Your browser doesn't support javascript.
loading
[Nirmatrelvir plus ritonavir (Paxlovid) a potent SARS-CoV-2 3CLpro protease inhibitor combination]. / Nirmatrelvir más ritonavir (Paxlovid) una potente combinación inhibidora de la proteasa 3CLpro del SARS-CoV-2.
Reina, J; Iglesias, C.
Afiliação
  • Reina J; Jordi Reina, Unidad de Virología, Servicio de Microbiología, Hospital Universitario Son Espases, Facultad de Medicina (UIB). Carretera Valldemossa 79, 07120 Palma de Mallorca. Spain. jorge.reina@ssib.es.
Rev Esp Quimioter ; 35(3): 236-240, 2022 Jun.
Article em Es | MEDLINE | ID: mdl-35183067
ABSTRACT
All coronavirus, including SARS-CoV-2, encode two proteases needed for the processing of PP1A and PP1AB polyproteins. The main protease 3CL (chemotripsine-like) gives rise to the formation of NSP11/16 proteins. The 3CL protease has been constituted as one of the possible therapeutic targets for the development of antiviral drugs against SARS-COV-2 due to its highly conserved sequence and structure among all coronaviruses. During the SARS-COV-1 pandemic, a hydroxymethyl ketone derivative (PF-00835231) was identified with an intense inhibitory activity against the 3CL protease. Subsequent chemical modifications gave rise to derivative PF-07321332 (nirmatrelvir) which has shown a high antiviral efficacy against SARS-COV-2. The company's data indicate that it is capable of reducing 89% the risk of hospitalization and death of patients infected with hardly adverse effects. Its effectiveness improves if it is administered orally in the first 24-48 hours and the duration of treatment has been established between 3-5 days. The commercial form has been associated with the antiviral ritonavir that has shown the metabolism of nirmatrelvir, lengthening its average life. This antiviral would be effective against current and future viral variants, since 3CL is not modified in them. The FDA approved this antiviral in November 2021 and EMA is in the final evaluation phase.
Assuntos
Palavras-chave

Texto completo: 1 Coleções: 01-internacional Contexto em Saúde: 4_TD Base de dados: MEDLINE Assunto principal: SARS-CoV-2 / Tratamento Farmacológico da COVID-19 Limite: Humans Idioma: Es Revista: Rev Esp Quimioter Ano de publicação: 2022 Tipo de documento: Article

Texto completo: 1 Coleções: 01-internacional Contexto em Saúde: 4_TD Base de dados: MEDLINE Assunto principal: SARS-CoV-2 / Tratamento Farmacológico da COVID-19 Limite: Humans Idioma: Es Revista: Rev Esp Quimioter Ano de publicação: 2022 Tipo de documento: Article