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Lead Program: NTY-184
A better bupropion

Bupropion is the active ingredient in 7 approved drugs for CNS disorders and has a 35-year history of clinical use over several indications including Depression, Seasonal Affective Disorder, Smoking Cessation, and Obesity.

However, bupropion is a racemic mixture of the R- and S-stereoisomers (enantiomers) that interconvert in solution at room temperature, and importantly, inside the body after dosing.

Bupropion is the only US-approved Dopamine Norepinephrine Re-uptake Inhibitor (NDRI) and is the active ingredient in products generating more than $3 billion in US sales in 2019.

How NTY-184 delivers the best of bupropion using DECS

Bupropion flips back and forth between the chiral R- and S-enantiomers. Each enantiomer interacts differently with human biology, which is chiral by nature.

Protonated Bupropion Conversion.png

Deuteration of the chiral carbon “locks” the R- and S-enantiomers into place, allowing the deuterium-stabilized enantiomers to be isolated, characterized, and a drug (NTY-184) with a superior pharmacologic profile to be developed.

Deuterated Bupropion.png

Target Product Profile

NTY-184’s improved potency and side-effect profile is supported by our preclinical program to date.

 

We anticipate NTY-184 to be a more potent and targeted drug. With dose optimization, we expect superior efficacy and an improved side-effect profile relative to current antidepressants, including racemic bupropion.

Improved Efficacy
  • More potent inhibition of DAT (dopamine active transporter) 

  • More potent inhibition of NET (norepinephrine transporter) 

  • Higher DAT:NET activity ratio favoring dopaminergic activity

Dopaminergic Benefits
  • Lack of weight gain

  • No sexual dysfunction

  • Relief from anhedonia

Better Safety and Side Effect Profile

  • Reduced seizure risk

  • Improved tolerability

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