Arbidol (umifenovir) / Pharmstandard - LARVOL DELTA

Strategic Design and Optimization of Umifenovir Analogues: Balancing Antiviral Efficacy and hERG Toxicity against SARS-CoV-2. (PubMed, J Med Chem) - "C3 modifications led to lead compounds 77, 79, and 81 (IC50 = 0.67-0.7 μM), achieving superior potency while eliminating hERG toxicity. Mechanism of entry inhibition and immunofluorescence confirmed compound 77 significantly reduced SARS-CoV-2 within Vero cells, supporting their preclinical potential."

Journal • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases

Design, Synthesis and Anti-Influenza Virus Activity of 4-Tert-Butyl-N-(3-Oxo-1-Thia-4-Azaspiro[4.5]Dec-4-yl)Benzamide Derivatives That Target Hemagglutinin-Mediated Fusion. (PubMed, Drug Dev Res) - "Computer-aided docking was performed to predict the possible binding pocket in the H3 HA trimer. Resistance data and in silico studies indicated that compound 2c has an overlapping binding pocket in the stem region of H3 HA with the known fusion inhibitors TBHQ and arbidol."

Journal • Infectious Disease • Influenza • Respiratory Diseases

Antiviral Medications for Treatment of Nonsevere Influenza: A Systematic Review and Network Meta-Analysis. (PubMed, JAMA Intern Med) - "All antiviral drugs (no data for peramivir and amantadine) had little or no effect on hospital admission for low-risk patients (high certainty)...For time to alleviation of symptoms, baloxavir probably reduced symptom duration (mean difference [MD], -1.02 days; 95% CI, -1.41 to -0.63; moderate certainty); umifenovir may have reduced symptom duration (MD, -1.10 days; 95% CI, -1.57 to -0.63; low certainty); oseltamivir probably had no important effect (MD, -0.75 days; 95% CI, -0.93 to -0.57; moderate certainty)...This systematic review and meta-analysis found that baloxavir probably reduced risk of hospital admission for high-risk patients and may reduce time to alleviation of symptoms, without increasing adverse events related to treatment in patients with nonsevere influenza. All other antiviral drugs either probably have little or no effect, or uncertain effects on patient-important outcomes."

Clinical • Journal • Retrospective data • Critical care • Infectious Disease • Influenza • Respiratory Diseases

A Glimpse for the subsistence from pandemic SARS-CoV-2 infection. (PubMed, Bioorg Chem) - "Although some drug regimens and vaccines have shown safety in trials, none have been entirely successful yet. This review highlights, some of the potential antibodies (tocilizumab, Sarilumab, Avdoralimab, Lenzilumab, Interferon (alfa /beta /gamma)) screened against SARS-CoV-2 and the most promising drugs (Favipiravir, Hydroxychloroquine, Niclosamide, Ribavirin, Baricitinib, Remdesivir, Arbidol Losartan, Ritonavir, Lopinavir, Baloxavir, Nitazoxanide, Camostat) in various stages of development with their synthetic protocol and their clinical projects are discussed to counter COVID -19."

Journal • Review • Cardiovascular • Gastrointestinal Disorder • Infectious Disease • Nephrology • Novel Coronavirus Disease • Pneumonia • Respiratory Diseases

CYCL-NTTF-2023: Study of Safety and Efficacy of the Drug Cycloferone in Patients with Acute Respiratory Viral Infection (clinicaltrials.gov) - P=N/A | N=742 | Completed | Sponsor: POLYSAN Scientific & Technological Pharmaceutical Company | Active, not recruiting ➔ Completed

Trial completion • Infectious Disease

Recent report on indoles as a privileged anti-viral scaffold in drug discovery. (PubMed, Eur J Med Chem) - "Indole-containing drugs, such as enfuvirtide (T-20), arbidol, and delavirdine, have demonstrated significant efficacy in treating viral diseases. The review includes discussions on synthetic protocols, inhibitory concentrations, SAR study, and computational study. This review shall identify new antiviral indoles that may help to combat new viral threats in the future."

