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How will CYP induction related PBPK applications be evaluated during the NDA reviews? 在NDA审查期间，如何评估CYP诱导相关的PBPK申请？
IF 2.7 4区 医学
Drug Metabolism and Pharmacokinetics Pub Date : 2025-06-01 Epub Date: 2025-06-03 DOI: 10.1016/j.dmpk.2025.101063
Ying-Hong Wang
{"title":"How will CYP induction related PBPK applications be evaluated during the NDA reviews?","authors":"Ying-Hong Wang","doi":"10.1016/j.dmpk.2025.101063","DOIUrl":"10.1016/j.dmpk.2025.101063","url":null,"abstract":"","PeriodicalId":11298,"journal":{"name":"Drug Metabolism and Pharmacokinetics","volume":"61 ","pages":"Article 101063"},"PeriodicalIF":2.7,"publicationDate":"2025-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144194658","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Quantitative analysis of gastrointestinal drug absorption and disposition using state-of-the-art technology 利用最新技术对胃肠道药物吸收和处置进行定量分析
IF 2.7 4区 医学
Drug Metabolism and Pharmacokinetics Pub Date : 2025-06-01 Epub Date: 2025-06-03 DOI: 10.1016/j.dmpk.2025.101068
Yoshiyuki Shirasaka
{"title":"Quantitative analysis of gastrointestinal drug absorption and disposition using state-of-the-art technology","authors":"Yoshiyuki Shirasaka","doi":"10.1016/j.dmpk.2025.101068","DOIUrl":"10.1016/j.dmpk.2025.101068","url":null,"abstract":"","PeriodicalId":11298,"journal":{"name":"Drug Metabolism and Pharmacokinetics","volume":"61 ","pages":"Article 101068"},"PeriodicalIF":2.7,"publicationDate":"2025-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144194664","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Human enteroid monolayers – A fit-for purpose model to elucidate intestinal natural product-drug interactions 人肠道单分子层-一个适合目的的模型来阐明肠道天然产物-药物相互作用
IF 2.7 4区 医学
Drug Metabolism and Pharmacokinetics Pub Date : 2025-06-01 Epub Date: 2025-06-03 DOI: 10.1016/j.dmpk.2025.101070
Kenneth E. Thummel, Eimear O’Mahony, Christopher Arian, Edward J. Kelly
{"title":"Human enteroid monolayers – A fit-for purpose model to elucidate intestinal natural product-drug interactions","authors":"Kenneth E. Thummel, Eimear O’Mahony, Christopher Arian, Edward J. Kelly","doi":"10.1016/j.dmpk.2025.101070","DOIUrl":"10.1016/j.dmpk.2025.101070","url":null,"abstract":"","PeriodicalId":11298,"journal":{"name":"Drug Metabolism and Pharmacokinetics","volume":"61 ","pages":"Article 101070"},"PeriodicalIF":2.7,"publicationDate":"2025-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144195401","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Discovery of PF-07817883, a second-generation oral SARS-CoV2 main protease inhibitor 第二代口服SARS-CoV2主要蛋白酶抑制剂PF-07817883的发现
IF 2.7 4区 医学
Drug Metabolism and Pharmacokinetics Pub Date : 2025-06-01 Epub Date: 2025-06-03 DOI: 10.1016/j.dmpk.2025.101106
Amit Kalgutkar
{"title":"Discovery of PF-07817883, a second-generation oral SARS-CoV2 main protease inhibitor","authors":"Amit Kalgutkar","doi":"10.1016/j.dmpk.2025.101106","DOIUrl":"10.1016/j.dmpk.2025.101106","url":null,"abstract":"","PeriodicalId":11298,"journal":{"name":"Drug Metabolism and Pharmacokinetics","volume":"61 ","pages":"Article 101106"},"PeriodicalIF":2.7,"publicationDate":"2025-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144195549","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Computer aided metid for small molecules and peptide drugs 小分子和多肽药物的计算机辅助方法
IF 2.7 4区 医学
Drug Metabolism and Pharmacokinetics Pub Date : 2025-06-01 Epub Date: 2025-06-03 DOI: 10.1016/j.dmpk.2025.101091
Ismael Zamora
