Overview
| Generic Names: | SQV; Saquinavir Mesylate; saquinavir |
|---|---|
| Trade Names: | Fortovase; Invirase; ROC |
| PharmGKB Accession Id: | PA451305 |
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 (source: Drug Bank)
Indication
For the treatment of HIV-1 with advanced immunodeficiency together with antiretroviral nucleoside analogues. (source: Drug Bank)
ATC Therapeutic Category
- J05AE:Protease inhibitors
Pharmacology, Interactions, and Contraindications
Mechanism Of Action
Saquinavir inhibits the HIV viral proteinase enzyme which prevents cleavage of the gag-pol polyprotein, resulting in noninfectious, immature viral particles. (source: Drug Bank)
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. (source: Drug Bank)
Food Interactions
Take after a full meal. (source: Drug Bank)
Absorption, Distribution, Metabolism, Elimination & Toxicity
Biotransformation
Hepatic (source: Drug Bank)
Protein Binding
98% (source: Drug Bank)
Absorption
Absolute bioavailability averages 4% (source: Drug Bank)
Toxicity
Probably experience pain in the throat (source: Drug Bank)
Isomeric SMILES Code:
CC(C)(C)NC(=O)[C@@H]1C[C@H]2CCCC[C@@H]2CN1C[C@H]([C@H](CC3=CC=CC=C3)NC(=O)[C@H](CC(=O)N)NC(=O)C4=NC5=CC=CC=C5C=C4)O (source: Drug Bank)
The following genes are in curated knowledge about this drug.
| Gene | Relationship | Evidence | |
|---|---|---|---|
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ABCB1 |
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Publications |
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CYP2D6 |
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Publications |
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CYP3A5 |
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Publications |
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NR1I2 |
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Publications |
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SLCO1A2 |
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Publications |
A list of non-curated publications that mention this drug along with other genes is available.
Drug Targets
| Gene | Description | |
|---|---|---|
| ABCB1 |
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(source: Drug Bank) |
| ABCC1 |
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(source: Drug Bank) |
| ABCC2 |
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(source: Drug Bank) |
| ABCG2 |
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(source: Drug Bank) |
| ALB |
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(source: Drug Bank) |
| TNF |
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(source: Drug Bank) |
The following drugs are in curated knowledge about this drug.
| Drug | Relationship | Evidence | |
|---|---|---|---|
|
|
tamoxifen |
|
Publications |
|
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warfarin |
|
Publications |
A list of non-curated publications that mention this drug along with other drugs is available.
Curated Information
The following diseases are in curated knowledge about this drug.
| Disease | Relationship | Evidence | |
|---|---|---|---|
|
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HIV |
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Publications |
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HIV Infections |
|
Publications |
Non-Curated Information
A list of non-curated publications that mention this drug along with other diseases is available.
Curated Phenotype Datasets
These datasets are sorted alphabetically by title.
Additional Datasets
These datasets are minimally curated and are sorted alphabetically by title.
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LinkOuts
Common Searches
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Non-Curated Publications
A list of non-curated publications that mention this drug is available.