Navacaprant

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Overview of the investigational drug Navacaprant


{{Drugbox | verifiedfields = changed | verifiedrevid = 477002123 | IUPAC_name = (1S,2R)-2-[[4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl]methyl]-N,N-dimethylcyclopropane-1-carboxamide | image = BTRX-335140.svg | image2 = | width = 200 | alt = | caption = Chemical structure of Navacaprant }}

Navacaprant (also known by its developmental code name BTRX-335140) is an investigational drug that acts as a selective antagonist of the kappa opioid receptor (KOR). It is being studied for its potential therapeutic effects in the treatment of major depressive disorder (MDD) and other neuropsychiatric disorders.

Pharmacology[edit | edit source]

Navacaprant is a potent and selective antagonist of the kappa opioid receptor. The kappa opioid receptor is one of the four types of opioid receptors in the body, which also include the mu opioid receptor, delta opioid receptor, and the nociceptin receptor. KORs are involved in modulating mood, stress, and pain perception. By blocking these receptors, Navacaprant may help alleviate symptoms of depression and anxiety.

Mechanism of Action[edit | edit source]

The mechanism of action of Navacaprant involves the inhibition of the kappa opioid receptor. KOR activation is associated with dysphoria, stress, and depressive-like behaviors. By antagonizing these receptors, Navacaprant may reduce these negative emotional states and improve mood. This mechanism is distinct from traditional antidepressants, which typically target the serotonin or norepinephrine systems.

Clinical Development[edit | edit source]

Navacaprant is currently undergoing clinical trials to evaluate its efficacy and safety in treating major depressive disorder. Early studies have shown promise, indicating that Navacaprant may be effective in reducing depressive symptoms in patients who have not responded to other treatments. The drug is also being explored for its potential use in treating other conditions such as anxiety disorders and substance use disorders.

Potential Benefits[edit | edit source]

The development of Navacaprant represents a novel approach to treating depression and other mood disorders. Unlike traditional antidepressants, which can take weeks to show effects, KOR antagonists like Navacaprant may offer more rapid relief of symptoms. Additionally, they may have a different side effect profile, potentially offering an alternative for patients who do not tolerate existing medications well.

Challenges and Considerations[edit | edit source]

While Navacaprant shows promise, there are challenges in its development. The precise role of kappa opioid receptors in mood regulation is complex, and further research is needed to fully understand the long-term effects of KOR antagonism. Additionally, as with any new drug, there are considerations regarding its safety, potential side effects, and interactions with other medications.

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Contributors: Prab R. Tumpati, MD