GTS-21

DB05708

small molecule investigational

Deskripsi

GTS-21 (also known as DMBX-A), is a novel, small-molecule, orally active and selective alpha-7 nicotinic acetylcholine (nACh) receptor agonist that has demonstrated memory and cognition enhancement activity in human clinical trials. Athenagen licensed the exclusive rights to the compound and a related library of analogs as part of the acquisition of Osprey Pharmaceutical Company in April 2006. GTS-21 has been studied in multiple Phase I studies in healthy volunteers and one Phase I/II study in schizophrenic patients. In all studies, the compound was well tolerated. In a Phase I multi-dose, double-blind, placebo controlled study in healthy adults, GTS-21 also demonstrated cognitive enhancement across all doses, with a statistically significant improvement in attention related and memory related tasks (Kitagawa, et al. Neuropsychopharmacology (2003), 28, 542-551).

Struktur Molekul 2D

Berat 308.3743
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) -
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Rapidly and extensively absorbed after oral administration. In rat, GTS-21 showed linear pharmacokinetics over doses ranging from 1 to 10 mg/kg with an absolute bioavailability of 23%. In dog, the absolute bioavailability was 27% at an oral dose of 3 mg/kg.

Metabolisme

GTS-21 was O-demethylated to yield compounds that were then subject to glucuronidation. Three of the metabolites in rat urine were isolated and characterized as 4-OH-GTS-21, 4-OH-GTS-21 glucuronide and 2-OH-GTS-21 glucuronide. The major urinary metabolites were 4-OH-GTS-21 glucuronide and 2-OH-GTS-21 glucuronide. In vitro chemical inhibition of cytochrome P450 in human liver microsomes indicated that CYPIA2 and CYP2E1 were the isoforms primarily responsible for the O-demethylation of GTS-21, with some contribution from CYP3A.

