Saquinavir (Fortovase) as an Antiviral Drug Candidate for SARS-CoV-2

Since December 2019, a new type of coronavirus (SARS-CoV-2) has begun to spread in China, triggering a large-scale virus infection. Due to the lack of effective treatment, as of early February 2020, this disease has not been effectively controlled. Obviously, the ultra-long cycle of new drug discovery cannot alleviate the current tension, so it is a pragmatic choice to find reliable virus inhibitors from some marketed drugs. Creative Biolabs can provide high-throughput screening (HTS) services to screen a number of potential drug candidates to identify effective drugs to defeat SARS-CoV-2. Based on Saquinavir, we can provide a range of testing services (in vitro and in vivo) to determine whether it can be used as a specific and potent drug candidate for SARS-CoV-2 suppression.

Pharmacodynamic Properties of Saquinavir

Saquinavir is an HIV protease inhibitor, a transition state mimetic of phenylalanine-proline (Phe-Pro) peptide bonds. It competitively inhibits HIV-1 and HIV-2 protease-mediated lysis of HIV gag and pol polyproteins. Phe-Pro proteolytic process is rare in mammalian systems, so saquinavir generally does not inhibit mammalian proteases indicating its safety for the human body.

In vitro experiments show that Saquinavir can inhibit the formation of HIV polyproteins, thereby preventing the formation of mature virus particles and reducing subsequent virus replication. In most studies, the Saquinavir concentration required to produce 50% inhibition of HIV-1 is about 2 to 7 nmol / L (about 1.5 to 5.4 μg / L). The combined use of Saquinavir with a nucleoside analogue inhibitor of HIV reverse transcriptase and / or other anti-HIV compounds can produce a synergistic inhibitory effect on HIV replication.

Molecular structure of Saquinavir. Fig.1 Molecular structure of Saquinavir.

Saquinavir Assessment and Validation Services at Creative Biolabs

The protease Mpro sequence of coronaviruses is usually very conserved. It releases a large number of functional polypeptides for virus replication through the hydrolysis of multiple proteins. In order to screen out potential protease inhibitor drugs that are effective for SARS-CoV-2, Creative Biolabs has devoted great attention to the pharmacological research and development of antiviral protease inhibitors. By analyzing the crystal structure of existing commercial drugs, we can help clients determine and evaluate whether Saquinavir has potential as an effective and specific antiviral agent against this SARS-CoV-2 outbreak.

With extensive experience in antiviral drug discovery, Creative Biolabs offers high-quality validation service of Saquinavir for the treatment of SARS-CoV-2. If you have any questions about our SARS-CoV-2 drug discovery services, you can contact us for more details.

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