The absorption, distribution, metabolism and elimination characteristics of small interfering RNA therapeutics and the opportunity to predict disposition in pregnant women [0.03%]
小干扰RNA药物的吸收、分布、代谢、排泄特征及其在孕妇中预测药动学的机会
Ogochukwu Amaeze,Nina Isoherranen,Sara Shum
Ogochukwu Amaeze
Small interfering RNA (siRNA) therapeutics represent an emerging class of pharmacotherapy with the potential to address previously hard-to-treat diseases. Currently approved siRNA therapeutics include lipid nanoparticle-encapsulated siRNA a...
Absolute membrane protein abundance of P-glycoprotein, breast cancer resistance protein, and multidrug resistance proteins in term human placenta tissue and commonly used cell systems: Application in physiologically based pharmacokinetic modeling of placental drug disposition [0.03%]
人胎盘组织和常用细胞系统中膜转运蛋白的绝对定量及其在基于生理的药代动力学模型中的应用
Zubida M Al-Majdoub,Jolien J M Freriksen,Angela Colbers et al.
Zubida M Al-Majdoub et al.
The placenta acts as a barrier, excluding noxious substances while actively transferring nutrients to the fetus, mediated by various transporters. This study quantified the expression of key placental transporters in term human placenta (n ...
Utility of physiologically based pharmacokinetic modeling in predicting and characterizing clinical drug interactions [0.03%]
基于生理的药代动力学模型预测和表征临床药物相互作用的价值
Robert S Foti
Robert S Foti
Physiologically based pharmacokinetic (PBPK) modeling is a mechanistic dynamic modeling approach that can be used to predict or retrospectively describe changes in drug exposure due to drug-drug interactions (DDIs). With advancements in com...
Comparative analysis of the physiological and transport functions of various sources of renal proximal tubule cells under static and fluidic conditions in PhysioMimix T12 platform [0.03%]
基于PhysioMimix T12平台的静态和流动条件下多种来源肾近端小管细胞生理及转运功能比较分析研究
Courtney Sakolish,Haley L Moyer,Han-Hsuan D Tsai et al.
Courtney Sakolish et al.
In vitro models that can faithfully replicate critical aspects of kidney tubule function such as directional drug transport are in high demand in pharmacology and toxicology. Accordingly, development and validation of new models is underway...
Impact of genetic polymorphisms and drug-drug interactions mediated by carboxylesterase 1 on remimazolam deactivation [0.03%]
羧酸酯酶1基因多态性和药物相互作用对雷米唑胺失活的影响
Zhuo Wang,Zachary McCalla,Li Lin et al.
Zhuo Wang et al.
Remimazolam (Byfavo, Acacia Pharma), a recent Food and Drug Administration-approved ester-linked benzodiazepine, offers advantages in sedation, such as rapid onset and predictable duration, making it suitable for broad anesthesia applicatio...
Physiologically based pharmacokinetic modeling of small molecules: How much progress have we made? [0.03%]
基于生理的药代动力学模型在小分子模拟方面的进展如何？
Nina Isoherranen
Nina Isoherranen
Physiologically based pharmacokinetic (PBPK) models of small molecules have become mainstream in drug development and in academic research. The use of PBPK models is continuously expanding, with the majority of work now focusing on predicti...
Uncovering the impact of COVID-19-mediated bidirectional dysregulation of cytochrome P450 3A4 on systemic and pulmonary drug concentrations using physiologically based pharmacokinetic modeling [0.03%]
基于生理的药代动力学模型揭示COVID-19介导的细胞色素P450 3A4双向调节对全身和肺药物浓度的影响
Chukwunonso K Nwabufo
Chukwunonso K Nwabufo
Several clinical studies have shown that COVID-19 increases the systemic concentration of drugs in hospitalized patients with COVID-19. However, it is unclear how COVID-19-mediated bidirectional dysregulation of hepatic and pulmonary cytoch...
Characterization of Nonclinical Drug Metabolism and Pharmacokinetic Properties of Phosphorodiamidate Morpholino Oligonucleotides, a Novel Drug Class for Duchenne Muscular Dystrophy [0.03%]
磷酸二酰胺吗啉寡核苷酸的非临床药物代谢和药代动力学性质的研究——一种杜氏肌营养不良症的新药类药物
Andrew K L Goey,Marie Claire Mukashyaka,Yogesh Patel et al.
Andrew K L Goey et al.
Eteplirsen, golodirsen, and casimersen are phosphorodiamidate morpholino oligomers (PMOs) that are approved in the United States for the treatment of patients with Duchenne muscular dystrophy (DMD) with mutations in the DMD gene that are am...
Impact of Genetic Polymorphisms and Drug-Drug Interactions Mediated by Carboxylesterase1 on Remimazolam Deactivation [0.03%]
羧酸酯酶1基因多态性及药物相互作用对瑞马唑仑再活化的影响
Zhuo Wang,Zachary McCalla,Li Lin et al.
Zhuo Wang et al.
Remimazolam (Byfavo®), a recent FDA-approved ester-linked benzodiazepine, offers advantages in sedation, such as rapid onset and predictable duration, making it suitable for broad anesthesia applications. Its favorable pharmacological prof...
Candesartan Has No Clinically Meaningful Effect on the Plasma Concentrations of Cytochrome P450 2C8 Substrate Repaglinide in Humans [0.03%]
坎地沙坦不会显著影响人类中以细胞色素P450 2C8为作用位点的底物利格列汀的血浆浓度
Mikael O W Piha,Kristiina Cajanus,Marica T Engström et al.
Mikael O W Piha et al.
In vitro evidence shows that the acyl-β-D-glucuronide metabolite of candesartan inhibits cytochrome P450 (CYP) 2C8 with an inhibition constant of 7.12 μM. We investigated the effect of candesartan on the plasma concentrations and glucose-...
Randomized Controlled Trial
Drug metabolism and disposition: the biological fate of chemicals. 2024 Nov 15;52(12):1388-1395. DOI:10.1124/dmd.124.001798 2024