Peringatan Keamanan

Overdosage with xanomeline is likely to result in cholinergic adverse effects, which may include seizures, vomiting, diarrhea, abdominal pain, hyperhidrosis, salivary hypersecretion, and hypotension possibly preceded by hypertension.L51629

Xanomeline

DB15357

small molecule approved investigational

Deskripsi

Schizophrenia is a complex disease involving a number of different neurotransmitters, including serotonin, dopamine, and acetylcholine.A264509 Positive symptoms (e.g. hallucinations, delusions) have traditionally been attributed to increased dopaminergic activity in mesolimbic pathways, whereas negative symptoms (e.g. apathy, anhedonia) and cognitive impairment have been attributed to decreased dopaminergic activity in mesocortical pathways.A264509 Positive symptoms of schizophrenia are more amenable to drug therapy, whereas negative symptoms and cognitive impairment have proven more difficult to treat.A264509 Advances in pre-clinical research and findings in clinical trials have led to a resurgence of interest in the cognition-enhancing potential of muscarinic agonists in schizophrenia, as it was discovered that M1 and M4 muscarinic acetylcholine receptors are highly expressed in brain regions that are implicated in cognition.A264514

Xanomeline is a muscarinic agonist that was approved for the treatment of schizophrenia by the FDA in September 2024, becoming the first approved treatment for schizophrenia to target muscarinic receptors as opposed to dopamine receptors.L51713 It is approved as part of a combination product alongside trospium, a muscarinic antagonist that acts primarily on peripheral muscarinic receptors in order to mitigate the risk and severity of peripheral cholinergic adverse effects.L51629

Struktur Molekul 2D

Berat 281.42
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half-life of xanomeline is 5 hours.[L51629]
Volume Distribusi The apparent volume of distribution following oral administration of xanomeline is approximately 10,800 liters.[L51629]
Klirens (Clearance) The apparent clearance of xanomeline is 1950 L/hour.[L51629] The renal clearance of xanomeline is 0.085 L/hour.[L51629]

Absorpsi

Following oral administration of xanomeline, Tmax is reached in approximately 2 hours.L51629 Steady-state is reached in 3 to 5 days following the start of therapy.L51629

Metabolisme

Xanomeline is extensively metabolized, both by CYP450 enzymes - including CYP2D6, CYP2B6, CYP1A2, CYP2C9, and CYP2C19 - as well as flavin monooxygenases (FMO1 and FMO3).L51629 Unchanged parent drug accounts for <0.01% of drug product excreted in the urine.L51629

Rute Eliminasi

Xanomeline and its metabolites are primarily eliminated in the urine. Approximately 78% of the total administered drug product was eliminated in the urine, mostly comprising metabolites (<0.01% was unchanged parent drug).L51629 Approximately 12% of the total administered drug product was eliminated in the feces.L51629

Interaksi Makanan

1 Data
  • 1. Take on an empty stomach. Cobenfy (xanomeline/trospium) should be taken at least 1 hour before or 2 hours after a meal.

