{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,6,24]],"date-time":"2026-06-24T04:10:51Z","timestamp":1782274251336,"version":"3.54.5"},"reference-count":38,"publisher":"Oxford University Press (OUP)","issue":"2","license":[{"start":{"date-parts":[[2024,10,23]],"date-time":"2024-10-23T00:00:00Z","timestamp":1729641600000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by-nc-nd\/4.0\/"}],"funder":[{"name":"Enanta Pharmaceuticals, Inc"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":[],"published-print":{"date-parts":[[2025,2,20]]},"abstract":"<jats:title>Abstract<\/jats:title>\n               <jats:sec>\n                  <jats:title>Background<\/jats:title>\n                  <jats:p>EDP-938 is an oral once-daily RSV nucleoprotein (N) inhibitor with potent antiviral activity. In a human RSV challenge trial, EDP-938 significantly reduced viral load and symptom severity. During antiviral development, it is critical to understand the propensity for resistance to develop. In vitro studies of EDP-938 suggest a higher barrier to resistance as compared to RSV fusion inhibitors. We evaluated the development of viral resistance to EDP-938 in a human challenge trial.<\/jats:p>\n               <\/jats:sec>\n               <jats:sec>\n                  <jats:title>Methods<\/jats:title>\n                  <jats:p>A subset of the 124 participants with RSV infection were chosen for genetic analysis; 159 nasal wash samples from 48 participants were analyzed using next-generation sequencing of the N gene of RSV. Of the 48 participant sampled, 37 were from EDP-938\u2013treated and 11 were placebo-treated participants, representing 45% and 26% of the participants, respectively. The effects of treatment-emergent mutations on viral load, EDP-938 efficacy, and viral fitness were evaluated.<\/jats:p>\n               <\/jats:sec>\n               <jats:sec>\n                  <jats:title>Results<\/jats:title>\n                  <jats:p>Two of the 37 EDP-938\u2013treated participants with samples sequenced had treatment-emergent mutations: N:L139I and N:E112G. From in vitro analysis, N:L139I reduced sensitivity to EDP-938 by approximately 10-fold, while N:E112G had no effect. However, N:L139I was associated with a reduction in viral fitness, suggesting clinical resistance is associated with fitness costs. Neither of these variants were associated with reduced viral clearance.<\/jats:p>\n               <\/jats:sec>\n               <jats:sec>\n                  <jats:title>Conclusions<\/jats:title>\n                  <jats:p>In human RSV infections treated with EDP-938, emergence of RSV variants with reduced sensitivity to EDP-938 occurred in only 1 participant and was associated with reduced viral fitness. EDP-938's high barrier to resistance highlights its robust mechanism of action.<\/jats:p>\n               <\/jats:sec>\n               <jats:sec>\n                  <jats:title>Clinical Trials Registration<\/jats:title>\n                  <jats:p>NCT03691623.<\/jats:p>\n               <\/jats:sec>","DOI":"10.1093\/infdis\/jiae471","type":"journal-article","created":{"date-parts":[[2024,9,23]],"date-time":"2024-09-23T19:21:50Z","timestamp":1727119310000},"page":"e290-e298","source":"Crossref","is-referenced-by-count":7,"title":["EDP-938 Has a High Barrier to Resistance in Healthy Adults Experimentally Infected with Respiratory Syncytial Virus"],"prefix":"10.1093","volume":"231","author":[{"given":"Rachel Emily","family":"Levene","sequence":"first","affiliation":[{"name":"Enanta Pharmaceuticals, Inc , Watertown, Massachusetts ,","place":["USA"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"John","family":"DeVincenzo","sequence":"additional","affiliation":[{"name":"Enanta Pharmaceuticals, Inc , Watertown, Massachusetts ,","place":["USA"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Annie L","family":"Conery","sequence":"additional","affiliation":[{"name":"Enanta Pharmaceuticals, Inc , Watertown, Massachusetts ,","place":["USA"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-6935-6748","authenticated-orcid":false,"given":"Alaa","family":"Ahmad","sequence":"additional","affiliation":[{"name":"Enanta Pharmaceuticals, Inc , Watertown, Massachusetts ,","place":["USA"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Yat