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New studies of Arbidol are being published all over the world. There is a need to get the information online for current reference. Studies will posted as they become available. Some of the new data will still be in the original language of publication like Russian, Chinese, German and other languages. The timeliness of current research out weights the need to translate before posting.

Please request studies you want translated first.

New Arbidol Studies:

Curr Pharm Des. 2009;15(11):1238-47. English publication .pdf

Synthetic and natural immunomodulators acting as interferon inducers.

Silin DS, Lyubomska OV, Ershov FI, Frolov VM, Kutsyna GA.

Laboratory of Molecular Virology, Medical and Biology Center, School of Biomedical Sciences, Queen's University Belfast, 97 Lisburn Road, Belfast, BT9 7BL, UK.

Interferons are first immunomodulatory molecules that have been shown to display a wide range of applications due to their antiviral, antibacterial, antitumor, and inflammatory activities. Natural and recombinant interferons are among most common biologic therapeutics worldwide. Interferon inducers, however, are less known and have been mostly developed and used in former socialist countries. Despite the fact that they are virtually unknown to the Western world, they represent a substantial market share of modern pharmacopoeia in former socialist republics. This review provides a brief description of most popular interferon inducers including Amyxin, Amizon, Anandin, Arbidol, Blasten, Cycloferon, Galavit, Groprinosine, Hepon, Immunoxel, Dzherelo, Kagocel, Larifan, Ligfol, Likopid, Mebavin, MIGI-KLP, V-5 Immunitor, SCV-07, Milife, Neovir, Poludan, Ragocin, Ridostin, Thymogen and Savratz, some of which were in use for several decades for the same clinical indications as for interferons. The variety and choice offered by the pharmaceutical industry behind the former "iron curtain" certainly deserves the appreciation, familiarity and application prospects for medical and research investigators worldwide.

Antiviral Res. 2009 Feb;81(2):132-40. Epub 2008 Nov 24. English publication .pdf

Characteristics of arbidol-resistant mutants of influenza virus: implications for the mechanism of anti-influenza action of arbidol.

Leneva IA, Russell RJ, Boriskin YS, Hay AJ.

The antiviral drug arbidol (ARB), which is licensed in Russia for use against influenza, is known to inhibit early membrane fusion events in influenza A and B virus replication. To investigate in more detail the target and mechanism of ARB action we generated and studied the characteristics of ARB-resistant influenza virus mutants. Observations of the ARB susceptibility of reassortants between A/Singapore/1/57(H2N2) and A/chicken/Germany/27(H7N7, "Weybridge" strain) and of mutants of the latter virus identified the virus haemagglutinin (HA) as the major determinant of ARB sensitivity. ARB-resistant mutants, selected from the most sensitive reassortant, possessed single amino acid substitutions in the HA2 subunit which caused an increase in the pH of fusion and the associated conformational change in HA. ARB was shown to stabilize the HA by causing a 0.2 pH unit reduction in the pH of the transition to the low pH form, which was specifically abrogated by the resistance mutations. Some of the resistance mutations, which reduce acid stability and would disrupt ARB-HA interactions, are located in the vicinity of a potential ARB binding site identified using the docking programme Gold. Together, the results of these investigations indicate that ARB falls within a class of inhibitor which interacts with HA to stabilize it against the low pH transition to its fusogenic state and consequently inhibit HA-mediated membrane fusion during influenza virus infection.

Antibiot Khimioter. 2008;53(7-8):27-30. Russian publication (not available at this time)

Therapeutic efficacy of Ingavirin, a new domestic formulation against influenza A virus (H3N2)

Loginova SIa, Borisevich SV, Maksimov VA, Bondarev VP, Nebol'sin VE.

Investigation of the therapeutic efficacy of Ingavirin (Valenta Farmacevtica, Russia) against influenza virus A (H3N2) vs. Tamiflu, Remantadin and Arbidol showed that in daily doses of 15 and 20 mg/kg (equal by the efficacy to the human doses of 90 and 120 mg) Ingavirin was effective in protection of the albino mice infected by the virus in a dose of 10 to 15 LD50. The protective efficacy was 38.3-39.2% and the increase of the average lifespan amounted to 4.2-4.4 days. The Ingavirin efficacy was comparable with that of Remantadine, markedly exceeded that of Arbidol and was lower than that of Tamiflu. Investigation of the Ingavirin influence in doses of 15 and 20 mg/kg on the dynamics and level of the influenza virus A/Aichi/2/68 reproduction in the lungs of the infected albino mice weighing 10-12 g revealed that during the whole observation period in the doses tested Ingavirin was effective in inhibition of the influenza virus reproduction. During the whole period of the observation (5 days) Ingavirin was effective in inhibiting the formation of the virus specific hemagglutinin in the target organ.

