Any inhibitor of cholesterylester transfer protein (CETP), which transfers cholesterol from high density lipoproteins (HDL, the 'good' cholesterol-containing particles) to low or very low density lipoproteins (LDL or VLDL, the 'bad' cholesterol-containing particles). Inhibition of this process results in higher HDL levels and lower LDL levels. CETP inhibitors are under investigation as potential drugs to reduce the risk of arteriosclerotic vascular disease (atherosclerosis).
ChEBI ID: 49205
| Member | Definition | Class |
|---|---|---|
| rosuvastatin | A dihydroxy monocarboxylic acid that is (6E)-7-{4-(4-fluorophenyl)-2-[methyl(methylsulfonyl)amino]-6-(propan-2-yl)pyrimidin-5-yl} hept-6-enoic acid carrying two hydroxy substituents at positions 3 and 5 (the 3R,5S-diastereomer). | rosuvastatin |
| rosuvastatin calcium | An organic calcium salt that is the hemicalcium salt of rosuvastatin. | rosuvastatin calcium |
| torcetrapib | torcetrapib |
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 1 (0.33) | 18.2507 |
| 2000's | 166 (54.79) | 29.6817 |
| 2010's | 127 (41.91) | 24.3611 |
| 2020's | 9 (2.97) | 2.80 |
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 28 (8.86%) | 5.53% |
| Reviews | 70 (22.15%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 218 (68.99%) | 84.16% |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 1.6933 | 1 | 1 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 27.8008 | 4 | 4 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 3-hydroxy-3-methylglutaryl-coenzyme A reductase | Homo sapiens (human) | IC50 | 0.0045 | 3 | 3 |
| 3-hydroxy-3-methylglutaryl-coenzyme A reductase | Homo sapiens (human) | Ki | 35.5004 | 2 | 2 |
| 3-hydroxy-3-methylglutaryl-coenzyme A reductase | Rattus norvegicus (Norway rat) | IC50 | 1.1315 | 8 | 8 |
| ATP-binding cassette sub-family C member 3 | Homo sapiens (human) | IC50 | 58.3000 | 1 | 1 |
| Bile salt export pump | Homo sapiens (human) | IC50 | 133.0000 | 1 | 1 |
| Canalicular multispecific organic anion transporter 1 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 1 |
| Cholesteryl ester transfer protein | Homo sapiens (human) | IC50 | 0.0152 | 4 | 4 |
| Multidrug resistance-associated protein 4 | Homo sapiens (human) | IC50 | 26.8000 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 3-hydroxy-3-methylglutaryl-coenzyme A reductase | Homo sapiens (human) | Kd | 0.0170 | 1 | 1 |
| Retinal rod rhodopsin-sensitive cGMP 3',5'-cyclic phosphodiesterase subunit delta | Homo sapiens (human) | Kd | 1.2500 | 1 | 1 |