Brecanavir

Brecanavir Uses, Dosage, Side Effects, Food Interaction and all others data.

Brecanavir (VX-385) an orally active aspartic protease inhibitor (PI), under investigation by Vertex and GlaxoSmithKline for the treatment of HIV. In July 2006, Vertex indicated that it expected GSK to initiate phase III trials of the drug in 2007. In December of 2006 GSK announced a decision to discontinue the development of brecanavir for the treatment of HIV. The decision was based on issues regarding the formulation of the drug.

Brecanavir is an orally active aspartic protease inhibitor (PI) under investigation by Vertex and GlaxoSmithKline for the treatment of HIV. Test-tube data suggest that it has activity against virus with resistance to the currently available protease inhibitors, and that it is more powerful against wild-type HIV that existing protease inhibitors, being active at concentrations much lower than most existing protease inhibitors. Unlike some other protease inhibitors, brecanavir does not have a significant interaction with the nucleotide reverse transcriptase inhibitor (NtRTI) tenofovir (Viread). In December of 2006 GlaxoSmithKline announced their decision to discontinue the development of brecanavir for the treatment of HIV. The decision was based on issues regarding the formulation of the drug.

Trade Name Brecanavir
Generic Brecanavir
Brecanavir Other Names Brecanavir
Type
Formula C33H41N3O10S2
Weight Average: 703.823
Monoisotopic: 703.223335927
Protein binding

Estimated be 97 to 98%

Groups Investigational
Therapeutic Class
Manufacturer
Available Country
Last Updated: September 19, 2023 at 7:00 am
Brecanavir
Brecanavir

Uses

For the treatment of HIV-1 infection in combination with other antiretroviral agents.

How Brecanavir works

Brecanavir inhibits the HIV viral proteinase enzyme which prevents cleavage of the gag-pol polyprotein, resulting in noninfectious, immature viral particles.

Elimination Route

Brecanavir, a CYP3A4 substrate, demonstrated low oral bioavailability in animals (0 to 30%), which increased to 60 to 100% following coadministration with oral ritonavir (a potent CYP3A inhibitor).

Innovators Monograph

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