Adverse Drug Reaction Classification System

Pharmaceutical Information
Drug Name Ezetimibe
Drug ID BADD_D00864
Description Ezetimibe is a lipid-lowering compound that inhibits intestinal cholesterol and phytosterol absorption. The discovery and research of this drug began in the early 1990s, after the intravenous administration of radiolabelled ezetimibe in rats revealed that it was being localized within enterocytes of the intestinal villi - this prompted studies investigating the effect of ezetimibe on intestinal cholesterol absorption.[A15202] Ezetimibe is used as an adjunctive therapy to a healthy diet to lower cholesterol levels in primary hyperlipidemia, mixed hyperlipidemia, homozygous familial hypercholesterolemia (HoFH), and homozygous sitosterolemia (phytosterolemia).[L11347] Unlike other classes of cholesterol-reducing compounds including statins and bile acid sequestrants, ezetimibe has a distinct mechanism of action involving the sterol transporter Niemann-Pick C1-Like 1 (NPC1L1), and is unique in that it does not affect the absorption of fat-soluble nutrients such as fat-soluble vitamins, triglycerides, or bile acids.[A33313] In genetically NPC1L1-deficient mice, a 70% reduction in intestinal cholesterol absorption was seen, and these mice were insensitive to ezetimibe treatment - it was determined based on these findings that NPC1L1 plays an essential role in promoting intestinal cholesterol uptake via an ezetimibe-sensitive pathway.[A15202] By interfering with the intestinal uptake of cholesterol and phytosterols, ezetimibe reduces the delivery of intestinal cholesterol to the liver.[L11347]
Indications and Usage For use as adjunctive therapy to diet for the reduction of elevated total-C, LDL-C, and Apo B in patients with primary (heterozygous familial and non-familial) hypercholesterolemia.
Marketing Status Prescription
ATC Code C10AX09
DrugBank ID DB00973
KEGG ID D01966
MeSH ID D000069438
PubChem ID 150311
TTD Drug ID D09LWS
NDC Product Code 60429-982; 72189-118; 63629-7413; 66039-839; 0591-3713; 70966-0027; 70518-2262; 0781-5690; 65096-0113; 69218-0400; 55111-079; 71205-277; 51660-200; 50228-379; 66039-896; 78206-178; 65015-812; 50268-298; 68382-773; 59651-052; 71335-1354; 50090-3657; 71335-0933; 71205-145; 16729-433; 75895-0281; 70518-3334; 58032-2004; 71335-1127; 50090-3087; 69218-0800; 15894-0011; 70771-1109; 66039-869; 68554-0085; 16714-813; 59651-056; 60687-373; 0615-8300; 0904-6664; 71335-0684; 64176-0042; 69238-1154; 0904-7103; 60505-2945; 14501-0008; 67877-490
Synonyms Ezetimibe | (1-(4-fluorophenyl)-(3R)-(3-(4-fluorophenyl)-(3S)-hydroxypropyl)-(4S)-(4-hydroxyphenyl)-2-azetidinone) | Ezetimib | Ezetrol | SCH 58235 | 58235, SCH | SCH-58235 | SCH58235 | Zetia
Chemical Information
Molecular Formula C24H21F2NO3
CAS Registry Number 163222-33-1
SMILES C1=CC(=CC=C1C2C(C(=O)N2C3=CC=C(C=C3)F)CCC(C4=CC=C(C=C4)F)O)O
Chemical Structure
ADR Related Proteins Induced by Drug
ADR Term Protein Name UniProt AC TTD Target ID PMID
Not AvailableNot AvailableNot AvailableNot AvailableNot Available
ADRs Induced by Drug
ADR Term ADReCS ID ADR Frequency (FAERS) ADR Severity Grade (FAERS) ADR Severity Grade (CTCAE)
Bone disorder15.02.04.004--Not Available
Bone pain15.02.01.0010.000314%
Bradycardia02.03.02.002--Not Available
Bruxism07.01.06.008; 19.11.03.0010.000314%Not Available
Cardiac failure02.05.01.001--
Cardiac failure congestive02.05.01.002--Not Available
Cardiomyopathy02.04.01.0010.000628%Not Available
Cardiovascular disorder24.03.02.009; 02.01.01.0010.000123%Not Available
Cerebrovascular accident17.08.01.007; 24.03.05.001--
Chest discomfort22.02.08.001; 08.01.08.019; 02.02.02.0090.001100%Not Available
Chest pain22.02.08.003; 08.01.08.002; 02.02.02.011--Not Available
Cholecystectomy25.09.01.001--Not Available
Cholecystitis09.03.01.001--
Cholelithiasis09.03.01.0020.000314%Not Available
Chromaturia20.02.01.0020.000314%
Colon cancer16.13.01.001; 07.21.01.0010.000314%Not Available
Coma17.02.09.0010.000314%Not Available
Compartment syndrome24.04.05.006; 15.05.05.0050.000328%Not Available
Confusional state19.13.01.001; 17.02.03.005--
Constipation07.02.02.001--
Cough22.02.03.001--
Deafness04.02.01.0010.000314%Not Available
Death08.04.01.001--
Depression19.15.01.001--
Dermatitis23.03.04.002--Not Available
Dermatomyositis23.03.02.001; 15.05.01.002; 10.04.02.001--Not Available
Diarrhoea07.02.01.0010.004241%
Discomfort08.01.08.003--Not Available
Disorientation19.13.01.002; 17.02.05.0150.000314%Not Available
Dizziness24.06.02.007; 17.02.05.003; 02.01.02.0040.002827%
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