INDUCTIVE EFFECTS OF NELFINAVIR AND RITONAVIR

奈非那韦和利托那韦的诱导作用

• 批准号: 7603474
• 负责人: Ann Cornwall Collier
• 金额: $ 2.11万
• 依托单位: UNIVERSITY OF WASHINGTON
• 依托单位国家: 美国
• 财政年份: 2007
• 资助国家: 美国
• 起止时间: 2007-04-01 至 2007-09-16
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/7603474
• 关键词: Computer Retrieval of Information on Scientific Projects Database; Cytochrome P450; Drug Interactions; Enzymes; Funding; Grant; HIV Protease Inhibitors; In Vitro; Institution; Measures; Nelfinavir; P-Glycoprotein; P-Glycoproteins; Pharmaceutical Preparations; Protease Inhibitor; Research; Research Personnel; Resources; Rifampin; Ritonavir; Source; United States National Institutes of Health; clinically relevant; enzyme activity; in vivo

This subproject is one of many research subprojects utilizing the resources provided by a Center grant funded by NIH/NCRR. The subproject and investigator (PI) may have received primary funding from another NIH source, and thus could be represented in other CRISP entries. The institution listed is for the Center, which is not necessarily the institution for the investigator. Anti-HIV protease inhibitors (PIs) like ritonavir and nelfinavir have the propensity to produce clinically-relevant inductive and inhibitory drug interactions. To quantify inductive drug interactions of the PIs, we wish to determine the extent to which nelfinavir or ritonavir induce the activity of the following cytochrome P450 enzymes (CYP): 1A2, 2C9, 2D6, 3A and P-glycoprotein (P-gp). We will accomplish this by administering drugs which will measure the in vivo activities of these enzymes and transporter, both before and after induction with nelfinavir or ritonavir. To aid in correlating these results to results obtained in vitro we will compare the in vivo induction of CYPs and P-gp by the PIs to that obtained with rifampin, a well known inducer of CYP enzymes and P-gp.

这个子项目是许多研究子项目中利用 资源由NIH/NCRR资助的中心拨款提供。子项目和 调查员(PI)可能从NIH的另一个来源获得了主要资金， 并因此可以在其他清晰的条目中表示。列出的机构是 该中心不一定是调查人员的机构。 抗HIV蛋白水解酶抑制剂(PI)如利托那韦和奈非那韦具有产生与临床相关的诱导性和抑制性药物相互作用的倾向。为了量化PI的诱导性药物相互作用，我们希望确定奈非那韦或利托那韦诱导以下细胞色素P450酶(CYP)的活性的程度：1A2、2C9、2D6、3A和P-糖蛋白(P-gp)。我们将通过给药来测量奈非那韦或利托那韦诱导前后体内这些酶和转运蛋白的活性，从而实现这一点。为了帮助将这些结果与体外获得的结果相关联，我们将比较PI在体内对CyPS和P-gp的诱导作用，以及用利福平获得的诱导作用，利福平是一种众所周知的CYP酶和P-gp的诱导剂。