{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,6,9]],"date-time":"2026-06-09T16:31:32Z","timestamp":1781022692188,"version":"3.54.1"},"reference-count":15,"publisher":"SAGE Publications","issue":"3","license":[{"start":{"date-parts":[[2019,4,1]],"date-time":"2019-04-01T00:00:00Z","timestamp":1554076800000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/journals.sagepub.com\/page\/policies\/text-and-data-mining-license"}],"content-domain":{"domain":["journals.sagepub.com"],"crossmark-restriction":true},"short-container-title":["Antiviral Therapy"],"published-print":{"date-parts":[[2020,4]]},"abstract":"<jats:sec>\n                    <jats:title>Background<\/jats:title>\n                    <jats:p>Selgantolimod is a novel oral, selective Toll-like receptor 8 (TLR8) agonist in development for the treatment of chronic hepatitis B (CHB). TLR8 is an endosomal innate immune receptor and a target for treatment of viral infections. This first-in-human study investigated the safety, tolerability, pharmacokinetics (PK) and pharmacodynamics (PD) of selgantolimod in healthy volunteers.<\/jats:p>\n                  <\/jats:sec>\n                  <jats:sec>\n                    <jats:title>Methods<\/jats:title>\n                    <jats:p>Of 71 subjects enrolled, 59 received a single dose of selgantolimod (0.5, 1.5, 3 or 5 mg) or placebo, and 12 were evaluated for food effect. Safety, PK and PD activity by induction of cytokines, chemokines and acute phase proteins were assessed. PK\/PD analyses were conducted.<\/jats:p>\n                  <\/jats:sec>\n                  <jats:sec>\n                    <jats:title>Results<\/jats:title>\n                    <jats:p>Single doses of 0.5\u20135 mg were generally safe. No serious adverse events (AEs) or AEs leading to discontinuation were reported, and most were Grade 1 in severity. Selgantolimod displayed rapid absorption and dose-proportional PK and PD activity. Food had minimal effect on PK but resulted in diminished PD activity. In PK\/PD analyses, near-saturation of induction for most evaluated biomarkers occurred at the 5-mg dose.<\/jats:p>\n                  <\/jats:sec>\n                  <jats:sec>\n                    <jats:title>Conclusions<\/jats:title>\n                    <jats:p>Single doses of up to 5 mg selgantolimod were safe and induced dose-dependent PD responses. These data support evaluation of selgantolimod in combination with other agents in future clinical studies of CHB. Australian New Zealand Clinical Trials Registration: ACTRN12616001646437.<\/jats:p>\n                  <\/jats:sec>","DOI":"10.3851\/imp3363","type":"journal-article","created":{"date-parts":[[2020,7,15]],"date-time":"2020-07-15T09:08:17Z","timestamp":1594804097000},"page":"171-180","update-policy":"https:\/\/doi.org\/10.1177\/sage-journals-update-policy","source":"Crossref","is-referenced-by-count":14,"title":["Safety, Pharmacokinetics and Pharmacodynamics of Selgantolimod, an Oral Toll-Like Receptor 8 Agonist: A Phase Ia Study in Healthy Subjects"],"prefix":"10.1177","volume":"25","author":[{"given":"Maribel","family":"Reyes","sequence":"first","affiliation":[{"name":"Clinical Pharmacology, Gilead Sciences, Foster City, CA, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Justin D","family":"Lutz","sequence":"additional","affiliation":[{"name":"Clinical Pharmacology, Gilead Sciences, Foster City, CA, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Audrey H","family":"Lau","sequence":"additional","affiliation":[{"name":"Clinical Research, Gilead Sciences, Foster City, CA, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Anuj","family":"Gaggar","sequence":"additional","affiliation":[{"name":"Clinical Research, Gilead Sciences, Foster City, CA, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Ethan P","family":"Grant","sequence":"additional","affiliation":[{"name":"Biology, Gilead Sciences, Foster City, CA, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Adarsh","family":"Joshi","sequence":"additional","affiliation":[{"name":"Biostatistics, Gilead Sciences, Foster City, CA, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Richard L","family":"Mackman","sequence":"additional","affiliation":[{"name":"Medicinal Chemistry, Gilead Sciences, Foster City, CA, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"John","family":"Ling","sequence":"additional","affiliation":[{"name":"Bioanalytical Chemistry, Gilead Sciences, Foster City, CA, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Susanna K","family":"Tan","sequence":"additional","affiliation":[{"name":"Clinical Research, Gilead Sciences, Foster City, CA, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Natarajan","family":"Ayithan","sequence":"additional","affiliation":[{"name":"Institute of Human Virology, University of Maryland, Baltimore, MD, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Stephane","family":"Daffis","sequence":"additional","affiliation":[{"name":"Biology, Gilead Sciences, Foster City, CA, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Jacky","family":"Woo","sequence":"additional","affiliation":[{"name":"Biology, Gilead Sciences, Foster City, CA, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Peiwen","family":"Wu","sequence":"additional","affiliation":[{"name":"Biostatistics, Gilead Sciences, Foster City, CA, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Tina","family":"Lam","sequence":"additional","affiliation":[{"name":"Clinical Operations, Gilead Sciences, Foster City, CA, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Simon P","family":"Fletcher","sequence":"additional","affiliation":[{"name":"Biology, Gilead Sciences, Foster City, CA, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Shyamasundaran","family":"Kottilil","sequence":"additional","affiliation":[{"name":"Institute of Human Virology, University of Maryland, Baltimore, MD, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Bhawna","family":"Poonia","sequence":"additional","affiliation":[{"name":"Institute of Human Virology, University of Maryland, Baltimore, MD, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Edward J","family":"Gane","sequence":"additional","affiliation":[{"name":"Auckland Clinical Studies, Auckland, New Zealand"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Anita","family":"Mathias","sequence":"additional","affiliation":[{"name":"Clinical Pharmacology, Gilead Sciences, Foster City, CA, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Polina","family":"German","sequence":"additional","affiliation":[{"name":"Clinical Pharmacology, Gilead Sciences, Foster City, CA, 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