Nepicastat

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Nepicastat is a potent and selective inhibitor of dopamine beta-hydroxylase, an enzyme that catalyzes the conversion of dopamine to norepinephrine. It was developed by Roche and is currently in clinical trials for the treatment of cocaine dependence and heart failure.

Pharmacology[edit | edit source]

Nepicastat works by inhibiting the enzyme dopamine beta-hydroxylase, which is responsible for the conversion of dopamine to norepinephrine. This results in a decrease in the levels of norepinephrine, a neurotransmitter that plays a key role in the reward pathway of the brain. By reducing the levels of norepinephrine, nepicastat may help to reduce the cravings and withdrawal symptoms associated with cocaine dependence.

Clinical Trials[edit | edit source]

Nepicastat has been tested in several clinical trials for its potential use in the treatment of cocaine dependence and heart failure. In a phase II trial, nepicastat was found to be safe and well-tolerated in patients with cocaine dependence. However, the results of the trial did not show a significant difference in cocaine use between the nepicastat and placebo groups.

In a separate trial, nepicastat was tested in patients with heart failure. The results of this trial showed that nepicastat was able to improve cardiac function and reduce the symptoms of heart failure.

Potential Uses[edit | edit source]

While the results of the clinical trials have been mixed, nepicastat still holds promise for the treatment of cocaine dependence and heart failure. Further research is needed to fully understand the potential benefits and risks of this drug.

See Also[edit | edit source]

Nepicastat Resources
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Contributors: Prab R. Tumpati, MD