Literature DB >> 28664942

Darunavir Stands Up as Preferred HIV Protease Inhibitor.

Josep Mallolas1.   

Abstract

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 transcrip- tase 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 lami- vudine 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.

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Year:  2017        PMID: 28664942

Source DB:  PubMed          Journal:  AIDS Rev        ISSN: 1139-6121            Impact factor:   2.500


  7 in total

1.  Molecular design of near-infrared (NIR) fluorescent probes targeting exopeptidase and application for detection of dipeptidyl peptidase 4 (DPP-4) activity.

Authors:  Yuki Hoshino; Kenjiro Hanaoka; Kei Sakamoto; Masahiro Yasunaga; Takashi Kojima; Daisuke Kotani; Ayumu Nomoto; Eita Sasaki; Toru Komatsu; Tasuku Ueno; Hiroyuki Takamaru; Yutaka Saito; Yasuyuki Seto; Yasuteru Urano
Journal:  RSC Chem Biol       Date:  2022-03-24

2.  Synthesis and Characterization of Long-Acting Darunavir Prodrugs.

Authors:  Mary G Banoub; Aditya N Bade; Zhiyi Lin; Denise Cobb; Nagsen Gautam; Bhagya Laxmi Dyavar Shetty; Melinda Wojtkiewicz; Yazen Alnouti; JoEllyn McMillan; Howard E Gendelman; Benson Edagwa
Journal:  Mol Pharm       Date:  2019-12-03       Impact factor: 4.939

Review 3.  Advances and challenges in the prevention and treatment of COVID-19.

Authors:  Yan-Jie Han; Zhi-Guang Ren; Xin-Xin Li; Ji-Liang Yan; Chun-Yan Ma; Dong-Dong Wu; Xin-Ying Ji
Journal:  Int J Med Sci       Date:  2020-07-09       Impact factor: 3.738

4.  Patient-Reported Outcomes in an Observational Cohort of HIV-1-Infected Adults on Darunavir/Cobicistat-Based Regimens: Beyond Viral Suppression.

Authors:  Andrea Antinori; Maria V Cossu; Barbara Menzaghi; Gaetana Sterrantino; Nicola Squillace; Valentina Di Cristo; Annamaria Cattelan; Emanuele Focà; Antonella Castagna; Giancarlo Orofino; Daniela Valenti; Gabriella D'Ettore; Lucia Aprea; Sergio Ferrara; Maria E Locatelli; Giordano Madeddu; Emanuele Pontali; Paolo Scerbo; Barbara Rossetti; Alessia Uglietti; Roberta Termini; Francesco Rucci; Andrea Gori; Daniela Mancusi
Journal:  Patient       Date:  2020-06       Impact factor: 3.883

5.  Single-Agent and Fixed-Dose Combination HIV-1 Protease Inhibitor Drugs in Fission Yeast (Schizosaccharomyces pombe).

Authors:  Jiantao Zhang; Kasey Vernon; Qi Li; Zsigmond Benko; Anthony Amoroso; Mohamed Nasr; Richard Y Zhao
Journal:  Pathogens       Date:  2021-06-24

Review 6.  Apples to Apples? A Comparison of Real-World Tolerability of Antiretrovirals in Patients with Human Immunodeficiency Virus Infection and Patients with Primary Biliary Cholangitis.

Authors:  Shannon L Turvey; Lynora Saxinger; Andrew L Mason
Journal:  Viruses       Date:  2022-03-03       Impact factor: 5.048

7.  Predicted antiviral drugs Darunavir, Amprenavir, Rimantadine and Saquinavir can potentially bind to neutralize SARS-CoV-2 conserved proteins.

Authors:  Umesh C Halder
Journal:  J Biol Res (Thessalon)       Date:  2021-08-04       Impact factor: 1.889

  7 in total

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