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Obat

424 Data
Deferasirox The serum concentration of GTS-21 can be increased when it is combined with Deferasirox.
Peginterferon alfa-2b The serum concentration of GTS-21 can be increased when it is combined with Peginterferon alfa-2b.
Leflunomide The serum concentration of GTS-21 can be decreased when it is combined with Leflunomide.
Teriflunomide The serum concentration of GTS-21 can be decreased when it is combined with Teriflunomide.
Abiraterone The serum concentration of GTS-21 can be increased when it is combined with Abiraterone.
Cyproterone acetate The metabolism of GTS-21 can be increased when combined with Cyproterone acetate.
Esmolol The risk or severity of adverse effects can be increased when Esmolol is combined with GTS-21.
Metoprolol The risk or severity of adverse effects can be increased when Metoprolol is combined with GTS-21.
Atenolol The risk or severity of adverse effects can be increased when Atenolol is combined with GTS-21.
Timolol The risk or severity of adverse effects can be increased when Timolol is combined with GTS-21.
Sotalol The risk or severity of adverse effects can be increased when Sotalol is combined with GTS-21.
Labetalol The risk or severity of adverse effects can be increased when Labetalol is combined with GTS-21.
Bisoprolol The risk or severity of adverse effects can be increased when Bisoprolol is combined with GTS-21.
Alprenolol The risk or severity of adverse effects can be increased when Alprenolol is combined with GTS-21.
Pindolol The risk or severity of adverse effects can be increased when Pindolol is combined with GTS-21.
Acebutolol The risk or severity of adverse effects can be increased when Acebutolol is combined with GTS-21.
Nadolol The risk or severity of adverse effects can be increased when Nadolol is combined with GTS-21.
Bevantolol The risk or severity of adverse effects can be increased when Bevantolol is combined with GTS-21.
Practolol The risk or severity of adverse effects can be increased when Practolol is combined with GTS-21.
Penbutolol The risk or severity of adverse effects can be increased when Penbutolol is combined with GTS-21.
Oxprenolol The risk or severity of adverse effects can be increased when Oxprenolol is combined with GTS-21.
Dexpropranolol The risk or severity of adverse effects can be increased when Dexpropranolol is combined with GTS-21.
Celiprolol The risk or severity of adverse effects can be increased when Celiprolol is combined with GTS-21.
Nebivolol The risk or severity of adverse effects can be increased when Nebivolol is combined with GTS-21.
Bufuralol The risk or severity of adverse effects can be increased when Bufuralol is combined with GTS-21.
Bopindolol The risk or severity of adverse effects can be increased when Bopindolol is combined with GTS-21.
Bupranolol The risk or severity of adverse effects can be increased when Bupranolol is combined with GTS-21.
Indenolol The risk or severity of adverse effects can be increased when Indenolol is combined with GTS-21.
Arotinolol The risk or severity of adverse effects can be increased when Arotinolol is combined with GTS-21.
Levobetaxolol The risk or severity of adverse effects can be increased when Levobetaxolol is combined with GTS-21.
Talinolol The risk or severity of adverse effects can be increased when Talinolol is combined with GTS-21.
Anisodamine The risk or severity of adverse effects can be increased when Anisodamine is combined with GTS-21.
Bucindolol The risk or severity of adverse effects can be increased when Bucindolol is combined with GTS-21.
Esatenolol The risk or severity of adverse effects can be increased when Esatenolol is combined with GTS-21.
Cloranolol The risk or severity of adverse effects can be increased when Cloranolol is combined with GTS-21.
Mepindolol The risk or severity of adverse effects can be increased when Mepindolol is combined with GTS-21.
Epanolol The risk or severity of adverse effects can be increased when Epanolol is combined with GTS-21.
Tertatolol The risk or severity of adverse effects can be increased when Tertatolol is combined with GTS-21.
Landiolol The risk or severity of adverse effects can be increased when Landiolol is combined with GTS-21.
Cimetropium GTS-21 may decrease the anticholinergic activities of Cimetropium.
Pegvisomant The risk or severity of adverse effects can be increased when Pegvisomant is combined with GTS-21.
Mefloquine The risk or severity of adverse effects can be increased when Mefloquine is combined with GTS-21.
Sulpiride The risk or severity of adverse effects can be increased when Sulpiride is combined with GTS-21.
Profenamine The risk or severity of adverse effects can be increased when Profenamine is combined with GTS-21.
Gallamine triethiodide The risk or severity of adverse effects can be increased when Gallamine triethiodide is combined with GTS-21.
Triflupromazine The risk or severity of adverse effects can be increased when Triflupromazine is combined with GTS-21.
Cisplatin The risk or severity of adverse effects can be increased when Cisplatin is combined with GTS-21.
Cinchocaine The risk or severity of adverse effects can be increased when Cinchocaine is combined with GTS-21.
Pyridostigmine The risk or severity of adverse effects can be increased when Pyridostigmine is combined with GTS-21.
Nizatidine The risk or severity of adverse effects can be increased when Nizatidine is combined with GTS-21.
Galantamine The risk or severity of adverse effects can be increased when Galantamine is combined with GTS-21.
Isoflurophate The risk or severity of adverse effects can be increased when Isoflurophate is combined with GTS-21.
Diethylcarbamazine The risk or severity of adverse effects can be increased when Diethylcarbamazine is combined with GTS-21.
Procaine The risk or severity of adverse effects can be increased when Procaine is combined with GTS-21.
Minaprine The risk or severity of adverse effects can be increased when Minaprine is combined with GTS-21.
Terbutaline The risk or severity of adverse effects can be increased when Terbutaline is combined with GTS-21.
Mechlorethamine The risk or severity of adverse effects can be increased when Mechlorethamine is combined with GTS-21.
Hexafluronium The risk or severity of adverse effects can be increased when Hexafluronium is combined with GTS-21.
Demecarium The risk or severity of adverse effects can be increased when Demecarium is combined with GTS-21.
Physostigmine The risk or severity of adverse effects can be increased when Physostigmine is combined with GTS-21.
Rivastigmine The risk or severity of adverse effects can be increased when Rivastigmine is combined with GTS-21.
Edrophonium The risk or severity of adverse effects can be increased when Edrophonium is combined with GTS-21.
Procainamide The risk or severity of adverse effects can be increased when Procainamide is combined with GTS-21.
Memantine The risk or severity of adverse effects can be increased when Memantine is combined with GTS-21.
Ambenonium The risk or severity of adverse effects can be increased when Ambenonium is combined with GTS-21.
Tubocurarine The risk or severity of adverse effects can be increased when Tubocurarine is combined with GTS-21.
Ketamine The risk or severity of adverse effects can be increased when Ketamine is combined with GTS-21.
Decamethonium The risk or severity of adverse effects can be increased when Decamethonium is combined with GTS-21.
Pancuronium The risk or severity of adverse effects can be increased when Pancuronium is combined with GTS-21.
Pipecuronium The risk or severity of adverse effects can be increased when Pipecuronium is combined with GTS-21.
Ginkgo biloba The risk or severity of adverse effects can be increased when Ginkgo biloba is combined with GTS-21.
Neostigmine The risk or severity of adverse effects can be increased when Neostigmine is combined with GTS-21.
Bambuterol The risk or severity of adverse effects can be increased when Bambuterol is combined with GTS-21.
1,10-Phenanthroline The risk or severity of adverse effects can be increased when 1,10-Phenanthroline is combined with GTS-21.
Thiotepa The risk or severity of adverse effects can be increased when Thiotepa is combined with GTS-21.
Huperzine A The risk or severity of adverse effects can be increased when Huperzine A is combined with GTS-21.
Phenserine The risk or severity of adverse effects can be increased when Phenserine is combined with GTS-21.
Regramostim The risk or severity of adverse effects can be increased when Regramostim is combined with GTS-21.
Aprotinin The risk or severity of adverse effects can be increased when Aprotinin is combined with GTS-21.
Betaine The risk or severity of adverse effects can be increased when Betaine is combined with GTS-21.
Coumaphos The risk or severity of adverse effects can be increased when Coumaphos is combined with GTS-21.
Dichlorvos The risk or severity of adverse effects can be increased when Dichlorvos is combined with GTS-21.
Fenthion The risk or severity of adverse effects can be increased when Fenthion is combined with GTS-21.
Metrifonate The risk or severity of adverse effects can be increased when Metrifonate is combined with GTS-21.
Acotiamide The risk or severity of adverse effects can be increased when Acotiamide is combined with GTS-21.
Methanesulfonyl Fluoride The risk or severity of adverse effects can be increased when Methanesulfonyl Fluoride is combined with GTS-21.
Paraoxon The risk or severity of adverse effects can be increased when Paraoxon is combined with GTS-21.
Tyrothricin The risk or severity of adverse effects can be increased when Tyrothricin is combined with GTS-21.
Ipidacrine The risk or severity of adverse effects can be increased when Ipidacrine is combined with GTS-21.
Distigmine The risk or severity of adverse effects can be increased when Distigmine is combined with GTS-21.
Tretamine The risk or severity of adverse effects can be increased when Tretamine is combined with GTS-21.
Posiphen The risk or severity of adverse effects can be increased when Posiphen is combined with GTS-21.
Methylphosphinic Acid The risk or severity of adverse effects can be increased when Methylphosphinic Acid is combined with GTS-21.
Carbamazepine The metabolism of GTS-21 can be increased when combined with Carbamazepine.
Primidone The metabolism of GTS-21 can be increased when combined with Primidone.
Rifampin The metabolism of GTS-21 can be increased when combined with Rifampicin.
Albendazole The metabolism of GTS-21 can be increased when combined with Albendazole.
Caffeine The metabolism of GTS-21 can be decreased when combined with Caffeine.
Moxifloxacin The metabolism of GTS-21 can be decreased when combined with Moxifloxacin.
Lidocaine The metabolism of GTS-21 can be decreased when combined with Lidocaine.

