naloxegol + ketoconazole

naloxegol + ketoconazole is an *unbranded combination* of naloxegol (NKTR-118), a peripherally acting mu-opioid receptor antagonist, and ketoconazole, a strong CYP3A4 and P-glycoprotein (P-gp) inhibitor. Naloxegol (developed as NKTR-118) is indicated for opioid-induced constipation and works by blocking opioid action in the gut without affecting central analgesia. Ketoconazole, an antifungal agent, is not used therapeutically in direct combination with naloxegol, but is clinically important due to its drug-drug interaction; when co-administered, ketoconazole dramatically increases plasma concentrations of naloxegol by inhibiting its metabolism (up to approximately 13-fold increase in exposure), increasing the risk of adverse effects. The combination is contraindicated because of this potentiation, and such coadministration is not recommended due to safety concerns, including significant risk of QTc prolongation and increased naloxegol toxicity[1][7].

Brand names

Movantik

Other names

naloxegol oxalateketoconazole (no unique brand for the combo)