Celiprolol

Celiprolol
Clinical data
AHFS/Drugs.com	International Drug Names
ATC code	C07AB08 (WHO) ;
Pharmacokinetic data
Bioavailability	30-70%
Elimination half-life	5 hours
Identifiers
	IUPAC name (RS)-N'-{3-Acetyl-4-[3-(tert-butylamino)-2-hydroxypropoxy]phenyl}-N,N-diethylurea;
CAS Number	56980-93-9;
PubChem CID	2663;
DrugBank	DB04846 ;
ChemSpider	2563;
UNII	DRB57K47QC;
KEGG	D07660;
ChEMBL	ChEMBL27810;
CompTox Dashboard (EPA)	DTXSID3020259 ;
ECHA InfoCard	100.054.980
Chemical and physical data
Formula	C20H33N3O4
Molar mass	379.501 g·mol−1
3D model (JSmol)	Interactive image;
Chirality	Racemic mixture
	SMILES 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

^ Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 461. ISBN 9783527607495.
^ 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.
^ Campbell P (25 June 2019). "FDA Denies NDA for Celiprolol". MD Magazine.
^ "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.

External links

Selectol Summary of Product Characteristics (from the IPHA Medicines Compendium)
Celiprolol data sheet for New Zealand

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[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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