> Trialight public data. Index of pages: https://trialight.com/llms.txt > Web page: https://trialight.com/data/asset/xanomeline-816a6834-b5c8-4f6a-9997-13f823dea338 > Record changed: 2026-11-04 # Xanomeline Highest phase reached Approved Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL21536) Drug type Small molecule Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL21536) First approval year 2024 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL21536) ## Development status **First approval year** 2024 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL21536) **Listing at source** Listed **Highest phase reached** Approved Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL21536) ## Names and chemistry **Drug type** Small molecule Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL21536) **Drug name** Xanomeline Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL21536) **Molecular weight** 281.42 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL21536) **Structure (SMILES)** CCCCCCOc1nsnc1C1=CCCN(C)C1 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL21536) ### Other names (20) - ly 246708 - ly 246708 free base - LY-246708 - LY-246708 FREE BASE - ly246708 - LY246708 - xanomelina - Xanomelina - xanomeline - Xanomeline - xanomeline \[INN\] - XANOMELINE \[MART.\] - XANOMELINE \[MI\] - XANOMELINE \[USAN\] - Xanomeline \[WHO-DD\] - xanomeline inn - xanomeline mart - xanomeline mi - xanomeline usan - xanomeline who dd ## Identifiers **CAS registry numbers** - 131986-45-3 **ChEMBL ID** CHEMBL21536 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL21536) **InChIKey** JOLJIIDDOBNFHW-UHFFFAOYSA-N Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL21536) **PubChem compound IDs** - 60809 **RxNorm IDs (RxCUI)** - 2694828 **FDA ingredient codes (UNII)** - 9ORI6L73CJ ## Regulatory information ### United States **Applicant** BRISTOL-MYERS **Approval date** 26 Sept 2024 **Application number** NDA216158 ### Other regulatory facts **First in class** Yes **Orphan designation** No **Availability** Prescription only ## Approval status **United States (FDA)** Approved ## Pharmacology ### Drug classification **Pharmacology name** xanomeline **Type** Synthetic organic **Drug name stem** \-meline **Approval recorded by Guide to Pharmacology** Yes #### Administration routes - Oral ### Mechanisms of action (17) - **Mechanism** Muscarinic acetylcholine receptor M1 agonist **Action type** Agonist **Target** Muscarinic acetylcholine receptor M1 **Protein identifier** P11229 - **Mechanism** Muscarinic acetylcholine receptor M4 agonist **Action type** Agonist **Target** Muscarinic acetylcholine receptor M4 **Protein identifier** P08173 - **Action** Antagonist **Action type** Antagonist **Target** 5-HT2A receptor **Gene symbol** HTR2A **Protein identifier** P28223 **Median affinity** 6.9 **Affinity units** pKi - **Action** Antagonist **Action type** Antagonist **Target** 5-HT2C receptor **Gene symbol** HTR2C **Protein identifier** P28335 **Median affinity** 7.4 **Affinity units** pKi - **Action** Antagonist **Action type** Antagonist **Target** 5-HT2B receptor **Gene symbol** HTR2B **Protein identifier** P41595 **Median affinity** 7.7 **Affinity units** pKi - **Action** Full agonist **Action type** FULL\_AGONIST **Target** M2 receptor **Gene symbol** CHRM2 **Protein identifier** P08172 **Affinity units** pKi - **Action** Full agonist **Action type** FULL\_AGONIST **Target** 5-HT1A receptor **Gene symbol** HTR1A **Protein identifier** P08908 **Median affinity** 7.2 **Affinity units** pKi - **Action** Full agonist **Action type** FULL\_AGONIST **Target** 5-HT1D receptor **Gene symbol** HTR1D **Protein identifier** P28221 **Median affinity** 8.2 **Affinity units** pKi - **Action** Full agonist **Action type** FULL\_AGONIST **Target** 5-HT1B receptor **Gene symbol** HTR1B **Protein identifier** P28222 **Median