D3 Receptor-Targeted Cariprazine: Insights from Lab to Bedside
- PMID: 38891871
- PMCID: PMC11172134
- DOI: 10.3390/ijms25115682
D3 Receptor-Targeted Cariprazine: Insights from Lab to Bedside
Abstract
Until the late 1800s, drug development was a chance finding based on observations and repeated trials and errors. Today, drug development must go through many iterations and tests to ensure it is safe, potent, and effective. This process is a long and costly endeavor, with many pitfalls and hurdles. The aim of the present review article is to explore what is needed for a molecule to move from the researcher bench to the patients' bedside, presented from an industry perspective through the development program of cariprazine. Cariprazine is a relatively novel antipsychotic medication, approved for the treatment of schizophrenia, bipolar mania, bipolar depression, and major depression as an add-on. It is a D3-preferring D3-D2 partial agonist with the highest binding to the D3 receptors compared to all other antipsychotics. Based on the example of cariprazine, there are several key factors that are needed for a molecule to move from the researcher bench to the patients' bedside, such as targeting an unmet medical need, having a novel mechanism of action, and a smart implementation of development plans.
Keywords: D3 receptor; cariprazine; clinical development program; drug development; partial agonist.
Conflict of interest statement
Á.B., Z.B.D., and G.N. are employees of Gedeon Richter Plc. The research was conducted in the absence of any commercial or financial relationships that could be construed as a potential conflict of interest.
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References
-
- Poduri R. Drug Discovery and Development: From Targets and Molecules to Medicines. Springer; Singapore: 2021. Historical Perspective of Drug Discovery and Development.
-
- Ng R. Drugs: From Discovery to Approval. John Wiley & Sons, Inc.; Hoboken, NJ, USA: 2009. History of Drug Discovery and Development; pp. 391–397.
-
- Mann S.K., Marwaha R. Chlorpromazine. [(accessed on 16 May 2024)]; Available online: https://www.ncbi.nlm.nih.gov/books/NBK553079/
-
- Bloom F.E. Antianxiety Drug. [(accessed on 16 May 2024)]. Available online: https://www.britannica.com/science/antianxiety-drug.
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