Celiprolol

In this article, we will explore the topic of Celiprolol in depth, addressing its different aspects, its importance in today's society and its relevance in the contemporary world. Along these lines, we will analyze the impact that Celiprolol has had in various areas, from culture and politics to technology and the economy. We will immerse ourselves in its history, its implications and its evolution over time, with the aim of better understanding its meaning and its influence on our daily lives. Furthermore, we will examine the future prospects of Celiprolol and its possible development in the coming years, as well as the controversies and debates it currently generates.

Celiprolol
Clinical data
AHFS/Drugs.comInternational Drug Names
ATC code
Pharmacokinetic data
Bioavailability30-70%
Elimination half-life5 hours
Identifiers
  • (RS)-N'-{3-Acetyl-4-phenyl}-N,N-diethylurea
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.054.980 Edit this at Wikidata
Chemical and physical data
FormulaC20H33N3O4
Molar mass379.501 g·mol−1
3D model (JSmol)
ChiralityRacemic mixture
  • O=C(N(CC)CC)Nc1ccc(OCC(O)CNC(C)(C)C)c(c1)C(=O)C

Celiprolol 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.

It was patented in 1973 and approved for medical use in 1982.[1]

Medical use

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] In 2019, a new drug application (NDA) for celiprolol was denied by the U.S. Food and Drug Administration (FDA), instead calling for an “adequate and well-controlled” trial to determine whether celiprolol reduced the risk of clinical events in patients with vEDS.[3] In June 2022, Acer Therapeutics Inc. sponsored "Clinical Trial to Compare the Efficacy of Celiprolol to Placebo in Patients With Vascular Ehlers-Danlos Syndrome (DiSCOVER)".[4]

Brand names

Brand names include Cardem, Selectol, Celipres, Celipro, Celol, Cordiax, Dilanorm

References

  1. ^ Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 461. ISBN 9783527607495.
  2. ^ Beridze N, Frishman WH (2012). "Vascular Ehlers-Danlos syndrome: pathophysiology, diagnosis, and prevention and treatment of its complications". Cardiology in Review. 20 (1): 4–7. doi:10.1097/CRD.0b013e3182342316. PMID 22143279. S2CID 9339508.
  3. ^ Campbell P (25 June 2019). "FDA Denies NDA for Celiprolol". MD Magazine.
  4. ^ "Clinical Trial to Compare the Efficacy of Celiprolol to Placebo in Patients With Vascular Ehlers-Danlos Syndrome (DiSCOVER)". NLM.gov Clinical Trials. 2022-06-21.


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