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DC Field | Value | Language |
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dc.contributor.author | Bae, Sung Hun | - |
dc.contributor.author | Kim, Hyo Sung | - |
dc.contributor.author | Choi, Hyeon Gyeom | - |
dc.contributor.author | Chang, Sun Young | - |
dc.contributor.author | Kim, So Hee | - |
dc.date.issued | 2022-01-01 | - |
dc.identifier.issn | 2005-4483 | - |
dc.identifier.uri | https://aurora.ajou.ac.kr/handle/2018.oak/33029 | - |
dc.identifier.uri | https://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=85140893971&origin=inward | - |
dc.description.abstract | Tofacitinib, 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.sponsorship | This 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.iso | eng | - |
dc.publisher | Korean Society of Applied Pharmacology | - |
dc.title | Effects of Dextran Sulfate Sodium-Induced Ulcerative Colitis on the Disposition of Tofacitinib in Rats | - |
dc.type | Article | - |
dc.citation.endPage | 519 | - |
dc.citation.number | 6 | - |
dc.citation.startPage | 510 | - |
dc.citation.title | Biomolecules and Therapeutics | - |
dc.citation.volume | 30 | - |
dc.identifier.bibliographicCitation | Biomolecules and Therapeutics, Vol.30 No.6, pp.510-519 | - |
dc.identifier.doi | 2-s2.0-85140893971 | - |
dc.identifier.scopusid | 2-s2.0-85140893971 | - |
dc.identifier.url | http://www.biomolther.org/ | - |
dc.subject.keyword | CYP2C11 | - |
dc.subject.keyword | CYP3A1/2 | - |
dc.subject.keyword | Dextran sulfate sodium | - |
dc.subject.keyword | Pharmacokinetics | - |
dc.subject.keyword | Tofacitinib | - |
dc.subject.keyword | Ulcerative colitis | - |
dc.type.other | Article | - |
dc.identifier.pissn | 1976-9148 | - |
dc.description.isoa | true | - |
dc.subject.subarea | Biochemistry | - |
dc.subject.subarea | Molecular Medicine | - |
dc.subject.subarea | Pharmacology | - |
dc.subject.subarea | Drug Discovery | - |
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