CERC-406

An orally active COMT inhibitor selective for MB-COMT, the predominant isoform expressed in the brain.

CERC-406

Targeting Improvement in motoric associated with Parkinson's Disease

CERC-406 is a small molecule, selective catechol-O-methyltransferase, or COMT, inhibitor that we are developing as an oral, brain penetrant adjunctive medication to levodopa / carbidopa in patients experiencing the "off-periods" of symptom management.

Attributes
of CERC-406

  • Orally active small molecule that crosses the blood brain barrier
  • Selective for MB-COMT, thus targeting PFC dopamine deficits
  • Potentially more effective in patients with the Val homozygote genetic polymorphism
  • Two identified bio-markers of efficacy

About Parkinson’s Disease

A Progressive neurodegenerative disease caused by a decrease in dopamine producing neuronal cells

Parkinson's disease is a type of movement disorder that can affect the ability to perform common, daily activities. According to the NIH and the Parkinson’s Disease Association there are an estimated 500,000 to 1 million Americans living with Parkinson's disease in the United States and more than 10 million people worldwide.

Parkinson's disease is caused by a gradual and progressive death of dopaminergic neurons in the substantia nigra pars compacta in the brain stem, which send dopamine releasing axons to the caudate nucleus and putamen. This loss of dopamine leads to the symptoms of Parkinson's disease including tremors, slow and uncertain movements, loss of motor control, and shuffling

Mechanism of Action

Selective, brain penetrant COMT inhibitor

CERC-406 is a CNS selective catechol-O-methyltransferase, or COMT, inhibitor that may selectively increase dopamine levels in the PFC, thereby reducing off-times frequently observed in Parkinson's Disease. We believe CERC-406 may avoid off‐target toxicity and side effects seen with the previous generation of COMT inhibitors, such as liver toxicity observed in tolcapone and diarrhea observed with entacapone and tolcapone.