GY48LS6

Феърфилд
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Дарунавир (Darunavir)
Международное непатентованное наименование Дарунавир (Darunavir)
Торговое наименование Prezcobix, Prezista, Дарунавир, Кемерувир
Производитель, страна Johnson & Johnson, USA; Фармасинтез, Россия; Биокад, Россия; Канонфарма, Россия; ИРВИН 2, Россия и др.
Лекарственная форма таблетки, покрытые пленочной оболочкой, 800 mg
Механизм действия

Darunavir is a nonpeptidic inhibitor of protease (PR) that lodges itself in the active site of PR through a number of hydrogen bonds. It was developed to increase interactions with HIV-1 protease and to be more resistant against HIV-1 protease mutations. With a Kd (dissociation constant) of 4.5 x 10−12 M, darunavir has a much stronger interaction with PR and its dissociation constant is 1/100 to 1/1000 of other protease inhibitors. 

Опыт использования

FDA-approved since 2015, approved to treat HIV-1 infection.

Публикации COVID-19

Suyash PantMeenakshi Singh, et al. Peptide-like and Small-Molecule Inhibitors Against Covid-19. J Biomol Struct Dyn. 2020 Apr 20;1-15. DOI: 10.1080/07391102.2020.1757510.

 

Costanzo M, De Giglio MAR, Roviello GN. SARS CoV-2: Recent Reports on Antiviral Therapies Based on Lopinavir/Ritonavir, Darunavir/Umifenovir, Hydroxychloroquine, Remdesivir, Favipiravir and Other Drugs for the Treatment of the New Coronavirus. Curr Med Chem. 2020 Apr 16. doi: 10.2174/0929867327666200416131117. PMID: 32297571.

D ZanonA Manca, et al. Data on the Stability of Darunavir/Cobicistat Suspension After Tablet Manipulation. Data Brief. 2020 Apr 12;105552. DOI: 10.1016/j.dib.2020.105552.
Клинические исследования
1.
Название протокола A 6 Week Prospective, Open Label, Randomized, in Multicenter Study of, Oseltamivir Plus Hydroxychloroquine Versus Lopipinavir/ Ritonavir Plus Oseltamivir Versus Darunavir/ Ritonavir Plus Oseltamivir Plus Hydroxychloroquine in Mild COVID-19 AND Lopipinavir/ Ritonavir Plus Oseltamivir Versus Favipiravir Plus Lopipinavir / Ritonavir Versus Darunavir/ Ritonavir Plus Oseltamivir Plus Hydroxychloroquine Versus Favipiravir Plus Darunavir and Ritonavir Plus Hydroxychloroquine in Moderate to Critically Ill COVID-19
Дата начала и окончания КИ April 15, 2020 - November 30, 2020
Название организации, проводящей КИ Rajavithi Hospital
Страны Thailand
Фаза III
Кол-во пациентов 320
2.
Название протокола Treatment of Non-severe Confirmed Cases of COVID-19 and Chemoprophylaxis of Their Contacts as Prevention Strategy: a Cluster Randomized Clinical Trial (PEP CoV-2 Study)
Дата начала и окончания КИ March 18, 2020 - June 15, 2020
Название организации, проводящей КИ Germans Trias i Pujol Hospital
Страны Spain
Фаза III
Кол-во пациентов 3040
3.
Название протокола A randomised, open, controlled trial for darunavir/cobicistat or Lopinavir/ritonavir combined with thymosin a1 in the treatment of novel coronavirus pneumonia (COVID-19)
Дата начала и окончания КИ February 1, 2020 - December 1, 2020
Название организации, проводящей КИ Zhongnan Hospital of Wuhan University
Страны China
Фаза -
Кол-во пациентов 100
4.
Название протокола Efficacy and Safety of Darunavir and Cobicistat for Treatment of COVID-19
Дата начала и окончания КИ January 30, 2020 - December 31, 2020
Название организации, проводящей КИ Shanghai Public Health Clinical Center
Страны China
Фаза III
Кол-во пациентов 30