Ezetimibe

From Proteopedia

Ezetimibe is a medication used to treat high blood cholesterol and certain other lipid abnormalities.[1][2] Generally it is used together with dietary changes and a statin.[3] It is also available in the fixed combinations ezetimibe/simvastatin (Vytorin),[4] ezetimibe/atorvastatin,[5] ezetimibe/rosuvastatin,[2][6] and ezetimibe/bempedoic acid.[7] See also [1]. Ezetimibe inhibits the absorption of cholesterol from the small intestine and decreases the amount of cholesterol normally available to liver cells. The lower levels of cholesterol in the liver cells leads them to absorb more cholesterol from circulation and thus lowering the levels of circulating cholesterol. It blocks the critical mediator of cholesterol absorption, the Niemann-Pick C1-like 1 (NPC1L1) protein on the gastrointestinal tract epithelial cells, as well as in hepatocytes; it blocks aminopeptidase N and interrupts a caveolin 1–annexin A2 complex involved in trafficking cholesterol.[8] Niemann-Pick C1-like 1 bound with Ezetimibe (7dfz). Ezetimibe binding site.

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References

1. ↑ DailyMed. 26 January 2011. Archived from the original on 10 May 2021. Retrieved 13 August 2022
2. ↑ ^{2.0 2.1} "Ezetimibe Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Archived from the original on 17 June 2019. Retrieved 13 April 2019.
3. ↑ British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 196. ISBN 9780857113382.
4. ↑ "Vytorin- ezetimibe and simvastatin tablet". DailyMed. 1 June 2022. Archived from the original on 14 August 2022. Retrieved 13 August 2022.
5. ↑ "Liptruzet (ezetimibe and atorvastatin) tablets for oral useInitial U.S. Approval: 2013". DailyMed. 30 September 2016. Archived from the original on 14 August 2022. Retrieved 13 August 2022.
6. ↑ "Roszet- rosuvastatin and ezetimibe tablet Roszet (- rosuvastatin and ezetimibe tablet". DailyMed. 15 September 2021. Archived from the original on 14 August 2022. Retrieved 13 August 2022.
7. ↑ "Nexlizet- bempedoic acid and ezetimibe tablet, film coated". DailyMed. 24 September 2021. Retrieved 13 August 2022.
8. ↑ Phan BA, Dayspring TD, Toth PP. Ezetimibe therapy: mechanism of action and clinical update. Vasc Health Risk Manag. 2012;8:415-27. PMID:22910633 doi:10.2147/VHRM.S33664