Darunavir Stands Up as Preferred HIV Protease Inhibitor

作者：Mallolas Josep^*

来源：AIDS Reviews, 2017, 19(2): 105-112.

• Darunavir
• Drug resistance
• Cobicistat
• Coformulations
• Dual therapy
• Universal antiretroviral regimens

Current antiretroviral therapy reaches and maintains viral suppression over the years in more than 90% of treated HIV-infected individuals. Although integrase inhibitors are the preferred third agent in antiretroviral therapy in the current guidelines, rilpivirine, a non-nucleoside reverse transcriptase inhibitor, and darunavir (DRV), a second-generation protease inhibitor, are the preferred third companion to be used along with a backbone of two nucleos(t) ide reverse transcriptase inhibitors as first-line triple HIV combination treatment. However, rilpivirine is not recommended in patients with plasma HIV-RNA above 100,000 copies/mL. Raltegravir requires uncomfortably twice daily dosing, whereas dolutegravir is often given as coformulation with abacavir, a drug that requires prior HLA-B5701 testing. Antiretroviral combinations based on DRV provide a unique robustness in terms of antiviral potency and resistance barrier, rendering this drug pivotal as part of rescue regimens for the treatment failures. Furthermore, dual antiretroviral therapy with DRV plus lamivudine has been tested with success as maintenance therapy. Finally, DRV has demonstrated its safety and efficacy in special patient populations, including pregnant women, pediatrics, HIV-2 infection, and individuals coinfected with viral hepatitis. Single-tablet regimens containing DRV coformulated with cobicistat alone or with other antiretrovirals should improve drug adherence. These fixed-dose combinations represent a step forward universal antiretroviral regimen, ensuring maximal efficacy, tolerability, and convenience.

• 出版日期2017-6