{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2024,11,27]],"date-time":"2024-11-27T05:32:46Z","timestamp":1732685566798,"version":"3.28.2"},"reference-count":16,"publisher":"Wiley","issue":"12","license":[{"start":{"date-parts":[[2024,8,1]],"date-time":"2024-08-01T00:00:00Z","timestamp":1722470400000},"content-version":"vor","delay-in-days":0,"URL":"http:\/\/creativecommons.org\/licenses\/by-nc\/4.0\/"}],"content-domain":{"domain":["accp1.onlinelibrary.wiley.com"],"crossmark-restriction":true},"short-container-title":["The Journal of Clinical Pharma"],"published-print":{"date-parts":[[2024,12]]},"abstract":"<jats:title>Abstract<\/jats:title><jats:p>We conducted this three\u2010part study in healthy subjects to investigate the pharmacokinetics of tasurgratinib (orally available selective inhibitor of fibroblast growth factor receptor 1\u20103) and M2 (its major metabolite) under different conditions. In Part A, subjects received tasurgratinib 35 mg either fed with a high\u2010fat meal or fasted. In Parts B and C, subjects received tasurgratinib 35 mg alone or with either rabeprazole (acid\u2010reducing agent) 20 mg (Part B) or rifampin (strong CYP3A inducer) 600 mg (Part C). Primary endpoints were maximum concentration (C<jats:sub>max<\/jats:sub>), and areas under the plasma concentration\u2010time curve to time of last quantifiable concentration (AUC<jats:sub>(0\u2010t)<\/jats:sub>) and extrapolated to infinite time (AUC<jats:sub>(0\u2010inf)<\/jats:sub>). Forty\u2010two subjects were enrolled, 14 each into Parts A, B, and C. In Part A, administration of tasurgratinib with a high\u2010fat meal resulted in 33% reduction in C<jats:sub>max<\/jats:sub> and \u223c23% reduction in AUC<jats:sub>(0\u2010t)<\/jats:sub> and AUC<jats:sub>(0\u2010inf)<\/jats:sub> of tasurgratinib, and 47% reduction in C<jats:sub>max<\/jats:sub> with \u223c30% reduction in AUC<jats:sub>(0\u2010t)<\/jats:sub> and AUC<jats:sub>(0\u2010inf)<\/jats:sub> of M2. In Part B, co\u2010administration of rabeprazole at steady state resulted in no\/weak interaction with tasurgratinib (\u223c8% increase in AUC<jats:sub>(0\u2010t)<\/jats:sub> and AUC<jats:sub>(0\u2010inf)<\/jats:sub> without an effect on C<jats:sub>max<\/jats:sub>) and M2 (\u223c18% increase in AUC<jats:sub>(0\u2010t)<\/jats:sub> and AUC<jats:sub>(0\u2010inf)<\/jats:sub> without an effect on C<jats:sub>max<\/jats:sub>). In Part C, co\u2010administration of rifampin at steady state resulted in a weak interaction with tasurgratinib (\u223c16% reduction in AUC<jats:sub>(0\u2010t)<\/jats:sub> and AUC<jats:sub>(0\u2010inf)<\/jats:sub>) and M2 (\u223c12% reduction in AUC<jats:sub>(0\u2010t)<\/jats:sub> and AUC<jats:sub>(0\u2010inf)<\/jats:sub>). Administration of tasurgratinib with a high\u2010fat meal appeared to reduce systemic exposure of tasurgratinib, however co\u2010administration with an acid\u2010reducing agent or a CYP3A inducer had a minimal impact on pharmacokinetics.<\/jats:p>","DOI":"10.1002\/jcph.6104","type":"journal-article","created":{"date-parts":[[2024,8,1]],"date-time":"2024-08-01T13:49:18Z","timestamp":1722520158000},"page":"1541-1551","update-policy":"http:\/\/dx.doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":0,"title":["Effects of Food, Gastric Acid Reduction, and Strong CYP3A Induction on the Pharmacokinetics of Tasurgratinib, a Novel Selective Fibroblast Growth Factor Receptor Inhibitor"],"prefix":"10.1002","volume":"64","author":[{"given":"Maiko","family":"Nomoto","sequence":"first","affiliation":[{"name":"Eisai Co., Ltd.  Tokyo Japan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Tomoko","family":"Hasunuma","sequence":"additional","affiliation":[{"name":"Department of Research Clinical Trial Center Kitasato University Kitasato Institute Hospital  Tokyo Japan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Cuiyuan","family":"Cai","sequence":"additional","affiliation":[{"name":"Eisai Co., Ltd.  Tokyo Japan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Ippei","family":"Suzuki","sequence":"additional","affiliation":[{"name":"Eisai Co., Ltd.  Tokyo Japan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Ayano","family":"Mikubo","sequence":"additional","affiliation":[{"name":"Eisai Co., Ltd.  