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Celiprolol

Brand and Other Names: Celiprolol
Mechanism of Action:
Indications:
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Description:

Not approved (NDA rejected) 

GOOGLE OVERVIEW

Celiprolol is a medication classified as a beta-blocker, primarily used to treat high blood pressure and other cardiovascular conditions. It's unique among beta-blockers due to its selectivity for the beta-1 adrenergic receptor, its mild vasodilating properties, and its lack of bronchoconstrictive effects.While widely used in some countries, it's not yet approved in the United States for any indication. 
 
Key Properties and Uses:
  • Celiprolol works by blocking the effects of adrenaline and noradrenaline on the heart, leading to a decrease in heart rate and blood pressure. 
     
  • It primarily targets beta-1 receptors, which are mainly found in the heart. This selectivity can reduce the risk of side effects like bronchoconstriction (narrowing of airways). 
     
Unlike some other beta-blockers, celiprolol also has mild vasodilating properties, meaning it can help relax and widen blood vessels. 
 
Celiprolol is being investigated for its potential role in treating vascular Ehlers-Danlos syndrome (vEDS), a rare genetic disorder that weakens blood vessels. The BBEST trial (Beta-Blockers in Ehlers-Danlos Syndrome Treatment) showed promising results in reducing vascular events in vEDS patients. 
 
FDA Status:
The FDA has not yet approved celiprolol for vEDS in the US, though it has been granted orphan drug status. Acer Therapeutics is sponsoring a clinical trial (DiSCOVER) to evaluate its efficacy in vEDS patients. 
 
Important Considerations:
Side Effects:
Like other beta-blockers, celiprolol can cause side effects such as dizziness, fatigue, and bradycardia (slow heart rate). 
 
Contraindications:
Celiprolol is not suitable for everyone, and it's contraindicated in individuals with certain heart conditions. 
 
Limited Availability:
While used in many countries, celiprolol is not yet approved for use in the US. 
 
Ongoing Research:
Research continues to explore the full potential of celiprolol in various cardiovascular conditions, including vEDS. 
 
 

 

See package insert for full prescribing information.