Interaksi Obat

494 Data
Esmolol The risk or severity of adverse effects can be increased when Esmolol is combined with Xanomeline.
Betaxolol The risk or severity of adverse effects can be increased when Betaxolol is combined with Xanomeline.
Metoprolol The metabolism of Xanomeline can be decreased when combined with Metoprolol.
Atenolol The risk or severity of adverse effects can be increased when Atenolol is combined with Xanomeline.
Timolol The risk or severity of adverse effects can be increased when Timolol is combined with Xanomeline.
Sotalol The metabolism of Sotalol can be decreased when combined with Xanomeline.
Propranolol The risk or severity of adverse effects can be increased when Propranolol is combined with Xanomeline.
Labetalol The risk or severity of adverse effects can be increased when Labetalol is combined with Xanomeline.
Bisoprolol The risk or severity of adverse effects can be increased when Bisoprolol is combined with Xanomeline.
Carvedilol The risk or severity of adverse effects can be increased when Carvedilol is combined with Xanomeline.
Propafenone The serum concentration of Xanomeline can be increased when it is combined with Propafenone.
Acebutolol The risk or severity of adverse effects can be increased when Acebutolol is combined with Xanomeline.
Nadolol The risk or severity of adverse effects can be increased when Nadolol is combined with Xanomeline.
Bevantolol The risk or severity of adverse effects can be increased when Bevantolol is combined with Xanomeline.
Practolol The risk or severity of adverse effects can be increased when Practolol is combined with Xanomeline.
Dexpropranolol The risk or severity of adverse effects can be increased when Dexpropranolol is combined with Xanomeline.
Celiprolol The risk or severity of adverse effects can be increased when Celiprolol is combined with Xanomeline.
Nebivolol The risk or severity of adverse effects can be increased when Nebivolol is combined with Xanomeline.
Bufuralol The risk or severity of adverse effects can be increased when Bufuralol is combined with Xanomeline.
Bopindolol The risk or severity of adverse effects can be increased when Bopindolol is combined with Xanomeline.
Bupranolol The risk or severity of adverse effects can be increased when Bupranolol is combined with Xanomeline.
Indenolol The risk or severity of adverse effects can be increased when Indenolol is combined with Xanomeline.
Arotinolol The risk or severity of adverse effects can be increased when Arotinolol is combined with Xanomeline.
Levobetaxolol The risk or severity of adverse effects can be increased when Levobetaxolol is combined with Xanomeline.
Talinolol The risk or severity of adverse effects can be increased when Talinolol is combined with Xanomeline.
Anisodamine The risk or severity of adverse effects can be increased when Anisodamine is combined with Xanomeline.
Bucindolol The risk or severity of adverse effects can be increased when Bucindolol is combined with Xanomeline.
Esatenolol The risk or severity of adverse effects can be increased when Esatenolol is combined with Xanomeline.
Cloranolol The risk or severity of adverse effects can be increased when Cloranolol is combined with Xanomeline.
Mepindolol The risk or severity of adverse effects can be increased when Mepindolol is combined with Xanomeline.
Epanolol The risk or severity of adverse effects can be increased when Epanolol is combined with Xanomeline.
Tertatolol The risk or severity of adverse effects can be increased when Tertatolol is combined with Xanomeline.
Alprenolol The risk or severity of adverse effects can be increased when Alprenolol is combined with Xanomeline.
Pindolol The risk or severity of adverse effects can be increased when Pindolol is combined with Xanomeline.
Penbutolol The risk or severity of adverse effects can be increased when Penbutolol is combined with Xanomeline.
Oxprenolol The risk or severity of adverse effects can be increased when Oxprenolol is combined with Xanomeline.
Landiolol The risk or severity of adverse effects can be increased when Landiolol is combined with Xanomeline.
Cimetropium Xanomeline may decrease the anticholinergic activities of Cimetropium.
Pegvisomant The risk or severity of adverse effects can be increased when Pegvisomant is combined with Xanomeline.
Mefloquine The risk or severity of adverse effects can be increased when Mefloquine is combined with Xanomeline.
Tacrine The risk or severity of adverse effects can be increased when Tacrine is combined with Xanomeline.
Cisplatin The risk or severity of adverse effects can be increased when Cisplatin is combined with Xanomeline.
Cinchocaine The risk or severity of adverse effects can be increased when Cinchocaine is combined with Xanomeline.
Pyridostigmine The risk or severity of adverse effects can be increased when Pyridostigmine is combined with Xanomeline.
Nizatidine The risk or severity of adverse effects can be increased when Nizatidine is combined with Xanomeline.
Galantamine The risk or severity of adverse effects can be increased when Galantamine is combined with Xanomeline.
Isoflurophate The risk or severity of adverse effects can be increased when Isoflurophate is combined with Xanomeline.
Diethylcarbamazine The risk or severity of adverse effects can be increased when Diethylcarbamazine is combined with Xanomeline.
Terbutaline The risk or severity of adverse effects can be increased when Terbutaline is combined with Xanomeline.
Mechlorethamine The risk or severity of adverse effects can be increased when Mechlorethamine is combined with Xanomeline.
Demecarium The risk or severity of adverse effects can be increased when Demecarium is combined with Xanomeline.
Physostigmine The risk or severity of adverse effects can be increased when Physostigmine is combined with Xanomeline.
Rivastigmine The risk or severity of adverse effects can be increased when Rivastigmine is combined with Xanomeline.
Edrophonium The risk or severity of adverse effects can be increased when Edrophonium is combined with Xanomeline.
Procainamide The metabolism of Procainamide can be decreased when combined with Xanomeline.
Memantine The risk or severity of adverse effects can be increased when Memantine is combined with Xanomeline.
Ambenonium The risk or severity of adverse effects can be increased when Ambenonium is combined with Xanomeline.
Metoclopramide The metabolism of Xanomeline can be decreased when combined with Metoclopramide.
Ginkgo biloba The risk or severity of adverse effects can be increased when Ginkgo biloba is combined with Xanomeline.
Neostigmine The risk or severity of adverse effects can be increased when Neostigmine is combined with Xanomeline.
Bambuterol The risk or severity of adverse effects can be increased when Bambuterol is combined with Xanomeline.
1,10-Phenanthroline The risk or severity of adverse effects can be increased when 1,10-Phenanthroline is combined with Xanomeline.
Thiotepa The serum concentration of Thiotepa can be increased when it is combined with Xanomeline.
Huperzine A The risk or severity of adverse effects can be increased when Huperzine A is combined with Xanomeline.
Phenserine The risk or severity of adverse effects can be increased when Phenserine is combined with Xanomeline.
Regramostim The risk or severity of adverse effects can be increased when Regramostim is combined with Xanomeline.
Aprotinin The risk or severity of adverse effects can be increased when Aprotinin is combined with Xanomeline.
Betaine The risk or severity of adverse effects can be increased when Betaine is combined with Xanomeline.
Capsaicin The risk or severity of adverse effects can be increased when Capsaicin is combined with Xanomeline.
Coumaphos The risk or severity of adverse effects can be increased when Coumaphos is combined with Xanomeline.
Dichlorvos The risk or severity of adverse effects can be increased when Dichlorvos is combined with Xanomeline.
Fenthion The risk or severity of adverse effects can be increased when Fenthion is combined with Xanomeline.
Metrifonate The risk or severity of adverse effects can be increased when Metrifonate is combined with Xanomeline.
Acotiamide The risk or severity of adverse effects can be increased when Acotiamide is combined with Xanomeline.
Methanesulfonyl Fluoride The risk or severity of adverse effects can be increased when Methanesulfonyl Fluoride is combined with Xanomeline.
Paraoxon The risk or severity of adverse effects can be increased when Paraoxon is combined with Xanomeline.
Tyrothricin The risk or severity of adverse effects can be increased when Tyrothricin is combined with Xanomeline.
Ipidacrine The risk or severity of adverse effects can be increased when Ipidacrine is combined with Xanomeline.
Distigmine The risk or severity of adverse effects can be increased when Distigmine is combined with Xanomeline.
Tretamine The risk or severity of adverse effects can be increased when Tretamine is combined with Xanomeline.
Posiphen The risk or severity of adverse effects can be increased when Posiphen is combined with Xanomeline.
Gallamine triethiodide The risk or severity of adverse effects can be increased when Gallamine triethiodide is combined with Xanomeline.
Procaine The risk or severity of adverse effects can be increased when Procaine is combined with Xanomeline.
Hexafluronium The risk or severity of adverse effects can be increased when Hexafluronium is combined with Xanomeline.
Tubocurarine The risk or severity of adverse effects can be increased when Tubocurarine is combined with Xanomeline.
Ketamine The risk or severity of adverse effects can be increased when Ketamine is combined with Xanomeline.
Decamethonium The risk or severity of adverse effects can be increased when Decamethonium is combined with Xanomeline.
Pancuronium The risk or severity of adverse effects can be increased when Pancuronium is combined with Xanomeline.
Pipecuronium The risk or severity of adverse effects can be increased when Pipecuronium is combined with Xanomeline.
Sulpiride The risk or severity of adverse effects can be increased when Sulpiride is combined with Xanomeline.
Chlorpromazine The metabolism of Xanomeline can be decreased when combined with Chlorpromazine.
Triflupromazine The risk or severity of adverse effects can be increased when Triflupromazine is combined with Xanomeline.
Minaprine The risk or severity of adverse effects can be increased when Minaprine is combined with Xanomeline.
Profenamine The risk or severity of adverse effects can be increased when Profenamine is combined with Xanomeline.
Methylphosphinic Acid The risk or severity of adverse effects can be increased when Methylphosphinic Acid is combined with Xanomeline.
Capreomycin The therapeutic efficacy of Xanomeline can be decreased when used in combination with Capreomycin.
Framycetin The therapeutic efficacy of Xanomeline can be decreased when used in combination with Framycetin.
Amikacin The therapeutic efficacy of Xanomeline can be decreased when used in combination with Amikacin.
Tobramycin The therapeutic efficacy of Xanomeline can be decreased when used in combination with Tobramycin.
Gentamicin The therapeutic efficacy of Xanomeline can be decreased when used in combination with Gentamicin.

