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Drug Metabolism and Pharmacokinetics最新文献

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Population pharmacokinetic analysis of sirolimus in Japanese pediatric and adult subjects receiving tablet or granule formulations. 西罗莫司在接受片剂或颗粒剂治疗的日本儿童和成人受试者中的群体药代动力学分析。
IF 2.7 4区 医学 Q2 PHARMACOLOGY & PHARMACY
Drug Metabolism and Pharmacokinetics
Pub Date : 2024-05-31 DOI: 10.1016/j.dmpk.2024.101024
Taichi Miyazaki, Daichi Hayashi, Akifumi Nozawa, Shiho Yasue, Saori Endo, Hidenori Ohnishi, Ryuta Asada, Mototoshi Kato, Akihiro Fujino, Tatsuo Kuroda, Takanobu Maekawa, Shigehisa Fumino, Naonori Kawakubo, Tatsuro Tajiri, Kenji Shimizu, Chihiro Sanada, Izumi Hamada, Yuko Ishikawa, Mayumi Hasegawa, Kashyap Patel, Yehua Xie, Michio Ozeki

A population pharmacokinetic (PopPK) analysis was conducted using data from 215 Japanese administered oral sirolimus (tablet and granule) including healthy subjects and patients with intractable vascular anomalies and other diseases. The analysis included neonates, infants, and adults, and identified covariates that influence sirolimus pharmacokinetics (PK). The final model was used to predict sirolimus trough concentrations for various dosing regimens and covariates of interest. The results showed that sirolimus trough concentrations were predicted to increase with higher levels of hemoglobin, and that the granule formulation had a 1.23-fold higher exposure than the tablet formulation. Coadministration of CYP3A4 inducers was found to decrease trough concentrations by 54 %. The PK simulations showed that administration of the granule formulation at doses of 0.02, 0.04, 0.06, and 0.08 mg/kg/day in ages <3 months, 3 to <6 months, 6 to <12 months, and ≥1 year, respectively, resulted in >70 % target attainment within the therapeutic trough concentration range (5-15 ng/mL). In conclusion, incorporation of time-varying covariates (body weight and age) into the PopPK model appropriately predicted sirolimus concentrations in Japanese subjects from infants to adult sub-populations. This PopPK model would therefore be able to provide a reference for clinical individualization of sirolimus dosing.

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引用次数: 0
Exploring the human 3D small intestinal model (epiintestinaltm) for improved prediction of oral absorption, metabolism and complex drug-drug interactions of small molecule drugs 探索人体三维小肠模型（epiintestinaltm），以改进小分子药物的口服吸收、代谢和复杂的药物相互作用预测
IF 2.1 4区 医学 Q2 PHARMACOLOGY & PHARMACY
Drug Metabolism and Pharmacokinetics
Pub Date : 2024-05-13 DOI: 10.1016/j.dmpk.2023.100908
Paresh Chothe, Andrea Whitcher-Johnstone, Niresh Hariparsad, Diane Ramsden
{"title":"Exploring the human 3D small intestinal model (epiintestinaltm) for improved prediction of oral absorption, metabolism and complex drug-drug interactions of small molecule drugs","authors":"Paresh Chothe, Andrea Whitcher-Johnstone, Niresh Hariparsad, Diane Ramsden","doi":"10.1016/j.dmpk.2023.100908","DOIUrl":"https://doi.org/10.1016/j.dmpk.2023.100908","url":null,"abstract":"","PeriodicalId":11298,"journal":{"name":"Drug Metabolism and Pharmacokinetics","volume":null,"pages":null},"PeriodicalIF":2.1,"publicationDate":"2024-05-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141504158","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
Plasma protein binding in special populations: do current PBPK models correctly account for potential changes to fraction unbound? 特殊人群的血浆蛋白结合：当前的 PBPK 模型是否正确地考虑了未结合部分的潜在变化？
IF 2.1 4区 医学 Q2 Pharmacology, Toxicology and Pharmaceutics
Drug Metabolism and Pharmacokinetics
Pub Date : 2024-05-13 DOI: 10.1016/j.dmpk.2023.100976
Jokha Al-Qassabi, Shawn Tan, Aleksandra Galetin, Amin Rostami-Hodjegan, Daniel Scotcher
