Drug Metabolism and Pharmacokinetics最新文献_第10页

Validation of QPCR method to detect human cells in mouse and rat tissues 小鼠和大鼠组织中检测人细胞的QPCR方法的验证

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.2025.101143

Kuniyoshi Abe, Haruka Inoue, Yuka Torikai, Naoki Kaname, Seulgi Lee, Akiko Suzuki, Yukiko Arimura, Yurie Okawa, Tetsuya Yoshikawa

引用次数: 0

Why and when do i use PBPK modeling 为什么以及何时使用PBPK建模

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.2025.101060

Kunal Taskar

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Species specificity and selection of animal models for drug oxygenations differently contributed by polymorphic human enzymes 多态酶对药物氧合作用的物种特异性和动物模型的选择

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.2025.101105

Hiroshi Yamazaki

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Drug-induced gastrointestinal toxicity due to disruption of the interinfluence between serotonin and gut microbiota 5 -羟色胺与肠道微生物群之间相互影响的破坏引起的药物诱导胃肠道毒性

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.2025.101121

Suguru Asaji , Yuta Funai , Yuta Seki , Kotone Banba , Jun Hida , Ikumi Tamai , Yoshiyuki Shirasaka

引用次数: 0

Preclinical DDI risk assessment in drug discovery and development 药物发现和开发中的临床前DDI风险评估

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.2025.101080

Niresh Hariparsad

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In vitro liver models for toxicological research 体外肝模型毒理学研究

IF 2.7 4区医学

Drug Metabolism and Pharmacokinetics Pub Date : 2025-06-01 Epub Date: 2025-03-13 DOI: 10.1016/j.dmpk.2025.101478

Ichiro Fukunaga , Takanori Takebe

{"title":"In vitro liver models for toxicological research","authors":"Ichiro Fukunaga , Takanori Takebe","doi":"10.1016/j.dmpk.2025.101478","DOIUrl":"10.1016/j.dmpk.2025.101478","url":null,"abstract":"<div><div>Drug-induced liver injury (DILI) presents a major challenge not only in new drug development but also in post-marketing withdrawals and the safety of food, cosmetics, and chemicals. Experimental model organisms such as the rodents have been widely used for preclinical toxicological testing. However, the tension exists associated with the ethical and sustainable use of animals in part because animals do not necessarily inform the human-specific ADME (adsorption, dynamics, metabolism and elimination) profiling. To establish alternative models in humans, in vitro hepatic tissue models have been proposed, ranging from primary hepatocytes, immortal hepatocytes, to the development of new cell resources such as stem cell-derived hepatocytes. Given the evolving number of novel alternative methods, understanding possible combinations of cell sources and culture methods will be crucial to develop the context-of-use assays. This review primarily focuses on 3D liver organoid models for conducting. We will review the relevant cell sources, bioengineering methods, selection of training compounds, and biomarkers towards the rationale design of in vitro toxicology testing.</div></div>","PeriodicalId":11298,"journal":{"name":"Drug Metabolism and Pharmacokinetics","volume":"62 ","pages":"Article 101478"},"PeriodicalIF":2.7,"publicationDate":"2025-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143799927","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

Exploring the effect of intracellular loop 1 genetic variants in human ABCG2 on transport activity and protein abundance 探讨人ABCG2细胞内环1遗传变异对转运活性和蛋白丰度的影响

IF 2.7 4区医学

Drug Metabolism and Pharmacokinetics Pub Date : 2025-06-01 Epub Date: 2025-03-15 DOI: 10.1016/j.dmpk.2025.101482

Noora Sjöstedt , Ritchie G.M. Timmermans , Marika Vieraankivi , Laura Suominen , Kati-Sisko Vellonen , Madhushree Bhattacharya , Seppo Auriola , Heidi Kidron

