Saquinavir: From HIV to COVID-19 and Cancer Treatment

Biomolecules. 2022 Jul 5;12(7):944. doi: 10.3390/biom12070944.

Abstract

Saquinavir was the first protease inhibitor developed for HIV therapy, and it changed the standard of treatment for this disease to a combination of drugs that ultimately led to increased survival of this otherwise deadly condition. Inhibiting the HIV protease impedes the virus from maturing and replicating. With this in mind, since the start of the COVID-19 outbreak, the research for already approved drugs (mainly antivirals) to repurpose for treatment of this disease has increased. Among the drugs tested, saquinavir showed promise in silico and in vitro in the inhibition of the SARS-CoV-2 main protease (3CLpro). Another field for saquinavir repurposing has been in anticancer treatment, in which it has shown effects in vitro and in vivo in several types of cancer, from Kaposi carcinoma to neuroblastoma, demonstrating cytotoxicity, apoptosis, inhibition of cell invasion, and improvement of radiosensibility of cancer cells. Despite the lack of follow-up in clinical trials for cancer use, there has been a renewed interest in this drug recently due to COVID-19, which shows similar pharmacological pathways and has developed superior in silico models that can be translated to oncologic research. This could help further testing and future approval of saquinavir repurposing for cancer treatment.

Keywords: COVID-19; HIV; cancer; drug repurposing; saquinavir.

Publication types

  • Review
  • Research Support, Non-U.S. Gov't

MeSH terms

  • COVID-19 Drug Treatment*
  • HIV Infections* / drug therapy
  • HIV Protease Inhibitors* / pharmacology
  • HIV Protease Inhibitors* / therapeutic use
  • Humans
  • Neoplasms* / drug therapy
  • SARS-CoV-2
  • Saquinavir / pharmacology
  • Saquinavir / therapeutic use

Substances

  • HIV Protease Inhibitors
  • Saquinavir

Grants and funding

This work was financed by FEDER—Fundo Europeu de Desenvolvimento Regional through the COMPETE 2020—Operational Programme for Competitiveness and Internationalization (POCI), Portugal 2020, and by Portuguese funds through FCT—Fundação para a Ciência e a Tecnologia, in a framework of the project in CINTESIS, R&D Unit (reference UIDB/4255/2020) and within the scope of the project “RISE—LA/P/0053/2020. Nuno Vale also thanks support from FCT and FEDER (European Union), award number IF/00092/2014/CP1255/CT0004 and CHAIR in Onco-Innovation at FMUP.