Preferred Label : Ezetimibe/Simvastatin;
NCIt synonyms : Butanoic Acid, 2,2-Dimethyl-, (1S,3R,7S,8S,8aR)-1,2,3,7,8,8a-hexahydro-3,7-dimethyl-8-(2-((2R,4R)-tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl)-1-naphthalenyl
Ester, Mixture with (3R,4S)-1-(4-Fluorophenyl)-3-((3S)-3-(4-fluorophenyl)-3-hydroxypropyl)-4-(4-hydroxyphenyl)-2-azetidinone;
NCIt definition : An orally bioavailable combination agent containing the cholesterol absorption inhibitor
ezetimibe and the hepatic hydroxymethyl-glutaryl coenzyme A (HMG-CoA) reductase inhibitor
simvastatin, with lipid-lowering activity. Upon oral administration, ezetimibe binds
to the sterol transporter Niemann-Pick C1-Like 1 (NPC1L1) at the brush border of the
small intestine and inhibits the intestinal absorption of biliary and dietary cholesterol
and related phytosterols. This decreases blood cholesterol levels, decreases the delivery
of intestinal cholesterol to the liver, reduces hepatic cholesterol stores and enhances
the clearance of cholesterol from the bloodstream. Upon administration of simvastatin
and subsequent hydrolyzation to its active beta-hydroxyacid form, this statin competitively
inhibits HMG-CoA reductase, the enzyme which catalyzes the conversion of HMG-CoA to
mevalonate, which is an essential step in cholesterol synthesis. Ezetimibe and simvastatin
together reduce blood levels of total cholesterol, low-density lipoprotein cholesterol
(LDL-C), triglycerides (TGs), very-low-density lipoproteins (VLDL), and apolipoprotein
B (Apo B), and increase the plasma concentration of high-density lipoprotein cholesterol
(HDL-C). Higher cholesterol blood levels appear to be associated with an increased
risk in the proliferation of certain cancer cells, such as prostate cancer cells.;
CAS number : 444313-53-5;
Drug name : Vytorin;
Origin ID : C123926;
UMLS CUI : C1532737;
Currated CISMeF NLP mapping
- See also inter- (CISMeF)
- Semantic type(s)
- UMLS correspondences (same concept)
- concept_is_in_subset
- has_target