Target Protein

Neuronal acetylcholine receptor subunit alpha-7 CHRNA7

Referensi & Sumber

Artikel (PubMed)
  • PMID: 15205879
    Martin LF, Kem WR, Freedman R: Alpha-7 nicotinic receptor agonists: potential new candidates for the treatment of schizophrenia. Psychopharmacology (Berl). 2004 Jun;174(1):54-64. Epub 2004 Feb 19.
  • PMID: 12629535
    Kitagawa H, Takenouchi T, Azuma R, Wesnes KA, Kramer WG, Clody DE, Burnett AL: Safety, pharmacokinetics, and effects on cognitive function of multiple doses of GTS-21 in healthy, male volunteers. Neuropsychopharmacology. 2003 Mar;28(3):542-51. Epub 2002 Jul 11.
  • PMID: 10942043
    Kem WR: The brain alpha7 nicotinic receptor may be an important therapeutic target for the treatment of Alzheimer's disease: studies with DMXBA (GTS-21). Behav Brain Res. 2000 Aug;113(1-2):169-81.
  • PMID: 10515327
    van Haaren F, Anderson KG, Haworth SC, Kem WR: GTS-21, a mixed nicotinic receptor agonist/antagonist, does not affect the nicotine cue. Pharmacol Biochem Behav. 1999 Oct;64(2):439-44.
  • PMID: 10456692
    Azuma R, Komuro M, Korsch BH, Andre JC, Onnagawa O, Black SR, Mathews JM: Metabolism and disposition of GTS-21, a novel drug for Alzheimer's disease. Xenobiotica. 1999 Jul;29(7):747-62.

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