Influence of inflammation on drug transporter expression in human airway epithelia: Implications for inhaled drug pharmacokinetics [0.03%]
炎症对人呼吸道上皮药物转运蛋白表达的影响：对吸入给药药代动力学的启示
Charles R Esther Jr,John K Fallon,Deborah M Cholon et al.
Charles R Esther Jr et al.
The efficacy of inhaled drugs is significantly influenced by airway epithelial transporters that mediate their transport and distribution. Because inhaled drugs are used across diverse populations with inflammatory airway diseases, understa...
Human absorption, distribution, metabolism, excretion, and reaction phenotyping of ervogastat (PF-06865571), a diacylglycerol O-acyltransferase 2 inhibitor [0.03%]
口服 evacagastat（PF-06865571，一种二酰基甘油O-酰基转移酶2抑制剂）的人体吸收、分布、代谢、排泄及反应表型研究
Manoli Vourvahis,Christine C Orozco,David Tess et al.
Manoli Vourvahis et al.
Ervogastat (PF-06865571) is a potent and selective small-molecule inhibitor of diacylglycerol-O-acyltransferase-2 currently in clinical development for treating metabolic dysfunction-associated steatohepatitis with liver fibrosis. A fixed s...
Transcriptomic and metabolite-centric profiling reveal aryl hydrocarbon receptor-mediated cytochrome P450 1A1 autoinduction of the selective modulator PM-4321 [0.03%]
转录组和代谢物谱分析揭示了PM-4321介导的芳香烃受体调控的细胞色素P450 1A1自身诱导作用
Seema Kumar,Keith Goodman,Sue Yi et al.
Seema Kumar et al.
PM-4321 is a selective aryl hydrocarbon receptor (AhR) modulator profiled as part of an AhR antagonist program for cancer immunotherapy. The AhR regulates transcription of xenobiotic metabolizing enzymes, including cytochrome P450 (CYP) 1A1...
Comparative study of absorption prediction using human intestinal organoid-derived cells in static and flow conditions [0.03%]
基于人体肠道类器官衍生细胞的吸收预测比较研究(static和flow条件)
Qianying Yuan,Julie Harney,James E Finley et al.
Qianying Yuan et al.
Reliable prediction of human oral drug absorption is critical in early-stage drug development. However, physiologically relevant intestine cell models capturing multiple drug disposition mechanisms including transport and metabolism are lim...
Impact of the gut microbiome on hepatic cytochrome P450 3A4 (CYP3A4) in humanized pregnane X receptor-constitutive androstane receptor-CYP3A4/3A7 mice [0.03%]
肠道微生物组对人源化孕烷X受体-构巢臼受体-CYP3A4 / 3A7小鼠肝脏CYP3A4的影响
Jennifer Liem,Xin Chen,Joe J Lim et al.
Jennifer Liem et al.
The interaction between the gut microbiome and drug metabolism is bidirectional and can influence the pharmacokinetics of certain drugs. In mice, the gut microbiome has been shown to influence Cyp3a11. However, evidence for microbial regula...
Evidence for endogenous amine conjugation and cytotoxicity arising from metabolic activation of trazodone [0.03%]
トラゾドンの代謝活性化に起因する内因性アミンとの結合及び細胞毒性に関する報告
Yang Wang,Yan Shen,Hao Zhou et al.
Yang Wang et al.
Trazodone (TRZ), a tetracyclic antidepressant, is commonly utilized either independently or in combination with other antidepressants to treat depression. It has also been reported to be associated with multiple cases of acute liver injury,...
Gut microbial resistance and metabolism of selective serotonin reuptake inhibitors drive multidrug resistance and contribute to antidepressant tachyphylaxis [0.03%]
肠道微生物对选择性五羟色胺回收抑制剂的抵抗及代谢作用促进多药耐受并导致抗抑郁药物速服
Ming-Che Cheng,Hsiao-Ching Lin,Chia-Ching Liaw et al.
Ming-Che Cheng et al.
Selective serotonin reuptake inhibitors (SSRIs) are among the most widely used antidepressant medications in modern clinical practice. However, the underlying mechanisms of the rapid onset of tolerance to antidepressants (antidepressant tac...
Loss of PPARα-UGT1 axis exacerbates triclosan-induced steatohepatitis in humanized UDP-glucuronosyltransferase 1 mice [0.03%]
PPARα-UGT1轴丢失加重人源化UDP葡萄糖醛酸转移酶1对三氯生诱导的肝炎的影响
Xiaojing Yang,Gabriela Bulli,Samantha Wong et al.
Xiaojing Yang et al.
Triclosan (TCS) is an antimicrobial toxicant found in a wide range of consumer products and has been detected in human tissues at concentrations ranging from 0.001 to 5 ppm. Hepatotoxic chemicals such as TCS can cause steatotic liver diseas...
Mechanistic prediction of apixaban and rivaroxaban secretion into human milk and infant systemic exposure through an integrated physiologically based pharmacokinetic framework [0.03%]
基于生理的药代动力学预测阿哌沙班和利伐沙班在人乳中的分泌及通过综合框架下的婴儿全身暴露量的研究
Bofang Yi,Sung Hun Bae,Yongzong Yang et al.
Bofang Yi et al.
Accurately characterizing the transfer of apixaban and rivaroxaban into human milk is essential for evaluating their safety during lactation and for guiding anticoagulant therapy in breastfeeding patients. This study aimed to establish a me...
Bile duct ligation impairs function and expression of breast cancer resistance protein in rat blood-retinal barrier mainly due to both the increased ammonia and bilirubin [0.03%]
胆管结扎通过增加氨和胆红素主要影响血视网膜屏障中乳腺癌耐药蛋白的功能及表达
Zijin Lin,Runze Wu,Yiting Yang et al.
Zijin Lin et al.
Patients with liver failure often suffer from hepatic retinopathy, partly due to the blood-retinal barrier (BRB) impairment. BRB includes the inner BRB formed by retinal microvascular endothelial cells and the outer BRB formed by retinal pi...