Apalutamide Absorption, Metabolism, and Excretion in Healthy Men, and Enzyme Reaction in Human Hepatocytes [0.03%]
阿帕鲁胺在健康男性中的吸收、代谢和排泄以及在人类肝细胞中的酶动力学研究
Ronald de Vries,Frank Jacobs,Geert Mannens et al.
Ronald de Vries et al.
In this phase 1 study, the absolute bioavailability and absorption, metabolism, and excretion (AME) of apalutamide, a competitive inhibitor of the androgen receptor, were evaluated in 12 healthy men. Subjects received 240 mg of apalutamide ...
Armina Abbasi,Erickson M Paragas,Carolyn A Joswig-Jones et al.
Armina Abbasi et al.
Many promising drug candidates metabolized by aldehyde oxidase (AOX) fail during clinical trial owing to underestimation of their clearance. AOX is species-specific, which makes traditional allometric studies a poor choice for estimating hu...
Oxidative Deamination of Emixustat by Human Vascular Adhesion Protein-1/Semicarbazide-Sensitive Amine Oxidase [0.03%]
人血管粘附蛋白-1/半卡巴腙敏感胺氧化酶对Emixustat的氧化脱氨作用
Michael J Reid,Russell Eyre,Terry Podoll
Michael J Reid
Emixustat potently inhibits the visual cycle isomerase retinal pigment epithelium protein 65 (RPE65) to reduce the accumulation of toxic bisretinoid by-products that lead to various retinopathies. Orally administered emixustat is cleared ra...
A Novel Unified Approach to Predict Human Hepatic Clearance for Both Enzyme- and Transporter-Mediated Mechanisms Using Suspended Human Hepatocytes [0.03%]
一种新颖的统一方法预测人肝清除率：采用悬浮式人肝细胞预测酶介导和转运蛋白介导的机制
Keith A Riccardi,David A Tess,Jian Lin et al.
Keith A Riccardi et al.
The accurate prediction of human pharmacokinetics is critically important in modern drug discovery since it drives both pharmacological and toxicological effects. Although significant progress has been made in predicting drug disposition by...
Ontogeny of ADME Processes during Postnatal Development in Man and Preclinical Species: A Comprehensive Review [0.03%]
人和预临床物种出生后发育过程中ADME过程的 ontogeny：全面回顾
Luc M De Schaepdrijver,Pieter P J Annaert,Connie L Chen
Luc M De Schaepdrijver
Akifumi Kogame,Yuu Moriya,Ikuo Mori et al.
Akifumi Kogame et al.
Fasiglifam, a potent and highly selective agonist of G protein-coupled receptor 40, was developed for the treatment of type 2 diabetes mellitus. However, phase III clinical programs were terminated owing to liver safety concerns. Fasiglifam...
Pharmacogenomic Next-Generation DNA Sequencing: Lessons from the Identification and Functional Characterization of Variants of Unknown Significance in CYP2C9 and CYP2C19 [0.03%]
药物基因组下一代DNA测序：从CYP2C9和CYP2C19中未知意义变异鉴定及功能表征获得的经验教训
Sandhya Devarajan,Irene Moon,Ming-Fen Ho et al.
Sandhya Devarajan et al.
CYP2C9 and CYP2C19 are highly polymorphic pharmacogenes; however, clinically actionable genetic variability in drug metabolism due to these genes has been limited to a few common alleles. The identification and functional characterization o...