Chung, Hye J. Lee, Joo H. Woo, Sung J. Park, Hee K. Koo, Chang H. Lee, Myung G. 2024-01-21T01:03:58Z 2024-01-21T01:03:58Z 2021-08-31 2007-05 0142-2782 https://pubs.kist.re.kr/handle/201004/134438 The pharmacokinetics of L-FMAUS after intravenous and oral administration (20, 50 and 100mg/kg) to rats, gastrointestinal first-pass effect of L-FMAUS (50mg/kg) in rats, in vitro stability of L-FMAUS, blood partition of L-FMAUS between plasma and blood cells of rat blood, and protein binding of L-FMAUS to 4% human SE-rum albumin were evaluated. L-FMAUS is being evaluated in a preclinical study as a novel antiviral agent. Although the dose-normalized AUC values of L-FMAUS were not significantly different among the three doses after intravenous and oral administration, no trend was apparent between the dose and dose-normalized AUC. After oral administration of L-FMAUS (50mg/kg), approximately 2.37% of the oral dose was not absorbed, and the extent of absolute oral bioavailability (F) was approximately 11.5%,. The gastrointestinal first-pass effect was approximately 85% of the oral dose. The first-pass effects of L-FMAUS in the lung, heart and liver were almost negligible, if any, ill rats. Hence, the small F of L-FMAUS in rats was mainly due to the considerable gastrointestinal first-pass effect. L-FMAUS was stable in rat gastric juices. The plasma-to-blood cells partition ratio of L-FMAUS was 2.17 in rat blood. The plasma protein binding of L-FMAUS in rats was 98.6%. Copyright (c) 2007 John Wiley & Sons, Ltd. English JOHN WILEY & SONS LTD DEOXYCYTIDINE KINASE DRUG ELIMINATION DOSAGE REGIMENS LIVER 2&apos -FLUORO-5-METHYL-BETA-L-ARABINOFURANOSYLURACIL ERYTHROCYTES METABOLISM FUROSEMIDE INHIBITOR BARRIERS Pharmacokinetics of L-FMAUS, a new antiviral agent, after intravenous and oral administration to rats: Contribution of gastrointestinal first-pass effect to low bioavailability Article 10.1002/bdd.545 1 BIOPHARMACEUTICS & DRUG DISPOSITION, v.28, no.4, pp.187 - 197 BIOPHARMACEUTICS & DRUG DISPOSITION 28 4 187 197 scie scopus 000246649400004 Pharmacology & Pharmacy Pharmacology & Pharmacy Article DEOXYCYTIDINE KINASE DRUG ELIMINATION DOSAGE REGIMENS LIVER 2&apos -FLUORO-5-METHYL-BETA-L-ARABINOFURANOSYLURACIL ERYTHROCYTES METABOLISM FUROSEMIDE INHIBITOR BARRIERS L-FMAUS pharmacokinetics gastrointestinal first-pass effect rats