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bucindolol
- Development stage
- Phase 3
- Lead developer
- Oruka Therapeutics
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Bucindolol is a third-generation, non-selective beta-adrenergic receptor blocker with additional mild vasodilator properties due to alpha-1 adrenergic receptor antagonism. It acts on both beta-1 and beta-2 adrenergic receptors and exhibits sympatholytic activity, reducing plasma norepinephrine levels. Bucindolol has been investigated primarily for the treatment of heart failure with reduced ejection fraction (HFREF) and for the prevention of atrial fibrillation/atrial flutter in genetically defined heart failure populations. Its mechanism includes high-affinity competitive antagonism at beta-receptors, partial agonist activity at human β1-adrenergic receptors under certain conditions, and weak alpha-1 adrenoceptor inhibition contributing to vasodilation. Bucindolol is not FDA approved but remains investigational[1][3][5][6][7].
- Brand names
- Gencaro
- Other names
- bucindolol hydrochloride
02
Targets
HTR2A (Serotonin receptor 5-HT2A)ADRA1A (α1A)ADRB2 (β2)ADRB1 (β1)HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))
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