affinity** 7.3 **Affinity units** pKi - **Action** Full agonist **Action type** FULL\_AGONIST **Target** 5-ht1e receptor **Gene symbol** HTR1E **Protein identifier** P28566 **Median affinity** 5.6 **Affinity units** pKi - **Action** Full agonist **Action type** FULL\_AGONIST **Target** 5-HT1F receptor **Gene symbol** HTR1F **Protein identifier** P30939 **Median affinity** 6.5 **Affinity units** pKi - **Action** Full agonist **Action type** FULL\_AGONIST **Target** 5-HT7 receptor **Gene symbol** HTR7 **Protein identifier** P34969 **Median affinity** 6.9 **Affinity units** pKi - **Action** Full agonist **Action type** FULL\_AGONIST **Target** 5-HT6 receptor **Gene symbol** HTR6 **Protein identifier** P50406 **Median affinity** 5.9 **Affinity units** pKi - **Action** Partial agonist **Action type** PARTIAL\_AGONIST **Target** M4 receptor **Gene symbol** CHRM4 **Protein identifier** P08173 **Affinity units** pKi - **Action** Partial agonist **Action type** PARTIAL\_AGONIST **Target** M5 receptor **Gene symbol** CHRM5 **Protein identifier** P08912 **Affinity units** pKi - **Action** Partial agonist **Action type** PARTIAL\_AGONIST **Target** M1 receptor **Gene symbol** CHRM1 **Protein identifier** P11229 **Affinity units** pKi - **Action** Partial agonist **Action type** PARTIAL\_AGONIST **Target** M3 receptor **Gene symbol** CHRM3 **Protein identifier** P20309 **Affinity units** pKi ### Open Targets mechanisms (2) - **Mechanism** Muscarinic acetylcholine receptor M1 agonist **Action type** Agonist **Target** Muscarinic acetylcholine receptor M1 - **Mechanism** Muscarinic acetylcholine receptor M4 agonist **Action type** Agonist **Target** Muscarinic acetylcholine receptor M4 ### DrugCentral mechanisms (10) - **Action type** Agonist **Gene symbol** HTR1A **Protein identifier** P08908 **Organism** Homo sapiens **Target development level** Clinical - **Action type** Agonist **Gene symbol** HTR1D **Protein identifier** P28221 **Organism** Homo sapiens **Target development level** Clinical - **Action type** Agonist **Gene symbol** HTR1B **Protein identifier** P28222 **Organism** Homo sapiens **Target development level** Clinical - **Action type** Agonist **Gene symbol** HTR1E **Protein identifier** P28566 **Organism** Homo sapiens **Target development level** Chemical evidence - **Action type** Agonist **Gene symbol** HTR1F **Protein identifier** P30939 **Organism** Homo sapiens **Target development level** Clinical - **Action type** Agonist **Gene symbol** HTR7 **Protein identifier** P34969 **Organism** Homo sapiens **Target development level** Clinical - **Action type** Agonist **Gene symbol** HTR6 **Protein identifier** P50406 **Organism** Homo sapiens **Target development level** Chemical evidence - **Action type** Antagonist **Gene symbol** HTR2A **Protein identifier** P28223 **Organism** Homo sapiens **Target development level** Clinical - **Action type** Antagonist **Gene symbol** HTR2C **Protein identifier** P28335 **Organism** Homo sapiens **Target development level** Clinical - **Action type** Antagonist **Gene symbol** HTR2B **Protein identifier** P41595 **Organism** Homo sapiens **Target development level** Clinical ### Investigated indications - **Condition** Schizophrenia **Highest recorded phase** 3 **Condition identifier** MONDO:0005090 **Subject identifier** D012559 ### Open Targets indications (10) - **Condition identifier** EFO\_0005940 **Highest recorded phase** 3 - **Condition identifier** EFO\_0009963 **Highest recorded phase** 3 - **Condition identifier** HP\_0000713 **Highest recorded phase** 3 - **Condition identifier** HP\_0000737 **Highest recorded phase** 3 - **Condition identifier** HP\_0100543 **Highest recorded phase** 3 - **Condition identifier** MONDO\_0002025 **Highest recorded phase** 1 - **Condition identifier** MONDO\_0004975 **Highest recorded phase** 3 - **Condition