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Enhanced effect of ionic liquid on intestinal absorption of macromolecules (< 10 kDa) 离子液体对肠道大分子(< 10 kDa)吸收的促进作用
IF 2.7 4区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2025-06-01 DOI: 10.1016/j.dmpk.2025.101137
Shoichiro Fukuda , Haruka Takata , Takashi Nakae , Noboru Tatsumi , Hidetoshi Hamamoto , Hidenori Ando , Tatsuhiro Ishida
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引用次数: 0
Utilizing PBPK modeling and in vitro data for predicting complex DDIS of OATP1B and CYP substrates caused by various perpetrators 利用PBPK模型和体外数据预测多种作案者引起的OATP1B和CYP底物的复杂DDIS
IF 2.7 4区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2025-06-01 DOI: 10.1016/j.dmpk.2025.101082
Yuichi Sugiyama
{"title":"Utilizing PBPK modeling and in vitro data for predicting complex DDIS of OATP1B and CYP substrates caused by various perpetrators","authors":"Yuichi Sugiyama","doi":"10.1016/j.dmpk.2025.101082","DOIUrl":"10.1016/j.dmpk.2025.101082","url":null,"abstract":"","PeriodicalId":11298,"journal":{"name":"Drug Metabolism and Pharmacokinetics","volume":"61 ","pages":"Article 101082"},"PeriodicalIF":2.7,"publicationDate":"2025-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144194470","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
Implementation of blood collection using the Tasso microsampling device to measure thyroid hormone biomarkers 利用Tasso微采样装置采集血液,测量甲状腺激素生物标志物
IF 2.7 4区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2025-06-01 DOI: 10.1016/j.dmpk.2025.101145
Chad Christianson, Brooke Whitson, Jason Watts, Jennifer Zimmer
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引用次数: 0
Assessment of ADME and DDI for LNP-MRNA therapeutics 评估ADME和DDI对LNP-MRNA治疗的影响
IF 2.7 4区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2025-06-01 DOI: 10.1016/j.dmpk.2025.101084
Lei Ci
{"title":"Assessment of ADME and DDI for LNP-MRNA therapeutics","authors":"Lei Ci","doi":"10.1016/j.dmpk.2025.101084","DOIUrl":"10.1016/j.dmpk.2025.101084","url":null,"abstract":"","PeriodicalId":11298,"journal":{"name":"Drug Metabolism and Pharmacokinetics","volume":"61 ","pages":"Article 101084"},"PeriodicalIF":2.7,"publicationDate":"2025-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144194472","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
Improving ADME properties of therapeutic antibodies by novel engineering technologies 利用新的工程技术改善治疗性抗体的ADME特性
IF 2.7 4区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2025-06-01 DOI: 10.1016/j.dmpk.2025.101086
Kenta Haraya
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引用次数: 0
Investigation of the mechanism of metronidazole-induced encephalopathy focusing on the possible effect on thiamine transport 甲硝唑致脑病机制的研究重点是对硫胺素运输的可能影响
IF 2.7 4区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2025-06-01 DOI: 10.1016/j.dmpk.2025.101130
Yoshiaki Yamagishi, Mitsuhiro Hashimoto, Miyuki Sugita, Satomi Watanabe, Nana Sekine, Yuki Takahashi, Yasuko Ogawa, Toshiyuki Kudo, Kiyomi Ito
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引用次数: 0
Uncovering Target-Mediated Drug Disposition (TMDD) of small molecule brain penetrant EBP inhibitors 揭示小分子脑渗透EBP抑制剂的靶介导药物处置(TMDD)
IF 2.7 4区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2025-06-01 DOI: 10.1016/j.dmpk.2025.101107
Laurent Salphati
{"title":"Uncovering Target-Mediated Drug Disposition (TMDD) of small molecule brain penetrant EBP inhibitors","authors":"Laurent Salphati","doi":"10.1016/j.dmpk.2025.101107","DOIUrl":"10.1016/j.dmpk.2025.101107","url":null,"abstract":"","PeriodicalId":11298,"journal":{"name":"Drug Metabolism and Pharmacokinetics","volume":"61 ","pages":"Article 101107"},"PeriodicalIF":2.7,"publicationDate":"2025-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144194666","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
Model-based meta-analysis of ethnic differences - General changes in clearance by pathways and aging 基于模型的种族差异荟萃分析-清除途径和衰老的一般变化
IF 2.7 4区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2025-06-01 DOI: 10.1016/j.dmpk.2025.101111
Akihiro Hisaka
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引用次数: 0
Does cannabidiol (CBD) or delta-9-tetrahydrocannabinol (THC) induce drug metabolizing enzymes in human hepatocytes? 大麻二酚(CBD)或德尔塔-9-四氢大麻酚(THC)诱导人肝细胞药物代谢酶吗?
IF 2.7 4区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2025-06-01 DOI: 10.1016/j.dmpk.2025.101126
Ankit Balhara, Yik Pui Tsang, Jashvant D. Unadkat
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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 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2025-06-01 DOI: 10.1016/j.dmpk.2025.101484
Shotaro Uehara , Yuichiro Higuchi , Nao Yoneda , Hiroshi Yamazaki , Hiroshi Suemizu
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 (P = 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.
人源化肝脏嵌合小鼠(人源化肝脏小鼠)是预测人体内药代动力学的一种有吸引力的替代方法。我们的目的是研究CYP2A6和PON1在人源肝小鼠匹罗卡品生物转化中的作用。单次口服剂量为10 mg/kg后,在人源化肝脏小鼠中观察到比非人源化小鼠更高的血浆浓度匹罗卡品和3-羟基匹罗卡品。与在非人源化小鼠中观察到的3-羟基匹罗卡品和匹罗卡酸相比,在人源化肝脏小鼠中,匹罗卡品的曲线下面积(AUC)与总AUC的比值更接近于在CYP2A6代谢表型广泛的人类中观察到的结果。人源化小鼠肝微粒体中的匹罗卡品3-羟化酶活性高于非人源化小鼠,而血浆中的匹罗卡品水解酶活性在两组之间具有可比性。人源化肝小鼠肝微粒体中CYP2A6水平与匹罗卡品3-羟化酶活性呈正相关(P = 0.04)。此外,在人CYP2A6或PON1抑制剂存在的情况下,人源化肝脏小鼠的肝微粒体3-羟化酶和血浆匹罗卡品水解酶活性均下降。在人源化肝小鼠中,匹罗卡品的血浆代谢物谱与人类相似,这突出了人源化肝小鼠用于研究人类cyp2a6和pon1依赖性药物生物转化的适用性。
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引用次数: 0
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Drug Metabolism and Pharmacokinetics
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