evacetrapib
Evacetrapib was a drug under development by Eli Lilly and Company that inhibits cholesterylester transfer protein. CETP collects triglycerides from very low-density lipoproteins (VLDL) or low-density lipoproteins (LDL) and exchanges them for cholesteryl esters from high-density lipoproteins (HDL), and vice versa, but primarily increasing high-density lipoprotein and lowering low-density lipoprotein. It is thought that modifying lipoprotein levels modifies the risk of cardiovascular disease. The first CETP inhibitor, torcetrapib, was unsuccessful because it increased levels of the hormone aldosterone and increased blood pressure, which led to excess cardiac events when it was studied. Evacetrapib does not have the same effect. When studied in a small clinical trial in people with elevated LDL and low HDL, significant improvements were noted in their lipid profile. — Wikipedia
Clinical trial activity
26 trials · 2 clinical orgs · 0 marketing orgs
Earliest trial started Apr 1, 2010 (NCT01105975)
Timeline
Indications
Mechanism of action
- Cholesteryl ester transfer proteinINHIBITOR
CETP inhibitor
Benzazepine-based CETP inhibitor
Chemistry & pharmacology
SMILES
Cc1cc(C)c2c(c1)[C@@H](N(Cc1cc(C(F)(F)F)cc(C(F)(F)F)c1)c1nnn(C)n1)CCCN2C[C@H]1CC[C@H](C(=O)O)CC1- Mol. weight
- 638.66 g/mol
- Lipinski Ro5
- 2 violation(s)
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaEvacetrapib ↗
- ChEMBLCHEMBL2017179 ↗
Also known as
- evacetrapib
- evacetrapib
- evacetrapib
- evacetrapib
- evacetrapib
- ly2484595
- ly2484595
- ly2484595
- ly 2484595
- ly-2484595
- ly-2484595
- ly-2484595
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT02497391 | Phase 1 | Jul 1, 2015 | Eli Lilly |
| NCT02260648 | Phase 3 | Jan 1, 2015 | Eli Lilly |
| NCT02365558 | Phase 1 | Jan 1, 2015 | Eli Lilly |
| NCT02260635 | Phase 3 | Nov 1, 2014 | Eli Lilly |
| NCT02271425 | Phase 1 | Oct 1, 2014 | Eli Lilly |
| NCT02227784 | Phase 3 | Oct 1, 2014 | Eli Lilly |
| NCT02226653 | Phase 1 | Sep 1, 2014 | Eli Lilly |
| NCT02156492 | Phase 1 | Jun 1, 2014 | Eli Lilly |
| NCT02161731 | Phase 1 | Jun 1, 2014 | Eli Lilly |
| NCT02168803 | Phase 1 | May 1, 2014 | Eli Lilly |
| NCT01958489 | Phase 1 | Oct 1, 2013 | Eli Lilly |
| NCT01903434 | Phase 1 | Jul 1, 2013 | Eli Lilly |
| NCT01897493 | Phase 1 | Jul 1, 2013 | Eli Lilly |
| NCT01908582 | Phase 1 | Jul 1, 2013 | Eli Lilly |
| NCT01836185 | Phase 1 | Apr 1, 2013 | Eli Lilly |
| NCT01825889 | Phase 1 | Apr 1, 2013 | Eli Lilly |
| NCT01825876 | Phase 1 | Apr 1, 2013 | Eli Lilly |
| NCT01810432 | Phase 1 | Mar 1, 2013 | Eli Lilly |
| NCT01736254 | Phase 1 | Dec 1, 2012 | Eli Lilly |
| NCT01746732 | Phase 1 | Dec 1, 2012 | Eli Lilly |
Organizations
Research & Development (2)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Eli Lilly | For profit | 26 | 26 | 3 | 2010 |
| University of Rochester | Academic/Hospital | 1 | 0 | 1 | 2012 |