Quantitative Prediction of Drug-Drug Interactions Caused by CYP3A Induction Using Endogenous Biomarker 4 β-Hydroxycholesterol [0.03%]
利用内源性生物标志物4β-羟基胆固醇定量预测由细胞色素P450 3A诱导引起的药物相互作用
Hiroaki Takubo,Toshio Taniguchi,Yukihiro Nomura
Hiroaki Takubo
Evaluation of the CYP3A induction risk is important in early drug development stages. This study focused on 4β-hydroxycholesterol (4β-HC) as an endogenous biomarker of drug-drug interactions (DDIs) caused by CYP3A induction. We investigat...
Utilization of a Human Liver Tissue Chip for Drug-Metabolizing Enzyme Induction Studies of Perpetrator and Victim Drugs [0.03%]
用于施害者和受害者药物诱导研究的人肝组织芯片的使用
Shivam Ohri,Paarth Parekh,Lauren Nichols et al.
Shivam Ohri et al.
Polypharmacy-related drug-drug interactions (DDIs) are a significant and growing healthcare concern. An increasing number of therapeutic drugs on the market underscores the necessity to accurately assess new drug combinations during pre-cli...
Early Prediction and Impact Assessment of CYP3A4-Related Drug-Drug Interactions for Small-Molecule Anticancer Drugs Using Human-CYP3A4-Transgenic Mouse Models [0.03%]
基于人CYP3A4转基因小鼠模型的抗肿瘤药物相互作用早期预测及影响评估研究
David Damoiseaux,Jos H Beijnen,Alwin D R Huitema et al.
David Damoiseaux et al.
Early detection of drug-drug interactions (DDIs) can facilitate timely drug development decisions, prevent unnecessary restrictions on patient enrollment, resulting in clinical study populations that are not representative of the indicated ...
CYP P450 and non-CYP P450 Drug Metabolizing Enzyme Families Exhibit Differential Sensitivities towards Proinflammatory Cytokine Modulation [0.03%]
细胞色素P450酶和非细胞色素P450药物代谢酶家族对促炎细胞因子调节的不同敏感性
Laura M de Jong,Chandan Harpal,Dirk-Jan van den Berg et al.
Laura M de Jong et al.
Compromised hepatic drug metabolism in response to proinflammatory cytokine release is primarily attributed to downregulation of cytochrome P450 (CYP) enzymes. However, whether inflammation also affects other phase I and phase II drug metab...
Differential Selectivity of Human and Mouse ABCC4/Abcc4 for Arsenic Metabolites [0.03%]
人和小鼠ABCC4/Abcc4对砷代射物的不同选择性
Brayden D Whitlock,Yingze Ma,Gwenaëlle Conseil et al.
Brayden D Whitlock et al.
Millions of people globally are exposed to the proven human carcinogen arsenic at unacceptable levels in drinking water. In contrast, arsenic is a poor rodent carcinogen, requiring >100-fold higher doses for tumor induction, which may be ex...
Absorption, Distribution, Metabolism, and Excretion of Icenticaftor (QBW251) in Healthy Male Volunteers at Steady State and In Vitro Phenotyping of Major Metabolites [0.03%]
艾塞曲韦（QBW251）在健康男性受试者中的稳态吸收、分布、代谢和排泄以及主要代谢产物的体外表型分析
Ulrike Glaenzel,Felix Huth,Fabian Eggimann et al.
Ulrike Glaenzel et al.
Icenticaftor (QBW251) is a potentiator of the cystic fibrosis transmembrane conductance regulator protein and is currently in clinical development for the treatment of chronic obstructive pulmonary disease and chronic bronchitis. An absorpt...
Age-Dependent Changes in Cytochrome P450 Abundance and Composition in Human Liver [0.03%]
人肝脏中年龄依赖性的细胞色素P450含量和组成的改变
Sandhya Subash,Bhagwat Prasad
Sandhya Subash
Cytochrome P450 (CYP) superfamily represents the major drug-metabolizing enzymes responsible for metabolizing over 65% of therapeutic drugs, including those for pediatric use. CYP-ontogeny based physiologically based pharmacokinetic (PBPK) ...
3- epi-18 β-Glycyrrhetinic Acid or Its Glucuronide, the Metabolites of Glycyrrhizinic Acid with Individual Differences, Correlated with Diagnostic Marker for Licorice-Induced Pseudoaldosteronism in Humans [0.03%]
甘草酸的代谢产物甘草次酸或其葡萄糖醛酸结合物与个体差异有关，可作为人类伪 aldosteronism 的诊断标志物
Ryota Sakoda,Kan&#x;ichiro Ishiuchi,Tetsuhiro Yoshino et al.
Ryota Sakoda et al.
Licorice is a crude drug that is used in traditional Japanese Kampo medicine and is also used as a sweetener. Occasionally, it causes pseudoaldosteronism (PsA) as a side effect. The major symptoms include hypokalemia, hypertension, edema, a...
Functional Characterization of Reduced Folate Carrier and Protein-Coupled Folate Transporter for Antifolates Accumulation in Non-Small Cell Lung Cancer Cells [0.03%]
非小细胞肺癌细胞的叶酸抗代谢物蓄积对叶酸运载蛋白及配体偶联叶酸转运蛋白的功能表征
Yuqing Wang,Jun Luo,Mengru Bai et al.
Yuqing Wang et al.
Antifolates are important for chemotherapy in non-small cell lung cancer (NSCLC). They mainly rely on reduced folate carrier (RFC) and proton-coupled folate transporter (PCFT) to enter cells. PCFT is supposed to be the dominant transporter ...
Quantitatively Predicting Effects of Exercise on Pharmacokinetics of Drugs Using a Physiologically Based Pharmacokinetic Model [0.03%]
基于生理的药代动力学模型定量预测运动对药物药代动力学影响
Zeyu Guo,Jingjing Gao,Li Liu et al.
Zeyu Guo et al.
Exercise significantly alters human physiological functions, such as increasing cardiac output and muscle blood flow and decreasing glomerular filtration rate (GFR) and liver blood flow, thereby altering the absorption, distribution, metabo...