perhexiline
Perhexiline (Pexsig) is a prophylactic antianginal agent used primarily in Australia and New Zealand. Perhexiline is thought to act by inhibiting mitochondrial carnitine palmitoyltransferase-1. This shifts myocardial metabolism from fatty acid to glucose utilisation which results in increased ATP production for the same O2 consumption and consequently increases myocardial efficiency. Its clinical use has been limited by its narrow therapeutic index and high inter- and intra-individual pharmacokinetic variability. It was outlawed in many countries due to its adverse effects on poor metabolisers (PM). The product has been reintroduced for patients who have contraindications, or have not responded to other treatments for angina. — Wikipedia
Clinical trial activity
9 trials · 8 clinical orgs · 0 marketing orgs
Earliest trial started Oct 1, 2006 (NCT00628056)
Timeline
Indications
Studied for
- Cardiac Output, Low · Phase 2/Phase 3
- Cardiomyopathy, Hypertrophic · Phase 3
- Cardiomyopathy, Hypertrophic, Familial · Phase 2
- Diabetic Cardiomyopathies · Phase 1/Phase 2
- Heart Failure · Phase 2
- Heart Failure, Diastolic · Phase 2
- Hypertrophy, Left Ventricular · Phase 2/Phase 3
- Myocardial Reperfusion Injury · Phase 2/Phase 3
Mechanism of action
- Carnitine palmitoyltransferase 2INHIBITOR
CPT2 inhibitor
Chemistry & pharmacology
SMILES
C1CCC(C(CC2CCCCN2)C2CCCCC2)CC1- Mol. weight
- 277.5 g/mol
- Lipinski Ro5
- 1 violation(s)
- Rule of 3
- No
- Chirality
- Racemic Mixture
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaPerhexiline ↗
- ChEMBLCHEMBL75880 ↗
Also known as
- (-)-2-(2,2-dicyclohexylethyl)piperidine
- (-)-2-(2,2-dicyclohexylethyl)piperidine
- (+)-2-(2,2-dicyclohexylethyl)piperidine
- (+)-2-(2,2-dicyclohexylethyl)piperidine
- 2-(2,2-dicyclohexylethyl)piperidine
- 2-(2,2-dicyclohexylethyl)piperidine
- perhexilene
- perhexilene
- perhexilina
- perhexilina
- perhexiline
- perhexiline
- perhexiline
- perhexiline
- perhexiline
- perhexiline
- perhexiline
- perhexiline
- perhexilinum
- perhexilinum
- perhexilline
- perhexilline
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT04426578 | Phase 2 | Aug 1, 2020 | Flinders University |
| NCT02862600 | Phase 2 | Aug 1, 2016 | Heart Metabolics |
| NCT02431221 | Phase 3 | Mar 1, 2016 | Heart Metabolics |
| NCT00989508 | Phase 2/Phase 3 (Phase 3) | Oct 1, 2009 | British Heart Foundation, University of Birmingham, University of Sussex |
| NCT00839228 | Phase 2 | Mar 1, 2009 | University of Aberdeen |
| NCT00841139 | Phase 2 | Feb 1, 2009 | British Heart Foundation, University of Birmingham |
| NCT00845364 | Phase 2/Phase 3 (Phase 3) | Feb 1, 2007 | British Heart Foundation, University of Birmingham, University of Sussex |
| NCT00500552 | Phase 2 | Dec 1, 2006 | British Heart Foundation, University of Birmingham, University of London, University of Oxford |
| NCT00628056 | Phase 1/Phase 2 (Phase 2) | Oct 1, 2006 | British Heart Foundation, University of Birmingham |
Organizations
Research & Development (8)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| British Heart Foundation | Academic/Hospital | 5 | 0 | 2 | 2006 |
| University of Birmingham | Academic/Hospital | 5 | 5 | 2 | 2006 |
| Heart Metabolics | For profit | 2 | 2 | 2 | 2016 |
| University of Sussex | Academic/Hospital | 2 | 0 | 1 | 2007 |
| Flinders University | Academic/Hospital | 1 | 1 | 1 | 2020 |
| University of Aberdeen | Academic/Hospital | 1 | 1 | 1 | 2009 |
| University of London | Academic/Hospital | 1 | 0 | 1 | 2006 |
| University of Oxford | Academic/Hospital | 1 | 0 | 1 | 2006 |