Naloxegol

DB09049

small molecule approved

Deskripsi

Naloxegol, for "PEGylated naloxol" is a peripherally-selective opioid antagonist developed by AstraZeneca. It was approved by the FDA in September 2014 and is indicated for the treatment of opioid-induced constipation (OIC) in adult patients with chronic non?cancer pain. The advantage of naloxegol over the opioid antagonist naloxone is that its PEGylated structure allows for high selectivity for peripheral opioid receptors and lack of entry into the central nervous system through the blood-brain barrier.

Struktur Molekul 2D

Berat 651.794
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 6-11 hours.
Volume Distribusi 968 to 2140 L.
Klirens (Clearance) Feces (68%), urine (16%).

Absorpsi

Following oral administration, naloxegol is absorbed with peak concentrations (Cmax) achieved in less than 2 hours.

Metabolisme

Naloxegol is metabolized primarily by the CYP P450 3A4 enzyme system and undergoes enterohepatic recycling. In a mass balance study in humans, a total of 6 metabolites were identified in plasma, urine and feces. These metabolites were formed via N-dealkylation, O-demethylation, oxidation and partial loss of the PEG chain. Human metabolism data suggests absence of major metabolites. The activity of the metabolites at the opioid receptor has not been determined.

Rute Eliminasi

Feces: 68% after oral administration. Urine: 16% after oral administration.

Interaksi Makanan

1 Data
  • 1. Take on an empty stomach. High-fat food increases drug absorption. Take naloxegol at least 1 hour prior to the first meal of the day or 2 hours after the meal.

