Results 81 to 90 of about 26,827 (219)

Development of a physiologically‐based pharmacokinetic model for Ritonavir characterizing exposure and drug interaction potential at both acute and steady‐state conditions

CPT: Pharmacometrics &Systems Pharmacology, Volume 14, Issue 3, Page 523-539, March 2025.
Abstract Ritonavir (RTV) is a potent CYP3A inhibitor that is widely used as a pharmacokinetic (PK) enhancer to increase exposure to select protease inhibitors. However, as a strong and complex perpetrator of CYP3A interactions, RTV can also enhance the exposure of other co‐administered CYP3A substrates, potentially causing toxicity.
Lien Thi Ngo, Woojin Jung, Tham Thi Bui, Hwi‐yeol Yun, Jung‐woo Chae, Jeremiah D. Momper   +5 more
wiley   +1 more source

Inhibition of rat microsomal lipid peroxidation by the oral administration of D002

Brazilian Journal of Medical and Biological Research, 2000
The effect of D002, a defined mixture of higher primary alcohols purified from bee wax, on in vivo and in vitro lipid peroxidation was studied. The extent of lipid peroxidation was measured on the basis of the levels of thiobarbituric acid reactive ...
Menéndez R., Amor A.M., González R.M., Jiménez S., Más R.   +4 more
doaj  

A Population Pharmacokinetic Approach to Understand the Effect of Efavirenz on CYP3A Activity in Healthy Volunteers Using Midazolam as a Probe

CPT: Pharmacometrics &Systems Pharmacology, EarlyView.
ABSTRACT Efavirenz induces and inhibits multiple drug‐metabolizing enzymes, contributing to significant drug–drug interactions. This study quantified the impact of multiple doses of efavirenz on CYP3A activity via midazolam metabolism using a population pharmacokinetic approach.
Kimberly S. Collins, Blessed W. Aruldhas, Ingrid F. Metzger, Jessica B. L. Lu, Michael A. Heathman, Sara K. Quinney, Zeruesenay Desta   +6 more
wiley   +1 more source

CL 277,082: a novel inhibitor of ACAT-catalyzed cholesterol esterification and cholesterol absorption.

Journal of Lipid Research, 1989
CL 277,082 (I) was found to be a potent inhibitor of acyl CoA:cholesterol acyltransferase (ACAT, EC 2.3.1.26) in microsomes from a variety of tissues with IC50 values of 0.14 microM for intestinal mucosal microsomes, 0.74 microM for liver, and 1.18 ...
E E Largis, C H Wang, V G DeVries, S A Schaffer   +3 more
doaj   +1 more source

Pharmacokinetics, pharmacodynamics, and safety interaction study of tunodafil hydrochloride and alcohol: A randomized, blinded, placebo‐controlled, three‐cycle crossover study in Chinese healthy men

Andrology, EarlyView.
Abstract Objectives This study aimed to evaluate the pharmacodynamic effects of administering tunodafil hydrochloride with alcohol on blood pressure and heart rate in healthy Chinese males, and to investigate the mutual pharmacokinetic interactions and safety of the combination.
Dingyuan Hu, Suping Niu, Fan Huang, Lu Jin, Qun Gu, Yanting Li, Chongyou Lee, Zhenwei Xie, Xiangxing Liu, Fang Men, Wenyan Zhao, Shuang Li, Yian Liu, Qian Wang, Huaying Fan, Jiaojiao Zhang, Shuangshuang Lin, Liming Chen, Yi Fang   +18 more
wiley   +1 more source

Dependence of microsomal lipid synthesis on added protein

Journal of Lipid Research, 1964
Lipid synthesis by rat liver microsomes from l-α-glycerophosphate-1-C14 in the presence of palmitic acid, ATP, CoA, and Mg2+ came to a standstill after 30 min while enough cofactors were still present to promote further synthesis.
Ruth Tzur, B. Shapiro
doaj   +1 more source

Opportunities of patient‐derived organoids in drug development

British Journal of Pharmacology, EarlyView.
Various model systems are utilised during drug development starting from basic research, moving to preclinical research and development for clinical applications in order to identify new drugs to improve human health. However, there are characteristics of humans that are not captured by established models.
Antonia Büning, Elena Reckzeh
wiley   +1 more source

Prediction of Hepatic Clearance of Stereoselective Metabolism of Carvedilol in Liver Microsomes and Hepatocytes of Sprague-Dawley and Cytochrome P450 2D-Deficient Dark Agouti Rats

Journal of Pharmacy & Pharmaceutical Sciences, 2019
Hepatic clearance (CLh) of carvedilol (CAR), which is eliminated via stereoselective metabolism by the CYP2D subfamily of cytochromes P450 (CYPs), was predicted using liver microsomes and hepatocytes from Sprague-Dawley (SD) rats and CYP2D-deficient Dark
Masahiro Iwaki, Toshiro Niwa, Hiroyuki Tanaka, Atsushi Kawase, Hiroshi Komura   +4 more
doaj   +1 more source

Chemical profiling and characterisation of anthraquinone‐based polyphenols as biocolourants from Cortinarius semisanguineus

Coloration Technology, EarlyView.
Abstract Anthraquinone dyes are known for their significant colour (brightness of shade in the red, blue and green areas) and light fastness properties compared with other synthetic dyes (such as azo‐based dyes). However, challenging multi‐step synthesis of anthraquinones and limited access to fewer substituents result in insufficient reactivity ...
Arvind Negi, Peppi Toukola, Riikka Räisänen   +2 more
wiley   +1 more source

Preclinical metabolism and metabolic drug–drug interaction profile of pedunculoside and rotundic acid

Clinical and Translational Science
Pedunculoside and rotundic acid, the most abundant components in plants of the genus Ilex L. (Aquifoliaceae), exhibit biological and pharmacological significance in the treatment of cardiovascular diseases.
Liang Wu, Linling Dong, Zhu Zhou, Xin Wang, Yujie Lin, Xuesong Shi, Peijing Wang, Suocheng Xu, Zhiyi Fang   +8 more
doaj   +1 more source