Ter Arkh. 2009;81(3):51-4. Russian publication .pdf

Efficacy of ingavirin in adults with influenza

Kolobukhina LV, Merkulova LN, Shchelkanov MIu, Burtseva EI, Isaeva EI, Malyshev NA, L'vov DK.

AIM: To compare therapeutic efficacy and safety of ingavirin and arbidol in patients with influenza. MATERIAL AND METHODS: The trial included 105 patients with a verified diagnosis of influenza, definite clinical symptoms, body temperature at least 38 degrees C and duration of the disease 36 hours maximum. Ingavirin efficacy was analysed basing on the evidence for 100 patients with uncomplicated influenza. The patients were randomized into three groups: taking ingavirin in a single daily dose 90 mg (n = 33), placebo (n = 36) or arbidol (200 mg 4 times a day). The duration of the treatment was 5 days. RESULTS: Intake of ingavirin in initial 24-36 hours of the disease significantly reduced fever compared to placebo and arbidol (34.5, 72.0 and 48.4 hours, respectively). Ingavirin was less toxic and had no side effects.

CONCLUSION: Ingavirin is safe and effective in the treatment of influenza. By some criteria it is more effective than arbidol.

Clinical Therapeutics/Volume 31, Number 4, 2009 English publication .pdf

Pharmacokinetic Properties and Bioequivalence of Two Formulations of Arbidol: An Open-Label, Single-Dose, Randomized-Sequence, Two-Period Crossover Study in Healthy Chinese Male Volunteers

Ming-Yan Liu, MD; Shuang Wang, MD; Wei-Fan Yao; Hui-zhe Wu, MD; Sheng-Nan Meng, MD, PhD; and Min-Jie Wei, MD, PhD

ABSTRACT: Background: Arbidol is an antiviral drug indicated for the prevention and treatment of all types of influenza infection and some other kinds of acute respiratory infections, specifically against influenza groups A and B, and severe acute respiratory syndrome. It is used to help prevent influenza infection as long as necessary with little risk for influenza mutation rendering it less effective.

Arch Virol (2009) 154:601–607 DOI 10.1007/s00705-009-0346-4 English publication .pdf

Antiviral activity of Arbidol against Coxsackie virus B5 in vitro and in vivo

Qiong Zhong, Zhanqiu Yang, Yuanyuan Liu, Haiying Deng, Hong Xiao, Liqiao Shi, Jing He

Abstract We investigated the antiviral activity of Arbidol, an antiviral chemical compound, against Coxsackie virus B5 (CVB5) in vitro and in vivo. Arbidol not only prevented the cytopathic effect (CPE) of CVB5, as demonstrated in an MTT colorimetric assay, when added during or after viral infection, with a 50% inhibitory concentration (IC50) from 2.66 to 6.62 lg/ml, but it also decreased the CVB5-RNA level in infected host cells, as shown in semi-quantitative RT-PCR. BALB/c mice were used as an animal model to test the Arbidol activity in vivo. Orally administered Arbidol at 50 mg/kg body weight/day (once a day) significantly reduced mean virus yields in the lungs and heart as well as mortality after infection for 6 days. Our results demonstrate that in vitro and in vivo infection with CVB5 can be effectively treated by Arbidol.

Acta Pharmacologica Sinica (2009) 30: 1015–1024; doi: 10.1038/aps.2009.53; published online 8 June 2009 English publication .pdf

Efficacy of arbidol on lethal hantaan virus infections in suckling mice and in vitro

Hai-ying DENG1, 2, Fan LUO1, Li-qiao SHI 1, Qiong ZHONG1, Ying-juan LIU 1, Zhan-qiu YANG1,*

Aim: Arbidol is an immunomodulator that was first developed in Russia. In this study, we report the antiviral activity of arbidol against Hantaan virus (HTNV) in vitro and in vivo.

Methods: The antiviral activity of arbidol in vitro was determined by plaque-forming assay, ranging from 0.5 to 8 µg/mL. To investigate whether arbidol has an antiviral effect in vivo, suckling BALB/c mice infected with HTNV were treated with arbidol at 24 h before infection with a 5, 10 or 20 mg·kg-1·d-1, once per day, for 10 days. On day 12 and 28 post infection (pi), histopathological changes and viral antigen were detected. On days 4, 8, 12, and 16 pi, the viral load of target organs and serum TNF-a levels of arbidol-treated animals were determined.

