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Effects of Dextran Sulfate Sodium-Induced Ulcerative Colitis on the Disposition of Tofacitinib in Ratsoa mark
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dc.contributor.authorBae, Sung Hun-
dc.contributor.authorKim, Hyo Sung-
dc.contributor.authorChoi, Hyeon Gyeom-
dc.contributor.authorChang, Sun Young-
dc.contributor.authorKim, So Hee-
dc.date.issued2022-01-01-
dc.identifier.issn2005-4483-
dc.identifier.urihttps://aurora.ajou.ac.kr/handle/2018.oak/33029-
dc.identifier.urihttps://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=85140893971&origin=inward-
dc.description.abstractTofacitinib, a Janus kinase 1 and 3 inhibitor, is mainly metabolized by CYP3A1/2 and CYP2C11 in the liver. The drug has been approved for the chronic treatment of severe ulcerative colitis, a chronic inflammatory bowel disease. This study investigated the pharmacokinetics of tofacitinib in rats with dextran sulfate sodium (DSS)-induced ulcerative colitis. After 1-min of intravenous infusion of tofacitinib (10 mg/kg), the area under the plasma concentration-time curves from time zero to time infinity (AUC) of tofacitinib significantly increased by 92.3%. The time-averaged total body clearance decreased significantly by 47.7% in DSS rats compared with control rats. After the oral administration of tofacitinib (20 mg/kg), the AUC increased by 85.5% in DSS rats. These results could be due to decreased intrinsic clearance of the drug caused by the reduction of CYP3A1/2 and CYP2C11 in the liver and intestine of DSS rats. In conclusion, ulcerative colitis inhibited CYP3A1/2 and CYP2C11 in the liver and intestines of DSS rats and slowed the metabolism of tofacitinib, resulting in increased plasma concentrations of tofacitinib in DSS rats.-
dc.description.sponsorshipThis work was supported by Basic Science Research Program (NRF-2021R1A2C1011142) through the National Research Foundation of Korea grant funded by the Ministry of Science and ICT, Republic of Korea.-
dc.language.isoeng-
dc.publisherKorean Society of Applied Pharmacology-
dc.titleEffects of Dextran Sulfate Sodium-Induced Ulcerative Colitis on the Disposition of Tofacitinib in Rats-
dc.typeArticle-
dc.citation.endPage519-
dc.citation.number6-
dc.citation.startPage510-
dc.citation.titleBiomolecules and Therapeutics-
dc.citation.volume30-
dc.identifier.bibliographicCitationBiomolecules and Therapeutics, Vol.30 No.6, pp.510-519-
dc.identifier.doi2-s2.0-85140893971-
dc.identifier.scopusid2-s2.0-85140893971-
dc.identifier.urlhttp://www.biomolther.org/-
dc.subject.keywordCYP2C11-
dc.subject.keywordCYP3A1/2-
dc.subject.keywordDextran sulfate sodium-
dc.subject.keywordPharmacokinetics-
dc.subject.keywordTofacitinib-
dc.subject.keywordUlcerative colitis-
dc.type.otherArticle-
dc.identifier.pissn1976-9148-
dc.description.isoatrue-
dc.subject.subareaBiochemistry-
dc.subject.subareaMolecular Medicine-
dc.subject.subareaPharmacology-
dc.subject.subareaDrug Discovery-
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