Results 141 to 150 of about 27,101 (273)

Impact of metabolic enzyme activity variability on dabrafenib disposition

Frontiers in Pharmacology
IntroductionThe systemic exposure of dabrafenib correlates with its adverse drug reactions. A thorough understanding of its pharmacokinetic profile is crucial for precise clinical application.MethodsAn optimized liver microsomal incubation system was ...
Shi-yu Wang, Shi-yu Wang, Qing Chen, Zhong-xi Chen, Jing Chen, Jing Yuan, Li-shang Dai, Lian-guo Chen, Xiao-dan Zhang, Xiao-dan Zhang   +9 more
doaj   +1 more source

Human liver microsomes study on the inhibitory effect of plantainoside D on the activity of cytochrome P450 activity. [PDF]

BMC Complement Med Ther, 2022
Zhou J, Qian X, Zhou Y, Xiong S, Ji S, Wang Y, Zhao P.   +6 more
europepmc   +1 more source

Phenylalanine Versus Tyrosine (Pos. 367/332 in MCT1/MCT4) in the Substrate Binding Site Defines Affinity and Preferred Directionality of Human Monocarboxylate Transporters 1–4

Acta Physiologica, Volume 242, Issue 7, July 2026.
ABSTRACT Aim Human monocarboxylate transporters 1–4, MCT, are key for the lactate/H+ exchange between glycolytic and oxidative cancer cells, white and red muscle fibers, or in the astrocyte‐neuron shuttle. The common MCT transport mechanism involves three conserved residues, that is, a substrate‐attracting Lys and a conformation‐locking Asp/Arg salt ...
Maike Menzel, Ioana‐Daniela Dumitru, Josh Peters, Jan‐Bernd Hövener, Andrey N. Pravdivtsev, Ana‐Nicoleta Bondar, Eric Beitz   +6 more
wiley   +1 more source

Kinetic Characteristics of Curcumin and Germacrone in Rat and Human Liver Microsomes: Involvement of CYP Enzymes. [PDF]

Molecules, 2022
Su S, Wu H, Zhou J, Yuan G, Wang H, Feng J.   +5 more
europepmc   +1 more source

Drug Interactions of Vebreltinib, a Novel Type I c‐Met Inhibitor, Coadministration With Rifampin or Itraconazole in Healthy Participants

Clinical and Translational Science, Volume 19, Issue 7, July 2026.
Pharmacokinetic and drug–drug interaction evaluation of vebreltinib in healthy participants, showing decreased exposure with rifampin and increased exposure with itraconazole. ABSTRACT Vebreltinib is a novel, highly selective type I c‐Met inhibitor developed for treating non–small cell lung cancer (NSCLC) and glioma.
Jingcheng Chen, Jingxuan Wu, Yuqin Song, Jiangshuo Li, Linna li, Lijun Li, Yanhong Kong, Xiaofang Wu, Hang Yin, Mengyu Hou, Bingyan Wang, Qiannan Gao, Ran Li, Le Wu, Weizhe Xue, Ruihua Dong   +15 more
wiley   +1 more source

Assessment of In Silico and In Vitro Selpercatinib Metabolic Stability in Human Liver Microsomes Using a Validated LC-MS/MS Method. [PDF]

Molecules, 2023
Attwa MW, AlRabiah H, Mostafa GAE, Bakheit AH, Kadi AA.   +4 more
europepmc   +1 more source

Metabolite Identification of HIV-1 Capsid Modulators PF74 and 11L in Human Liver Microsomes. [PDF]

Metabolites, 2022
Xu S, Sun L, Ding D, Zhang X, Liu X, Zhan P.   +5 more
europepmc   +1 more source

Oxidative metabolism of BDE-47, BDE-99, and HBCDs by cat liver microsomes: Implications of cats as sentinel species to monitor human exposure to environmental pollutants

, 2016
: The in vitro oxidative metabolism of 2,2',4,4'-tetrabromodiphenyl ether (BDE-47), 2,2',4,4',5-pentabromodiphenyl ether (BDE-99), and individual alpha-, beta- and gamma-hexabromocyclododecane (HBCD) isomers catalyzed by cytochrome P450 (CYP) enzymes was
Covaci, Adrian, Zheng, Xiabo, Luo, Xiaojun, Mai, Bixian, Zheng, Xiaobo, Erratico, Claudio   +5 more
core   +1 more source

In Vitro characterization of narciclasine: solubility, metabolic stability, and P-glycoprotein substrate status

Frontiers in Pharmacology
BackgroundNarciclasine has demonstrated anticancer activity at low nanomolar concentrations in various preclinical cancer models, but no clinical data in cancer patients are available. Although its biological activity and structure-activity relationships
Ravi Akkireddy, Ravi Akkireddy, In-Hyoung Yang, In-Hyoung Yang, Srinivas Lenkalapelly, Srinivas Lenkalapelly, Ganesh J. Kshirsagar, Ganesh J. Kshirsagar, Harry A. May, Harry A. May, Harry A. May, Min H. Kang, Min H. Kang   +12 more
doaj   +1 more source

Development of an LC-MS/MS Method for Quantification of Sapitinib in Human Liver Microsomes: In Silico and In Vitro Metabolic Stability Evaluation. [PDF]

Molecules, 2023
Attwa MW, AlRabiah H, Mostafa GAE, Kadi AA.   +3 more
europepmc   +1 more source