Delving into the Latest Updates on Triazavirin with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Riamilovir, riamilovir sodium dihydrate

Target

SARS-CoV-2 antigen

Mechanism

SARS-CoV-2 antigen inhibitors, RNA synthesis inhibitors

Therapeutic Areas

Infectious Diseases

Active Indication

Influenza in Birds

Inactive Indication

COVID-19

Originator Organization

Russian Academy of Sciences

Active Organization

Medsintez Pharmaceutical Plant

Inactive Organization

Russian Academy of Sciences

Drug Highest PhaseApproved

First Approval Date-

Regulation-

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Structure

Molecular FormulaC5H4N6O3S

InChIKeyIDVQGNMSSHPZSJ-UHFFFAOYSA-N

CAS Registry123606-06-4

OBJECTIVEThis study aimed to explore the efficacy and safety of small-molecule antivirals for treating coronavirus disease 2019 (COVID-19).METHODSSeven databases were searched from their inception to 01 June 2023. The risk of bias in randomised controlled trials and retrospective studies was evaluated individually using the Cochrane risk-of-bias tool and Newcastle Ottawa Scale.RESULTSIn total, 160 studies involving 933 409 COVID-19 patients were evaluated. Compared with placebo or standard of care, proxalutamide demonstrated remarkable efficacy in reducing mortality rates, hospitalisation rates, serious adverse events, and the need for mechanical ventilation. Furthermore, it significantly enhanced both the rate of clinical improvement and expedited the duration of clinical recovery when compared with control groups. In patients with mild-to-moderate COVID-19, proxalutamide exhibited the above advantages, except for mortality reduction. Triazavirin was the most effective treatment for reducing the time required for viral clearance and improving the discharge rate. Leritrelvir and VV116 were ranked first in terms of enhancing the viral clearance rate on days 7 and 14, respectively. Molnupiravir was the most effective treatment for reducing the need for oxygen support. Overall, these findings remained consistent across the various subgroups.CONCLUSIONSA thorough evaluation of effectiveness, applicable to both mild-to-moderate and unstratified populations, highlights the specific advantages of proxalutamide, nirmatrelvir/ritonavir, triazavirin, azvudine, molnupiravir, and VV116 in combating COVID-19. Additional clinical data are required to confirm the efficacy and safety of simnotrelvir/ritonavir and leritrelvir. The safety profiles of these antivirals were deemed acceptable.

13 Oct 2023·Journal of Biomolecular Structure and Dynamics

Quantum chemical studies on the binding domain of SARS-CoV-2 S-protein: human ACE2 interface complex

Article

Author: Suresh, Cherumuttathu H. ; Haritha, Mambatta

A two-layer ONIOM(B3LYP/6-31G*:PM7) method is used to model the binding of several drug/drug-like molecules (L) at the SARS-CoV-2 S-protein: human ACE2 protein interface cavity. The selected molecules include a set of thirty-five ligands from the study of Smith and Smith which showed a high docking score in the range of -7.0 to -7.7 kcal/mol and another set of seven repurposing drugs, viz. favipiravir, remdesivir, EIDD, galidesivir, triazavirin, ruxolitinib, and baricitinib. The ONIOM model of the cavity (M) showed a highly polarized electron distribution along its top-to-bottom direction while Ls with lengths in the range 1.0 - 1.5 nm fitted well inside the cavity in a head-to-tail fashion to yield ML complexes. The ligands showed a large variation in the ONIOM-level binding energy (E_b), in the range -2.7 to -85.4 kcal/mol. The E_b of ML complexes better than -40.0 kcal/mol is observed for myricetin, fidarestat, protirelin, m-digallic acid, glucogallin, benserazide hydrochlorideseradie, remdesivir, tazobactum, sapropterin, nitrofurantoin, quinonoid, pyruvic acid calcium isoniazid, and aspartame, and among them the highest E_b -85.4 kcal/mol is observed for myricetin. A hydroxy substitution is suggested for the phenyl ring of aspartame to improve its binding behavior at the cavity, and the resulting ligand 43 showed the best E_b -84.5 kcal/mol. The ONIOM-level study is found to be effective for the interpretation of the noncovalent interactions resulting from residues such as arginine, histidine, tyrosine, lysine, carboxylate, and amide moieties in the active site and suggests rational design strategies for COVID-19 drug development.Communicated by Ramaswamy H. Sarma.

01 May 2022·Bulletin of Experimental Biology and Medicine

Antiplatelet Activity of Riamilovir under Conditions of Lipopolysaccharide Intoxication

Article

Author: Uskov, G M ; Spasov, A A ; Sirotenko, V S ; Kucheryavenko, A F ; Gaidukova, K A

We studied the effect of antiviral agent riamilovir on ADP-induced platelet aggregation in the absence and presence of LPS. Unlike acetylsalicylic acid (reference drug), riamilovir did not exhibit antiplatelet effect in vitro. However, it markedly suppressed platelet reactivity in LPS-treated blood samples and was 2.2-fold superior to acetylsalicylic acid in terms of IC₅₀ value. In in vivo experiments, riamilovir under conditions of hypercytokinemia blocked platelet aggregation in rats by 64%.

100 Deals associated with Triazavirin

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