Drug intelligence / Profile preview

arotinolol

Development stage
Phase 4
Lead developer
Sumitomo Pharma
Modality
Small Molecules
Administration
Oral
01

Overview

Arotinolol is a small molecule, non-selective adrenergic receptor blocker that acts as both an alpha (α1) and beta (β1, β2) adrenergic antagonist, with additional partial agonist activity at the β3 receptor. Developed in Japan by Sumitomo Chemical (now Sumitomo Dainippon Pharma), it is primarily used for the treatment of hypertension and essential tremor. Its mechanism of action involves blocking β1-, β2-, and α1-adrenoceptors, leading to reduced cardiac output via β-blockade and inhibition of counter-regulatory increases in peripheral resistance via α-blockade. This results in decreased blood pressure, alleviation of angina attacks, suppression of arrhythmia, and relief from tremors through its effects on skeletal muscle. Arotinolol has also been studied for use in chronic heart failure due to its ability to lower heart rate and reduce sympathetic nervous system excitability[1][2][3][4][6].

Brand names
Almarl
Other names
arotinolol hydrochlorideArotinolol HCl
02

Targets

ADRB1 (β1)ADRB2 (β2)ADRB3 (β3)ADRA1A (α1A)

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