Sun","family":"Or","sequence":"additional","affiliation":[{"name":"Enanta Pharmaceuticals, Inc , Watertown, Massachusetts ,","place":["USA"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-4032-7545","authenticated-orcid":false,"given":"Michael H J","family":"Rhodin","sequence":"additional","affiliation":[{"name":"Enanta Pharmaceuticals, Inc , Watertown, Massachusetts ,","place":["USA"]}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"286","published-online":{"date-parts":[[2024,10,23]]},"reference":[{"key":"2025022016432024000_jiae471-B1","doi-asserted-by":"crossref","first-page":"1322","DOI":"10.3324\/haematol.2018.215152","article-title":"Respiratory syncytial virus in hematopoietic cell transplant recipients and patients with hematologic malignancies","volume":"104","author":"Khawaja","year":"2019","journal-title":"Haematologica"},{"key":"2025022016432024000_jiae471-B2","doi-asserted-by":"crossref","first-page":"1749","DOI":"10.1056\/NEJMoa043951","article-title":"Respiratory syncytial virus infection in elderly and high-risk adults","volume":"352","author":"Falsey","year":"2005","journal-title":"N Engl J Med"},{"key":"2025022016432024000_jiae471-B3","doi-asserted-by":"crossref","first-page":"588","DOI":"10.1056\/NEJMoa0804877","article-title":"The burden of respiratory syncytial virus infection in young children","volume":"360","author":"Hall","year":"2009","journal-title":"N Engl J Med"},{"key":"2025022016432024000_jiae471-B4","doi-asserted-by":"crossref","first-page":"40","DOI":"10.1007\/s41061-017-0129-4","article-title":"Recent advances in developing antiviral therapies for respiratory syncytial virus","volume":"375","author":"Shook","year":"2017","journal-title":"Top Curr Chem"},{"key":"2025022016432024000_jiae471-B5","doi-asserted-by":"crossref","first-page":"284","DOI":"10.1097\/01.inf.0000121203.33560.f9","article-title":"Risk of severe respiratory syncytial virus disease, identification of high risk infants and recommendations for prophylaxis with palivizumab","volume":"23","author":"Meissner","year":"2004","journal-title":"Pediatr Infect Dis J"},{"key":"2025022016432024000_jiae471-B6","author":"Food and Drug Administration"},{"key":"2025022016432024000_jiae471-B7"},{"key":"2025022016432024000_jiae471-B8","doi-asserted-by":"crossref","first-page":"519","DOI":"10.1542\/pir.35.12.519","article-title":"Respiratory syncytial virus infection and bronchiolitis","volume":"35","author":"Piedimonte","year":"2014","journal-title":"Pediatr Rev"},{"key":"2025022016432024000_jiae471-B9","doi-asserted-by":"crossref","first-page":"e1009428","DOI":"10.1371\/journal.ppat.1009428","article-title":"EDP-938, a novel nucleoprotein inhibitor of respiratory syncytial virus, demonstrates potent antiviral activities in vitro and in a non-human primate model","volume":"17","author":"Rhodin","year":"2021","journal-title":"PLoS Pathog"},{"key":"2025022016432024000_jiae471-B10"},{"key":"2025022016432024000_jiae471-B11","doi-asserted-by":"crossref","first-page":"655","DOI":"10.1056\/NEJMoa2108903","article-title":"EDP-938, a respiratory syncytial virus inhibitor, in a human virus challenge","volume":"386","author":"Ahmad","year":"2022","journal-title":"N Engl J Med"},{"key":"2025022016432024000_jiae471-B12","doi-asserted-by":"crossref","first-page":"1264","DOI":"10.1128\/AAC.01497-15","article-title":"GS-5806 inhibits a broad range of respiratory syncytial virus clinical isolates by blocking the virus-cell fusion process","volume":"60","author":"Perron","year":"2015","journal-title":"Antimicrob Agents Chemother"},{"key":"2025022016432024000_jiae471-B13","doi-asserted-by":"crossref","first-page":"6003","DOI":"10.1021\/acs.jmedchem.9b00654","article-title":"Discovery of Ziresovir as a potent, selective, and orally bioavailable respiratory syncytial virus fusion protein inhibitor","volume":"62","author":"Zheng","year":"2019","journal-title":"J Med Chem"},{"key":"2025022016432024000_jiae471-B14","doi-asserted-by":"crossref","first-page":"3658","DOI":"10.1021\/acs.jmedchem.0c01882","article-title":"Discovery of Sisunatovir (RV521), an inhibitor of respiratory syncytial virus fusion","volume":"64","author":"Cockerill","year":"2021","journal-title":"J Med