Drug Metabolism and Pharmacokinetics This is an RSS file. You can use it to subscribe to this data in your favourite RSS reader or to display this data on your own website or blog.

Unveiling the intra-tumor fate of trastuzumab deruxtecan in a xenograft model to support its mechanism of action
Drug Metab Pharmacokinet. 2024 Jan 23;56:101001. doi: 10.1016/j.dmpk.2024.101001. Online ahead of print.ABSTRACTTrastuzumab deruxtecan (T-DXd) is an antibody-drug conjugate used for cancer treatment comprising an anti-human epidermal growth factor receptor type 2 (HER2) antibody and the topoisomerase I inhibitor DXd. The present study investigated the intratumor fate of T-DXd. Fluorescence-labeled T-DXd was found to accumulate in tumors of HER2-positive tumor xenograft mice and was observed to be distributed within lysosomes of in vitro tumor cells in accordance with their HER2 expression. DXd was released by cysteine prot...
Source: Drug Metabolism and Pharmacokinetics - April 21, 2024 Category: Drugs & Pharmacology Authors: Yoko Nagai Masataka Oitate Takahiro Shibayama Hideo Takakusa Nobuaki Watanabe Source Type: research

Construction of a fused grid-based CYP2C8-Template system and the application
Drug Metab Pharmacokinet. 2023 Jan 20:100492. doi: 10.1016/j.dmpk.2023.100492. Online ahead of print.ABSTRACTA ligand-accessible space in the CYP2C8 active site was reconstituted as a fused grid-based Template∗ with the use of structural data of the ligands. An evaluation system of CYP2C8-mediated metabolism has been developed on Template with the introduction of the idea of Trigger-residue initiated ligand-movement and fastening. Reciprocal comparison of the data of simulation on Template with experimental results suggested a unified way of the interaction of CYP2C8 and its ligands through the simultaneous plural-contac...
Source: Drug Metabolism and Pharmacokinetics - April 12, 2024 Category: Drugs & Pharmacology Authors: Yasushi Yamazoe Yoshiya Yamamura Kouichi Yoshinari Source Type: research

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