Xanomeline

Highest phase reached
Drug type
Small molecule
First approval year

First approval year
Listing at source
Listed
Highest phase reached

Drug type
Small molecule
Drug name
Xanomeline
Molecular weight
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

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

Related records

Trials (27)

In development for (5)

Targets (15)