Results: Arbidol was found to have potent inhibitory activity against HTNV when added in vitro before or after viral infection, with a 50% inhibitory concentration (IC50) of 0.9 and 1.2 µg/mL, respectively. The 50% lethal dose (LD50) of arbidol for suckling mice was 78.42 mg·kg-1·d-1. Oral administration of arbidol increased both survival rate and mean time to death (MTD). Treatment with arbidol reduced histopathological changes, decreased viral load and viral antigen levels, and modulated the level of serum TNF-a.

Conclusion: Arbidol has the ability to elicit protective antiviral activity against HTNV in vivo and in vitro.

J. Mass Spectrom. 2008; 43: 1099–1109 Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 646 Songtao Road, Shanghai 201203, China English publication .pdf

Metabolite identification of arbidol in human urine by the study of CID fragmentation pathways using HPLC coupled with ion trap mass spectrometry

Yuya Wang, Xiaoyan Chen, Qiang Li and Dafang Zhong*

The metabolism of arbidol in humans was studied using liquid chromatography-electrospray ionization (ESI) ion trap mass spectrometry (ITMS) after an oral dose of 300-mg arbidol. A total of 17 metabolites were identified including the glucuronide arbidol and the glucuronide sulfinylarbidol as the major metabolites.

Vopr Virusol. 2008 Jan-Feb;53(1):31-3 (Russian publication .pdf) English translation not available at this time

Evaluation of the efficacy of wiferon and arbidol in adult influenza

Kolobukhina LV, Malinovskaia VV, Gatich RZ, Merkulova LN, Burtseva EI, Isaeva EI, Parshina OV, Guseva TS, Orlova TG, Voronina FV

The therapeutic efficacy of wiferon (recombinant alpha2beta-interferon) versus arbidol was studied in a double-blind controlled study in patients with laboratorily verified influenza. Within the first 24-36 hours after the onset of the disease, wiferon and arbidol reduced the duration of fever, intoxication, and the catarrhal symptoms of the disease as a whole. The agents were shown to have an immunomodulating effect.

Original Russian Document .pdf

Institute of Virology, Moscow, Russia; 2Chemical and Pharmaceutical Institute, Moscow, Russia; 3IBCP; CNRS, UMR 5086; Université Lyon 1; IFR 128, Lyon, France; 4 Department of Laboratory Medicine, University of Washington, School of Medicine, Seattle, USA English publication .pdf

Arbidol: A Broad-Spectrum Antiviral Compound that Blocks Viral Fusion

Y.S. Boriskin, I. A. Leneva, E.-I. Pécheur and S. J. Polyak*

Arbidol (ARB; ethyl-6-bromo-4-[(dimethylamino)methyl]-5-hydroxy-1-methyl-2-[(phenylthio)methyl]-indole-3-carboxylate hydrochloride monohydrate), is a Russian-made potent broad-spectrum antiviral with demonstrated activity against a number of enveloped and non-enveloped viruses. ARB is well known in Russia and China, although to a lesser extent in western countries. Unlike other broad-spectrum antivirals, ARB has an established molecular mechanism of action against influenza A and B viruses, which is different from that of available influenza antivirals, and a more recently established mechanism of inhibition of hepatitis C virus (HCV). For both viral infections the anti-viral mechanism involves ARB inhibition of virus-mediated fusion with target membrane and a resulting block of virus entry into target cells. However, ARB inhibition of fusion exploits different ARB modalities in case of influenza viruses or HCV. This review aims to summarize the available evidence of ARB effects against different groups of viruses, also, to compare various aspects of ARB anti-fusion mechanisms against influenza virus and HCV (with reference to different stringency of pH-dependence of these two viral fusogens) and to discuss further prospects for ARB and its improved derivatives of the parent compounds.

State Key Laboratory of Virology, Institute of Medical Virology, Wuhan University, Wuhan, P.R. China English publication .pdf

Antiviral activity of arbidol against influenza A virus, respiratory syncytial virus, rhinovirus, coxsackie virus and adenovirus in vitro and in vivo

Shi L, Xiong H, He J, Deng H, Li Q, Zhong Q, Hou W, Cheng L, Xiao H, Yang Z.

