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Bufuralol

Development stage: Discontinued
Lead developer: Onbio
Modality: Small Molecules
Administration: Oral

Overview

Bufuralol is a non-selective beta-adrenoceptor antagonist (beta-blocker) with partial agonist (intrinsic sympathomimetic) activity. It binds to both β1 and β2 adrenergic receptors, blocking the effects of endogenous catecholamines such as adrenaline and noradrenaline, which results in decreased heart rate and blood pressure. Bufuralol has been investigated primarily for the treatment of hypertension and cardiac arrhythmias. The drug is metabolized mainly by cytochrome P450 isoform CYP2D6, making it a common probe substrate for studying CYP2D6 activity in pharmacogenetic research[1][4][5][6][7]. Clinical development reached up to phase II/III trials but was discontinued before approval[1][6].

Other names: bufuralolumbufuralolum [INN-Latin]

Targets

ADRA1A (α1A)ADRB1 (β1)ADRB2 (β2)

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