Drug intelligence / Profile preview

droxidopa

Development stage
Approved
Lead developer
Lundbeck
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Droxidopa is an orally active synthetic amino acid precursor of norepinephrine, classified as a vasopressor and alpha/beta adrenergic agonist. It is primarily used to treat symptomatic neurogenic orthostatic hypotension (nOH) in adults with conditions such as Parkinson’s disease, multiple system atrophy, pure autonomic failure, dopamine beta-hydroxylase deficiency, or non-diabetic autonomic neuropathy. Droxidopa works by being converted via decarboxylation to norepinephrine both peripherally and centrally (after crossing the blood-brain barrier), thereby increasing norepinephrine levels. This leads to vasoconstriction through activation of alpha-adrenergic receptors and increased cardiac output via beta-adrenergic receptor stimulation[1][3][4]. The drug was developed by Sumitomo Pharma and is marketed under the brand name Northera.

Brand names
Northera
Other names
L-threo-dihydroxyphenylserineL-DOPS
02

Targets

ADRB2 (β2)DDC (Aromatic L-amino acid decarboxylase)ADRA1A (α1A)ADRA1B (α1B)ADRA1D (α1D)ADRA2A (α2A)ADRA2B (α2B)ADRA2C (α2C)ADRB1 (β1)ADRB3 (β3)

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