{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,9,2]],"date-time":"2026-09-02T14:17:18Z","timestamp":1788358638172,"version":"build-2803163510"},"reference-count":23,"publisher":"Wiley","issue":"2","license":[{"start":{"date-parts":[[2020,11,28]],"date-time":"2020-11-28T00:00:00Z","timestamp":1606521600000},"content-version":"vor","delay-in-days":0,"URL":"http:\/\/onlinelibrary.wiley.com\/termsAndConditions#vor"}],"funder":[{"DOI":"10.13039\/501100001809","name":"National Natural Science Foundation of China","doi-asserted-by":"publisher","award":["81602897"],"award-info":[{"award-number":["81602897"]}],"id":[{"id":"10.13039\/501100001809","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":["onlinelibrary.wiley.com"],"crossmark-restriction":true},"short-container-title":["Aliment Pharmacol Ther"],"published-print":{"date-parts":[[2021,1]]},"abstract":"<jats:title>Summary<\/jats:title><jats:sec><jats:title>Background<\/jats:title><jats:p>HS\u201010234 is a novel prodrug of tenofovir developed to increase anti\u2010viral potency and to reduce systemic toxicities.<\/jats:p><\/jats:sec><jats:sec><jats:title>Aims<\/jats:title><jats:p>To evaluate the tolerability, pharmacokinetics and anti\u2010viral efficacy of HS\u201010234 in patients with chronic hepatitis B (CHB) infection<\/jats:p><\/jats:sec><jats:sec><jats:title>Methods<\/jats:title><jats:p>Treatment\u2010na\u00efve subjects with non\u2010cirrhotic CHB were divided into three groups (n\u00a0=\u00a012\/group) and randomised within each group to receive 10, 25 or 40\u00a0mg of HS\u201010234, or 300\u00a0mg of tenofovir disoproxil fumarate (TDF) once a day for 28\u00a0days.<\/jats:p><\/jats:sec><jats:sec><jats:title>Results<\/jats:title><jats:p>Among 36 enrolled subjects, 33.3% were hepatitis B e antigen\u2010negative with a mean hepatitis B virus (HBV) DNA level of 6.32\u20107.42\u00a0log<jats:sub>10<\/jats:sub>\u00a0IU\/mL. Nephrotoxicity and serious adverse events were not observed; all adverse events were mild or moderate and non\u2010specific. The mean reductions in serum HBV DNA after 28\u00a0days were \u22122.70, \u22122.89, \u22122.72 and \u22123.04\u00a0log<jats:sub>10<\/jats:sub>\u00a0IU\/mL for treatment with 10, 25 or 40\u00a0mg HS\u201010234, and 300\u00a0mg TDF, respectively. HS\u201010234 and its metabolite TFV showed linear, dose\u2010proportional pharmacokinetics. The concentrations of active TFV\u2010DP in peripheral blood mononuclear cells were higher (approximately 2\u2010 to 11\u2010fold increase) and TFV in plasma were lower (approximately 4.5\u2010 to 25\u2010fold reduction) in subjects taking HS\u201010234 than those in the TDF group.<\/jats:p><\/jats:sec><jats:sec><jats:title>Conclusions<\/jats:title><jats:p>HS\u201010234 was well tolerated during a 4\u2010week course. TDF and HS\u201010234 had comparable potency in inhibiting HBV replication. A daily dose of 10\u201025\u00a0mg of HS\u201010234 is recommended for CHB treatment. 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