Dexloxiglumide

DB04856

small molecule investigational

Deskripsi

Dexloxiglumide is a selective cholecystokinin type A (CCKA) receptor antagonist in phase III testing by Rottapharm in Europe only, as U.S. trials have been discontinued. As the D-isomer of loxiglumide, it retains all pharmacological properties of loxiglumide but is more potent.

Struktur Molekul 2D

Berat 461.379
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 single oral administration in humans with an absolute bioavailability of 48%. The incomplete bioavailability is due to both incomplete absorption and hepatic first-pass effect.

Metabolisme

Cytochrome P450 (CYP) 3A4/5 and CYP2C9 have been implicated in the metabolism of dexloxiglumide to produce O-demethyl dexloxi-glumide. This metabolite is further oxidised to dexloxiglumide carboxylic acid. These two major metabolites (accounting for up to 50% of dexloxiglumide elimination) have been identified. However, in human plasma the unchanged drug represents the major (up to 91%) component of the metabolic profile. The parent drug is believed to be the major contributor to the efficacy of the compound, since its major metabolites are pharmacologically inactive.

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Obat

476 Data
Pitolisant The serum concentration of Dexloxiglumide can be decreased when it is combined with Pitolisant.
Metreleptin The metabolism of Dexloxiglumide can be increased when combined with Metreleptin.
Diltiazem The metabolism of Dexloxiglumide can be decreased when combined with Diltiazem.
Cimetidine The metabolism of Dexloxiglumide can be decreased when combined with Cimetidine.
Ciprofloxacin The metabolism of Dexloxiglumide can be decreased when combined with Ciprofloxacin.
Verapamil The metabolism of Dexloxiglumide can be decreased when combined with Verapamil.
Isavuconazole The metabolism of Dexloxiglumide can be decreased when combined with Isavuconazole.
Erythromycin The serum concentration of Dexloxiglumide can be increased when it is combined with Erythromycin.
Troglitazone The metabolism of Dexloxiglumide can be decreased when combined with Troglitazone.
Chloramphenicol The metabolism of Dexloxiglumide can be decreased when combined with Chloramphenicol.
Fluticasone propionate The metabolism of Dexloxiglumide can be decreased when combined with Fluticasone propionate.
Imatinib The metabolism of Dexloxiglumide can be decreased when combined with Imatinib.
Aprepitant The metabolism of Dexloxiglumide can be decreased when combined with Aprepitant.
Mibefradil The metabolism of Dexloxiglumide can be decreased when combined with Mibefradil.
Gestodene The metabolism of Dexloxiglumide can be decreased when combined with Gestodene.
Seproxetine The metabolism of Dexloxiglumide can be decreased when combined with Seproxetine.
Fluticasone furoate The metabolism of Fluticasone furoate can be decreased when combined with Dexloxiglumide.
Letermovir The metabolism of Dexloxiglumide can be decreased when combined with Letermovir.
Rucaparib The metabolism of Dexloxiglumide can be decreased when combined with Rucaparib.
Fluticasone The metabolism of Dexloxiglumide can be decreased when combined with Fluticasone.
Medical Cannabis The metabolism of Dexloxiglumide can be decreased when combined with Medical Cannabis.
Nabiximols The metabolism of Dexloxiglumide can be decreased when combined with Nabiximols.
Curcumin sulfate The metabolism of Dexloxiglumide can be decreased when combined with Curcumin sulfate.
Methylene blue The metabolism of Dexloxiglumide can be decreased when combined with Methylene blue.
Clofazimine The metabolism of Dexloxiglumide can be decreased when combined with Clofazimine.
Pralsetinib The metabolism of Dexloxiglumide can be decreased when combined with Pralsetinib.
Levoketoconazole The metabolism of Dexloxiglumide can be decreased when combined with Levoketoconazole.
