"Search For Safer Azole Antifungal Drugs: Studies of New Ketoconazole (K) Derivatives," by Christina Pyrgakil, Lajos Gera et al; "Role of Cytochrome P450s in the Reductive Metabolism of Tamoxifen N-Oxide," by Priyanka Parte and David Kupfer; "Sulfation of Tibolone Metabolites by Postmenopausal...
“Phase I and Phase II” Drug Metabolism: Terminology that we Should Phase Out?: Drug Metabolism Reviews: Vol 37, No 4 Click to increase image sizeClick to decrease image size PD Josephy,FP Guengerich - 《Drug Metabolism Reviews》 被引量: 64发表: 2005年 Pharmacokinetics of traditional ...
The role of pharmacokinetics, drug interactions and pharmacogenetics in the acquired long QT syndrome Biotransformation of drugs is accomplished by phase I (P450 enzymes) and phase II metabolism (conjugation) predominantly in the small intestine and liver. ... BAUMAN,J - 《European Heart Journal Sup...
The role of drug metabolism in drug discovery (lead compound selection) and the traditional role of identifying the enzymes involved in biotransformation pathways (reaction phenotyping) have both relied heavily on the availability and use of a human liver bank. The assessment of drug metabolizing enzy...
药物代谢的酶 Enzymes for Drug Metabolism 第I相生物转化是官能团化反应,是在体内多种酶系的催化下,对药物分子引入新的官能团或改变原有的官能团的过程。参与药物体内I相生物转化的酶类,主要是氧化-还原酶和水解酶。 细胞色素P-450酶系(Cytochrome P-450 Enzyme System) ...
Much focus has been given to genetic based differences in the activity of certain cytochrome P450 (CYP) enzymes responsible for the metabolism of a wide variety of commonly used drugs, in particular in psychiatry and the treatment of depression. Table 1 summarizes important cytochrome P450 isoforms...
0期(Phase 0/Microdosing) 也被称为人体微量给药(Microdosing)研究,由FDA在2004年提出,在I期试验之前进行,以预测药物是否适用于下一阶段的试验,这不是新药临床研究必需的。 在这个阶段给药剂量极低,不会有治疗效果,难以产生全身效应,但足以研究细胞反应。这个阶段将提供药物的药代动力学和药效学的初步数据,如果...
It is well appreciated that microbial metabolism of drugs can influence treatment efficacy. Microbial β-glucuronidases in the gut can reactivate the excreted, inactive metabolite of irinotecan, a first-line chemotherapeutic for metastatic colorectal can
Simeprevir has demonstrated high SVR rates in patients with HCV genotype 1 infection during phase II and III trials [4–10]. In the phase II COSMOS trial, combination therapy with simeprevir and sofosbuvir (±RBV), an IFN-free regimen, was demonstrated to have an SVR 12 weeks after the pla...
Dysregulation of iron homeostasis occurs in haematological disorders and in other diseases such as cancer and neurodegeneration. Crielaard and colleagues discuss the progress made in interfering with iron metabolism as a therapeutic strategy, as well as