BMB-101

BMB-101 is a serotonin 5-HT_2C receptor agonist which is under development for the treatment of absence epilepsy, Pitt-Hopkins syndrome, Dravet syndrome, binge-eating disorder, Lennox-Gastaut syndrome, and opioid-related disorders.^{[1][2][3][4][5]} It is taken by mouth.^[1]

BMB-101

Clinical data
Other names	BMB101
Routes of administration	Oral[1]
Drug class	Serotonin 5-HT2C receptor agonist[1]

The drug acts as a highly selective biased agonist of the serotonin 5-HT_2C receptor.^[1][6][3][5] It has greater that 100-fold selectivity for the serotonin 5-HT_2C receptor over other serotonin receptors, including the serotonin 5-HT_2A and 5-HT_2B receptors.^[3][5] BMB-101 shows functional selectivity at the serotonin 5-HT_2C receptor for activation of G_q signaling with minimal β-arrestin recruitment.^[6][3][5] This in turn appears to minimize receptor desensitization and development of tolerance.^[6][3] Due to its much greater selectivity for the serotonin 5-HT_2C receptor, BMB-101 is not expected to possess the psychedelic effects or cardiotoxicity that have been associated with existing drugs like fenfluramine and lorcaserin at therapeutic or supratherapeutic doses.^[3][4][5] In accordance with its mechanism of action, BMB-101 produces anticonvulsant effects in animals.^[4]

BMB-101 is under development by Bright Minds Biosciences.^[1][2] As of October 2023, it is in phase 2 clinical trials for absence epilepsy and Pitt-Hopkins syndrome, phase 1 clinical trials for Dravet syndrome, and is in preclinical research for binge-eating disorder, Lennox-Gastaut syndrome, and opioid-related disorders.^[1][2] The chemical structure of BMB-101 does not yet appear to have been disclosed.^[1][2]

The activation of 5HT2c receptors has been shown to reduce epileptic seizure activity by inhibiting CaV3 calcium channels which mediate the T-type calcium current.^[7] CaV3 calcium channels facilitate high frequency burst firing in princible neurons of the subiculum. This firing pattern is upregulated following status epilepticus, with these hyperactive neurons often serving as the initiation point for seizures.^[8][9][10]

See also

• Bexicaserin
• Vabicaserin