions: | substrate | |
References: |
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UniProt ID: | P33261 | |
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Gene: | CYP2C19 | |
Actions: | inhibitor | |
References: |
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UniProt ID: | P10632 | |
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Gene: | CYP2C8 | |
Actions: | inhibitor | |
References: |
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UniProt ID: | P11712 | |
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Gene: | CYP2C9 | |
Actions: | inhibitor | |
References: |
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UniProt ID: | P10635 | |
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Gene: | CYP2D6 | |
Actions: | substrate, inhibitor | |
References: |
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UniProt ID: | P08183 | ||||||||
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Gene: | ABCB1 | ||||||||
Actions: | substrate, inhibitor, inducer | ||||||||
References: |
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UniProt ID: | O15245 | |
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Gene: | SLC22A1 | |
Actions: | inhibitor | |
References: |
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UniProt ID: | P46721 | |
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Gene: | SLCO1A2 | |
Actions: | inhibitor | |
References: |
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UniProt ID: | Q9UNQ0 | ||
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Gene: | ABCG2 | ||
Actions: | inhibitor | ||
References: |
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UniProt ID: | Q9Y6L6 | |
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Gene: | SLCO1B1 | |
Actions: | inhibitor | |
References: |
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UniProt ID: | P33527 | |
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Gene: | ABCC1 | |
Actions: | substrate | |
References: |
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UniProt ID: | Q92887 | ||||
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Gene: | ABCC2 | ||||
Actions: | substrate | ||||
References: |
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UniProt ID: | P02763 | |
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Gene: | ORM1 | |
References: |
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UniProt ID: | P02768 | |
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Gene: | ALB | |
References: |
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