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Drug metabolism/pharmacokinetics and drug interaction studies have been extensively carried out in order to secure the druggability and safety of new chemical entities throughout the development of new drugs. Recently, drug metabolism and transport by phase II drug metabolizing enzymes and drug transporters, respectively, as well as phase I drug metabolizing enzymes, have been studied. A combination of biochemical advances in the function and regulation of drug metabolizing enzymes and automated analytical technologies are revolutionizing drug metabolism research. There are also potential drug–drug interactions with co-administered drugs due to inhibition and/or induction of drug metabolic enzymes and drug transporters. In addition, drug interaction studies have been actively performed to develop substrate cocktails that do not interfere with each other and a simultaneous analytical method of substrate drugs and their metabolites using a tandem mass spectrometer. This Special Issue has the aim of highlighting current progress in drug metabolism/pharmacokinetics, drug interactions, and bioanalysis.

human liver microsomes --- alcohol addiction --- UGT --- ultra-high-pressure liquid chromatography --- adalimumab --- procainamide --- LC-MS/MS --- DA-9805 --- paeonol --- LC-QTOF-MS/MS --- YRA-1909 --- chlorogenic acid --- immunoprecipitation --- Eurycoma longifolia --- CYP --- caffeic acid --- rat --- pharmaceutical excipient --- Korean red ginseng extract --- Stauntonia hexaphylla leaf extract --- bioanalysis --- HPLC-MS/MS --- B6 --- eurycomanone --- bioavailability --- drying technology --- GB3 --- diclofenac --- 129-Glatm1Kul/J --- aglycone --- caffeic acid O-glucuronides --- organic anion transporting polypeptide --- protein precipitation --- metabolic stability --- Fabry disease --- biopharmaceuticals --- imperatorin --- neochlorogenic acid --- gastric ulcer --- saikosaponin a --- hair --- anthraquinone --- acetyl tributyl citrate --- pharmacokinetics --- brain distribution --- mematine --- ethyl glucuronide --- pharmacokinetic --- loxoprofen --- liquid chromatography-quadrupole TOF MS --- glucuronidation --- esomeprazole --- metformin --- cytochrome P450 --- glycoside --- AUDIT score --- protein stability --- efficacy --- LC-HR/MS --- cryptochlorogenic acid --- aceclofenac --- drug interaction --- liquid chromatography-tandem mass spectrometry --- Osthenol --- plasma --- N-acetylprocainamide --- diabetes --- Drugs --- Metabolism. --- Drug metabolism --- Pharmacokinetics