brecanavir

Description: Brecanavir is a novel, tyrosyl-based arylsulfonamide-based protease inhibitor (PI) for the treatment of human immunodeficiency virus type-1. It potently inhibited HIV-1 in cell culture assays with 50% effective concentrations (EC(50)s) of 0.2 to 0.53 nM and was equally active against HIV strains utilizing either the CXCR4 or CCR5 coreceptor, as was found with other PIs. Brecanavir had a< 5-fold increase in EC(50)s against 80% of patient isolates tested and had a greater mean in vitro potency than amprenavir, indinavir, lopinavir, atazanavir, tipranavir, and darunavir. Brecanavir is by a substantial margin the most potent and broadly active antiviral agent among the PIs tested in vitro.

References: Velthuisen EJ, Baughman TM, Johns BA, Temelkoff DP, Weatherhead JG. Synthesis and pharmacokinetic profile of highly deuterated brecanavir analogs. Eur J Med Chem. 2013 May; 63:202-12. doi: 10.1016/j.ejmech.2013.02.001. Epub 2013 Feb 14. PubMed PMID: 23474906.