Results 1 to 10 of about 848,131 (265)

Investigation of the human metabolism and disposition of the prolyl hydrolase inhibitor daprodustat using IV microtracer with Entero‐Test bile string

Pharmacology Research & Perspectives, 2023
Daprodustat is an oral small molecule hypoxia‐inducible factor (HIF) prolyl hydroxylase inhibitor (PHI) approved in Japan and the United States for the treatment of anemia associated with chronic kidney disease.
Guoying Tai, Fangming Xia, Cathy Chen, Adrian Pereira, Jill Pirhalla, Xiusheng Miao, Graeme Young, Claire Beaumont, Liangfu Chen   +8 more
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Application of a PBPK model to elucidate the changes of systemic and liver exposures for rosuvastatin, carotegrast, and bromfenac followed by OATP inhibition in monkeys

Clinical and Translational Science, 2021
The impact of organic anion‐transporting polypeptide (OATP) inhibition on systemic and liver exposures of three OATP substrates was investigated in cynomolgus monkeys.
Yaofeng Cheng, Xiaomin Liang, Jia Hao, Congrong Niu, Yurong Lai   +4 more
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Biological fate and interaction with cytochromes P450 of the nanocarrier material, d-α-tocopheryl polyethylene glycol 1000 succinate

Acta Pharmaceutica Sinica B, 2022
d-α-Tocopheryl polyethylene glycol 1000 succinate (TPGS, also known as vitamin E-TPGS) is a biodegradable amphiphilic polymer prepared by esterification of vitamin E with polyethylene glycol (PEG) 1000.
Tianming Ren, Runzhi Li, Liqiang Zhao, J. Paul Fawcett, Dong Sun, Jingkai Gu   +5 more
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Applicability of free drug hypothesis to drugs with good membrane permeability that are not efflux transporter substrates: A microdialysis study in rats

Pharmacology Research & Perspectives, 2020
In clinical pharmacology, the free drug hypothesis has been widely applied in the interpretation of the relationship between pharmacokinetics and pharmacodynamics (PK/PD).
Chun Chen, Hongyu Zhou, Chi Guan, Huanhuan Zhang, Yingying Li, Xue Jiang, Zheng Dong, Yuanyuan Tao, Juan Du, Shuyao Wang, Teng Zhang, Na Du, Junyang Guo, Yaqiong Wu, Zehai Song, Haofei Luan, Yu Wang, Hongwen Du, Shaofeng Zhang, Chen Li, Hang Chang, Tao Wang   +21 more
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A novel SRSF3 inhibitor, SFI003, exerts anticancer activity against colorectal cancer by modulating the SRSF3/DHCR24/ROS axis

Cell Death Discovery, 2022
As the modulation of serine/arginine-rich splicing factor 3 (SRSF3) may be therapeutically beneficial to colorectal cancer (CRC) treatment, the identification of novel SRSF3 inhibitors is highly anticipated. However, pharmaceutical agents targeting SRSF3
Yawen Zhang, Mengmeng Wang, Fanyi Meng, Man Yang, Yinshuang Chen, Xuqin Guo, Weiwei Wang, Yifan Zhu, Yundi Guo, Chunlai Feng, Shen Tian, Hongjian Zhang, Huanqiu Li, Jing Sun, Weipeng Wang   +14 more
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A Physiologically Based Pharmacokinetic Model for Studying the Biowaiver Risk of Biopharmaceutics Classification System Class I Drugs With Rapid Elimination: Dexketoprofen Trometamol Case Study

Frontiers in Pharmacology, 2022
Biowaiver based on the biopharmaceutics classification system (BCS) has been widely used in the global market for the approval of new generic drug products to avoid unnecessary in vivo bioequivalence (BE) studies.
Xian Zhang, Xuxiao Ye, Kuan Hu, Wenping Li, Wenqian Li, Qingqing Xiao, Lin Chen, Jin Yang   +7 more
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POE Immunoassay: Plate-based oligonucleotide electro-chemiluminescent immunoassay for the quantification of nucleic acids in biological matrices

Scientific Reports, 2020
Oligonucleotide therapeutics use short interfering RNA (siRNA) or antisense oligonucleotide (ASO) molecules to exploit endogenous systems—neutralizing target RNA to prevent subsequent protein translation. While the potential clinical application is vast,
Mai B. Thayer, Sara C. Humphreys, Kyu S. Chung, Julie M. Lade, Kevin D. Cook, Brooke M. Rock   +5 more
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Preclinical characterization of the ADME properties of a surrogate anti-IL-36R monoclonal antibody antagonist in mouse serum and tissues

mAbs, 2020
The decision to pursue a monoclonal antibody (mAb) as a therapeutic for disease intervention requires the assessment of many factors, such as target-biology, including the total target burden and its accessibility at the intended site of action, as well ...
Kip P. Conner, Cinthia V. Pastuskovas, Marcus Soto, Veena A. Thomas, Mylo Wagner, Dan A. Rock   +5 more
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A Whole-Body Physiologically Based Pharmacokinetic Model Characterizing Interplay of OCTs and MATEs in Intestine, Liver and Kidney to Predict Drug-Drug Interactions of Metformin with Perpetrators

Pharmaceutics, 2021
Transmembrane transport of metformin is highly controlled by transporters including organic cation transporters (OCTs), plasma membrane monoamine transporter (PMAT), and multidrug/toxin extrusions (MATEs).
Yiting Yang, Zexin Zhang, Ping Li, Weimin Kong, Xiaodong Liu, Li Liu   +5 more
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Pharmacokinetics, mass balance, tissue distribution, metabolism, and excretion of praliciguat, a clinical‐stage soluble guanylate cyclase stimulator in rats

Pharmacology Research & Perspectives, 2020
The pharmacokinetics (PK), metabolism, excretion, mass balance, and tissue distribution of [14C]praliciguat were evaluated following oral administration of a 3‐mg/kg dose in Sprague‐Dawley rats and in a quantitative whole‐body autoradiography (QWBA ...
Ali R. Banijamali, Andrew E. Carvalho, James D. Wakefield, Peter Germano, Timothy C. Barden, Jenny V. Tobin, Daniel P. Zimmer, Jaime L. Masferrer, Albert T. Profy, Mark G. Currie, G. Todd Milne   +10 more
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