{"title":"Computer aided metid for small molecules and peptide drugs","authors":"Ismael Zamora","doi":"10.1016/j.dmpk.2025.101091","DOIUrl":"10.1016/j.dmpk.2025.101091","url":null,"abstract":"","PeriodicalId":11298,"journal":{"name":"Drug Metabolism and Pharmacokinetics","volume":"61 ","pages":"Article 101091"},"PeriodicalIF":2.7,"publicationDate":"2025-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144195715","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Membrane transporters in drug development and as determinants of precision medicine; an update from the international transporter consortium 膜转运蛋白在药物开发和精准医疗的决定因素来自国际运输联盟的最新消息
IF 2.7 4区 医学
Drug Metabolism and Pharmacokinetics Pub Date : 2025-06-01 Epub Date: 2025-06-03 DOI: 10.1016/j.dmpk.2025.101092
Kim Brouwer
{"title":"Membrane transporters in drug development and as determinants of precision medicine; an update from the international transporter consortium","authors":"Kim Brouwer","doi":"10.1016/j.dmpk.2025.101092","DOIUrl":"10.1016/j.dmpk.2025.101092","url":null,"abstract":"","PeriodicalId":11298,"journal":{"name":"Drug Metabolism and Pharmacokinetics","volume":"61 ","pages":"Article 101092"},"PeriodicalIF":2.7,"publicationDate":"2025-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144195716","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Incorporation of well-stirred, dispersion and parallel tube liver models into simple and permeability limited PBPK frameworks for clearance prediction 将充分搅拌、分散和平行管肝模型纳入简单和渗透率有限的PBPK框架，用于预测清除
IF 2.7 4区 医学
Drug Metabolism and Pharmacokinetics Pub Date : 2025-06-01 Epub Date: 2025-06-03 DOI: 10.1016/j.dmpk.2025.101147
Swati Nagar, Rachel Parise, Ken Korzekwa
{"title":"Incorporation of well-stirred, dispersion and parallel tube liver models into simple and permeability limited PBPK frameworks for clearance prediction","authors":"Swati Nagar, Rachel Parise, Ken Korzekwa","doi":"10.1016/j.dmpk.2025.101147","DOIUrl":"10.1016/j.dmpk.2025.101147","url":null,"abstract":"","PeriodicalId":11298,"journal":{"name":"Drug Metabolism and Pharmacokinetics","volume":"61 ","pages":"Article 101147"},"PeriodicalIF":2.7,"publicationDate":"2025-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144195722","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Investigation of pilocarpine oxidative and hydrolytic metabolism in chimeric mice with humanized liver 人肝嵌合小鼠匹罗卡品氧化和水解代谢的研究
IF 2.7 4区 医学
Drug Metabolism and Pharmacokinetics Pub Date : 2025-06-01 Epub Date: 2025-04-14 DOI: 10.1016/j.dmpk.2025.101484
Shotaro Uehara , Yuichiro Higuchi , Nao Yoneda , Hiroshi Yamazaki , Hiroshi Suemizu
{"title":"Investigation of pilocarpine oxidative and hydrolytic metabolism in chimeric mice with humanized liver","authors":"Shotaro Uehara ,&nbsp;Yuichiro Higuchi ,&nbsp;Nao Yoneda ,&nbsp;Hiroshi Yamazaki ,&nbsp;Hiroshi Suemizu","doi":"10.1016/j.dmpk.2025.101484","DOIUrl":"10.1016/j.dmpk.2025.101484","url":null,"abstract":"<div><div>Chimeric mice with humanized liver (humanized-liver mice) are an attractive alternative to conventional animals for predicting pharmacokinetics in humans. We aimed to investigate the role of CYP2A6 and PON1 on pilocarpine biotransformation in humanized-liver mice. Following a single oral dose of 10 mg/kg, higher plasma concentrations of pilocarpine and 3-hydroxypilocarpine were observed in humanized-liver mice than in non-humanized mice. The ratios of area under the curve (AUC) to total AUC for pilocarpine in humanized-liver mice were more similar to those observed in humans with extensive metabolizer phenotypes for CYP2A6 compared to those in non-humanized