Yi, Min Li, Qiuxia Zhao, Yuhang Nie, Shanshan Wu, Ning Wang, Dongsheng
Published in
Drug metabolism and pharmacokinetics
The present study aims is to investigate the metabolic mechanism of Xue-Fu-Zhu-Yu decoction (XFZYD) in the treatment of blood-stasis syndrome in Coronary Heart Disease (CHD). To that end, 30 CHD patients with Blood-Stasis Syndrome (BSS) and 20 healthy subjects were enrolled. LC-Q-TOF/MS analysis determined that in comparison between CHD with BSS pa...
Gotoh-Saito, Saki Abe, Takayuki Furukawa, Yoichi Oda, Shingo Yokoi, Tsuyoshi Finel, Moshe Hatakeyama, Masahiko Fukami, Tatsuki Nakajima, Miki
Published in
Drug metabolism and pharmacokinetics
UDP-Glucuronosyltransferase (UGT) 2A3 belongs to a UGT superfamily of phase II drug-metabolizing enzymes that catalyzes the glucuronidation of many endobiotics and xenobiotics. Previous studies have demonstrated that UGT2A3 is expressed in the human liver, small intestine, and kidney at the mRNA level; however, its protein expression has not been d...
Means, Shawn A Ho, Harvey
Published in
Drug metabolism and pharmacokinetics
The metabolism zonation in liver lobules is well known yet its incorporation into the mathematical models of acetaminophen (APAP) metabolism is still primitive - only the oxidation pathway via reaction with the cytochrome P450 (CYP450) has been considered, yet the zonal heterogeneity exhibits in all three pathways including sulphation, glucuronidat...
Mori, Daiki Kashihara, Yushi Yoshikado, Takashi Kimura, Miyuki Hirota, Takeshi Matsuki, Shunji Maeda, Kazuya Irie, Shin Ieiri, Ichiro Sugiyama, Yuichi
...
Published in
Drug metabolism and pharmacokinetics
This study aimed to elucidate the impact of OATP1B1 genotype (*1b/*1b, *1b/*15, and *15/*15) on plasma concentrations of endogenous OATP1B1 substrates. Healthy volunteers with OATP1B1 *1b/*1b (n = 10), *1b/*15 (n = 7), or *15/*15 (n = 2) received oral administration of a cocktail of statins (atorvastatin, pitavastatin, rosuvastatin, and fluvastatin...
Iwamoto, Noriko Shimada, Takashi
Published in
Drug metabolism and pharmacokinetics
In recent studies, the development of bioanalysis technologies using liquid chromatography-tandem mass spectrometry (LC-MS/MS) has attracted attention. Our developed nano-surface and molecular-orientation limited (nSMOL) proteolysis enables Fab-specific proteolysis and is optimal for LC-MS/MS analysis of antibody drugs and Fc-fusion proteins in bio...
Uno, Yasuhiro Shimizu, Makiko Yoda, Hiromi Origuchi, Yumi Yamazaki, Hiroshi
Published in
Drug metabolism and pharmacokinetics
Polymorphic human flavin-containing monooxygenase (FMO) 3 is an important drug-metabolizing enzyme for nitrogen- or sulfur-containing compounds. Cynomolgus macaques, a non-human primate species widely used in drug metabolism studies, have corresponding FMO3 molecular and enzymatic similarities to humans; however, genetic polymorphisms have not been...
Tachibana, Tatsuhiko Kuwabara, Takashi
Published in
Drug metabolism and pharmacokinetics
Imaoka, Ayuko Seki, Kohei Akiyoshi, Takeshi Ohtani, Hisakazu
Published in
Drug metabolism and pharmacokinetics
Activated charcoal decreases gastrointestinal absorption of concomitantly administered drugs. The absorption of amlodipine (AML) was reported as almost completely attenuated by 25 g of activated charcoal under a fasted condition, but not affected by 2 g of activated charcoal under a fed condition. However, it is not clear whether this difference re...
Kito, Tomoko Ito, Sumito Mizuno, Tadahaya Maeda, Kazuya Kusuhara, Hiroyuki
Published in
Drug metabolism and pharmacokinetics
The purpose of this study was to elucidate the involvement of Mate1 in the tubular secretion of trimethoprim and saturation of Mate1-mediated efflux to address the mechanisms underlying the pharmacokinetic drug interactions with trimethoprim. Trimethoprim is a more potent inhibitor of MATE2-K than MATE1 with Ki values (μM) of 0.030-0.28 and 2.4-5.9...
Iwasaki, Kazuhide Uno, Yasuhiro Utoh, Masahiro Yamazaki, Hiroshi
Published in
Drug metabolism and pharmacokinetics
Animal species used in the preclinical studies for development of monoclonal antibody (mAb) drugs are surveyed in this review. Relevant animal species for preclinical studies of mAb candidates are those express desired epitope of mAb candidates. Cynomolgus monkeys cross-react with mAb drugs much higher than other animal species commonly used in pre...
