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Darunavir

In the Treatment of HIV-1 Infection

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Abstract

  • ▲ Darunavir (TMC114) is a nonpeptidic peptidomimetic HIV protease inhibitor (PI), with a high binding affinity and a close fit within the substrate envelope.

  • ▲ Darunavir shows potent in vitro activity against a broad range of clinical isolates of HIV type 1 (HIV-1), including those with decreased susceptibility to most available PIs.

  • ▲ The bioavailability of oral darunavir is increased when it is coadministered with ritonavir. Thus, darunavir must be administered in combination with low-dose (100mg) ritonavir.

  • ▲ In the POWER 1 and POWER 2 trials, two 144-week randomised phase IIb trials, a reduction in plasma HIV-1 RNA levels of ≥1 log 10 copies/mL (primary endpoint) occurred in 77% and 62% of treatment-experienced recipients of darunavir plus ritonavir (darunavir/ritonavir) 600mg/100mg twice daily (in combination with an optimised background regimen) [vs 25% and 14% of control PI (CPI) recipients; p < 0.001] at week 24. Results are from primary analyses (n = 301 and 201).

  • ▲ In a pooled subgroup analysis of data from the POWER 1 and 2 trials, reductions in HIV-1 RNA levels of ≥1 log 10 copies/mL were achieved in 61% of patients treated with darunavir/ritonavir 600mg/ 100mg twice daily versus 15% of CPI recipients (p < 0.0001) at week 48.

  • ▲ Darunavir/ritonavir 600mg/100mg was generally well tolerated in the POWER 1 and 2 trials, with a tolerability profile similar to that of comparator CPIs.

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Notes

  1. The use of trade names is for product identification purposes only and does not imply endorsement.

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Acknowledgements and Disclosure

The manuscript was reviewed by: M. Holodniy, AIDS Research Center, Department of Medicine, Stanford University, Palo Alto, California, USA; R. Sherer, International AIDS Training Center, Department of Medicine, University of Chicago, Chicago, Illinois, USA.

The preparation of this review was not supported by any external funding. During the peer review process, the manufacturer of the agent under review was also offered an opportunity to comment on this article. Changes resulting from comments received were made on the basis of scientific and editorial merit.

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  1. Wolters Kluwer Health ¦ Adis, 41 Centorian Drive, Private Bag 65901, Mairangi Bay, North Shore 0754, Auckland, New Zealand

    Caroline Fenton & Caroline M. Perry

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  1. Caroline Fenton
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  2. Caroline M. Perry
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Correspondence to Caroline M. Perry.

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Fenton, C., Perry, C.M. Darunavir. Drugs 67, 2791–2801 (2007). https://doi.org/10.2165/00003495-200767180-00010

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