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xanomeline
- Development stage
- Phase 4
- Lead developer
- Bristol Myers Squibb
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Xanomeline is a small molecule muscarinic acetylcholine receptor agonist, functionally preferring the M1 and M4 subtypes in the central nervous system. It was developed as an antipsychotic agent for the treatment of schizophrenia, representing a novel mechanism distinct from traditional dopamine receptor antagonists. Xanomeline binds with similar affinity to all five muscarinic receptor subtypes (M1–M5), but its therapeutic effects are believed to be primarily mediated through agonism at M1 and M4 receptors, which are highly expressed in brain regions implicated in cognition and psychosis. In addition to its activity at muscarinic receptors, xanomeline also exhibits partial agonist or antagonist activity at several serotonin receptors (notably 5-HT1A, 5-HT1B as partial agonist; 5-HT2A/2B/2C as antagonist). The drug was approved by the FDA in September 2024 for use (in combination with trospium) for adults with schizophrenia[1][3][7].
- Brand names
- CobenfyKarXT
- Other names
- xanomeline
02
Targets
HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))HTR1B (5-Hydroxytryptamine Receptor 1B)HTR2A (Serotonin receptor 5-HT2A)HTR2B (5-Hydroxytryptamine Receptor 2B)HTR2C (5-hydroxytryptamine 2C receptor)M1 (Muscarinic acetylcholine receptor M1)CHRM2 (M2)CHRM3 (M3)CHRM4 (M4)CHRM5 (M5)
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