Journal • Review • Dengue Fever • Ebola Virus Disease • Hepatology • Human Immunodeficiency Virus • Infectious Disease • Inflammation • Influenza • Novel Coronavirus Disease • Respiratory Diseases

Dominance of Dengue Virus Serotype-2 in Pakistan (2023-2024): Molecular Characterization of the Envelope Gene and Exploration of Antiviral Targets. (PubMed, Virus Res) - "Computational modeling of the envelope protein structure identified potential antiviral binding sites and further molecular docking studies suggested that specific antiviral compounds like Arbidol and Quercetin can inhibit early steps in viral infection. Additionally, BepiPred-3.0 predicted several B-cell epitopes, which could be useful for vaccine development. These findings enhance our understanding of dengue epidemiology in Pakistan and contribute to the development of targeted antiviral therapies, potentially informing future vaccination strategies and outbreak management."

Journal • Dengue Fever • Hematological Disorders • Infectious Disease

A fast solid-phase microextraction scheme for in vivo monitoring of bio-accumulation and bio-transformation of arbidol in living plants. (PubMed, Sci Total Environ) - "Additionally, the plant root secretion was found to be significantly altered by arbidol exposure. To summarized, the combination of in vivo SPME and the FT-ICR-MS analysis provide new and important information regarding arbidol contamination and related alternation of plant root metabolism."

Journal • Preclinical • Infectious Disease • Influenza • Novel Coronavirus Disease • Respiratory Diseases

PREGNANCY OUTCOMES IN THE ETRASIMOD CLINICAL PROGRAMME (UEGW 2024) - "Pregnancy outcomes during the etrasimod clinical development programmeFoetal deathCongenital malformationSpontaneous abortionHealthy newbornMedical terminationLost to follow-upMaternalexposure, n (%)(N = 9)01 (11.1)a1 (11.1)2 (22.2)b4 (44.4)c,d,e1 (11.1)fPaternalexposure, n (%)(N = 5)002 (40.0)2 (40.0)01 (20.0)Data on pregnancy events and outcomes were taken from the Pfizer internal data warehouse on serious adverse events that included pregnancy.aPremature 34-week delivery due to premature rupture of membranes, open (patent) foramen ovale (heart) with circulatory failure and transient tachypnoea of the newborn, which were all considered non-serious concomitant events.bBoth patients had full-term birth, caesarean delivery.cReasons for medical termination were not known in two cases.dOne patient with an anembryonic gestation where umifenovir (received for a respiratory tract infection) was a co-suspected drug. Few pregnancies have been reported in the etrasimod clinical..."

Clinical • Alopecia • Atopic Dermatitis • Crohn's disease • Dermatitis • Dermatology • Eosinophilic Esophagitis • Gastroenterology • Gastrointestinal Disorder • Infectious Disease • Inflammatory Bowel Disease • Long-acting Reversible Contraceptives • Respiratory Diseases • Ulcerative Colitis

Comparative assessment of the clinical effectiveness of direct-acting antiviral drugs in outpatient patients with acute respiratory viral infections (PubMed, Ter Arkh) - "The use of direct antiviral drugs contributes to the rapid relief of ARVI symptoms in patients receiving medical care on an outpatient basis. The antiviral drug riamilovir showed the most pronounced effectiveness (clinical and laboratory)."

Clinical • Journal • Cough • Gene Therapies • Infectious Disease • Inflammation • Pain • Respiratory Diseases

An Inhalable Nanoshield for Effective Prevention of Influenza Virus Infections. (PubMed, ACS Nano) - "Here, we developed a triple-protective nanoshield against IV infection in the lungs, formed by self-assembling DSPE-PEG amphiphilic polymers encapsulating the flu-preventive antiviral drug Arbidol internally. The preventive effect of the nanoshield against virus infection includes increasing the viscosity in the surrounding environment to physically defend against viral entry, forming a hydrated layer to block the interaction between viruses and cells, and inhibiting virus replication. Our finding suggested that a single inhalation of the nanoshield provides effective protection against IV infection for at least 8 h. Thus, this nanoshield may be a potential pandemic protection agent against IV, especially in viral environments, where no prophylactic or therapeutic measures are available."

