Details
Stereochemistry | ACHIRAL |
Molecular Formula | C21H17Cl3O3 |
Molecular Weight | 423.717 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
COC1=CC=C(OCC2=CC=C(COC3=C(Cl)C=CC=C3Cl)C=C2)C(Cl)=C1
InChI
InChIKey=XXMDDBVNWRWNCW-UHFFFAOYSA-N
InChI=1S/C21H17Cl3O3/c1-25-16-9-10-20(19(24)11-16)26-12-14-5-7-15(8-6-14)13-27-21-17(22)3-2-4-18(21)23/h2-11H,12-13H2,1H3
Pocapavir is a capsid-binding molecule. It is a capsid inhibitor that blocks virus uncoating and viral RNA release into cells, which in turn prevents virus replication. Pocapavir is a potent, selective, anti-enterovirus molecule with in vitro and in vivo activities. Antiviral testing against viruses of the 15 most commonly isolated enterovirus serotypes indicates that pocapavir inhibits 80% of the immunotypes (154 viruses) at a concentration that is within the levels of the molecule achievable in plasma after oral dosing in higher animals. Persistent low viral load after therapy completion may indicate lack of antiviral effect from pocapavir for neonatal enteroviral sepsis treatment. Pocapavir had been in phase II clinical trial for the treatment of poliomyelitis but no recent reports on development were identified.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: CHEMBL5127 Sources: https://www.ncbi.nlm.nih.gov/pubmed/9174174 |
88.5 nM [Ki] |
PubMed
Title | Date | PubMed |
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Structure of poliovirus type 2 Lansing complexed with antiviral agent SCH48973: comparison of the structural and biological properties of three poliovirus serotypes. | 1997 Jul 15 |
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SCH 48973: a potent, broad-spectrum, antienterovirus compound. | 1997 Jun |
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In vitro antiviral activity of V-073 against polioviruses. | 2009 Oct |
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Immunological and pathogenic properties of poliovirus variants selected for resistance to antiviral drug V-073. | 2011 |
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Immunogenicity of inactivated polio vaccine with concurrent antiviral V-073 administration in mice. | 2011 Aug |
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Towards the design of combination therapy for the treatment of enterovirus infections. | 2011 Jun |
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Combating enterovirus replication: state-of-the-art on antiviral research. | 2012 Jan 15 |
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Characterization of poliovirus variants selected for resistance to the antiviral compound V-073. | 2012 Nov |
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Anti-poliovirus activity of protease inhibitor AG-7404, and assessment of in vitro activity in combination with antiviral capsid inhibitor compounds. | 2013 May |
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Highlights in antiviral drug research: antivirals at the horizon. | 2013 Nov |
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Human monoclonal antibodies that neutralize vaccine and wild-type poliovirus strains. | 2014 Aug |
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The enteroviruses: problems in need of treatments. | 2014 Jan |
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Progress in the development of poliovirus antiviral agents and their essential role in reducing risks that threaten eradication. | 2014 Nov 1 |
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H1PVAT is a novel and potent early-stage inhibitor of poliovirus replication that targets VP1. | 2014 Oct |
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First use of investigational antiviral drug pocapavir (v-073) for treating neonatal enteroviral sepsis. | 2015 Jan |
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Enteroviruses in X-Linked Agammaglobulinemia: Update on Epidemiology and Therapy. | 2016 Nov-Dec |
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Completing Polio Eradication: The Case for Antiviral Drugs. | 2017 Feb 1 |
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Antiviral Activity of Pocapavir in a Randomized, Blinded, Placebo-Controlled Human Oral Poliovirus Vaccine Challenge Model. | 2017 Feb 1 |
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Neonatal Enterovirus Myocarditis With Severe Dystrophic Calcification: Novel Treatment With Pocapavir. | 2017 Jul-Sep |
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Neonatal nonpolio enterovirus and parechovirus infections. | 2018 Apr |
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Successful treatment of fulminant neonatal enteroviral myocarditis in monochorionic diamniotic twins with cardiopulmonary support, intravenous immunoglobulin and pocapavir. | 2018 May 18 |
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Classification Tree | Code System | Code | ||
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EU-Orphan Drug |
EU/3/12/1021
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FDA ORPHAN DRUG |
357811
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NCI_THESAURUS |
C281
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9602
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C132145
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100000181867
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1455
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4ILA3VOV97
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146949-21-5
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DTXSID00163548
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ACTIVE MOIETY