Drug intelligence / Profile preview

KarXT long-acting injectable

Development stage
Unknown
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Intramuscular
01

Overview

KarXT long-acting injectable (LAI) is a sustained-release formulation of the combination therapy xanomeline and trospium chloride, currently being developed by Bristol Myers Squibb following its acquisition of Karuna Therapeutics. This formulation is designed to provide a long-term dosing option for the treatment of schizophrenia, aiming to improve medication adherence compared to the oral version (Cobenfy). Xanomeline acts as a dual M1 and M4 muscarinic acetylcholine receptor agonist, which modulates neurotransmission in the brain to address the positive, negative, and cognitive symptoms of schizophrenia without the dopamine D2 receptor blockade characteristic of traditional antipsychotics. Trospium chloride is a peripherally restricted muscarinic antagonist that does not cross the blood-brain barrier; it is included to block muscarinic receptors in peripheral tissues, thereby mitigating systemic side effects like nausea and vomiting caused by xanomeline's peripheral activity.

Other names
xanomeline + trospium long-acting injectablexanomeline and trospium long-acting injectable
02

Targets

M1 (Muscarinic acetylcholine receptor M1)CHRM3 (M3)CHRM5 (M5)CHRM2 (M2)CHRM4 (M4)

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