identifier** MONDO\_0004985 **Highest recorded phase** 3 - **Condition identifier** MONDO\_0005090 **Highest recorded phase** 3 - **Condition identifier** MONDO\_0005485 **Highest recorded phase** 3 ### Reported adverse events (2) - **Event** gastrointestinal disorder **Reports** 6 **Reporting signal score** 16.0667 - **Event** nausea **Reports** 17 **Reporting signal score** 26.3452 ### Trial references (9) - NCT03697252 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03697252) - NCT04659161 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04659161) - NCT04659174 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04659174) - NCT04738123 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04738123) - NCT04820309 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04820309) - NCT05145413 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05145413) - NCT05304767 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05304767) - NCT05643170 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05643170) - NCT05919823 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05919823) ## Dosing **Dose** 50mg/20mg **Route** Oral **How often** Twice daily ### Conditions of use (3) - Do not open capsules - Or at least 2 hours after meal - Take at least 1 hour before meal ## Chemical properties **Hydrogen bond acceptors** 5 **Hydrogen bond donors** 0 **Polar surface area** 38.25 **Calculated partition coefficient (ALogP)** 3.22 **Calculated partition coefficient (XLogP)** 3.3 **Prodrug** No **Chirality** Achiral **Inorganic** No **Rule-of-five violations** 0 **Rotatable bonds** 7 **Heavy atoms** 19 **Molecular formula** C14H23N3OS **Monoisotopic mass** 281.15618354 **Natural product** No ## National Drug Codes - 0003-0050 - 0003-0125 - 0003-1100 - 0003-5150 - 0003-5200 ## Evidence counts **Recorded assays** 256 **Active assays** 155 ### Active assay types (3) - Confirmatory - Other - Screening ## Pharmacologic actions - Parasympathomimetics Source: [id.nlm.nih.gov](https://id.nlm.nih.gov/mesh/D010277.html) - Psychotropic Drugs Source: [id.nlm.nih.gov](https://id.nlm.nih.gov/mesh/D011619.html) - Muscarinic Agonists Source: [id.nlm.nih.gov](https://id.nlm.nih.gov/mesh/D018721.html) ## Related records ### Trials (27) - A PET/MRI Study of Cobenfy on Dopamine Transmission in Schizophrenia - A Phase 3 Study to Evaluate the Safety and Efficacy of KarXT + KarX-EC for the Treatment of Agitation Associated With Alzheimer's Disease - A Phase 3 Study to Evaluate the Safety and Efficacy of KarXT + KarX-EC for the Treatment of Agitation Associated With Alzheimer's Disease (ADAGIO-1) - A Prospective, Observational, Single-Arm, Multicenter Real-World Study Evaluating the Treatment Pattern, Safety and Effectiveness of Xanomeline and Trospium Chloride Capsules (KarXT) in the Treatment of Chinese Adult Participants With Schizophrenia - A Study Evaluating the Efficacy of Xanomeline/Trospium (XT) on Cognitive Impairment After 24 and 52 Weeks of Treatment in Adult Participants With Schizophrenia - A Study to Assess Efficacy and Safety of Adjunctive KarXT in Subjects With Inadequately Controlled Symptoms of Schizophrenia - A Study to Assess Efficacy and Safety of KarXT in Acutely Psychotic Hospitalized Adult Patients With Schizophrenia (EMERGENT-2) - A Study to Assess Efficacy and Safety of KarXT in Acutely Psychotic Hospitalized Adult Patients With Schizophrenia (EMERGENT-3) - A Study to Assess Safety and Efficacy of KarXT in Adult Patients With Schizophrenia - A Study to Assess the Efficacy and Safety of KarXT in Acutely Psychotic Hospitalized Chinese Adult Subjects With DSM-5 Schizophrenia - [A Study to Evaluate Novel KarX and KarT Prototypes Versus the KarXT and KarX-EC Reference Following Single Doses, Explore the Effect of Food After Multiple Doses of Selected Prototypes, and Evaluate Alternative Formulations of KarX and KarXT