Landiolol

DB12212ApprovedInvestigationalSmall moleculeAdrenergic beta-Antagonists

Landiolol is a rapid-acting selective beta-blocker used to reduce ventricular rate in supraventricular tachycardia in adults. Landiolol is a rapid-acting beta (β)-1 adrenergic receptor blocker that blocks the positive chronotropic effect of the beta-1 selective agonist norepinephrine.

Mechanism: Beta (β)-1 adrenoceptors are predominantly found in the myocardium, to which endogenous catecholamines, epinephrine and norepinephrine, bind. These receptors activate intracellular molecules and signalling pathways, such as the stimulatory G protein (Gs) and cyclic AMP.
Landiolol is a selective beta-1 adrenoreceptor antagonist that inhibits the positive chronotropic effects of the catecholamines. Landiolol reduces the sympathetic drive, resulting in the reduction of heart rate, decreasing the spontaneous firing of ectopic pacemakers, while slowing the conduction and increasing the refractory period of the atrioventricular node.
Curator reviewed · 6 references
Primary indication: Landiolol is indicated for the short-term reduction of ventricular rate in adults with supraventricular tachycardia including atrial fibrillation and atrial flutter.Curator reviewed · 3 structured indications
Formula / weight: C₂₅H₃₉N₃O₈ · 509.6 g/mol (avg)
First approval: Canada, 2023 · United States, 2025
Also known as: (-)-2,2-dimethyl-1,3-dioxolan-4S-ylmethyl 3-[4-[3-[2-(morpholinocarbonylamino)ethylamino]-2S-hydroxypropoxy]phenyl]propionate · [(4S)-2,2-dimethyl-1,3-dioxolan-4-yl]methyl 3-(4-{(2S)-2-hydroxy-3-[{2-[(morpholin-4-ylcarbonyl)amino]ethyl}amino]propoxy}phenyl)propanoate · Benzenepropanoic acid, 4-[(2S)-2-hydroxy-3-[[2-[(4-morpholinylcarbonyl)amino]ethyl]amino]propoxy]-, [(4S)-2,2-dimethyl-1,3-dioxolan-4-yl]methyl ester
Code names: AOP-200704 · LDLL-600 · ONO-1101
Brand names: Rapiblyk