Acalabrutinib The metabolism of Dexloxiglumide can be decreased when combined with Acalabrutinib.
Osilodrostat The metabolism of Dexloxiglumide can be decreased when combined with Osilodrostat.
Modafinil The metabolism of Dexloxiglumide can be increased when combined with Modafinil.
Budesonide The metabolism of Dexloxiglumide can be increased when combined with Budesonide.
Icotinib The metabolism of Dexloxiglumide can be increased when combined with Icotinib.
Dexamethasone acetate The metabolism of Dexloxiglumide can be increased when combined with Dexamethasone acetate.
Reserpine The metabolism of Dexloxiglumide can be increased when combined with Reserpine.
Beclomethasone dipropionate The metabolism of Dexloxiglumide can be increased when combined with Beclomethasone dipropionate.
Triamcinolone The metabolism of Dexloxiglumide can be increased when combined with Triamcinolone.
Daunorubicin The metabolism of Dexloxiglumide can be increased when combined with Daunorubicin.
Oxcarbazepine The metabolism of Dexloxiglumide can be increased when combined with Oxcarbazepine.
Thalidomide The metabolism of Dexloxiglumide can be increased when combined with Thalidomide.
Cortisone acetate The metabolism of Dexloxiglumide can be increased when combined with Cortisone acetate.
Paramethasone The metabolism of Dexloxiglumide can be increased when combined with Paramethasone.
Armodafinil The metabolism of Dexloxiglumide can be increased when combined with Armodafinil.
Fluprednidene The metabolism of Dexloxiglumide can be increased when combined with Fluprednidene.
Meprednisone The metabolism of Dexloxiglumide can be increased when combined with Meprednisone.
Dexamethasone isonicotinate The metabolism of Dexloxiglumide can be increased when combined with Dexamethasone isonicotinate.
Cortivazol The metabolism of Dexloxiglumide can be increased when combined with Cortivazol.
Prednylidene The metabolism of Dexloxiglumide can be increased when combined with Prednylidene.
Cloprednol The metabolism of Dexloxiglumide can be increased when combined with Cloprednol.
Mometasone furoate The metabolism of Dexloxiglumide can be increased when combined with Mometasone furoate.
Prednisolone phosphate The metabolism of Dexloxiglumide can be increased when combined with Prednisolone phosphate.
Prednisolone hemisuccinate The metabolism of Dexloxiglumide can be increased when combined with Prednisolone hemisuccinate.
Prednisone acetate The metabolism of Dexloxiglumide can be increased when combined with Prednisone acetate.
Clocortolone acetate The metabolism of Dexloxiglumide can be increased when combined with Clocortolone acetate.
Melengestrol acetate The metabolism of Dexloxiglumide can be increased when combined with Melengestrol acetate.
Betamethasone phosphate The metabolism of Dexloxiglumide can be increased when combined with Betamethasone phosphate.
Cortisone The metabolism of Dexloxiglumide can be increased when combined with Cortisone.
Clobetasol propionate The metabolism of Dexloxiglumide can be increased when combined with Clobetasol propionate.
Fluocinonide The metabolism of Dexloxiglumide can be increased when combined with Fluocinonide.
Mometasone The metabolism of Dexloxiglumide can be increased when combined with Mometasone.
Fluocortolone The metabolism of Dexloxiglumide can be increased when combined with Fluocortolone.
Difluocortolone The metabolism of Dexloxiglumide can be increased when combined with Difluocortolone.
Betamethasone The metabolism of Dexloxiglumide can be increased when combined with Betamethasone.
Lidocaine The metabolism of Dexloxiglumide can be decreased when combined with Lidocaine.
Gefitinib The metabolism of Dexloxiglumide can be decreased when combined with Gefitinib.
Levonorgestrel The metabolism of Dexloxiglumide can be decreased when combined with Levonorgestrel.