Chem"},{"key":"2025022016432024000_jiae471-B15","doi-asserted-by":"crossref","first-page":"1468","DOI":"10.1093\/infdis\/jiaa028","article-title":"Drug resistance assessment following administration of respiratory syncytial virus (RSV) fusion inhibitor Presatovir to participants experimentally infected with RSV","volume":"222","author":"Stray","year":"2020","journal-title":"J Infect Dis"},{"key":"2025022016432024000_jiae471-B16","doi-asserted-by":"crossref","first-page":"e01884","DOI":"10.1128\/AAC.01884-19","article-title":"A randomized, placebo-controlled, respiratory syncytial virus human challenge study of the antiviral efficacy, safety, and pharmacokinetics of RV521, an inhibitor of the RSV-F protein","volume":"64","author":"DeVincenzo","year":"2020","journal-title":"Antimicrob Agents Chemother"},{"key":"2025022016432024000_jiae471-B17","doi-asserted-by":"crossref","first-page":"e02312","DOI":"10.1128\/AAC.02312-19","article-title":"Assessment of drug resistance during phase 2b clinical trials of Presatovir in adults naturally infected with respiratory syncytial virus","volume":"64","author":"Porter","year":"2020","journal-title":"Antimicrob Agents Chemother"},{"key":"2025022016432024000_jiae471-B18","doi-asserted-by":"crossref","first-page":"87","DOI":"10.1038\/nchembio.1982","article-title":"Molecular mechanism of respiratory syncytial virus fusion inhibitors","volume":"12","author":"Battles","year":"2016","journal-title":"Nat Chem Biol"},{"key":"2025022016432024000_jiae471-B19","doi-asserted-by":"crossref","first-page":"e0120521","DOI":"10.1128\/JVI.01205-21","article-title":"Mechanism of cross-resistance to fusion inhibitors conferred by the K394R mutation in respiratory syncytial virus fusion protein","volume":"95","author":"Tang","year":"2021","journal-title":"J Virol"},{"key":"2025022016432024000_jiae471-B20","doi-asserted-by":"crossref","first-page":"129","DOI":"10.1016\/j.virol.2012.09.022","article-title":"A stabilized respiratory syncytial virus reverse genetics system amenable to recombination-mediated mutagenesis","volume":"434","author":"Hotard","year":"2012","journal-title":"Virology"},{"key":"2025022016432024000_jiae471-B21","doi-asserted-by":"crossref","first-page":"e113100","DOI":"10.1371\/journal.pone.0113100","article-title":"Respiratory syncytial virus human experimental infection model: provenance, production, and sequence of low-passaged Memphis-37 challenge virus","volume":"9","author":"Kim","year":"2014","journal-title":"PLoS One"},{"key":"2025022016432024000_jiae471-B22","author":"ArkBio"},{"key":"2025022016432024000_jiae471-B23","volume-title":"EDP-323, a novel L-protein inhibitor, for the treatment of respiratory syncytial virus","author":"Rhodin","year":"2022"},{"key":"2025022016432024000_jiae471-B24","volume-title":"In vivo efficacy of EDP-323, a novel L-protein inhibitor, for the treatment of respiratory syncytial virus","author":"Levene","year":"2023"},{"key":"2025022016432024000_jiae471-B25","author":"Enanta Pharmaceuticals, Inc"},{"key":"2025022016432024000_jiae471-B26","doi-asserted-by":"crossref","first-page":"3346","DOI":"10.1128\/AAC.00211-07","article-title":"RSV604, a novel inhibitor of respiratory syncytial virus replication","volume":"51","author":"Chapman","year":"2007","journal-title":"Antimicrob Agents Chemother"},{"key":"2025022016432024000_jiae471-B27","doi-asserted-by":"crossref","first-page":"367","DOI":"10.1002\/9780470929353.ch26","author":"Chapman","year":"2011","journal-title":"Antiviral drugs: from basic discovery through clinical trials"},{"key":"2025022016432024000_jiae471-B28","doi-asserted-by":"crossref","first-page":"11129","DOI":"10.1128\/JVI.01612-15","article-title":"A druggable pocket at the nucleocapsid\/phosphoprotein interaction site of human respiratory syncytial virus","volume":"89","author":"Ouizougun-Oubari","year":"2015","journal-title":"J Virol"},{"key":"2025022016432024000_jiae471-B29","doi-asserted-by":"crossref","first-page":"8375","DOI":"10.1128\/JVI.00058-12","article-title":"Characterization of a viral phosphoprotein binding site on the surface of the respiratory syncytial nucleoprotein","volume":"86","author":"Galloux","year":"2012","journal-title":"J