Latest research on Darunavir

Darunavir is a protease inhibitor used to treat HIV. It acts on the HIV aspartyl protease which the virus needs to cleave the HIV polyprotein into its functional fragments.

Latest findings

The phase III clinical trials POWER 1 (Performance of TMC114/r When evaluated in treatment-Experienced patients with PI Resistance) and POWER 2 randomized highly treatment-experienced patients to ritonavir-boosted Darunavir plus OB (Darunavir/r + OB) or a comparator PI plus OB (cPI) (Clotet et al 2007). [source, 2008]
Because tipranavir and Darunavir were licensed only in June 2005 and 2006, respectively, these drugs were not available at all time points of the study, so resistance or susceptibility to these drugs was not considered. [source, 2008]
Recent developed drugs such as etravirine, raltegravir, maraviroc, Darunavir, tipranavir and enfuvirtide will improve the outcome of a significant number of patients. [source, 2008]
A similar comparative trial design has been used successfully for the pivotal trials showing superiority of the last four antiretroviral drugs approved in the United States (enfuvirtide, tipranavir, Darunavir, and maraviroc) [27,28]. [source, 2007]
Finally, the lower-left part of the figure contains a cluster with seven of the 11 mutations recently reported to be associated with phenotypic and clinical resistance to the newest PI, Darunavir (V32I, L33F, I47V, I50V, I54L/M, and L76V). [source, 2007]
This new cluster of mutations is associated with decreased susceptibility to all PIs, including the salvage therapy PIs Amprenavir and Lopinavir and the recently approved PI Darunavir. [source, 2007]
Although none of the sequences in this study were from patients who received Darunavir, this drug is highly similar to Amprenavir and is affected by the same PI-resistance mutations. [source, 2007]
In the more advanced treatment population on the other hand, several other new protease inhibitors such as Darunavir (TMC-114) (so far only licensed in the US) and brecanavir will become available soon, which are currently in phase II-III of development with encouraging in vitro data showing good susceptibility as well as results from first clinical trials demonstrating good virological efficacy against PI-resistant HIV strains (King et al 2004; Koh et al 2003; Katlama et al 2005; Wilkin et al 2005). [source, 2007]
Indeed, in the POWER-1 trial in patients who were enfurvirtide-naive and received Darunavir in combination with enfurvirtide 63% of patients achieved less than 50 copies/ml at week 24 (n = 19) highlighting the antiretroviral potency of the new compound. [source, 2007]
However, no studies have yet directly compared TMC-114 or brecanavir to tipranavir. [source, 2007]