Drug intelligence / Profile preview

labetalol + hydralazine + enalapril

Development stage
Unknown
Lead developer
GSK
Modality
Small Molecules
Administration
Oral, Intravenous, Intramuscular
01

Overview

This is a combination therapy consisting of three antihypertensive agents—labetalol, hydralazine, and enalapril—used together for the management of severe or resistant hypertension. - **Labetalol** is a non-selective beta-adrenergic blocker with selective alpha-1 adrenergic blocking activity, leading to decreased blood pressure through vasodilation and reduced heart rate[4][6]. - **Hydralazine** is a direct vasodilator that acts primarily on arterioles to decrease peripheral resistance and lower blood pressure[5][6]. - **Enalapril** is an angiotensin-converting enzyme (ACE) inhibitor that reduces the formation of angiotensin II, resulting in vasodilation and decreased aldosterone secretion[1][2]. The combination targets multiple mechanisms involved in hypertension control. Clinical experience suggests this regimen can be effective for patients with severe essential or renovascular hypertension who require multi-drug therapy for adequate blood pressure control[1][6]. This approach may be used when monotherapy or dual therapy does not achieve target blood pressures.

02

Targets

PHD1 (Prolyl hydroxylase domain-containing protein 1)ADRA1 (Alpha-1 adrenergic receptor family)P4H (Prolyl 4-hydroxylase subunit alpha-3)ACE (Angiotensin Converting Enzyme)ADRB1 (β1)IP3R (Inositol Trisphosphate Receptor)

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