Impact of Lipid Partitioning on the Design, Analysis, and Interpretation of Microsomal Time-Dependent Inactivation [0.03%]
脂质分区对微粒体时间依赖型灭活设计、分析和解释的影响
Jaydeep Yadav,Ken Korzekwa,Swati Nagar
Jaydeep Yadav
Nonspecific drug partitioning into microsomal membranes must be considered for in vitro-in vivo correlations. This work evaluated the effect of including lipid partitioning in the analysis of complex TDI kinetics with numerical methods. The...
Mechanisms Influencing the Pharmacokinetics and Disposition of Monoclonal Antibodies and Peptides [0.03%]
影响单克隆抗体和肽类药代动力学及体内分布的机制
Amita Datta-Mannan
Amita Datta-Mannan
Monoclonal antibodies (mAbs) and peptides are an important class of therapeutic modalities that have brought improved health outcomes in areas with limited therapeutic optionality. Presently, there more than 90 mAb and peptide therapeutics ...
Contributions of Hepatic and Intestinal Metabolism to the Disposition of Niclosamide, a Repurposed Drug with Poor Bioavailability [0.03%]
肝脏和肠道代谢对尼氯霜（一种生物利用度低的再创新药物）体内处置的影响
Xiaoyu Fan,Hongmin Li,Xinxin Ding et al.
Xiaoyu Fan et al.
Niclosamide, an antiparasitic, has been repositioned as a potential therapeutic drug for systemic diseases based on its antiviral, anticancer, and anti-infection properties. However, low bioavailability limits its in vivo efficacy. Our aim ...
Indinavir Increases Midazolam N-Glucuronidation in Humans: Identification of an Alternate CYP3A Inhibitor Using an In Vitro to In Vivo Approach [0.03%]
恩夫韦肽通过体内外研究鉴定一种新的细胞色素P450 3A代谢底物中期唑胺N-葡萄糖醛酸化的调节剂
Dan-Dan Tian,Cathrine Leonowens,Emily J Cox et al.
Dan-Dan Tian et al.
Midazolam is a widely used index substrate for assessing effects of xenobiotics on CYP3A activity. A previous study involving human hepatocytes showed the primary route of midazolam metabolism, 1'-hydroxylation, shifted to N-glucuronidation...
Randomized Controlled Trial
Drug metabolism and disposition: the biological fate of chemicals. 2019 Jul;47(7):724-731. DOI:10.1124/dmd.119.087007 2019
Potential for Underestimation of d-Methylphenidate Bioavailability Using Chiral Derivatization/Gas Chromatography [0.03%]
以光学衍生化/气相色谱法评估d-甲基苯环己烃生物利用度的潜在误差分析
Kennerly S Patrick,Wendy Rodriguez
Kennerly S Patrick
A tenable hypothesis is presented which explains disparities between older oral dl-MPH bioavailability data generated using chiral derivatization-gas chromatography versus more recent findings using chiral liquid chromatography. These dispa...
Effects of Epacadostat on Brain Extracellular Fluid Concentrations of Serotonin-an Intracerebral Microdialysis Study in Sprague-Dawley Rats [0.03%]
Epacadostat对大脑细胞外液中5-HT浓度的影响-SD大鼠脑室内微透析研究
Yan Zhang,Kevin Bowman,Janet Maleski et al.
Yan Zhang et al.
Epacadostat (EPAC) is an indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor that has been examined in multiple clinical trials. The substrate for IDO1 is tryptophan and there is a theoretical concern that inhibition of IDO1 may increase the con...
Pharmacokinetic Interaction between Naloxone and Naltrexone Following Intranasal Administration to Healthy Subjects [0.03%]
健康受试者鼻内给药后纳洛酮与纳曲酮的药物相互作用研究
Philip Krieter,C Nora Chiang,Shwe Gyaw et al.
Philip Krieter et al.
Naloxone (17-allyl-4,5α-epoxy-3,14-dihydroxymorphinan-6-one HCl), a μ-opioid receptor antagonist, is administered intranasally to reverse an opioid overdose but its short half-life may necessitate subsequent doses. The addition of naltrex...
Randomized Controlled Trial
Drug metabolism and disposition: the biological fate of chemicals. 2019 Jul;47(7):690-698. DOI:10.1124/dmd.118.085977 2019
RNA Editing Enzymes Modulate the Expression of Hepatic CYP2B6, CYP2C8, and Other Cytochrome P450 Isoforms [0.03%]
RNA编辑酶调节肝CYP2B6、CYP2C8和其他细胞色素P450同工酶的表达
Kaori Nozaki,Masataka Nakano,Chika Iwakami et al.
Kaori Nozaki et al.
A-to-I RNA editing, the most frequent type of RNA editing in mammals, is catalyzed by adenosine deaminase acting on RNA (ADAR) enzymes. Recently, we found that there is a large interindividual variation in the expression of ADAR1 protein in...