Repositioning Candidate Details
| Candidate ID: | R0311 |
| Source ID: | DB01039 |
| Source Type: | approved |
| Compound Type: | small molecule |
| Compound Name: | Fenofibrate |
| Synonyms: | |
| Molecular Formula: | C20H21ClO4 |
| SMILES: | CC(C)OC(=O)C(C)(C)OC1=CC=C(C=C1)C(=O)C1=CC=C(Cl)C=C1 |
| Structure: |
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| DrugBank Description: | Fenofibrate is a fibric acid derivative like [clofibrate] and [gemfibrozil].[A185954] Fenofibrate is used to treat primary hypercholesterolemia, mixed dyslipidemia, severe hypertriglyceridemia.[L8588,L8591] Fenofibrate was granted FDA approval on 31 December 1993.[L8585] |
| CAS Number: | 49562-28-9 |
| Molecular Weight: | 360.831 |
| DrugBank Indication: | Fenofibrate is indicated as adjunctive therapy to diet to reduce elevated LDL-C, Total-C, Triglycerides, and Apo B, and to increase HDL-C adults with primary hypercholesterolemia or mixed dyslipidemia.[L8588,L8591] Fenofibrate is also indicated to treat adults with severe hypertriglyceridemia.[L8588,L8591] |
| DrugBank Pharmacology: | Fenofibrate is a fibrate that activates peroxisome proliferator activated receptor alpha (PPARα) to alter lipid metabolism and treat primary hypercholesterolemia, mixed dyslipidemia, and severe hypertriglyceridemia.[A186002,L8588,L8591] Fenofibrate requires once daily dosing and has a half life of 19-27 hours so its duration of action is long.[A36366,L8588,L8591] Fenofibrate capsules are given at a dose of 50-150mg daily so the therapeutic index is wide.[L8591] Patients should be counselled about the risk of rhabdomyolysis, myopathy, and cholelithiasis when taking fibrates.[L8588,L8591] |
| DrugBank MoA: | Fenofibrate activates peroxisome proliferator activated receptor alpha (PPARα), increasing lipolysis, activating lipoprotein lipase, and reducing apoprotein C-III.[A186002,L8588,L8591] PPARα is a nuclear receptor and its activation alters lipid, glucose, and amino acid homeostasis.[A186002] Activation of PPARα activates transcription of gene transcription and translation that generates peroxisomes filled with hydrogen peroxide, reactive oxygen species, and hydroxyl radicals that also participate in lipolysis.[A186005] This mechanism of increased lipid metabolism is also associated with increased oxidative stress on the liver.[A186005] In rare cases this stress can lead to cirrhosis and chronic active hepatitis.[A186002,L8588,L8591] |
| Targets: | Peroxisome proliferator-activated receptor alpha; Nuclear receptor subfamily 1 group I member 2; Matrix metalloproteinase-25 |
| Inclusion Criteria: |
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