Elie Marcheteau, Estelle Mosca, Gaelle Frenois-Veyrat, Sandrine Kappler-Gratias, Laetitia Boutin, Sokunthea Top, Thomas Mathieu, Cyril Colas, Patrick Favetta, Tony Garnier, Peggy Barbe, Mathilde Keck, Daniel Gillet, Alicia Mas, Ali Alejo, Yinyi Yu, Karoly Toth, Getahun Abate, Vincent Roy, Janet Skerry, Kelly S Wetzel, Joshua D Shamblin, Joseph W Golden, Rekha G Panchal, Eric M Mucker, Rajini Mudhasani, Luigi A Agrofoglio, Frederic Iseni, Franck Gallardo
{"title":"磷酸无环核苷前药LAVR-289对痘病毒和非洲猪瘟病毒的抗病毒活性研究","authors":"Elie Marcheteau, Estelle Mosca, Gaelle Frenois-Veyrat, Sandrine Kappler-Gratias, Laetitia Boutin, Sokunthea Top, Thomas Mathieu, Cyril Colas, Patrick Favetta, Tony Garnier, Peggy Barbe, Mathilde Keck, Daniel Gillet, Alicia Mas, Ali Alejo, Yinyi Yu, Karoly Toth, Getahun Abate, Vincent Roy, Janet Skerry, Kelly S Wetzel, Joshua D Shamblin, Joseph W Golden, Rekha G Panchal, Eric M Mucker, Rajini Mudhasani, Luigi A Agrofoglio, Frederic Iseni, Franck Gallardo","doi":"10.1021/acsinfecdis.5c00169","DOIUrl":null,"url":null,"abstract":"<p><p>Poxviruses are double-stranded DNA viruses including relevant zoonotic pathogens with high morbidity and potential biological warfare threats. Although African swine fever virus belongs to the <i>Asfarviridae</i> family and is not strictly classified as a <i>Poxviridae</i> member, both fall within the same class of <i>Pokkesviricetes</i> that replicate in the cytoplasm. Among compounds targeting these viruses, acyclic nucleoside phosphonate (ANP) prodrugs are promising inhibitors of viral DNA polymerases. However, some limitations related to their toxicity and the rapid emergence of resistance highlight the need for new antiviral molecules. In this study, we tested a new ANP called LAVR-289. This product effectively inhibits viral replication by targeting a specific domain in the poxvirus DNA polymerase. Using monkeypox virus models, the subcutaneous or oral administration of LAVR-289 demonstrated protective efficacy in infected animals without toxicity. Its <i>in vivo</i> half-life, long on-the-shelf stability and broad-spectrum efficacy make LAVR-289 a promising candidate for further development and stockpiling as a medical countermeasure against dsDNA virus outbreaks. LAVR-289 can be positioned in the context of recurrent viral epidemics, bioterrorism risk, and the emergence of resistant strains in the population.</p>","PeriodicalId":17,"journal":{"name":"ACS Infectious Diseases","volume":" ","pages":"1623-1634"},"PeriodicalIF":3.8000,"publicationDate":"2025-06-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Antiviral Activity of the Acyclic Nucleoside Phosphonate Prodrug LAVR-289 against Poxviruses and African Swine Fever Virus.\",\"authors\":\"Elie Marcheteau, Estelle Mosca, Gaelle Frenois-Veyrat, Sandrine Kappler-Gratias, Laetitia Boutin, Sokunthea Top, Thomas Mathieu, Cyril Colas, Patrick Favetta, Tony Garnier, Peggy Barbe, Mathilde Keck, Daniel Gillet, Alicia Mas, Ali Alejo, Yinyi Yu, Karoly Toth, Getahun Abate, Vincent Roy, Janet Skerry, Kelly S Wetzel, Joshua D Shamblin, Joseph W Golden, Rekha G Panchal, Eric M Mucker, Rajini Mudhasani, Luigi A Agrofoglio, Frederic Iseni, Franck Gallardo\",\"doi\":\"10.1021/acsinfecdis.5c00169\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>Poxviruses are double-stranded DNA viruses including relevant zoonotic pathogens with high morbidity and potential biological warfare threats. Although African swine fever virus belongs to the <i>Asfarviridae</i> family and is not strictly classified as a <i>Poxviridae</i> member, both fall within the same class of <i>Pokkesviricetes</i> that replicate in the cytoplasm. Among compounds targeting these viruses, acyclic nucleoside phosphonate (ANP) prodrugs are promising inhibitors of viral DNA polymerases. However, some limitations related to their toxicity and the rapid emergence of resistance highlight the need for new antiviral molecules. In this study, we tested a new ANP called LAVR-289. This product effectively inhibits viral replication by targeting a specific domain in the poxvirus DNA polymerase. Using monkeypox virus models, the subcutaneous or oral administration of LAVR-289 demonstrated protective efficacy in infected animals without toxicity. Its <i>in vivo</i> half-life, long on-the-shelf stability and broad-spectrum efficacy make LAVR-289 a promising candidate for further development and stockpiling as a medical countermeasure against dsDNA virus outbreaks. LAVR-289 can be positioned in the context of recurrent viral epidemics, bioterrorism risk, and the emergence of resistant strains in the population.