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KB-128 is a novel small molecule developed by Küleon Bioscience, characterized as a "trifunctional" serotonergic agent. It acts as a full agonist at the 5-HT2C receptor and a full antagonist at both the 5-HT2A and 5-HT2B receptors. This unique pharmacological profile is considered groundbreaking for potential treatment of multiple neuropsychiatric disorders, including schizophrenia, Alzheimer's psychosis, depression, obesity, and addiction. The drug exhibits strong G protein signaling bias with minimal β-arrestin recruitment at the 5-HT2C receptor—a property associated with long-term therapeutic efficacy and reduced risk of tolerance development[1].
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