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In vitro demonstration of antedrug mechanism of a pharmacokinetic booster to improve CYP3A4 substrates by CYP3A4-mediated metabolism inhibition
In conclusion, B-01 ester compounds may be safe PK boosters with antedrug characteristics.PMID:38663182 | DOI:10.1016/j.dmpk.2024.101005 (Source: Drug Metabolism and Pharmacokinetics)
Source: Drug Metabolism and Pharmacokinetics - April 25, 2024 Category: Drugs & Pharmacology Authors: Makoto Kataoka Sae Takenaka Shota Fujii Takato Masada Keiko Minami Toshihide Takagi Masaaki Omote Kentaro Kawai Shinji Yamashita Source Type: research

Prediction of drug-drug interaction risk of P-glycoprotein substrate in drug discovery
Drug Metab Pharmacokinet. 2024 Mar 11;56:101008. doi: 10.1016/j.dmpk.2024.101008. Online ahead of print.ABSTRACTWe aimed at predicting the drug-drug interaction (DDI) risk of P-glycoprotein (P-gp) substrates by using P-gp expressing LLC-PK1 cells and its knockout mice (KO). The area under the curve (AUC) of 16 marketed drugs and plasma concentration (Cplasma) of 207 screening compounds, with corrected efflux ratio (CER) ≥ 2, were compared between P-gp KO mice and wild type mice (WT). At permeability (Papp) ≥ 10 × 10-6 cm/s in parent LLC-PK1 cells, AUC ratios (KO/WT) and Cplasma ratios (KO/WT) of these compounds were w...
Source: Drug Metabolism and Pharmacokinetics - April 25, 2024 Category: Drugs & Pharmacology Authors: Yasuto Kido Isamu Nanchi Takanobu Matsuzaki Ryosuke Watari Hayato Kiyohara Naomi Seki Tomohiko Okuda Source Type: research

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