</p>\",\"PeriodicalId\":17,\"journal\":{\"name\":\"ACS Infectious Diseases\",\"volume\":\" \",\"pages\":\"1623-1634\"},\"PeriodicalIF\":3.8000,\"publicationDate\":\"2025-06-13\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"ACS Infectious Diseases\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.1021/acsinfecdis.5c00169\",\"RegionNum\":2,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"2025/5/22 0:00:00\",\"PubModel\":\"Epub\",\"JCR\":\"Q2\",\"JCRName\":\"CHEMISTRY, MEDICINAL\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"ACS Infectious Diseases","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1021/acsinfecdis.5c00169","RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2025/5/22 0:00:00","PubModel":"Epub","JCR":"Q2","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
Antiviral Activity of the Acyclic Nucleoside Phosphonate Prodrug LAVR-289 against Poxviruses and African Swine Fever Virus.
Poxviruses are double-stranded DNA viruses including relevant zoonotic pathogens with high morbidity and potential biological warfare threats. Although African swine fever virus belongs to the Asfarviridae family and is not strictly classified as a Poxviridae member, both fall within the same class of Pokkesviricetes that replicate in the cytoplasm. Among compounds targeting these viruses, acyclic nucleoside phosphonate (ANP) prodrugs are promising inhibitors of viral DNA polymerases. However, some limitations related to their toxicity and the rapid emergence of resistance highlight the need for new antiviral molecules. In this study, we tested a new ANP called LAVR-289. This product effectively inhibits viral replication by targeting a specific domain in the poxvirus DNA polymerase. Using monkeypox virus models, the subcutaneous or oral administration of LAVR-289 demonstrated protective efficacy in infected animals without toxicity. Its in vivo half-life, long on-the-shelf stability and broad-spectrum efficacy make LAVR-289 a promising candidate for further development and stockpiling as a medical countermeasure against dsDNA virus outbreaks. LAVR-289 can be positioned in the context of recurrent viral epidemics, bioterrorism risk, and the emergence of resistant strains in the population.
期刊介绍:
ACS Infectious Diseases will be the first journal to highlight chemistry and its role in this multidisciplinary and collaborative research area. The journal will cover a diverse array of topics including, but not limited to:
* Discovery and development of new antimicrobial agents — identified through target- or phenotypic-based approaches as well as compounds that induce synergy with antimicrobials.
* Characterization and validation of drug target or pathways — use of single target and genome-wide knockdown and knockouts, biochemical studies, structural biology, new technologies to facilitate characterization and prioritization of potential drug targets.
* Mechanism of drug resistance — fundamental research that advances our understanding of resistance; strategies to prevent resistance.
* Mechanisms of action — use of genetic, metabolomic, and activity- and affinity-based protein profiling to elucidate the mechanism of action of clinical and experimental antimicrobial agents.
* Host-pathogen interactions — tools for studying host-pathogen interactions, cellular biochemistry of hosts and pathogens, and molecular interactions of pathogens with host microbiota.
* Small molecule vaccine adjuvants for infectious disease.
* Viral and bacterial biochemistry and molecular biology.