Lopinavir/ritonavir: Repurposing an old drug for HIV infection in COVID-19 treatment

Magro, Paola; Zanella, Isabella; Pescarolo, Marta; Castelli, Francesco; Quiros-Roldan, Eugenia

doi:10.1016/j.bj.2020.11.005

Cited by 53 publications

(37 citation statements)

References 68 publications

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“…Currently, it is the only antiviral medication approved for COVID-19 [ 7 ]. Early during the COVID-19 pandemic, lopinavir/ritonavir, an old drug used for human immunodeficiency virus (HIV) treatment, was also extensively used as a potential therapy against the new virus [ 8 ]. Lopinavir is a type 1 aspartate protease inhibitor with in vitro and in vivo activity against SARS-CoV and in an animal model against MERS-CoV [ 9 ]; however, after the first wave of COVID-19 it was soon abandoned due to its lack of effectiveness in clinical trials [ 10 , 11 , 12 ].…”

Section: Introductionmentioning

confidence: 99%

“…Generally, immunocompromised patients are more susceptible to bacterial, fungal, viral, and parasitic infections than healthy persons due to their inability to mount successful immune responses. For these reasons, at the beginning of pandemic, HIV-infected patients, who constitute 0.5% of the world population [ 13 ] were considered as high risk for severe COVID-19 [ 14 , 15 ], and if their antiviral therapy could be shifted to lopinavir without decreasing efficacy against HIV infection, it was done during the first wave [ 8 , 15 , 16 , 17 ]. Today, lopinavir is no longer used for COVID-19 treatment outside of clinical trials [ 18 ].…”

Section: Introductionmentioning

confidence: 99%

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Tenofovir, Another Inexpensive, Well-Known and Widely Available Old Drug Repurposed for SARS-COV-2 Infection

et al. 2021

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Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) infection is spreading worldwide with different clinical manifestations. Age and comorbidities may explain severity in critical cases and people living with human immunodeficiency virus (HIV) might be at particularly high risk for severe progression. Nonetheless, current data, although sometimes contradictory, do not confirm higher morbidity, risk of more severe COVID-19 or higher mortality in HIV-infected people with complete access to antiretroviral therapy (ART). A possible protective role of ART has been hypothesized to explain these observations. Anti-viral drugs used to treat HIV infection have been repurposed for COVID-19 treatment; this is also based on previous studies on severe acute respiratory syndrome virus (SARS-CoV) and Middle East respiratory syndrome virus (MERS-CoV). Among them, lopinavir/ritonavir, an inhibitor of viral protease, was extensively used early in the pandemic but it was soon abandoned due to lack of effectiveness in clinical trials. However, remdesivir, a nucleotide analog that acts as reverse-transcriptase inhibitor, which was tested early during the pandemic because of its wide range of antiviral activity against several RNA viruses and its safety profile, is currently the only antiviral medication approved for COVID-19. Tenofovir, another nucleotide analog used extensively for HIV treatment and pre-exposure prophylaxis (PrEP), has also been hypothesized as effective in COVID-19. No data on tenofovir’s efficacy in coronavirus infections other than COVID-19 are currently available, although information relating to SARS-CoV-2 infection is starting to come out. Here, we review the currently available evidence on tenofovir’s efficacy against SARS-CoV-2.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Tenofovir, Another Inexpensive, Well-Known and Widely Available Old Drug Repurposed for SARS-COV-2 Infection

et al. 2021

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“…As such, there is to respite for the research to decipher the disease mechanism, monitor its evolution, and hunt for efficient therapies. This issue of the Biomedical Journal fully focuses on the most essential facets of fighting this global threat, comprising detection methods [ 2 ], vaccine design [ 3 ], drug development [ [4] , [5] , [6] , [7] , [8] ], and model systems.…”