{"title":"Plasma protein binding in special populations: do current PBPK models correctly account for potential changes to fraction unbound?","authors":"Jokha Al-Qassabi, Shawn Tan, Aleksandra Galetin, Amin Rostami-Hodjegan, Daniel Scotcher","doi":"10.1016/j.dmpk.2023.100976","DOIUrl":"https://doi.org/10.1016/j.dmpk.2023.100976","url":null,"abstract":"","PeriodicalId":11298,"journal":{"name":"Drug Metabolism and Pharmacokinetics","volume":null,"pages":null},"PeriodicalIF":2.1,"publicationDate":"2024-05-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141058820","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
Understanding CYP3A4 and P-GP mediated drug-drug interactions through PBPK modeling - case example of pralsetinib 通过 PBPK 建模了解 CYP3A4 和 P-GP 介导的药物间相互作用--普拉塞替尼案例
IF 2.1 4区 医学 Q2 Pharmacology, Toxicology and Pharmaceutics
Drug Metabolism and Pharmacokinetics
Pub Date : 2024-05-13 DOI: 10.1016/j.dmpk.2023.100969
Christine Bowman, Michael Dolton, Fang Ma, Sravanthi Cheeti, Denison Kuruvilla, Rucha Sane, Nastya Kassir, Yuan Chen
{"title":"Understanding CYP3A4 and P-GP mediated drug-drug interactions through PBPK modeling - case example of pralsetinib","authors":"Christine Bowman, Michael Dolton, Fang Ma, Sravanthi Cheeti, Denison Kuruvilla, Rucha Sane, Nastya Kassir, Yuan Chen","doi":"10.1016/j.dmpk.2023.100969","DOIUrl":"https://doi.org/10.1016/j.dmpk.2023.100969","url":null,"abstract":"","PeriodicalId":11298,"journal":{"name":"Drug Metabolism and Pharmacokinetics","volume":null,"pages":null},"PeriodicalIF":2.1,"publicationDate":"2024-05-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141058822","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
Strategies for DDI risk assessment between novel oncology agents and combination generic standard of care (SOC) agents 新型肿瘤药物与普通标准疗法 (SOC) 联合用药之间的 DDI 风险评估策略
IF 2.1 4区 医学 Q2 Pharmacology, Toxicology and Pharmaceutics
Drug Metabolism and Pharmacokinetics
Pub Date : 2024-05-13 DOI: 10.1016/j.dmpk.2023.100945
Ravi Visswanathan, Elaine Tseng, Loretta Cox, Julie Cianfrogna, R. Scott Obach, Rhys Jones
{"title":"Strategies for DDI risk assessment between novel oncology agents and combination generic standard of care (SOC) agents","authors":"Ravi Visswanathan, Elaine Tseng, Loretta Cox, Julie Cianfrogna, R. Scott Obach, Rhys Jones","doi":"10.1016/j.dmpk.2023.100945","DOIUrl":"https://doi.org/10.1016/j.dmpk.2023.100945","url":null,"abstract":"","PeriodicalId":11298,"journal":{"name":"Drug Metabolism and Pharmacokinetics","volume":null,"pages":null},"PeriodicalIF":2.1,"publicationDate":"2024-05-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141058864","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
Biotransformation of protein degraders bavdegalutamide and XL01126 in permeabilized cryopreserved human hepatocytes 蛋白质降解剂巴夫地加鲁胺和 XL01126 在透化低温保存的人肝细胞中的生物转化
IF 2.1 4区 医学 Q2 Pharmacology, Toxicology and Pharmaceutics
Drug Metabolism and Pharmacokinetics
Pub Date : 2024-05-13 DOI: 10.1016/j.dmpk.2023.100934
Bin Ma, Susan Wong, Joyce Liu, Jingwei Cai, Cyrus Khojasteh, Donglu Zhang
{"title":"Biotransformation of protein degraders bavdegalutamide and XL01126 in permeabilized cryopreserved human hepatocytes","authors":"Bin Ma, Susan Wong, Joyce Liu, Jingwei Cai, Cyrus Khojasteh, Donglu Zhang","doi":"10.1016/j.dmpk.2023.100934","DOIUrl":"https://doi.org/10.1016/j.dmpk.2023.100934","url":null,"abstract":"","PeriodicalId":11298,"journal":{"name":"Drug Metabolism and Pharmacokinetics","volume":null,"pages":null},"PeriodicalIF":2.1,"publicationDate":"2024-05-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141058861","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
Tenofovir activation is diminished in the brain and liver of creatine kinase brain-type knockout mice 脑型肌酸激酶基因敲除小鼠的大脑和肝脏中替诺福韦的激活作用减弱
IF 2.1 4区 医学 Q2 Pharmacology, Toxicology and Pharmaceutics
