BMB-101
5-HT2C receptor agonist
From Wikipedia, the free encyclopedia
BMB-101 is a serotonin 5-HT2C 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 dependence.[1][2][3][4][5] It is taken orally.[1]
| Clinical data | |
|---|---|
| Other names | BMB101 |
| Routes of administration | Oral[1] |
| Drug class | Serotonin 5-HT2C receptor agonist |
Pharmacology
Pharmacodynamics
BMB-101 acts as a highly selective biased agonist of the serotonin 5-HT2C receptor.[1][6][3][5] It has greater that 100-fold selectivity for the serotonin 5-HT2C receptor over other serotonin receptors, including the serotonin 5-HT2A and 5-HT2B receptors.[3][5] BMB-101 shows functional selectivity at the serotonin 5-HT2C receptor for activation of Gq 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-HT2C 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]
The activation of serotonin 5-HT2C receptors has been shown to reduce epileptic seizure activity by inhibiting T-type calcium channels (Cav3).[7] These calcium channels facilitate high frequency burst firing in principal 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]
Chemistry
The chemical structure of BMB-101 does not yet appear to have been disclosed.[1][2] However, lumocaserin (INN; CAS no. 1656330-84-5), a serotonin 5-HT2C receptor agonist described as an anticonvulsant, has been patented by Bright Minds Biosciences-associated researchers including Alan Kozikowski and Jianjun Cheng.[11][12] Lumocaserin's INN was registered in January 2026.[13] Various structurally related serotonin 5-HT2C receptor agonists have also been studied and described by Kozikowski and colleagues.[14][15]
Research
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 drug has been found to increase REM sleep time by 90% (from 56 minutes to 107 minutes) without altering total sleep duration (9.1 hours vs. 8.9 hours) in people with absence seizures in a clinical study.[16]