Drug intelligence / Profile preview

levodopa + carbidopa + entacapone

Development stage
Approved
Lead developer
Orion
Modality
Small Molecules
Administration
Oral
01

Overview

levodopa + carbidopa + entacapone is a fixed-dose combination therapy developed by Novartis and Orion Corporation for the treatment of Parkinson's disease. It is specifically indicated for patients who experience end-of-dose motor fluctuations, known as wearing-off. The combination works through three distinct mechanisms: levodopa serves as a metabolic precursor to dopamine, crossing the blood-brain barrier to replenish depleted dopamine levels; carbidopa is a peripheral DOPA decarboxylase inhibitor that prevents the premature conversion of levodopa to dopamine outside the central nervous system, thereby reducing side effects and increasing levodopa bioavailability; and entacapone is a selective, reversible inhibitor of catechol-O-methyltransferase (COMT), which further prevents the breakdown of levodopa, extending its therapeutic half-life and providing more stable plasma levels.

Brand names
Stalevo
Other names
levodopa/carbidopa/entacapone
02

Targets

DDC (Aromatic L-amino acid decarboxylase)COMT (Catechol-O-methyltransferase)SLC7A5 (Large neutral amino acid transporter small subunit 1)DRD (Dopamine receptors)

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