Arbidol, ethyl-6-bromo-4-[(dimethylamino)-methyl] -5-hydroxy-1-methyl-2- [(phenylthio)methyl]- in dole-3-carboxylate hydrochloride monohydrate, is an antiviral chemical agent. In this report, we studied the antiviral activity of arbidol against a panel of human respiratory viruses, namely influenza A virus (FLU-A, A/PR/8/34 H1N1), respiratory syncytial virus (RSV), human rhinovirus type 14 (HRV 14), coxsackie virus B3 (CVB3) and adenovirus type 7 (AdV-7) in vitro in cell culture. Arbidol was found to present potent inhibitory activity against enveloped and non-enveloped RNA viruses, including FLU-A, RSV, HRV 14 and CVB3 when added before, during, or after viral infection, with 50% inhibitory concentration (IC(50)) ranging from 2.7 to 13.8 microg/ml. However, arbidol showed selective antiviral activity against AdV-7, a DNA virus, only when added after infection (therapeutic index (TI) = 5.5). Orally administered arbidol at 50 or 100 mg/kg/day beginning 24 h pre-virus exposure for 6 days significantly reduced mean pulmonary virus yields and the rate of mortality in mice infected with FLU-A (A/PR/8/34 H1N1).

Our results suggest that arbidol has the ability to elicit protective broad-spectrum antiviral activity against a number of human pathogenic respiratory viruses.

Volprosy Virusologii Volume: 51 Issue: 5 2006 Pages 4-7 English translation not available at this time

Rimantadine and arbidol sensitivity of influenza viruses that caused epidemic morbidity rise in Russia in the 2004-2005 season

The study of the activity of arbidol against epidemic influenza A and B virus strains (2002-2005) in the cultured MDCK cells showed the higher sensitivity of enzyme immunoassay than that of hemagglutination test. The influenza A virus strains tested, including those resistant to rimantadine (5 microg/ml), were sensitive to arbidol (10 microg/ml). The population of influenza B virus strains was heterogeneous in this indicator, 43% of the strains being less sensitive to arbidol. There was an increase in the number of rimantadine-resistant influenza A(H3N2) virus strains (10-18%) in our country during 3 epidemic seasons. The sequencing analysis of protein M2-endoding gene revealed the amino acid replacement of serine by asparagine in position 31, which is characteristic of rimantadine-resistant strains. Arbidol in combination with rimantadine potentiated the effect of viral reproduction in the cultured cells, as compared with the effect produced by the same concentrations of the drugs used alone.

Original Russian Document .pdf

Health UA 10 4 2006 English (professional translation .pdf)

Specific Molecular-Biological Actions of the Antiviral Drug Arbidol

Arbidol is an antiviral drug which is effective against Group A and B influenza strains. The molecular-biological action which distinguishes Arbidol from other drugs is its ability to inhibit viral reproduction in the early stages; the drug acts by changing the regulation of cell metabolism. Arbidol differs from rimantadine in the molecular mechanism of its antiviral action.

Original Russian Document .pdf

Volprosy Virusologii Volume: 51 Issue: 5 2006 Pages 4-7 English translation not available at this time

Antiviral Etiotropic efficacy against Influenza A subtype H5N1

N.A. Leneva, A. M. Shuster

The paper analyzes data of an experimental study of the efficacy of antiviral agents (amantadine, rementadine, ozeltamivir, zanamivir, arbidol, ribavirin) in the cultured cells and on a model of murine influenza pneumonia against influenza A viruses subtype H5N1. It also gives data on their use in the treatment of human beings during avian influenza outbreak. The mechanism of action of the agents, pharmacokinetics, adverse reactions, and their potential resistance are considered.

Original Russian Document .pdf

Journal of Pharmaceutical and Biomedical Analysis Vol. 43, No. 1, pages 371-375 (2007) English translation not available at this time

Determination of arbidol in human plasma by LC-ESI-MS

Liu, X., Huang, Y.W., Li, J., Li, X.B., Bi, K.S., Chen, X.H.

Abstract: A sensitive, specific and accurate method for determination of arbidol in human plasma was developed. Arbidol and internal standard were extracted from plasma samples by liquid-liquid extraction with diethyl ether. The chromatographic separation was accomplished on a Shiseido C"1"8 3@mm analytical column (100mmx2.0mm i.d.) at a flow rate of 0.3mL/min isocratically. Detection was performed on a single quadrupole mass spectrometer by selected ion monitoring (SIM) mode via electrospray ionization (ESI) source. The method had a chromatographic run time of 6min and a good linear relationship over the range 1-1000ng/mL. The limit of quantitation for arbidol in plasma was 1ng/mL. The intra-day and inter-day precision (R.S.D.%) was lower than 7% and accuracy ranged from 95 to 105%. The proposed method enables unambiguous identification and quantification of arbidol in vivo and has been successfully applied to study the pharmacokinetics of arbidol in healthy male Chinese volunteers.

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