Entacapone is a potent, orally active, selective inhibitor of peripher
al catechol-O-methyltransferase (COMT), which has therapeutic potentia
l as an adjunct to levodopa therapy in patients with Parkinson's disea
se. Entacapone decreases peripheral conversion of levodopa to 3-O-metb
yldopa and improves central uptake of levodopa. Addition of entacapone
to levodopa/carbidopa or levodopa/benserazide increased the duration
of clinical response in patients with Parkinson's disease: the duratio
n of 'on' time was increased and the duration of 'off' time was decrea
sed. Levodopa requirements were reduced in patients with Parkinson's d
isease who received adjunctive entacapone therapy. Entacapone was gene
rally well tolerated, with few reported adverse events.