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Predicting muscarinic receptor occupancy in human bladder mucosa from urinary concentrations of antimuscarinic agents for overactive bladder
Drug Metab Pharmacokinet. 2024 Jan 15;56:100998. doi: 10.1016/j.dmpk.2024.100998. Online ahead of print.ABSTRACTTo assess the pharmacologically relevant and selective muscarinic receptor occupancy in the bladder mucosa, we considered not only plasma drug concentrations but also urinary drug concentrations. The purpose of this study was to predict muscarinic receptor occupancy in the human bladder mucosa based on urinary concentrations in response to clinical dosages of antimuscarinic agents used to treat overactive bladder. The calculated mean plasma or serum unbound steady state concentrations were 0.06-11 nM in clinical ...
Source: Drug Metabolism and Pharmacokinetics - April 7, 2024 Category: Drugs & Pharmacology Authors: Mizuki Shiho Gaku Akashita Eriko Nakatani Shimako Tanaka Shizuo Yamada Takashi Okura Source Type: research

Population pharmacokinetics of everolimus in renal transplant recipients receiving long-term multiple immunosuppressive therapy
This study aimed to develop a population pharmacokinetic (PopPK) model of everolimus using therapeutic drug monitoring (TDM) data of patients under long-term multiple immunosuppressive therapy, including tacrolimus. To develop the model, 185 renal transplant recipients with 3358 everolimus blood concentrations during a median postoperative period of 35.3 months were included. The PopPK model is described as a one-compartment model with first-order absorption. The population mean of apparent clearance is 8.92 L/h (relative standard error = 3.6%), and this negatively correlated with the dose-normalized concentration (C/D) of...
Source: Drug Metabolism and Pharmacokinetics - March 28, 2024 Category: Drugs & Pharmacology Authors: Tomoyuki Sakaue Kazuhiro Yamamoto Kotaro Itohara Yumi Kitahiro Takahito Endo Naoki Yokoyama Takeshi Ishimura Tomohiro Omura Ikuko Yano Source Type: research

Physiologically based pharmacokinetic modeling to predict the clinical effect of azole antifungal agents as CYP3A inhibitors on azelnidipine pharmacokinetics
In this study, a physiologically based pharmacokinetic (PBPK) model of the cytochrome P450 3A (CYP3A) substrate azelnidipine was developed using in vitro and clinical data to predict the effects of azole antifungals on azelnidipine pharmacokinetics. Modeling and simulations were conducted using the Simcyp™ PBPK simulator. The azelnidipine model consisted of a full PBPK model and a first-order absorption model. CYP3A was assumed as the only azelnidipine elimination route, and CYP3A clearance was optimized using the pharmacokinetic profile of single-dose 5-mg azelnidipine in healthy participants. The model reproduced the r...
Source: Drug Metabolism and Pharmacokinetics - March 8, 2024 Category: Drugs & Pharmacology Authors: Akiko Watanabe Masakatsu Kotsuma Source Type: research