Nisoldipine The metabolism of Dexloxiglumide can be decreased when combined with Nisoldipine.
Cerivastatin The metabolism of Dexloxiglumide can be decreased when combined with Cerivastatin.
Buspirone The metabolism of Dexloxiglumide can be decreased when combined with Buspirone.
Oxycodone The metabolism of Dexloxiglumide can be decreased when combined with Oxycodone.
Flutamide The metabolism of Dexloxiglumide can be decreased when combined with Flutamide.
Lercanidipine The metabolism of Dexloxiglumide can be decreased when combined with Lercanidipine.
Propranolol The metabolism of Dexloxiglumide can be decreased when combined with Propranolol.
Cisapride The metabolism of Dexloxiglumide can be decreased when combined with Cisapride.
Chloroquine The metabolism of Dexloxiglumide can be decreased when combined with Chloroquine.
Simvastatin The metabolism of Dexloxiglumide can be decreased when combined with Simvastatin.
Trazodone The metabolism of Dexloxiglumide can be decreased when combined with Trazodone.
Midazolam The metabolism of Dexloxiglumide can be decreased when combined with Midazolam.
Mycophenolate mofetil The metabolism of Dexloxiglumide can be decreased when combined with Mycophenolate mofetil.
Eplerenone The metabolism of Dexloxiglumide can be decreased when combined with Eplerenone.
Norethisterone The metabolism of Dexloxiglumide can be decreased when combined with Norethisterone.
Risperidone The metabolism of Dexloxiglumide can be decreased when combined with Risperidone.
Pentamidine The metabolism of Dexloxiglumide can be decreased when combined with Pentamidine.
Hydrocortisone The metabolism of Dexloxiglumide can be decreased when combined with Hydrocortisone.
Irinotecan The metabolism of Dexloxiglumide can be decreased when combined with Irinotecan.
Disulfiram The metabolism of Dexloxiglumide can be decreased when combined with Disulfiram.
Mifepristone The metabolism of Dexloxiglumide can be decreased when combined with Mifepristone.
Vardenafil The metabolism of Vardenafil can be decreased when combined with Dexloxiglumide.
Triazolam The metabolism of Dexloxiglumide can be decreased when combined with Triazolam.
Zonisamide The metabolism of Dexloxiglumide can be decreased when combined with Zonisamide.
Metronidazole The metabolism of Dexloxiglumide can be decreased when combined with Metronidazole.
Salmeterol The metabolism of Dexloxiglumide can be decreased when combined with Salmeterol.
Zaleplon The metabolism of Dexloxiglumide can be decreased when combined with Zaleplon.
Felodipine The metabolism of Dexloxiglumide can be decreased when combined with Felodipine.
Nitrendipine The metabolism of Dexloxiglumide can be decreased when combined with Nitrendipine.
Praziquantel The metabolism of Dexloxiglumide can be decreased when combined with Praziquantel.
Oxybutynin The metabolism of Dexloxiglumide can be decreased when combined with Oxybutynin.
Atorvastatin The metabolism of Dexloxiglumide can be decreased when combined with Atorvastatin.
Quinacrine The metabolism of Dexloxiglumide can be decreased when combined with Quinacrine.
Chlorpheniramine The metabolism of Dexloxiglumide can be decreased when combined with Chlorpheniramine.
Nifedipine The metabolism of Dexloxiglumide can be decreased when combined with Nifedipine.

Target Protein

Gastrin/cholecystokinin type B receptor CCKBR
Cholecystokinin receptor type A CCKAR

Referensi & Sumber

Artikel (PubMed)
  • PMID: 17112294
    Persiani S, D'Amato M, Jakate A, Roy P, Wangsa J, Kapil R, Rovati LC: Pharmacokinetic profile of dexloxiglumide. Clin Pharmacokinet. 2006;45(12):1177-88.
  • PMID: 16484960
    Maselli MA, Mennuni L: CCK1 receptor antagonist, dexloxiglumide: effects on human isolated gallbladder. Potential clinical applications. Minerva Gastroenterol Dietol. 2003 Sep;49(3):211-6.

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