Journal • Infectious Disease • Influenza • Respiratory Diseases

Transport and retention of COVID-19-related antiviral drugs in saturated porous media under various hydrochemical conditions. (PubMed, Ecotoxicol Environ Saf) - "Results showed that the mobility of the drugs was primarily contingent on their hydrophobicity, with ribavirin and favipiravir exhibiting the highest transportability, while arbidol displaying the greatest retention. Ribavirin and remdesivir warrant particular attention due to their relatively high transportability and propensity for environmentally acquired antiviral resistance. These findings contribute to an enhanced understanding of the leachate potential and transport of COVID-19-related antivirals in sandy porous media, furnishing fundamental data for predicting their environmental fate and associated risks."

Journal • Infectious Disease • Novel Coronavirus Disease

Preclinical and Clinical Investigations of Potential Drugs and Vaccines for COVID-19 Therapy: A Comprehensive Review With Recent Update. (PubMed, Clin Pathol) - "Among the repurposed drugs, remdesivir is considered as the most promising agent, while favipiravir, molnupiravir, paxlovid, and lopinavir/ritonavir exhibited improved therapeutic effects in terms of elimination of viruses. However, the outcomes of treatment with oseltamivir, umifenovir, disulfiram, teicoplanin, and ivermectin were not significant...Tocilizumab is presently employed for the treatment of patients who exhibit COVID-19-related pneumonia. Numerous antiviral drugs such as galidesivir, griffithsin, and thapsigargin are under clinical trials which could be promising for treating COVID-19 individuals with severe symptoms. Supportive treatment for patients of COVID-19 may involve the use of corticosteroids, convalescent plasma, stem cells, pooled antibodies, vitamins, and natural substances. This study provides an updated progress in SARS-CoV-2 medications and a crucial guide for inventing novel interventions against COVID-19."

Journal • Preclinical • Review • Infectious Disease • Novel Coronavirus Disease • Pneumonia • Respiratory Diseases

Arbidol, an antiviral drug, identified as a sodium channel blocker with anticonvulsant activity. (PubMed, Br J Pharmacol) - "Arbidol shows promising potential as an anticonvulsant agent, providing a unique mode of action that sets it apart from existing SCBs."

Journal • Anesthesia • CNS Disorders • Epilepsy • NAV1

Efficacy and Safety of Arbidol in the Treatment of Allergic Rhinitis (clinicaltrials.gov) - P=N/A | N=15 | Not yet recruiting | Sponsor: Zheng Liu

New trial • Allergic Rhinitis • Immunology • Inflammation

QSPR/QSAR study of antiviral drugs modeled as multigraphs by using TI's and MLR method to treat COVID-19 disease. (PubMed, Sci Rep) - "The aim of the study is to employ M-polynomial, neighborhood M-polynomial approach and QSPR/QSAR analysis to evaluate specific antiviral drugs including Lopinavir, Ritonavir, Arbidol, Thalidomide, Chloroquine, Hydroxychloroquine, Theaflavin and Remdesivir. The primary objective is to showcase the valuable contribution of multigraphs to QSPR and QSAR analyses, offering crucial insights into molecular structures and antiviral properties. The integration of physicochemical applications enhances our understanding of factors influencing antiviral drug efficacy, essential for combating emerging viral strains effectively."

Journal • Infectious Disease • Novel Coronavirus Disease

Research Progress on Spike-Dependent SARS-CoV-2 Fusion Inhibitors and Small Molecules Targeting the S2 Subunit of Spike. (PubMed, Viruses) - "While most substitutions to the Spike protein to date in variants of concern (VOCs) have been localized to the S1 subunit, the S2 subunit sequence is more conserved, with only a few observed substitutions in proximity to S2 binding sites. Several recent small molecules targeting S2 have been shown to have robust activity over recent VOC mutant strains and/or greater broad-spectrum antiviral activity for other more distantly related coronaviruses."

Journal • Review • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases

Toxic mechanisms of the antiviral drug arbidol on microalgae in algal bloom water at transcriptomic level. (PubMed, J Hazard Mater) - "Moreover, the down-regulation of genes related to nucleotide metabolism and DNA replication might influence the reproduction of algae. These findings provided effective strategies to elucidate toxic mechanisms of contaminants on algae in algal bloom water."