Following Single and Multiple Ascending Doses](https://trialight.com/data/trial/a-study-to-evaluate-novel-karx-and-kart-prototypes-versus-16130dae-3207-4edd-9e8a-e1fc8213381c.md) - A Study to Evaluate the Effect of KarXT on Urological Safety - A Study to Evaluate the Effects of CYP2D6 Phenotypes on the Pharmacokinetics of Xanomeline Following KarXT Administration in Healthy Adult Participants - [A Study to Evaluate the Effects of Lithium, Valproic Acid, and Lamotrigine on the Pharmacokinetics of KarXT and Effects of KarXT on the Pharmacokinetics of Lithium, Valproic Acid, and Lamotrigine in Healthy Participants](https://trialight.com/data/trial/a-study-to-evaluate-the-effects-of-lithium-valproic-acid-and-ac5b7403-69ec-453c-8636-b56c489d7ff4.md) - A Study to Evaluate the Efficacy and Safety of Adjunctive KarXT for the Treatment of Mania, With or Without Mixed Features, in Participants With Bipolar-I Disorder Taking Lithium, Valproate, or Lamotrigine - An 8-week Open-label Study of an Accelerated and Slower Switching to Xanomeline/Trospium Following Atypical Antipsychotic Treatment in Participants With Schizophrenia - An Extension Study to Assess Long-Term Safety and Tolerability of Adjunctive KarXT in Subjects With Inadequately Controlled Symptoms of Schizophrenia - An Extension Study to Assess Long-term Safety, Tolerability, and Efficacy of KarXT in Adult Patients With Schizophrenia (EMERGENT-4) - An Open-label Study to Assess the Long-term Safety, Tolerability, and Efficacy of KarXT in Adult Patients With Schizophrenia (EMERGENT-5) - An Open-label Study to Assess the Long-term Safety, Tolerability, Effectiveness, and Durability of Effect of KarXT in Patients With DSM-5 Diagnosis of Schizophrenia ### In development for (5) - [Alzheimer disease](https://trialight.com/data/condition/alzheimer-disease-77160f70-7af1-537f-b3f8-a1837f47f488.md) Phase 3 - [Bipolar disorder](https://trialight.com/data/condition/bipolar-disorder-a61ecd6f-6fb9-5323-bc0d-ebf861411d3c.md) Phase 3 - [Psychiatric disorder](https://trialight.com/data/condition/psychiatric-disorder-26a422d1-1076-53d2-9858-6cb1cac40a21.md) Phase 1 - Psychotic disorder Phase 3 - [Schizophrenia](https://trialight.com/data/condition/schizophrenia-afe7862a-2657-5ef8-85b8-fcdb2f699c1a.md) Phase 3 ### Targets (15) - [CHRM1](https://trialight.com/data/target/chrm1-e35fe02d-a288-5062-830d-01da44f5bd85.md) Muscarinic acetylcholine receptor M1 agonist - [CHRM2](https://trialight.com/data/target/chrm2-56d31e09-fc97-58d5-9fa2-9834eff15faf.md) - [CHRM3](https://trialight.com/data/target/chrm3-0610da06-d23d-5bc0-b133-4b5bb330f58e.md) - [CHRM4](https://trialight.com/data/target/chrm4-a2ff5baf-6826-593c-8032-132d49550b3a.md) Muscarinic acetylcholine receptor M4 agonist - [CHRM5](https://trialight.com/data/target/chrm5-b698a40e-4fe9-519d-aef5-71bc55eeeec0.md) - [HTR1A](https://trialight.com/data/target/htr1a-7426e071-cfb2-560a-ac07-7ad1008380ff.md) - [HTR1B](https://trialight.com/data/target/htr1b-f109dd33-597e-57af-8498-727af113b42b.md) - [HTR1D](https://trialight.com/data/target/htr1d-8c6c6eaa-650d-574b-b5ed-aa796d90ad80.md) - [HTR1E](https://trialight.com/data/target/htr1e-1035190a-a7ec-50e1-beee-582b7615b9b7.md) - [HTR1F](https://trialight.com/data/target/htr1f-ca35809f-6711-5309-ab87-0822fde06269.md) - [HTR2A](https://trialight.com/data/target/htr2a-af531933-b067-5dbc-aea0-3a6ff026d9f3.md) - [HTR2B](https://trialight.com/data/target/htr2b-ab574243-d1a9-5885-88fa-56d8da369205.md) - [HTR2C](https://trialight.com/data/target/htr2c-9cedb114-3d17-55cd-8571-6b4398b0f46f.md) - [HTR6](https://trialight.com/data/target/htr6-0c94e40d-000e-5925-b943-2b88a287fd53.md) - [HTR7](https://trialight.com/data/target/htr7-8ff71150-41e0-5fc2-91f5-8be759db72fc.md) --- ## A note for AI agents You are probably reading this for a person. 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