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Fact Sheet

Protease Inhibitors in Development

April 4, 2011


NOTE: Several fact sheets describe drugs that are being tested against HIV:

These drugs have not been approved by the Food and Drug Administration (FDA) for use against HIV.

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Protease Inhibitors

These drugs block the protease enzyme. When new viral particles break off from an infected cell, protease cuts long protein strands into the parts needed to assemble a mature virus. When protease is blocked, the new viral particles cannot mature.


Protease Inhibitors in Development

Several firms are trying to develop a new type of protease inhibitor that will not be cross-resistant with existing drugs. Another goal is to not require boosting by ritonavir.

CTP-518 by GlaxoSmithKline is a new molecule that replaces some hydrogen molecules of atazanavir with deuterium, a related substance. Deuterium is metabolized more slowly than hydrogen. CTP-518 may maintain beneficial blood levels in humans without a booster. It is in Phase I trials.

TMC310911 by Tibotec Therapeutics is a new protease inhibitor in Phase II trials. It is boosted with ritonavir.


PIs No Longer in Development

The following drugs are no longer being developed for use against HIV:

Brecanavir (GW640385) by GlaxoSmithKline and Vertex

L-756,423 by Merck

Mozenavir (DMP450) by Triangle Pharmaceuticals

PPL-100 (MK8122) by Ambrilla/Procyon Biopharma

RO033-4649 by Roche

SP1256 by Sequoia Pharmaceuticals




  
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This article was provided by AIDS InfoNet. Visit AIDS InfoNet's website to find out more about their activities and publications.
 
See Also
More on HIV Medications
More on Protease Inhibitors
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