Xanomeline
Highest phase reached
Approved
Drug type
Small molecule
First approval year
2024
- First approval year
- 2024
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Xanomeline
- Molecular weight
- 281.42
- Structure (SMILES)
- CCCCCCOc1nsnc1C1=CCCN(C)C1
- 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
- CAS registry numbers
- 131986-45-3
- ChEMBL ID
- CHEMBL21536
- InChIKey
- JOLJIIDDOBNFHW-UHFFFAOYSA-N
- PubChem compound IDs
- 60809
- RxNorm IDs (RxCUI)
- 2694828
- FDA ingredient codes (UNII)
- 9ORI6L73CJ
- Applicant
- BRISTOL-MYERS
- Approval date
- 26 Sept 2024
- Application number
- NDA216158
- First in class
- Yes
- Orphan designation
- No
- Availability
- Prescription only
- United States (FDA)
- Approved
- Pharmacology name
- xanomeline
- Type
- Synthetic organic
- Drug name stem
- -meline
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- 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
- 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
- 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
- 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
- Event
- gastrointestinal disorder
- Reports
- 6
- Reporting signal score
- 16.0667
- Event
- nausea
- Reports
- 17
- Reporting signal score
- 26.3452
- NCT03697252
- NCT04659161
- NCT04659174
- NCT04738123
- NCT04820309
- NCT05145413
- NCT05304767
- NCT05643170
- NCT05919823
- Dose
- 50mg/20mg
- Route
- Oral
- How often
- Twice daily
- Do not open capsules
- Or at least 2 hours after meal
- Take at least 1 hour before meal
- 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
- 0003-0050
- 0003-0125
- 0003-1100
- 0003-5150
- 0003-5200
- Recorded assays
- 256
- Active assays
- 155
- Confirmatory
- Other
- Screening
- Parasympathomimetics
- Psychotropic Drugs
- Muscarinic Agonists
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
- 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
- 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 Phase 3
- Bipolar disorder Phase 3
- Psychiatric disorder Phase 1
- Psychotic disorder Phase 3
- Schizophrenia Phase 3