4β-Hydroxycholesterol as an endogenous biomarker for CYP3A induction: Scientific rationale, clinical utility, and future perspectives [0.03%]
内源性生物标志物4β-羟基胆固醇在CYP3A诱导中的科学依据、临床应用和未来前景
Barry Jones
Barry Jones
4β-Hydroxycholesterol (4β-HC) is an oxysterol formed via CYP3A-mediated hydroxylation of cholesterol. It is a sensitive and non-invasive biomarker for assessing CYP3A enzyme activity. 4β-HC exhibits a long half-life with estimates rangin...
PBPK Modeling Addresses Oral Absorption-Mediated Drug Interactions [0.03%]
基于生理的药代动力学模型可解决由口服吸收介导的药物相互作用问题
Xinyuan Zhang,Grace Fraczkiewicz,Viera Lukacova
Xinyuan Zhang
Absorption is the first and imperative step to understanding the pharmacokinetics (PK) and ADME (absorption, distribution, metabolism, and excretion) of a drug product. Drug interactions also occur during the absorption process and have the...
Integrating renal transporter biomarkers into drug development: Discovery, clinical assessment, and precision medicine [0.03%]
肾脏转运蛋白生物标志物在药物研发中的应用：发现、临床评价与精准医疗
Sook Wah Yee,Bhagwat Prasad,Hiroyuki Kusuhara et al.
Sook Wah Yee et al.
Renal transporters play a critical role in the renal secretion of prescription drugs and endogenous metabolites. Inhibition of these transporters can increase the plasma exposure of a co-administered drug by reducing its renal clearance, po...
Evaluation of OATP1B inhibitory potential using an endogenous biomarker coproporphyrin-I in new drug applications: Case reports submitted by 2024 [0.03%]
利用内源性生物标志物粪卟啉I评估药物候选者OATP1B抑制潜能：2024年前提交的案例报告
Ryosuke Watari
Ryosuke Watari
Coproporphyrin-I (CP-I), an endogenous biomarker for organic anion transporting polypeptide (OATP) 1B, is a critical tool for evaluating the inhibitory potential of OATP1B in humans. The final International Council for Harmonisation of Tech...
Current status of prediction of IL-6 mediated cytochrome P450 activity modulation using in vitro data and PBPK modeling [0.03%]
利用体外数据和生理基于 PK 模型预测白细胞介素 6 引起的细胞色素 P450 同工酶活性改变的现状研究
Viktor Georgiev,Isabelle Anderka,Delia Bucher et al.
Viktor Georgiev et al.
This review focuses on use of in vitro data and physiologically based pharmacokinetic (PBPK) modeling to predict disease-drug and therapeutic-protein-drug interactions for Cytochrome P450 CYP substrates mediated by interleukin-6 (IL-6). We ...
The rational use of PBPK to assess the changing DDI liability in pediatrics: Model qualification and the move towards best practice [0.03%]
从儿科角度合理利用PBPK评估DDI的变化责任：模型认证和最佳实践的转变
Trevor N Johnson,Jean Dinh,Roz Southall et al.
Trevor N Johnson et al.
Many drug-drug interactions (DDIs) in the pediatric population are managed based on data generated in adults, however this is done with little clinical evidence and the assumption of DDIs being similar between adults and pediatric may not b...
Elaine Tseng,R Scott Obach
Elaine Tseng
Cytochrome P450 reaction phenotyping refers to the in vitro experimental approach that estimates the quantitative contributions of individual P450 enzymes to the metabolism of a drug. Methods for this are well-established and have existed f...
Positive implications of PBPK platform qualification for predicting drug-drug interactions: Taking on cracks only to see bigger gaps! [0.03%]
基于PBPK平台预测药物相互作用的积极意义：解决了分歧问题却发现更大的差距！
Amin Rostami-Hodjegan
Amin Rostami-Hodjegan
In this mini-review, the readers are provided with series of key references which highlight the latest trends in the space of physiologically-based pharmacokinetics (PBPK) concerning assessment and management of drug-drug interactions (DDI)...
Nina Isoherranen
Nina Isoherranen
Since the publication of the metabolites in safety testing (MIST) guidance by the US FDA in 2009, there has been continuous interest and expansion in research aimed at predicting and characterizing circulating metabolites. Several systemati...
Future directions in drug-drug interaction evaluations: Industry perspective on the ICH M12 guidance [0.03%]
药品相互作用评估的未来方向——关于ICH M12指导原则的产业视角
Kenichi Umehara,Andrew Harrell,Chandra Prakash et al.
Kenichi Umehara et al.
The ICH M12 Guidance, adopted by the International Council for Harmonisation in 2024, provides a global framework for assessing drug-drug interaction (DDI) risks mediated by metabolic enzymes and drug transporters. The DDI Discussion Group ...