Application of machine learning techniques in population pharmacokinetics/pharmacodynamics modeling [0.03%]
机器学习技术在人群药动/药效模型中的应用
Mizuki Uno,Yuta Nakamaru,Fumiyoshi Yamashita
Mizuki Uno
Population pharmacokinetics/pharmacodynamics (pop-PK/PD) consolidates pharmacokinetic and pharmacodynamic data from many subjects to understand inter- and intra-individual variability due to patient backgrounds, including disease state and ...
Prediction of drug-drug interaction risk of P-glycoprotein substrate in drug discovery [0.03%]
药物发现中P-糖蛋白底物药物相互作用风险的预测
Yasuto Kido,Isamu Nanchi,Takanobu Matsuzaki et al.
Yasuto Kido et al.
We 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 ...
In vitro demonstration of antedrug mechanism of a pharmacokinetic booster to improve CYP3A4 substrates by CYP3A4-mediated metabolism inhibition [0.03%]
体外研究药物代谢酶CYP3A4底物前药机制以改善由CYP3A4介导的代谢抑制的效果
Makoto Kataoka,Sae Takenaka,Shota Fujii et al.
Makoto Kataoka et al.
We previously reported novel benzyl-ether derivatives with an imidazole ring and a hydroxyl group (A-01) or carboxyl group (B-01) and esters (2 esters of A-01, and 7 esters of B-01) as pharmacokinetics (PK) boosters. This study demonstrates...
Unveiling the intra-tumor fate of trastuzumab deruxtecan in a xenograft model to support its mechanism of action [0.03%]
在异种移植模型中揭示德鲁替康的肿瘤内作用机制以支持其作用机理研究
Yoko Nagai,Masataka Oitate,Takahiro Shibayama et al.
Yoko Nagai et al.
Trastuzumab 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 th...
Construction of a fused grid-based CYP2C8-Template system and the application [0.03%]
基于融合网格的CYP2C8-Template系统构建及应用研究
Yasushi Yamazoe,Yoshiya Yamamura,Kouichi Yoshinari
Yasushi Yamazoe
A 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 th...
Predicting muscarinic receptor occupancy in human bladder mucosa from urinary concentrations of antimuscarinic agents for overactive bladder [0.03%]
通过尿抗胆碱能药物浓度预测过活动膀胱患者人体膀胱粘膜胆碱能受体occupancy率
Mizuki Shiho,Gaku Akashita,Eriko Nakatani et al.
Mizuki Shiho et al.
To 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 mus...
Population pharmacokinetics of everolimus in renal transplant recipients receiving long-term multiple immunosuppressive therapy [0.03%]
长期多种免疫抑制治疗的肾移植受者的依维莫司群体药代动力学
Tomoyuki Sakaue,Kazuhiro Yamamoto,Kotaro Itohara et al.
Tomoyuki Sakaue et al.
Everolimus is used for immunosuppression after renal transplantation. This study aimed to develop a population pharmacokinetic (PopPK) model of everolimus using therapeutic drug monitoring (TDM) data of patients under long-term multiple imm...
Physiologically based pharmacokinetic modeling to predict the clinical effect of azole antifungal agents as CYP3A inhibitors on azelnidipine pharmacokinetics [0.03%]
基于生理的药代动力学建模预测唑类抗真菌药物作为CYP3A抑制剂对阿扎他定药代动力学的临床影响
Akiko Watanabe,Masakatsu Kotsuma
Akiko Watanabe
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 pharmaco...
Air-liquid interface culture and modified culture medium promote the differentiation of human induced pluripotent stem cells into intestinal epithelial cells [0.03%]
空气液界面培养和改良的培养基促进人诱导多能干细胞向肠上皮细胞分化
Kotaro Shirai,Shimeng Qiu,Hanako Minowa et al.
Kotaro Shirai et al.
An in vitro system that evaluates pharmacokinetics in the small intestine is crucial for the development of oral drugs. We produced human induced pluripotent stem cell-derived small intestinal epithelial cells (hiSIECs) with high drug metab...
Transcript abundance of hepatic drug-metabolizing enzymes in two dog breeds compared with 14 species including humans [0.03%]
两种犬类与包括人类在内的14种物种的肝脏药物代谢酶转录丰度比较
Yasuhiro Uno,Osamu Yamato,Hiroshi Yamazaki
Yasuhiro Uno
Drug-metabolizing enzymes are important in drug development and therapy, but have not been fully identified and characterized in many species, lines, and breeds. Liver transcriptomic data were analyzed for phase I cytochromes P450, flavin-c...