What is the mechanism of saquinavir?

What is the mechanism of saquinavir?

Saquinavir is a peptide-like substrate analogue that binds to the protease active site and inhibits the activity of the enzyme. Saquinavir inhibition prevents cleavage of the viral polyproteins resulting in the formation of immature noninfectious virus particles.

What is the brand name of saquinavir?

Saquinavir (brand name: Invirase) is a prescription medicine approved by the U.S. Food and Drug Administration (FDA) for the treatment of HIV infection in people over 16 years of age. Saquinavir is always used in combination with the HIV medicine ritonavir (brand name: Norvir) and other HIV medicines.

What drug must be taken with saquinavir?

Saquinavir belongs to a class of drugs known as protease inhibitors. It must be given with ritonavir, another protease inhibitor, to increase (“boost”) the levels of saquinavir.

Is saquinavir an enzyme?

Saquinavir is an inhibitor of the HIV-1 protease enzyme. Its design is based on the “peptidomimetic” principle, wherein the molecule contains a hydroxyethylene scaffold that mimics the normal peptide linkage (cleaved by HIV protease) but which itself cannot be cleaved.

Is saquinavir a competitive or non competitive inhibitor?

Kinetic analysis for wild type and mutant protease showed mixed-type competitive-uncompetitive inhibition for darunavir and the chemically related amprenavir, while saquinavir showed competitive inhibition.

Is saquinavir a protease inhibitor?

Saquinavir is a selective, peptidomimetic HIV protease inhibitor of the hydroxyethylamine class. A soft gel capsule formulation of saquinavir has been introduced to achieve higher drug plasma concentrations and to increase its antiviral activity.

When was saquinavir discovered?

The first reports of highly selective antagonists against the HIV protease were revealed in 1987. Phase I trials of saquinavir began in 1989 and it was the first HIV protease inhibitor to be approved for prescription use in 1995. Four months later, two other protease inhibitors, ritonavir and indinavir, were approved.

Is saquinavir still used?

Saquinavir was approved for use in the United States in 1995 and is still widely used in combination with other antiretroviral agents for the prevention and treatment of HIV infection in adults and children. Saquinavir is available under the brand name Invirase in 200 mg capsules and 500 mg tablets.

How do you take saquinavir?

Saquinavir comes as a capsule and a tablet to take by mouth. It is usually taken at the same time as ritonavir (Norvir) two times a day within 2 hours after a full meal. It may be easier to remember to take saquinavir if you take it with meals. Take saquinavir at around the same times every day.

How many chiral centers does saquinavir have?

Saquinavir possesses six chiral centres resulting in 64 possible stereoisomers but only one stereoisomer is selected for the formulation intended for marketing. The synthesis of the active substance consists of a multi steps process.

How do you administer saquinavir?

When do you take saquinavir?

Is saquinavir still available?

As the demand for this protease inhibitor has decreased significantly over the past 20 years, the manufacturer of saquinavir, Hoffmann-La Roche, has announced that it will discontinue the manufacture and supply of the 200 mg capsule (the 500 mg tablet will continue to be available).