Virol"},{"key":"2025022016432024000_jiae471-B30","doi-asserted-by":"crossref","first-page":"1080","DOI":"10.1128\/AAC.04119-14","article-title":"Mechanism of action for respiratory syncytial virus inhibitor RSV604","volume":"59","author":"Challa","year":"2015","journal-title":"Antimicrob Agents Chemother"},{"key":"2025022016432024000_jiae471-B31","first-page":"3","article-title":"Respiratory syncytial virus: virology, reverse genetics, and pathogenesis of disease","volume":"372","author":"Collins","year":"2013","journal-title":"Curr Top Microbiol Immunol"},{"key":"2025022016432024000_jiae471-B32","doi-asserted-by":"crossref","first-page":"6660","DOI":"10.1016\/j.vaccine.2018.09.056","article-title":"Antigenic and sequence variability of the human respiratory syncytial virus F glycoprotein compared to related viruses in a comprehensive dataset","volume":"36","author":"Mas","year":"2018","journal-title":"Vaccine"},{"key":"2025022016432024000_jiae471-B33","doi-asserted-by":"crossref","first-page":"975","DOI":"10.1086\/423213","article-title":"Surveillance of clinical isolates of respiratory syncytial virus for palivizumab (Synagis)-resistant mutants","volume":"190","author":"DeVincenzo","year":"2004","journal-title":"J Infect Dis"},{"key":"2025022016432024000_jiae471-B34","doi-asserted-by":"crossref","first-page":"185","DOI":"10.1086\/653534","article-title":"Palivizumab-resistant human respiratory syncytial virus infection in infancy","volume":"51","author":"Adams","year":"2010","journal-title":"Clin Infect Dis"},{"key":"2025022016432024000_jiae471-B35","doi-asserted-by":"crossref","first-page":"120","DOI":"10.3201\/eid1801.110515","article-title":"Molecular evolution of respiratory syncytial virus fusion gene, Canada, 2006\u20132010","volume":"18","author":"Papenburg","year":"2012","journal-title":"Emerg Infect Dis"},{"key":"2025022016432024000_jiae471-B36","doi-asserted-by":"crossref","first-page":"674","DOI":"10.1093\/infdis\/jiq100","article-title":"Analysis of respiratory syncytial virus preclinical and clinical variants resistant to neutralization by monoclonal antibodies palivizumab and\/or motavizumab","volume":"203","author":"Zhu","year":"2011","journal-title":"J Infect Dis"},{"key":"2025022016432024000_jiae471-B37","doi-asserted-by":"crossref","first-page":"26","DOI":"10.1016\/j.jcv.2015.01.016","article-title":"Molecular characterization of respiratory syncytial viruses infecting children reported to have received palivizumab immunoprophylaxis","volume":"65","author":"Oliveira","year":"2015","journal-title":"J Clin Virol"},{"key":"2025022016432024000_jiae471-B38","doi-asserted-by":"crossref","first-page":"78","DOI":"10.1067\/mpd.2000.105350","article-title":"Increased burden of respiratory viral associated severe lower respiratory tract infections in children infected with human immunodeficiency virus type-1","volume":"137","author":"Madhi","year":"2000","journal-title":"J Pediatr"}],"container-title":["The Journal of Infectious Diseases"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/academic.oup.com\/jid\/advance-article-pdf\/doi\/10.1093\/infdis\/jiae471\/60772843\/jiae471.pdf","content-type":"application\/pdf","content-version":"am","intended-application":"syndication"},{"URL":"https:\/\/academic.oup.com\/jid\/article-pdf\/231\/2\/e290\/60772843\/jiae471.pdf","content-type":"application\/pdf","content-version":"vor","intended-application":"syndication"},{"URL":"https:\/\/academic.oup.com\/jid\/article-pdf\/231\/2\/e290\/60772843\/jiae471.pdf","content-type":"unspecified","content-version":"vor","intended-application":"similarity-checking"}],"deposited":{"date-parts":[[2025,2,20]],"date-time":"2025-02-20T16:44:10Z","timestamp":1740069850000},"score":1,"resource":{"primary":{"URL":"https:\/\/academic.oup.com\/jid\/article\/231\/2\/e290\/7824591"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2024,10,23]]},"references-count":38,"journal-issue":{"issue":"2","published-online":{"date-parts":[[2024,10,23]]},"published-print":{"date-parts":[[2025,2,20]]}},"URL":"https:\/\/doi.org\/10.1093\/infdis\/jiae471","relation":{},"ISSN":["0022-1899","1537-6613"],"issn-type":[{"value":"0022-1899","type":"print"},{"value":"1537-6613","type":"electronic"}],"subject":[],"published-other":{"date-parts":[[2025,2,15]]},"published":{"date-parts":[[2024,10,23]]}}}