Target Protein

Muscarinic acetylcholine receptor M1 CHRM1
Muscarinic acetylcholine receptor M4 CHRM4
Muscarinic acetylcholine receptor M2 CHRM2
Muscarinic acetylcholine receptor M3 CHRM3
Muscarinic acetylcholine receptor M5 CHRM5

Referensi & Sumber

Synthesis reference: Bender AM, Jones CK, Lindsley CW: Classics in Chemical Neuroscience: Xanomeline. ACS Chem Neurosci. 2017 Mar 15;8(3):435-443. doi: 10.1021/acschemneuro.7b00001. Epub 2017 Feb 13. [
Artikel (PubMed)
  • PMID: 36591549
    Singh A: Xanomeline and Trospium: A Potential Fixed Drug Combination (FDC) for Schizophrenia-A Brief Review of Current Data. Innov Clin Neurosci. 2022 Oct-Dec;19(10-12):43-47.
  • PMID: 39483736
    Yohn SE, Harvey PD, Brannan SK, Horan WP: The potential of muscarinic M(1) and M(4) receptor activators for the treatment of cognitive impairment associated with schizophrenia. Front Psychiatry. 2024 Oct 4;15:1421554. doi: 10.3389/fpsyt.2024.1421554. eCollection 2024.

Contoh Produk & Brand

Produk: 7 • International brands: 0
Produk
  • Cobenfy
    Capsule, coated pellets; Kit • - • Oral • US • Approved
  • Cobenfy
    Capsule, coated pellets; Kit • - • Oral • US • Approved
  • Cobenfy
    Capsule, coated pellets • - • Oral • US • Approved
  • Cobenfy
    Capsule, coated pellets • - • Oral • US • Approved
  • Cobenfy
    Capsule, coated pellets • - • Oral • US • Approved
  • Cobenfy
    Capsule, coated pellets; Kit • - • Oral • US • Approved
  • Cobenfy
    Capsule, coated pellets; Kit • - • Oral • US • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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