Journal

The Dual-Targeted Fusion Inhibitor Clofazimine Binds to the S2 Segment of the SARS-CoV-2 Spike Protein. (PubMed, Viruses) - "Clofazimine and Arbidol have both been reported to be effective in vitro SARS-CoV-2 fusion inhibitors. Results related to molecular docking and modeling of the structure-activity relationship (SAR) of a newly reported series of Clofazimine derivatives support the proposed Clofazimine binding site on the S2 segment. When the proposed Clofazimine binding site is superimposed with other experimentally determined coronavirus structures in structure-sequence alignments, the changes in sequence and structure may rationalize the broad-spectrum antiviral activity of Clofazimine in closely related coronaviruses such as SARS-CoV, MERS, hCoV-229E, and hCoV-OC43."

Journal • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases

Study of Safety and Efficacy of the Drug Cycloferone in Patients With Acute Respiratory Viral Infection (clinicaltrials.gov) - P=N/A | N=742 | Active, not recruiting | Sponsor: POLYSAN Scientific & Technological Pharmaceutical Company

New trial • Infectious Disease

Red recombination enables a wide variety of markerless manipulation of porcine epidemic diarrhea virus genome to generate recombinant virus. (PubMed, Front Cell Infect Microbiol) - "Among the three drugs, Bergenin, Umifenovir hydrochloride (Arbidol), and Ganoderma lucidum triterpenoids (GLTs), we found that GLTs inhibited PEDV replication mainly after the stage of virus "Entry". Overall, this study will broaden insight into the method for manipulating the PEDV genome and provide a powerful tool for screening anti-PEDV agents."

Journal • Preclinical • Infectious Disease • Novel Coronavirus Disease

Favipiravir for treating COVID-19. (PubMed, Cochrane Database Syst Rev) - "The low- to very low-certainty evidence means that we do not know whether favipiravir is efficacious in people with COVID-19 illness, irrespective of severity or admission status. Treatment with favipiravir may result in an overall increase in the incidence of adverse events but may not result in serious adverse events."

Journal • Review • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases

Arbidol attenuates liver fibrosis and activation of hepatic stellate cells by blocking TGF-β1 signaling. (PubMed, Eur J Pharmacol) - "We further demonstrate that ARB mitigated Smad2/3 phosphorylation in both activated HSCs and BDL mice. These data together demonstrate that the therapeutic efficacy of ARB on liver fibrosis is independent of its antiviral activity and likely is achieved by blocking TGF-β1 signaling-mediated HSC activation."

Journal • Fibrosis • Hepatology • Immunology • Infectious Disease • Influenza • Liver Cirrhosis • Liver Failure • Novel Coronavirus Disease • Respiratory Diseases • MMP9 • TGFB1 • TGFBR2

Comparative efficacy and safety of anti-infective drugs for patients with mild to severe COVID-19: A systematic review and network meta-analysis of randomized controlled trials. (PubMed, Ethiop Med J) - "For clinical recovery at 14 days Ivermectin (OR= 3.00, 95%CI: [1.82; 4.96]; p < 0.0001; moderate certainty evidence), Baricitinib plus Remdesivir (OR= 2.20, 95%CI: [1.35; 3.53]; p = 0.005; low certainty evidence), and Favipiravir (OR= 2.16, 95%CI: [1.27; 3.68]; p = 0.004; moderate certainty evidence) were statistically effective than standard of care...Arbidol (RR= 0.46, 95% CI: [0.23; 0.95]; p = 0.04) was statistically safe drug than standard of care. This Network Meta-analysis suggests that Baricitinib plus Remdesivir is more effective than the other anti-infective drugs in treating patients with COVID-19 in terms of clinical recovery at 14 days, mortality and adverse events outcomes."

Journal • Retrospective data • Review • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases

The environmental risks of antiviral drug arbidol in eutrophic lake: Interactions with Microcystis aeruginosa. (PubMed, J Hazard Mater) - "Interestingly, the toxicity of arbidol was reduced after algal biodegradation, and most of the degradation products exhibited lower toxicity than arbidol. This study revealed the environmental risks and transformation behavior of arbidol in algal bloom waters."

Journal