Section: Level Up For Culture Models - How 3d Cell Culture Models Benmentioning

confidence: 99%

“…There are two recurrent themes to the frenetic scramble for treatment of COVID-19, one of them being the attempt to repurpose known drugs and molecules in order to shorten clinical trial time and limit safety issues [ 48 ], the other one being the investigation of natural compounds for similar reasons. Several articles in this issue of the Biomedical Journal tackle these themes [ 5 , 6 , 8 ].…”

Section: Also In This Issuementioning

confidence: 99%

“…For instance, Magro et al focus on the available literature concerning the effectiveness and safety of treating COVID-19 patients with the drug Lopinavir/ritonavir (LPV/r), a combination of protease inhibitors [ 5 ]. So far, they have been used as a second line treatment upon Human Immunodeficiency Virus (HIV) infection, and showed some potential against SARS-CoV and MERS-CoV.…”

Section: Also In This Issuementioning

confidence: 99%

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Level up for culture models - How 3D cell culture models benefit SARS-CoV-2 research

Häfner¹

2021

Biomedical Journal

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Welcome to a new decade and a new issue of the Biomedical Journal - casting a sorrowful look onto a year that will go down in history as a tombstone etched by the COVID-19 pandemic, but also a hopeful glance into the future, now that multiple vaccination programs against the SARS-CoV-2 virus have started. This issue is dedicated to the continuous effort by researchers all around the globe to understand and counter the pathogen, as well as to be better prepared for future threats. Therefore, we learn about the advantages of complex 3D cell culture models for studying host-virus interactions, and the disease course of COVID-19 in children. Moreover, we discover how neutralising monoclonal antibodies and peptide-based vaccines against SARS-CoV-2 are developed, and the therapeutic potentials of lopinavir/ritonavir, mesenchymal stem cells, as well as plant and algae extracts. Finally, we ponder over the lessons to be learnt from SARS-CoV and MERS, and hear about differences between different nucleotide-based SARS-CoV-2 detection methods.

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Design, Synthesis, Biological Evaluation and Molecular Docking Studies of New Thiazolidinone Derivatives as NNRTIs and SARS‐CoV‐2 Main Protease Inhibitors

Fesatidou,

Petrou,

Geronikaki

2024

Chemistry & Biodiversity

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HIV‐1 remains a major health problem worldwide since the virus has developed drug‐resistant strains, so, the need for novel agents is urgent. The protein reverse transcriptase plays fundamental role in the viruses’ replication cycle. FDA approved Delavirdine bearing a sulfonamide moiety, while thiazolidinone has demonstrated significant anti‐HIV activity as a core heterocycle or derivative of substituted heterocycles. In this study, thirty new thiazolidinone derivatives (series A, B and C) bearing sulfonamide group were designed, synthesized and evaluated for their HIV‐1 RT inhibition activity predicted by computer program PASS taking into account the best features of available NNRTIs as well as against SARS‐COV‐2 main protease. Seven compounds showed good anti‐HIV inhibitory activity, with two of them, C1 and C2 being better (IC50 0.18 μΜ & 0.12 μΜ respectively) than the reference drug nevirapine (IC50 0.31 μΜ). The evaluation of molecules to inhibit the main protease revealed that 6 of the synthesized compounds exhibited excellent to moderate activity with two of them (B4 and B10) having better IC50 values (0.15 & 0.19 μΜ respectively) than the reference inhibitor GC376 (IC50 0.439 μΜ). The docking studies is coincides with experimental results, showing good binding mode to both enzymes.

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Lopinavir/ritonavir: Repurposing an old drug for HIV infection in COVID-19 treatment

Cited by 53 publications

References 68 publications

Tenofovir, Another Inexpensive, Well-Known and Widely Available Old Drug Repurposed for SARS-COV-2 Infection

Tenofovir, Another Inexpensive, Well-Known and Widely Available Old Drug Repurposed for SARS-COV-2 Infection

Level up for culture models - How 3D cell culture models benefit SARS-CoV-2 research

Design, Synthesis, Biological Evaluation and Molecular Docking Studies of New Thiazolidinone Derivatives as NNRTIs and SARS‐CoV‐2 Main Protease Inhibitors

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