SYN-117

Dopamine β-hydroxylase (DβH)

SYN-117 is a potent, competitive, and selective inhibitor of the enzyme dopamine β-hydroxylase and is under investigation for the treatment of drug dependency and post-traumatic stress disorder (PTSD).

Dopamine β-hydroxylase is the main enzyme responsible for the conversion of dopamine into norepinephrine. The inhibition of this enzyme has been shown to raise dopamine levels in the central nervous system (CNS).

SYN-117 is available as an oral treatment and has been well-tolerated in preclinical models at doses significantly above the expected therapeutic range for the current central nervous system (CNS) indications under investigation.

The rationale for treatment of cocaine dependency is based firstly on animal pharmacology in normal mice and in mice lacking the enzyme dopamine β-hydroxylase and secondly on human clinical studies using disulfiram, a weak dopamine β-hydroxylase inhibitor.

Synosia has completed a laboratory study in humans, evaluating firstly the safety of SYN-117 when co-administered with cocaine and secondly the effect of SYN-117 on subjective responses to cocaine. Based upon the positive data obtained from this study, Synosia plans to continue development.

A Phase II study of SYN-117 in post traumatic stress disorder (PTSD) funded by the Department of Defense is ongoing. Pending grant funding, Synosia will initiate a Phase IIb study of SYN-117 in cocaine dependency.

Source: Roche
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