Drug Metabolism and Pharmacokinetics
Pub Date : 2024-05-13 DOI: 10.1016/j.dmpk.2023.100956
Colten Eberhard, Benjamin Orsburn, Namandjé Bumpus
{"title":"Tenofovir activation is diminished in the brain and liver of creatine kinase brain-type knockout mice","authors":"Colten Eberhard, Benjamin Orsburn, Namandjé Bumpus","doi":"10.1016/j.dmpk.2023.100956","DOIUrl":"https://doi.org/10.1016/j.dmpk.2023.100956","url":null,"abstract":"","PeriodicalId":11298,"journal":{"name":"Drug Metabolism and Pharmacokinetics","volume":null,"pages":null},"PeriodicalIF":2.1,"publicationDate":"2024-05-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141058857","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
Prevention of irinotecan-induced intestinal toxicity by locally bioavailable herbal components via maintaining gut oxidative stress homeostasis 局部生物活性草药成分通过维持肠道氧化应激平衡预防伊立替康诱导的肠道毒性
IF 2.1 4区 医学 Q2 PHARMACOLOGY & PHARMACY
Drug Metabolism and Pharmacokinetics
Pub Date : 2024-05-13 DOI: 10.1016/j.dmpk.2023.100892
Vesna Tumbas Saponjac, Rongjin Sun, Zicong Zheng, Jie Chen, Songpol Srinual, Ming Hu, Rashim Singh
{"title":"Prevention of irinotecan-induced intestinal toxicity by locally bioavailable herbal components via maintaining gut oxidative stress homeostasis","authors":"Vesna Tumbas Saponjac, Rongjin Sun, Zicong Zheng, Jie Chen, Songpol Srinual, Ming Hu, Rashim Singh","doi":"10.1016/j.dmpk.2023.100892","DOIUrl":"https://doi.org/10.1016/j.dmpk.2023.100892","url":null,"abstract":"","PeriodicalId":11298,"journal":{"name":"Drug Metabolism and Pharmacokinetics","volume":null,"pages":null},"PeriodicalIF":2.1,"publicationDate":"2024-05-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141518091","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
Exposure to mixed microplastic particles altered the fecal microbiome and its associated predictive functional pathways in mice 暴露于混合微塑料颗粒会改变小鼠的粪便微生物群及其相关的预测功能途径
IF 2.1 4区 医学 Q2 PHARMACOLOGY & PHARMACY
Drug Metabolism and Pharmacokinetics
Pub Date : 2024-05-13 DOI: 10.1016/j.dmpk.2023.100928
Kyle Kim, Julia Cui, Haiwei Gu, Marcus Garcia, Matthew Campen, Eliseo Castillo, Aaron Romero
{"title":"Exposure to mixed microplastic particles altered the fecal microbiome and its associated predictive functional pathways in mice","authors":"Kyle Kim, Julia Cui, Haiwei Gu, Marcus Garcia, Matthew Campen, Eliseo Castillo, Aaron Romero","doi":"10.1016/j.dmpk.2023.100928","DOIUrl":"https://doi.org/10.1016/j.dmpk.2023.100928","url":null,"abstract":"","PeriodicalId":11298,"journal":{"name":"Drug Metabolism and Pharmacokinetics","volume":null,"pages":null},"PeriodicalIF":2.1,"publicationDate":"2024-05-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141504156","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
Identification and characterization of erlotinib as a potent mechanism-based inactivator of human aldehyde oxidase 厄洛替尼作为基于机制的人类醛氧化酶强效失活剂的鉴定和表征
IF 2.1 4区 医学 Q2 Pharmacology, Toxicology and Pharmaceutics
Drug Metabolism and Pharmacokinetics
Pub Date : 2024-05-13 DOI: 10.1016/j.dmpk.2023.100952
Ryan A. Dick, Xiaomin Liang, Hailing Sun, Bernard P. Murray, Bill J. Smith
{"title":"Identification and characterization of erlotinib as a potent mechanism-based inactivator of human aldehyde oxidase","authors":"Ryan A. Dick, Xiaomin Liang, Hailing Sun, Bernard P. Murray, Bill J. Smith","doi":"10.1016/j.dmpk.2023.100952","DOIUrl":"https://doi.org/10.1016/j.dmpk.2023.100952","url":null,"abstract":"","PeriodicalId":11298,"journal":{"name":"Drug Metabolism and Pharmacokinetics","volume":null,"pages":null},"PeriodicalIF":2.1,"publicationDate":"2024-05-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141058859","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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