Tokyo Japan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Setsuo","family":"Funasaka","sequence":"additional","affiliation":[{"name":"Eisai Co., Ltd.  Tokyo Japan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Yohei","family":"Otake","sequence":"additional","affiliation":[{"name":"Eisai Co., Ltd.  Tokyo Japan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Kenya","family":"Nakai","sequence":"additional","affiliation":[{"name":"Eisai Co., Ltd.  Tokyo Japan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Sanae","family":"Yasuda","sequence":"additional","affiliation":[{"name":"Eisai Inc.  Nutley NJ USA"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"311","published-online":{"date-parts":[[2024,8]]},"reference":[{"key":"e_1_2_9_2_1","doi-asserted-by":"publisher","DOI":"10.1002\/mco2.367"},{"key":"e_1_2_9_3_1","doi-asserted-by":"publisher","DOI":"10.1111\/cas.14265"},{"key":"e_1_2_9_4_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.annonc.2020.10.149"},{"key":"e_1_2_9_5_1","doi-asserted-by":"publisher","DOI":"10.1200\/JCO.2024.42.3_suppl.471"},{"key":"e_1_2_9_6_1","doi-asserted-by":"publisher","DOI":"10.1007\/s40265-017-0832-z"},{"key":"e_1_2_9_7_1","doi-asserted-by":"publisher","DOI":"10.1146\/annurev.nu.16.070196.002123"},{"volume-title":"United States Food and Drug Administration","author":"Assessing the Effects of Food on Drugs in INDs and NDAs \u2014 Clinical Pharmacology Considerations","key":"e_1_2_9_8_1"},{"volume-title":"United States Food and Drug Administration","author":"Evaluation of Gastric pH\u2010Dependent Drug Interactions With Acid\u2010Reducing Agents: Study Design","key":"e_1_2_9_9_1"},{"volume-title":"European Medicines Agency","author":"(CHMP) CfHMP","key":"e_1_2_9_10_1"},{"key":"e_1_2_9_11_1","doi-asserted-by":"publisher","DOI":"10.1038\/clpt.2014.87"},{"issue":"3","key":"e_1_2_9_12_1","first-page":"363","article-title":"A review of rabeprazole in the treatment of acid\u2010related diseases","volume":"3","author":"Pace F","year":"2007","journal-title":"Ther Clin Risk Manag"},{"key":"e_1_2_9_13_1","doi-asserted-by":"publisher","DOI":"10.1046\/j.1365-2036.2002.01292.x"},{"key":"e_1_2_9_14_1","doi-asserted-by":"publisher","DOI":"10.1002\/jcph.510"},{"volume-title":"United States Food and Drug Administration","author":"Assessing the Effects of Food on Drugs in INDs and NDAs \u2014 Clinical Pharmacology Considerations [Draft Guidance]","key":"e_1_2_9_15_1"},{"key":"e_1_2_9_16_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.jpba.2023.115866"},{"volume-title":"United States Food and Drug Administration","author":"For Healthcare Professionals | FDA's Examples of Drugs that Interact with CYP Enzymes and Transporter Systems","key":"e_1_2_9_17_1"}],"container-title":["The Journal of Clinical Pharmacology"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/accp1.onlinelibrary.wiley.com\/doi\/pdf\/10.1002\/jcph.6104","content-type":"unspecified","content-version":"vor","intended-application":"similarity-checking"}],"deposited":{"date-parts":[[2024,11,26]],"date-time":"2024-11-26T16:04:14Z","timestamp":1732637054000},"score":1,"resource":{"primary":{"URL":"https:\/\/accp1.onlinelibrary.wiley.com\/doi\/10.1002\/jcph.6104"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2024,8]]},"references-count":16,"journal-issue":{"issue":"12","published-print":{"date-parts":[[2024,12]]}},"alternative-id":["10.1002\/jcph.6104"],"URL":"https:\/\/doi.org\/10.1002\/jcph.6104","archive":["Portico"],"relation":{},"ISSN":["0091-2700","1552-4604"],"issn-type":[{"type":"print","value":"0091-2700"},{"type":"electronic","value":"1552-4604"}],"subject":[],"published":{"date-parts":[[2024,8]]},"assertion":[{"value":"2024-04-03","order":0,"name":"received","label":"Received","group":{"name":"publication_history","label":"Publication History"}},{"value":"2024-07-15","order":2,"name":"accepted","label":"Accepted","group":{"name":"publication_history","label":"Publication History"}},{"value":"2024-08-01","order":3,"name":"published","label":"Published","group":{"name":"publication_history","label":"Publication History"}}]}}