Celiprolol
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| Clinical data | |
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| AHFS/Drugs.com | International Drug Names |
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| Pharmacokinetic data | |
| Bioavailability | 30-70% |
| Elimination half-life | 5 hours |
| Identifiers | |
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| CAS Number | |
| PubChem CID | |
| DrugBank | |
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| KEGG | |
| ChEMBL | |
| ECHA InfoCard |
100.054.980  |
| Chemical and physical data | |
| Formula | C20H33N3O4 |
| Molar mass | 379.49 g/mol |
| 3D model (JSmol) | |
| Chirality | Racemic mixture |
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Celiprolol (brand names Cardem, Selectol, Celipres, Celipro, Celol, Cordiax, Dilanorm) is a medication in the class of beta blockers, used in the treatment of high blood pressure. It has a unique pharmacology: it is a selective β1 receptor antagonist, but a β2 receptor partial agonist. It is also a weak α2 receptor antagonist.
In 2010, a clinical trial has suggested a use for this medication in the prevention of vascular complications of a rare inherited disease called vascular Ehlers–Danlos syndrome. This study demonstrated decreased incidence of arterial rupture or dissection (a specific type of arterial rupture in which the layers of the vessel separate prior to complete failure of the artery wall).[1]
Celiprolol is believed to provide clinical benefit for people with vascular Ehlers–Danlos syndrome by promoting normal collagen synthesis in the blood vessels, and by shifting the pressure load away from the vessels most prone to dissection and rupture. [2] Acer Therapeutics is currently developing celiprolol as a potential treatment option specifically for people with vEDS. In 2015, the U.S. Food and Drug Administration (FDA) granted celiprolol orphan drug designation for the treatment of vascular Ehlers–Danlos syndrome.
References
- ↑ Ong K-T; et al. (2010). "Effect of celiprolol on prevention of cardiovascular events in vascular Ehlers-Danlos syndrome: a prospective randomised, open, blinded-endpoints trial". Lancet. 376 (9751): 1476–1484. doi:10.1016/S0140-6736(10)60960-9. PMID 20825986.
- ↑ Beridze N, Frishman WH (2012). "Vascular Ehlers-Danlos syndrome: pathophysiology, diagnosis, and prevention and treatment of its complications". Cardiol Rev. 1: 4–7. doi:10.1097/CRD.0b013e3182342316. PMID 22143279.
External links
- Selectol Summary of Product Characteristics (from the IPHA Medicines Compendium)
- Celiprolol data sheet for New Zealand