{"title":"Exploring the effect of intracellular loop 1 genetic variants in human ABCG2 on transport activity and protein abundance","authors":"Noora Sjöstedt , Ritchie G.M. Timmermans , Marika Vieraankivi , Laura Suominen , Kati-Sisko Vellonen , Madhushree Bhattacharya , Seppo Auriola , Heidi Kidron","doi":"10.1016/j.dmpk.2025.101482","DOIUrl":"10.1016/j.dmpk.2025.101482","url":null,"abstract":"<div><div>ABCG2 (breast cancer resistance protein, BCRP), can affect drug disposition, and thus, variation in the <em>ABCG2</em> gene may alter drug exposure. We studied non-synonymous naturally occurring single-nucleotide variants (SNVs) in intracellular loop 1 (ICL1), which contains a coupling helix that transmits conformational changes in the protein. Reference ABCG2, the common SNVs V12M and Q141K, and five SNVs (K453R, I456V, H457R, G462R and G462V) in ICL1 were expressed in HEK293 cells. Additionally, combinations of selected SNVs were expressed to determine if an activating substitution in ICL1 could compensate for an inactivating substitution elsewhere. Transport of Lucifer yellow, estrone sulfate and rosuvastatin was studied using membrane vesicles and the ABCG2 abundance was quantified. While K453R and I456V abundance was similar to the reference ABCG2, abundance was lower for H457R and G462R/V. Apparent transport activities were partially substrate dependent, but excluding G462R/V, the ICL variants transported at least one of the substrates similarly to the reference ABCG2. In double substitutions, I456V had a more consistent effect than H457R on both transport activity and protein abundance. Altogether, SNVs in ICL1 can have both detrimental and beneficial effects on ABCG2 activity. Effects may be hard to predict, especially if more than one SNV is present.</div></div>","PeriodicalId":11298,"journal":{"name":"Drug Metabolism and Pharmacokinetics","volume":"62 ","pages":"Article 101482"},"PeriodicalIF":2.7,"publicationDate":"2025-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143791013","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Review of finalized ICH M12 guideline on drug interaction studies 对ICH M12药物相互作用研究指南定稿的审查

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.2025.101079

Akihiro Ishiguro

引用次数: 0

A tale of preclinical insights into bile salt homeostasis disruption in DILI DILI患者胆盐稳态紊乱的临床前研究

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.2025.101108

Yurong Lai

引用次数: 0

Current status of Imaging Mass Spectrometry in drug discovery and development: A survey highlighting technical challenges and future directions 成像质谱在药物发现和开发中的现状：突出技术挑战和未来方向的调查

IF 2.7 4区医学

Drug Metabolism and Pharmacokinetics Pub Date : 2025-06-01 Epub Date: 2025-04-17 DOI: 10.1016/j.dmpk.2025.101485

Yukari Tanaka , Hiroyuki Yokoi , Hidefumi Kaji , Yoko Urasaki , Masanobu Nishidate , Shin-ichiro Nitta , Kenichi Watanabe , Tomomi Ishida , Kouji Tanaka , Rika Komatsu , Kenji Yoshida , Kosuke Saito , Yoshiro Saito , Hiroshi Yamazaki

{"title":"Current status of Imaging Mass Spectrometry in drug discovery and development: A survey highlighting technical challenges and future directions","authors":"Yukari Tanaka , Hiroyuki Yokoi , Hidefumi Kaji , Yoko Urasaki , Masanobu Nishidate , Shin-ichiro Nitta , Kenichi Watanabe , Tomomi Ishida , Kouji Tanaka , Rika Komatsu , Kenji Yoshida , Kosuke Saito , Yoshiro Saito , Hiroshi Yamazaki","doi":"10.1016/j.dmpk.2025.101485","DOIUrl":"10.1016/j.dmpk.2025.101485","url":null,"abstract":"<div><div>Imaging mass spectrometry (IMS) is used in various fields of pharmaceutical research and development, including the targeted delivery of administered drugs, drug distribution in tissues, drug toxicity analysis, and disease mechanisms. However, IMS is a relatively new technology that requires further validation before being accepted by authorities for regulatory compliance of new drugs. In 2020, an international survey was conducted in collaboration with the Imaging Mass Spectrometry Society (IMSS) and the Japan Association for Imaging Mass Spectrometry (JAIMS) to understand the status of IMS and to identify problems with its application. The survey revealed technical challenges in sample preparation, quantitative analysis of drugs in tissues, and data acquisition. Based on the 2020 survey results, we recently conducted a further detailed survey and had discussions within the JAIMS aimed at translating the results into specific experimental procedures and proposing feasible standard methods. This survey involved detailed questions on five themes: sample collection and storage, tissue section preparation, sample preparation, data analysis (including quantitative analysis and data correction methods), and data reproducibility. The questions were answered by JAIMS members working for ten companies. To resolve technical issues identified by the survey, we propose some realistic approaches toward standardization.</div></div>","PeriodicalId":11298,"journal":{"name":"Drug Metabolism and Pharmacokinetics","volume":"62 ","pages":"Article 101485"},"PeriodicalIF":2.7,"publicationDate":"2025-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"143935162","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