mice for both 3-hydroxypilocarpine and pilocarpic acid. Pilocarpine 3-hydroxylase activity in liver microsomes was higher in humanized-liver mice than in non-humanized mice, whereas the pilocarpine hydrolase activity in plasma was comparable between both groups. CYP2A6 levels and pilocarpine 3-hydroxylase activities in liver microsomes from humanized-liver mice were correlated (<em>P</em> = 0.04). Furthermore, both hepatic microsomal 3-hydroxylase and plasma hydrolase activities of pilocarpine in humanized-liver mice decreased in the presence of respective human CYP2A6 or PON1 inhibitors. The plasma metabolite profiles of pilocarpine in humanized-liver mice were similar to those in humans, highlighting the suitability of humanized-liver mice for investigating CYP2A6-and PON1-dependent drug biotransformation in humans.</div></div>","PeriodicalId":11298,"journal":{"name":"Drug Metabolism and Pharmacokinetics","volume":"62 ","pages":"Article 101484"},"PeriodicalIF":2.7,"publicationDate":"2025-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144230645","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Addressing the challenges of determining fraction metabolized for low turnover drugs – An update from the quantitative fraction metabolized working group of the IQ consortium 解决确定低周转率药物代谢分数的挑战-来自IQ联盟定量代谢分数工作组的更新
IF 2.7 4区 医学
Drug Metabolism and Pharmacokinetics Pub Date : 2025-06-01 Epub Date: 2025-06-03 DOI: 10.1016/j.dmpk.2025.101146
Lawrence Cohen , Priscilla Brun , Upendra Dahal , Angela Doran , Sarah Glass , Niresh Hariparsad , Felix Huth , Gary Jenkins , Charles Locuson , Birk Poller , Lilian Richter , Dustin Smith
{"title":"Addressing the challenges of determining fraction metabolized for low turnover drugs – An update from the quantitative fraction metabolized working group of the IQ consortium","authors":"Lawrence Cohen ,&nbsp;Priscilla Brun ,&nbsp;Upendra Dahal ,&nbsp;Angela Doran ,&nbsp;Sarah Glass ,&nbsp;Niresh Hariparsad ,&nbsp;Felix Huth ,&nbsp;Gary Jenkins ,&nbsp;Charles Locuson ,&nbsp;Birk Poller ,&nbsp;Lilian Richter ,&nbsp;Dustin Smith","doi":"10.1016/j.dmpk.2025.101146","DOIUrl":"10.1016/j.dmpk.2025.101146","url":null,"abstract":"","PeriodicalId":11298,"journal":{"name":"Drug Metabolism and Pharmacokinetics","volume":"61 ","pages":"Article 101146"},"PeriodicalIF":2.7,"publicationDate":"2025-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144195025","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Confounding effects of B-glucuronidase on UDP-Glucuronosyltransferase stability: Development of a modified metabolic stability assay to enable SAR for a discovery program b -葡糖醛酸酶对udp -葡糖醛酸基转移酶稳定性的混淆影响：开发一种改进的代谢稳定性测定方法，使SAR能够用于发现计划
IF 2.7 4区 医学
Drug Metabolism and Pharmacokinetics Pub Date : 2025-06-01 Epub Date: 2025-06-03 DOI: 10.1016/j.dmpk.2025.101150
Sarah Glass, Isaiah Swauncy, Annie Caudle, Kevin Coe
{"title":"Confounding effects of B-glucuronidase on UDP-Glucuronosyltransferase stability: Development of a modified metabolic stability assay to enable SAR for a discovery program","authors":"Sarah Glass,&nbsp;Isaiah Swauncy,&nbsp;Annie Caudle,&nbsp;Kevin Coe","doi":"10.1016/j.dmpk.2025.101150","DOIUrl":"10.1016/j.dmpk.2025.101150","url":null,"abstract":"","PeriodicalId":11298,"journal":{"name":"Drug Metabolism and Pharmacokinetics","volume":"61 ","pages":"Article 101150"},"PeriodicalIF":2.7,"publicationDate":"2025-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144195224","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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