Interaksi Obat

680 Data
Fluconazole The serum concentration of Naloxegol can be increased when it is combined with Fluconazole.
Erythromycin The serum concentration of Naloxegol can be increased when it is combined with Erythromycin.
Sildenafil The serum concentration of Naloxegol can be increased when it is combined with Sildenafil.
Reserpine The serum concentration of Naloxegol can be increased when it is combined with Reserpine.
Ranolazine The serum concentration of Naloxegol can be increased when it is combined with Ranolazine.
Sorafenib The serum concentration of Naloxegol can be increased when it is combined with Sorafenib.
Loxapine The serum concentration of Naloxegol can be increased when it is combined with Loxapine.
Quinine The serum concentration of Naloxegol can be increased when it is combined with Quinine.
Ritonavir The serum concentration of Naloxegol can be increased when it is combined with Ritonavir.
Toremifene The serum concentration of Naloxegol can be increased when it is combined with Toremifene.
Simvastatin The serum concentration of Naloxegol can be increased when it is combined with Simvastatin.
Verapamil The serum concentration of Naloxegol can be increased when it is combined with Verapamil.
Tamoxifen The serum concentration of Naloxegol can be increased when it is combined with Tamoxifen.
Mifepristone The serum concentration of Naloxegol can be increased when it is combined with Mifepristone.
Vardenafil The serum concentration of Naloxegol can be increased when it is combined with Vardenafil.
Tacrolimus The serum concentration of Naloxegol can be increased when it is combined with Tacrolimus.
Conivaptan The serum concentration of Naloxegol can be increased when it is combined with Conivaptan.
Quinidine The serum concentration of Naloxegol can be increased when it is combined with Quinidine.
Zonisamide The serum concentration of Naloxegol can be increased when it is combined with Zonisamide.
Tipranavir The serum concentration of Naloxegol can be increased when it is combined with Tipranavir.
Ketoconazole The serum concentration of Naloxegol can be increased when it is combined with Ketoconazole.
Amiodarone The serum concentration of Naloxegol can be increased when it is combined with Amiodarone.
Carvedilol The serum concentration of Naloxegol can be increased when it is combined with Carvedilol.
Itraconazole The serum concentration of Naloxegol can be increased when it is combined with Itraconazole.
Propafenone The serum concentration of Naloxegol can be increased when it is combined with Propafenone.
Clarithromycin The serum concentration of Naloxegol can be increased when it is combined with Clarithromycin.
Saquinavir The serum concentration of Naloxegol can be increased when it is combined with Saquinavir.
Lapatinib The serum concentration of Naloxegol can be increased when it is combined with Lapatinib.
Paliperidone The serum concentration of Naloxegol can be increased when it is combined with Paliperidone.
Mibefradil The serum concentration of Naloxegol can be increased when it is combined with Mibefradil.
Lopinavir The serum concentration of Naloxegol can be increased when it is combined with Lopinavir.
Biricodar The serum concentration of Naloxegol can be increased when it is combined with Biricodar.
Dronedarone The serum concentration of Naloxegol can be increased when it is combined with Dronedarone.
Nilotinib The serum concentration of Naloxegol can be increased when it is combined with Nilotinib.
Elacridar The serum concentration of Naloxegol can be increased when it is combined with Elacridar.
Flibanserin The serum concentration of Naloxegol can be increased when it is combined with Flibanserin.
Vandetanib The serum concentration of Naloxegol can be increased when it is combined with Vandetanib.
Telaprevir The serum concentration of Naloxegol can be increased when it is combined with Telaprevir.
Zosuquidar The serum concentration of Naloxegol can be increased when it is combined with Zosuquidar.
Tariquidar The serum concentration of Naloxegol can be increased when it is combined with Tariquidar.
Temsirolimus The serum concentration of Naloxegol can be increased when it is combined with Temsirolimus.
Simeprevir The serum concentration of Naloxegol can be increased when it is combined with Simeprevir.
Isavuconazonium The serum concentration of Naloxegol can be increased when it is combined with Isavuconazonium.
Brefeldin A The serum concentration of Naloxegol can be increased when it is combined with Brefeldin A.
Ticagrelor The serum concentration of Naloxegol can be increased when it is combined with Ticagrelor.
Ivacaftor The serum concentration of Naloxegol can be increased when it is combined with Ivacaftor.
Lomitapide The serum concentration of Naloxegol can be increased when it is combined with Lomitapide.
Crizotinib The serum concentration of Naloxegol can be increased when it is combined with Crizotinib.
Vemurafenib The serum concentration of Naloxegol can be increased when it is combined with Vemurafenib.
Linagliptin The serum concentration of Naloxegol can be increased when it is combined with Linagliptin.
Mirabegron The serum concentration of Naloxegol can be increased when it is combined with Mirabegron.
Regorafenib The serum concentration of Naloxegol can be increased when it is combined with Regorafenib.
Enzalutamide The serum concentration of Naloxegol can be decreased when it is combined with Enzalutamide.
Ponatinib The serum concentration of Naloxegol can be increased when it is combined with Ponatinib.
