Rankings / Mental Health

Xanomeline-trospium (KarXT / Cobenfy)

Mental Health · M1/M4 muscarinic agonist + peripheral antagonist

Tier B+

cholinergicprescription
7.1 / 10
Tier B+
Ev 8.0 Bn 8.0 Sf 5.0 Ax 6.0

What this is

Bristol Myers Squibb (acquired Karuna 2024). First fundamentally new schizophrenia mechanism since clozapine (1989). Avoids dopamine D2 blockade entirely — sidesteps weight gain, EPS, prolactin elevation, and tardive dyskinesia. Active investigation in Alzheimer's psychosis, ADHD, BPD. Major clinical advance even though efficacy is comparable to atypicals.

Mechanism

Combination drug: xanomeline is a centrally acting M1/M4 muscarinic acetylcholine receptor agonist (developed in 1990s but shelved due to peripheral cholinergic side effects); trospium is a peripherally restricted muscarinic antagonist that blocks the GI/cardiac side effects without crossing the BBB — allowing the central effect to be tolerated; first novel mechanism for schizophrenia in 50+ years

Dose & route

50/20 mg twice daily, titrate up to 125/30 mg twice daily

Citations

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