CVL-354
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Icalcaprant (developmental code name CVL-354) is an
opioid antagonist An opioid antagonist, or opioid receptor antagonist, is a receptor antagonist that acts on one or more of the opioid receptors. Naloxone and naltrexone are commonly used opioid antagonist drugs which are competitive antagonists that bind to ...
which is under development for the treatment of
major depressive disorder Major depressive disorder (MDD), also known as clinical depression, is a mental disorder characterized by at least two weeks of pervasive depression (mood), low mood, low self-esteem, and anhedonia, loss of interest or pleasure in normally ...
and
substance-related disorder Substance-related disorders is a class of mental disorders that affect a person's brain and behavior, leading to their inability to control their use of substances like drugs, alcohol, or medications. The disorders can lead to large societal probl ...
s. It is taken
by mouth Oral administration is a route of administration whereby a substance is taken through the Human mouth, mouth, swallowed, and then processed via the digestive system. This is a common route of administration for many medications. Oral administ ...
. It acts as a selective
antagonist An antagonist is a character in a story who is presented as the main enemy or rival of the protagonist and is often depicted as a villain.κ-opioid receptor The κ-opioid receptor or kappa opioid receptor, abbreviated KOR or KOP for its ligand ketazocine, is a G protein-coupled receptor that in humans is encoded by the ''OPRK1'' gene. The KOR is coupled to the G protein Gi/G0 and is one of four re ...
. The drug is also more weakly an antagonist of the
μ-opioid receptor The μ-opioid receptors (MOR) are a class of opioid receptors with a high affinity for enkephalins and beta-endorphin, but a low affinity for dynorphins. They are also referred to as μ(''mu'')-opioid peptide (MOP) receptors. The prototypical ...
, with about 31-fold lower
affinity Affinity may refer to: Commerce, finance and law * Affinity (law), kinship by marriage * Affinity analysis, a market research and business management technique * Affinity Credit Union, a Saskatchewan-based credit union * Affinity Equity Pa ...
and 27-fold lower inhibitory
potency Potency may refer to: * Potency (pharmacology), a measure of the activity of a drug in a biological system * Virility * Cell potency, a measure of the differentiation potential of stem cells * In homeopathic dilutions, potency is a measure of ho ...
at the μ-opioid receptor relative to the κ-opioid receptor. It was originated by
Pfizer Pfizer Inc. ( ) is an American Multinational corporation, multinational Pharmaceutical industry, pharmaceutical and biotechnology corporation headquartered at The Spiral (New York City), The Spiral in Manhattan, New York City. Founded in 184 ...
and is under development by
Cerevel Therapeutics Cerevel Therapeutics Holdings, Inc. was an American biotechnology and pharmaceuticals company based in Cambridge, Massachusetts, focused on the development of novel therapies for mental and neurological illnesses. History Cerevel was establish ...
(a subsidiary of
AbbVie AbbVie Inc. is an American pharmaceutical company headquartered in North Chicago, Illinois. It is ranked sixth on the list of largest biomedical companies by revenue. In 2023, the company's seat in Forbes Global 2000 was 74, and rank 89 on the ...
). As of September 2022, icalcaprant is in phase 1
clinical trial Clinical trials are prospective biomedical or behavioral research studies on human subject research, human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel v ...
s for major depressive disorder and is in the preclincal stage of development for substance-related disorders.


See also

* κ-Opioid receptor § Antagonists * List of investigational antidepressants § κ-Opioid receptor antagonists


References

Experimental antidepressants Experimental drugs Kappa-opioid receptor antagonists Mu-opioid receptor antagonists Synthetic opioids {{Nervous-system-drug-stub