Canagliflozin The serum concentration of Naloxegol can be increased when it is combined with Canagliflozin.
Afatinib The serum concentration of Naloxegol can be increased when it is combined with Afatinib.
Ledipasvir The serum concentration of Naloxegol can be increased when it is combined with Ledipasvir.
Vorapaxar The serum concentration of Naloxegol can be increased when it is combined with Vorapaxar.
Suvorexant The serum concentration of Naloxegol can be increased when it is combined with Suvorexant.
Netupitant The serum concentration of Naloxegol can be increased when it is combined with Netupitant.
Cobicistat The serum concentration of Naloxegol can be increased when it is combined with Cobicistat.
Palbociclib The serum concentration of Naloxegol can be increased when it is combined with Palbociclib.
Daclatasvir The serum concentration of Naloxegol can be increased when it is combined with Daclatasvir.
Niguldipine The serum concentration of Naloxegol can be increased when it is combined with Niguldipine.
Lumacaftor The serum concentration of Naloxegol can be increased when it is combined with Lumacaftor.
Rolapitant The serum concentration of Naloxegol can be increased when it is combined with Rolapitant.
Venetoclax The serum concentration of Naloxegol can be increased when it is combined with Venetoclax.
Asunaprevir The serum concentration of Naloxegol can be increased when it is combined with Asunaprevir.
Velpatasvir The serum concentration of Naloxegol can be increased when it is combined with Velpatasvir.
Isavuconazole The serum concentration of Naloxegol can be increased when it is combined with Isavuconazole.
Neratinib The serum concentration of Naloxegol can be increased when it is combined with Neratinib.
Valspodar The serum concentration of Naloxegol can be increased when it is combined with Valspodar.
Dacomitinib The serum concentration of Naloxegol can be increased when it is combined with Dacomitinib.
Glasdegib The serum concentration of Naloxegol can be increased when it is combined with Glasdegib.
Voxilaprevir The serum concentration of Naloxegol can be increased when it is combined with Voxilaprevir.
Sarecycline The serum concentration of Naloxegol can be increased when it is combined with Sarecycline.
Erdafitinib The serum concentration of Naloxegol can be increased when it is combined with Erdafitinib.
Laniquidar The serum concentration of Naloxegol can be increased when it is combined with Laniquidar.
Enasidenib The serum concentration of Naloxegol can be increased when it is combined with Enasidenib.
Pibrentasvir The serum concentration of Naloxegol can be increased when it is combined with Pibrentasvir.
Glecaprevir The serum concentration of Naloxegol can be increased when it is combined with Glecaprevir.
Dexniguldipine The serum concentration of Naloxegol can be increased when it is combined with Dexniguldipine.
ONT-093 The serum concentration of Naloxegol can be increased when it is combined with ONT-093.
Ivosidenib The metabolism of Naloxegol can be increased when combined with Ivosidenib.
Norgestimate The serum concentration of Naloxegol can be increased when it is combined with Norgestimate.
Elagolix The serum concentration of Naloxegol can be increased when it is combined with Elagolix.
Entrectinib The serum concentration of Naloxegol can be increased when it is combined with Entrectinib.
Fedratinib The serum concentration of Naloxegol can be increased when it is combined with Fedratinib.
Istradefylline The serum concentration of Naloxegol can be increased when it is combined with Istradefylline.
Lasmiditan The serum concentration of Naloxegol can be increased when it is combined with Lasmiditan.
Carfilzomib The serum concentration of Naloxegol can be increased when it is combined with Carfilzomib.
Favipiravir The serum concentration of Naloxegol can be increased when it is combined with Favipiravir.
Methylene blue The serum concentration of Naloxegol can be increased when it is combined with Methylene blue.
Ripretinib The serum concentration of Naloxegol can be increased when it is combined with Ripretinib.
Pralsetinib The serum concentration of Naloxegol can be increased when it is combined with Pralsetinib.
Lonafarnib The serum concentration of Naloxegol can be increased when it is combined with Lonafarnib.
Clofazimine The serum concentration of Naloxegol can be increased when it is combined with Clofazimine.
Arsenic trioxide The serum concentration of Naloxegol can be increased when it is combined with Arsenic trioxide.
Mefloquine The serum concentration of Naloxegol can be increased when it is combined with Mefloquine.
Everolimus The serum concentration of Naloxegol can be increased when it is combined with Everolimus.

Target Protein

Mu-type opioid receptor OPRM1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 25471070
    Leonard J, Baker DE: Naloxegol: treatment for opioid-induced constipation in chronic non-cancer pain. Ann Pharmacother. 2015 Mar;49(3):360-5. doi: 10.1177/1060028014560191. Epub 2014 Dec 3.
  • PMID: 26312011
    Anantharamu T, Sharma S, Gupta AK, Dahiya N, Singh Brashier DB, Sharma AK: Naloxegol: First oral peripherally acting mu opioid receptor antagonists for opioid-induced constipation. J Pharmacol Pharmacother. 2015 Jul-Sep;6(3):188-92. doi: 10.4103/0976-500X.162015.
  • PMID: 26150678
    Jones R, Prommer E, Backstedt D: Naloxegol: A Novel Therapy in the Management of Opioid-Induced Constipation. Am J Hosp Palliat Care. 2015 Jul 6. pii: 1049909115593937.

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