Comparison of the activity and disposition of the novel cholesterol absorption inhibitor, SCH58235, and its glucuronide, SCH60663
โ Scribed by Margaret Van Heek; Constance Farley; Douglas S Compton; Lizbeth Hoos; Kevin B Alton; Edmund J Sybertz; Harry R Davis Jr
- Book ID
- 110004914
- Publisher
- Nature Publishing Group
- Year
- 2000
- Tongue
- English
- Weight
- 183 KB
- Volume
- 129
- Category
- Article
- ISSN
- 0007-1188
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๐ SIMILAR VOLUMES
Our search for potent cholesterol absorption inhibitors led to the discovery of the I~-lactam SCH 48461. Structure activity relationship studies prompted us to this study of y-lactams, ring homologs of 13lactam SCH 48461, to determine their potential as cholesterol absorption inhibitors. The results
The lipid lowering agent ezetimibe (EZ) and its intestinally formed glucuronide (GLUC) were shown to be substrates of the efflux transporters P-glycoprotein (P-gp) and the multidrug resistance associated protein 2 (MRP2) which markedly influences the disposition and efficacy of EZ in man. This study