Esprolol

Esprolol
Clinical data
Other names	(S)-ACC-9369; (S)-ACC9369
Routes of; administration	Sublingual
Drug class	Beta blocker; β1-Adrenergic receptor antagonist
ATC code	None;
Pharmacokinetic data
Metabolism	Esterases
Metabolites	Amoxolol
Onset of action	"Rapid"
Duration of action	"Short"
Identifiers
	IUPAC name ethyl 3-[2-[(2S)-2-hydroxy-3-(propan-2-ylamino)propoxy]phenyl]propanoate;
CAS Number	396654-09-4 ; 112805-65-9 (hydrochloride);
PubChem CID	9950099;
ChemSpider	8125710;
UNII	50PY5PGT61;
Chemical and physical data
Formula	C17H27NO4
Molar mass	309.406 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CCOC(=O)CCC1=CC=CC=C1OC[C@H](CNC(C)C)O;
	InChI InChI=1S/C17H27NO4/c1-4-21-17(20)10-9-14-7-5-6-8-16(14)22-12-15(19)11-18-13(2)3/h5-8,13,15,18-19H,4,9-12H2,1-3H3/t15-/m0/s1; Key:DMLSVZSUDBKLED-HNNXBMFYSA-N;

Esprolol, also known as (S)-ACC-9369, is a beta blocker which was under development for the treatment of angina pectoris, anxiety disorders, and migraine.^[1]^[3]^[2] It is taken sublingually and has a rapid onset of action, short time to peak, and short duration.^[1]^[2] The drug is a prodrug of amoxolol, which is formed from esprolol via esterase enzymes.^[2] It is a selective β₁-adrenergic receptor antagonist.^[2]^[4] Esprolol was under development by Selectus Pharmaceuticals.^[1]^[3] It reached phase 2 clinical trials for all indications prior to the discontinuation of its development in 2001.^[1]^[3]

References

1 2 3 4 5 6 "Esprolol". AdisInsight. 25 June 2001. Retrieved 5 June 2026.
1 2 3 4 5 6 7 8 9 Matier WL, Patil G (2000). "Esprolol hydrochloride: a new beta adrenergic antagonist with a rapid onset of effect". Heart Dis. 2 (2): 146–150. PMID 11728252.
1 2 3 "Delving into the Latest Updates on Esprolol Hydrochloride with Synapse". Synapse. 30 May 2026. Retrieved 5 June 2026.
↑ Frishman WH, Alwarshetty M (2002). "Beta-adrenergic blockers in systemic hypertension: pharmacokinetic considerations related to the current guidelines". Clin Pharmacokinet. 41 (7): 505–516. doi:10.2165/00003088-200241070-00004. PMID 12083978. A sublingual β1-selective blocker, esprolol, is now being evaluated in clinical trials.[30]

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