SCH-48461
SCH-48461 is a cholesterol absorption inhibitor that was developed by Schering-Plough. It is a potent and selective inhibitor of the Niemann-Pick C1-Like 1 (NPC1L1) protein, which is a critical mediator of cholesterol absorption in the intestine. SCH-48461 has been shown to reduce cholesterol absorption in both animals and humans, and it has potential therapeutic applications in the treatment of hypercholesterolemia and related conditions.
Mechanism of Action[edit | edit source]
SCH-48461 inhibits cholesterol absorption by binding to the NPC1L1 protein in the enterocytes of the small intestine. This prevents the uptake of dietary and biliary cholesterol into the body, thereby reducing the amount of cholesterol that is available for incorporation into lipoprotein particles and secretion into the bloodstream.
Pharmacology[edit | edit source]
In preclinical studies, SCH-48461 has been shown to have a high degree of selectivity for the NPC1L1 protein, with minimal off-target effects. It is orally active and has a long duration of action, which makes it suitable for once-daily dosing. In human studies, SCH-48461 has been shown to reduce cholesterol absorption by approximately 50%, with a corresponding decrease in plasma cholesterol levels.
Clinical Development[edit | edit source]
SCH-48461 has undergone Phase I and II clinical trials for the treatment of hypercholesterolemia. In these trials, it was generally well tolerated and showed a significant cholesterol-lowering effect. However, further development of SCH-48461 was discontinued for undisclosed reasons.
See Also[edit | edit source]
- Ezetimibe, another cholesterol absorption inhibitor that is currently marketed for the treatment of hypercholesterolemia.
- Niemann-Pick disease, a genetic disorder that is caused by mutations in the NPC1 and NPC2 genes.
| SCH-48461 Resources | |
|---|---|
|
 |
Search WikiMD
Ad.Tired of being Overweight? Try W8MD's physician weight loss program.
Semaglutide (Ozempic / Wegovy and Tirzepatide (Mounjaro / Zepbound) available.
Advertise on WikiMD
|
WikiMD's Wellness Encyclopedia |
| Let Food Be Thy Medicine Medicine Thy Food - Hippocrates |
Translate this page: - East Asian
中文,
日本,
한국어,
South Asian
हिन्दी,
தமிழ்,
తెలుగు,
Urdu,
ಕನ್ನಡ,
Southeast Asian
Indonesian,
Vietnamese,
Thai,
မြန်မာဘာသာ,
বাংলা
European
español,
Deutsch,
français,
Greek,
português do Brasil,
polski,
română,
русский,
Nederlands,
norsk,
svenska,
suomi,
Italian
Middle Eastern & African
عربى,
Turkish,
Persian,
Hebrew,
Afrikaans,
isiZulu,
Kiswahili,
Other
Bulgarian,
Hungarian,
Czech,
Swedish,
മലയാളം,
मराठी,
ਪੰਜਾਬੀ,
ગુજરાતી,
Portuguese,
Ukrainian
Medical Disclaimer: WikiMD is not a substitute for professional medical advice. The information on WikiMD is provided as an information resource only, may be incorrect, outdated or misleading, and is not to be used or relied on for any diagnostic or treatment purposes. Please consult your health care provider before making any healthcare decisions or for guidance about a specific medical condition. WikiMD expressly disclaims responsibility, and shall have no liability, for any damages, loss, injury, or liability whatsoever suffered as a result of your reliance on the information contained in this site. By visiting this site you agree to the foregoing terms and conditions, which may from time to time be changed or supplemented by WikiMD. If you do not agree to the foregoing terms and conditions, you should not enter or use this site. See full disclaimer.
Credits:Most images are courtesy of Wikimedia commons, and templates Wikipedia, licensed under CC BY SA or similar.
Contributors: Prab R. Tumpati, MD
