Glutathione-reversible inactivation of aldehyde oxidase by hydralazine contributes to inter-lot inhibition variability in human hepatocytes [0.03%]
肼屈嗪通过谷胱甘肽可逆性失活醛氧化酶导致人肝细胞系批间抑制差异性研究
Lloyd Wei Tat Tang
Lloyd Wei Tat Tang
Hydralazine is commonly employed as a time-dependent inhibitor of aldehyde oxidase (AO) in human hepatocytes for reaction phenotyping yet profound inter-lot variability in its inhibitory effects has been reported. To date, the exact mechani...
Points to consider in the in vitro estimation of kinetic parameters for quantitative prediction of the drug-drug interactions caused by reversible inhibition of enzymes/transporters [0.03%]
体外定量预测可逆性酶/转运体抑制引起药物相互作用的 kinetic 参数测定要点
Kazuya Maeda
Kazuya Maeda
In the drug development process, quantitative prediction of drug-drug interaction (DDI) risk must be a vital evaluation item to ensure drug safety in real clinical settings. Therefore, according to the ICH M12 regulatory guideline, it is st...
N6-methyladenosine modification of MRP7 mRNA modulates its expression and paclitaxel sensitivity in lung cancer-derived A549 cells [0.03%]
肺腺癌A549细胞中MRP7 mRNA的m6A修饰调控其表达和紫杉醇敏感性
Takuto Inamoto,Masataka Nakano,Tatsuki Fukami et al.
Takuto Inamoto et al.
Methylation of adenosine at the N6 position (m6A modification) is the most prevalent epitranscriptomic modification in mammals, regulating RNA stability, splicing, translation, and decay. Growing evidence has revealed that m6A modification ...
Impact of unit notations on quantitative biodistribution analysis of adeno-associated virus vectors-based gene therapy products [0.03%]
载体单位表示方法对基于腺相关病毒载体的基因治疗药物生物分布定量分析的影响研究
Miyu Nakayama,Sho Sato,Syunsuke Yamamoto
Miyu Nakayama
In gene therapy involving the use of adeno-associated virus (AAV) vectors, the biodistribution of vector genome has been expressed in units of "copies/μg genomic DNA (gDNA)." However, gDNA content vary across tissues, thus affecting the bi...
Advances and challenges for drug interaction evaluation - Perspectives on the ICH M12 guideline [0.03%]
药物相互作用评价的新进展与挑战——关于ICH M12指导原则的思考
Xinning Yang,Carolien Versantvoort,Motohiro Hoshino et al.
Xinning Yang et al.
Drug-drug interaction (DDI) is an important factor to consider when determining the drug and optimal dose for individual patients. The DDI potential of an investigational drug is routinely evaluated during development. For pharmacokinetics-...
Quantitative prediction of human pharmacokinetic drug-drug interactions and drug clearance using humanized liver chimeric mice: a review [0.03%]
用人源化肝小鼠定量预测药物相互作用和清除率的药动学：综述
Taiji Miyake,Haruka Tsutsui
Taiji Miyake
Humanized liver chimeric mice, including hu-PXB, hu-FRG, and hu-TK-NOG mice, have emerged as valuable tools for predicting human pharmacokinetics in drug discovery and development. These models, featuring human hepatocytes transplanted into...
Applications of in vitro transporter assays for mechanistic characterization and prediction of clinical drug-drug interactions [0.03%]
体外转运蛋白检测在阐释药物相互作用的作用机制及临床预测中的应用
Krisztina Herédi-Szabó,Sumito Ito,Xiaomin Liang et al.
Krisztina Herédi-Szabó et al.
Drug transporters play essential roles in governing the absorption, distribution, metabolism, and excretion (ADME) of therapeutic drugs. Transporter modulation frequently contributes to clinically significant drug-drug interactions (DDIs). ...
UDP-Glucuronosyl transferase mediated drug-drug interactions: An Industry perspective on recommended in vitro studies [0.03%]
从工业视角推荐的体外研究：UDP-葡萄糖醛酸转移酶介导的药物相互作用
David M Stresser,Michael A Zientek
David M Stresser
Uridine 5'-diphospho-glucuronosyltransferases (UGT) are the best known and most well characterized sugar conjugation biotransformation enzymes. Their main function is to catalyze conjugation of glucuronic acid (sugar) to an exposed (or crea...
Polarized secretion of extracellular vesicles from the placenta to maternal and fetal bloodstreams in rats [0.03%]
大鼠胎盘向母体和胎儿血液循环极化分泌细胞外囊泡
Kazunari Sasaki,Mai Inagaki,Masanori Tachikawa
Kazunari Sasaki
The placenta is a maternal organ that secretes various proteins that support maternal pregnancy and fetal growth. Placenta-derived extracellular vesicles (EVs) encapsulate these proteins and are secreted into the maternal or fetal bloodstre...
Characterization of drug-drug interaction for antibody-drug conjugates and risk assessment using various approaches including physiologically based pharmacokinetic modeling [0.03%]
抗体-药物偶联物的药物相互作用特征及包括基于生理学的药代动力学模型在内的各种方法的风险评估
Dan Lu,Donglu Zhang,Jin Yan Jin et al.
Dan Lu et al.
ADCs represent a rapidly growing class of cancer therapeutics and hold significant promise. As of December 2025, fourteen ADCs have received FDA approval, with more than 100 additional ADCs currently in clinical development. Assessment of A...