Torcetrapib
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Also known as CP-529,414CP-529414TORCETRAPIB (CP-529414)
Summary
Torcetrapib (CHEMBL479527) is a phase-3 clinical-stage small-molecule anticholesteremic drug; indicated across 9 conditions including familial hypercholesterolemia and coronary artery disorder.
At a glance
- Status: Max clinical phase 3 (not approved)
- Modality: Small molecule
- Indications: 9 conditions
- Clinical trials: 14
- Chemistry: 600.5 Da · C26H25F9N2O4
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL479527 |
| Name | Torcetrapib |
| Type | Small molecule |
| Max phase | 3 |
| FDA approved | no |
| PubChem CID | 159325 |
| ChEBI | CHEBI:49203 |
| Molecular formula | C26H25F9N2O4 |
| Molecular weight | 600.5 |
| InChIKey | CMSGWTNRGKRWGS-NQIIRXRSSA-N |
SMILES: CC[C@@H]1C[C@@H](C2=C(N1C(=O)OCC)C=CC(=C2)C(F)(F)F)N(CC3=CC(=CC(=C3)C(F)(F)F)C(F)(F)F)C(=O)OC
IUPAC name: ethyl (2R,4S)-4-[[3,5-bis(trifluoromethyl)phenyl]methyl-methoxycarbonylamino]-2-ethyl-6-(trifluoromethyl)-3,4-dihydro-2H-quinoline-1-carboxylate
Pharmacological roles (ChEBI): anticholesteremic drug, CETP inhibitor.
Also known as: CP-529,414, CP-529414, Torcetrapib, torcetrapib, TORCETRAPIB, TORCETRAPIB (CP-529414), Torcetrapib (CP-529414)
Patent coverage: 1,766 distinct patent families (7,803 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 7,753 (99%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.
Targets
Targets
Broader ChEMBL bioactivity targets: 1 (assay-derived). Sample: Cholesteryl ester transfer protein.
Bioactivity
ChEMBL activities: 10 potent at pChembl ≥ 5 of 10 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| CETP | 8.52 | IC50 | 3 | nM | CHEMBL_ACT_3191895 |
| CETP | 7.92 | IC50 | 12 | nM | CHEMBL_ACT_19090871 |
| CETP | 7.89 | IC50 | 13 | nM | CHEMBL_ACT_8037210 |
| CETP | 7.75 | IC50 | 18 | nM | CHEMBL_ACT_18143900 |
| CETP | 7.75 | IC50 | 18 | nM | CHEMBL_ACT_3191862 |
| CETP | 7.7 | IC50 | 20 | nM | CHEMBL_ACT_3191894 |
| CETP | 7.41 | IC50 | 39 | nM | CHEMBL_ACT_10855496 |
| CETP | 7.41 | IC50 | 39 | nM | CHEMBL_ACT_10890888 |
| CETP | 7 | IC50 | 100 | nM | CHEMBL_ACT_19090872 |
| CETP | 6.96 | IC50 | 110 | nM | CHEMBL_ACT_12095378 |
Target pathways
No target-pathway data for this drug (no mapped target genes).
Indications & clinical
Indications
9 indications (0 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).
| Indication | Trial phase | MONDO | EFO |
|---|---|---|---|
| familial hypercholesterolemia | 3 | MONDO:0005439 | EFO:0004911 |
| coronary artery disorder | 3 | MONDO:0005010 | EFO:0001645 |
| hypertriglyceridemia | 3 | MONDO:0005347 | EFO:0004211 |
| hyperlipidemia | 3 | MONDO:0021187 | MONDO:0021187 |
5 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 14.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE3 | 14 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT00134173 | PHASE3 | COMPLETED | A Coronary IVUS Study to Compare Torcetrapib/Atorvastatin to Atorvastatin Alone in Subjects With Coronary Heart Disease |
| NCT00134238 | PHASE3 | TERMINATED | Carotid B-mode Ultrasound Study to Compare Anti-Atherosclerotic Effect of Torcetrapib/Atorvastatin to Atorvastatin. |
| NCT00134264 | PHASE3 | TERMINATED | A Study Examining Torcetrapib/Atorvastatin And Atorvastatin Effects On Clinical CV Events In Patients With Heart Disease |
| NCT00134485 | PHASE3 | COMPLETED | Study To Evaluate The Safety And Efficacy Of Torcetrapib/Atorvastatin In Subjects With Familial Hypercholerolemia |
| NCT00134498 | PHASE3 | COMPLETED | A Study Comparing The Efficacy & Safety Of Torcetrapib/Atorvastatin And Atorvastatin In Subjects With High Triglycerides |
| NCT00134511 | PHASE3 | COMPLETED | Study To Evaluate The Effect Of Torcetrapib/Atorvastatin In Patients With Genetic High Cholesterol Disorder |
| NCT00136981 | PHASE3 | COMPLETED | Carotid B-Mode Ultrasound Study to Compare Anti-Atherosclerotic Effect of Torcetrpib/Atorvastatin to Atorvastatin Alone. |
| NCT00137462 | PHASE3 | COMPLETED | Lipitor Trial To Study The Effect Of Torcetrpib/Atorvastatin To Atorvastatin Alone. |
| NCT00138762 | PHASE3 | COMPLETED | A Study of Torcetrapib/Atorvastatin vs Atorvastatin Alone or Placebo in Patients With High Cholesterol |
| NCT00139061 | PHASE3 | COMPLETED | Assess HDL-C Increase And Non-HDL Lowering Effect Of Torcetrapib/Atorvastatin Vs. Fenofibrate |
| NCT00145431 | PHASE3 | TERMINATED | Study To Evaluate The Effect Of Torcetrapib/Atorvastatin In Subjects With A Genetic Cholesterol Disorder. |
| NCT00267254 | PHASE3 | COMPLETED | A Clinical Trial Comparing Torcetrapib/Atorvastatin To Simvastatin In Subjects With High Cholesterol. |
| NCT00267267 | PHASE3 | TERMINATED | A Clinical Trial Comparing Torcetrapib/Atorvastatin to Ezetimibe/Simvastatin In Subjects With A Cholesterol Disorder. |
| NCT00267280 | PHASE3 | TERMINATED | A Clinical Trial Comparing Torcetrapib/Atorvastatin To Simvastatin In Subjects With High Cholesterol (A5091031). |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.
Related molecules
Related molecules
No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).