In vitro metabolism studies of 5 acrylamide covalent drugs: Comparison with metabolism and disposition in human [0.03%]
体外酰胺类共价药物代谢研究：与人体内的代谢及分布对比分析
Ruixing Li,Qingfeng Shi,Mingshe Zhu et al.
Ruixing Li et al.
Targeted covalent inhibitors, such as acrylamide covalent drugs (ACDs), offer advantages in potency, selectivity, and duration of effect compared with traditional small-molecule inhibitors. However, ACDs undergo unique biotransformation pat...
Importance of extracellular disulfide bonds for the surface expression and function of human organic anion transporting polypeptide 1B1 [0.03%]
二硫键对人有机阴离子转运多肽1B1膜表达及功能的重要性研究
Ting Liang,Yao Dong,Ru Huan et al.
Ting Liang et al.
Organic anion transporting polypeptide 1B1 (OATP1B1) is an important member of the solute carrier organic anion transporter family and is exclusively expressed on the basolateral membrane of human hepatocytes. As a membrane protein, its ext...
Mechanism-based inactivation of CYP2C19 by bicuculline and related alteration in pharmacokinetics of clopidogrel [0.03%]
药物双股兰因作用于酶CYP2C19而导致的失活及其对氯吡格雷药动学的影响机制研究
Yan Zhang,Zihao Cheng,Jie Dai et al.
Yan Zhang et al.
Corydalis Decumbentis Rhizoma (CDR) is a traditional Chinese herbal medicine, which has been clinically used for treating migraine, relieving the symptoms of rheumatoid arthritis, and reversing osteoporosis. Bicuculline (BIC) is one of the ...
Gut microbiota influence pharmacokinetics variability in aging mice: Effects vary from drug to drug [0.03%]
肠道微生物群影响衰老小鼠的药代动力学变异：药物间的影响不同
Qing-Xuan Xie,Xiao-Na Zeng,Yun-Hui Wang et al.
Qing-Xuan Xie et al.
Pharmacokinetics (PKs) changes in the aging state are relatively common in clinical practice, but their underlying mechanisms remain unclear. This study aims to explore the potential effects of gut microbiota on PK of P450 probe drugs in ol...
Corrigendum to "Intestine versus liver? Uncovering the hidden major metabolic organs of silybin in rats" [Drug Metabolism and Disposition 53 (2025) 100005] [0.03%]
关于“肠道还是肝脏？揭开大鼠体内硅-bin 隐藏的主要代谢器官的面纱”[药物代谢和处置 53 (2025) 100005] 的勘误表
Yuanbo Sun,Like Xie,Jing Zhang et al.
Yuanbo Sun et al.
Encequidar is a multispecies gut-restricted P-glycoprotein inhibitor that delineates between intestinal secretion and biliary elimination in animals and predicts human disposition pathways [0.03%]
一种多物种肠道特异性P-糖蛋白抑制剂，可区分动物的肠分泌和胆汁排泄并预测人类处置途径
Murali Subramanian,Josh Yu,Gregg Schwarzwalder et al.
Murali Subramanian et al.
Encequidar is a gut-restricted P-glycoprotein inhibitor that is a useful tool molecule to boost the oral bioavailability of P-glycoprotein substrates. In this article, we demonstrate that encequidar has moderate to high clearance and volume...
Preclinical translational physiologically based pharmacokinetic modeling for predicting human pharmacokinetics of proteolysis targeting chimeras: Case studies of vepdegestrant (ARV-471) and bavdegalutamide (ARV-110) [0.03%]
基于生理的药代动力学建模在蛋白酶靶向连接物临床转化中的应用：VERDE-02和VERDE-03研究中VEPDEGESTRANT（ARV-471）和BAVDegalutamide（ARV-110）的人体药代动力学预测案例研究
Ramakrishna Rachumallu,Jonathan Cheong,Gauri Deshmukh et al.
Ramakrishna Rachumallu et al.
Proteolysis targeting chimeras (PROTACs), a class of targeted protein degraders, are advancing in clinical development, necessitating the accurate prediction of human pharmacokinetics (PK). This study developed a physiologically based pharm...
Improving the predictivity of human maximum plasma concentrations for soybean isoflavones and glucosides using an improved culture method of human induced pluripotent stem cell-derived small intestinal epithelial cells [0.03%]
改进人诱导多能干细胞来源的小肠上皮细胞培养方法以提高大豆异黄酮和糖苷类化合物人体最大血药浓度预测性的研究
Takashi Kitaguchi,Kotaro Shirai,Isamu Ogawa et al.
Takashi Kitaguchi et al.
Accurately predicting human exposure to food-related compounds is crucial for evaluating their health effects without conducting animal testing. We previously reported an in vitro method using human induced pluripotent stem cell-derived sma...
Influence of 3-dimensional architecture and coculture on in vitro CYP enzyme metabolism and induction: Benchmarking human hepatic spheroids for studies in drug development [0.03%]
三维结构和共培养对体外CYP酶代谢及诱导的影响：用人肝类器官体基准法进行药物研发研究
Ann-Kathrin Lenich,Sanja Alsdorf,Stephanie Ruez
Ann-Kathrin Lenich
3-dimensional (3D) primary hepatic spheroid cultures better mimic in vivo liver architecture and maintain a more stable cellular phenotype than the current gold standard of sandwich-cultured primary human hepatocytes. Therefore, they are a ...
Insights into the human pharmacokinetics and metabolism of branaplam, a splicing modulator of a survival motor neuron-2 and huntingtin pre-mRNAs, in infants and adults [0.03%]
关于分支拉普胺的药代动力学和代谢见解，这是一种用于存活电机神经元-2和亨廷顿蛋白前mRNA的剪接调节剂，在婴儿和成人中的研究结果
F Lozac&#x;h,A Demailly,M Raccuglia et al.
F Lozac&#x;h et al.
This study examined the absorption, distribution, metabolism, and excretion of branaplam in healthy adult male volunteers and, additionally, compared the adult metabolite profiles obtained in plasma and urine to those obtained in infants wi...