Absorption, distribution, metabolism, and excretion of radiolabeled naldemedine in healthy subjects

@article{Ohnishi2019AbsorptionDM,
  title={Absorption, distribution, metabolism, and excretion of radiolabeled naldemedine in healthy subjects},
  author={Shuichi Ohnishi and Kazuya Fukumura and Ryuji Kubota and Toshihiro Wajima},
  journal={Xenobiotica},
  year={2019},
  volume={49},
  pages={1044 - 1053}
}
Abstract 1. Naldemedine is a peripherally acting μ-opioid receptor antagonist for the treatment of opioid-induced constipation. 2. This phase 1 study investigated the absorption, distribution, metabolism and excretion of naldemedine, following a single oral 2-mg dose of [oxadiazole-14C]-naldemedine or [carbonyl-14C]-naldemedine to 12 healthy adult male subjects. Pharmacokinetic assessments were performed on blood, urine and fecal samples collected at defined intervals. 3. Naldemedine was the… 
5 Citations
The Influence of Renal or Hepatic Impairment on the Pharmacokinetics, Safety, and Tolerability of Naldemedine
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Investigation of the pharmacokinetics and safety of a 0.2‐mg oral dose of naldemedine in subjects with renal impairment or hepatic impairment found it to be well tolerated, and reported adverse events were generally consistent with the known safety profile.
Clinical Drug-Drug Interaction Studies to Evaluate the Effects of a P-Glycoprotein Inhibitor, CYP3A Inhibitors, and a CYP3A Inducer on the Pharmacokinetics of Naldemedine in Healthy Subjects
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Coadministration of naldemedine with a P-glycoprotein inhibitor or a strong/moderate CYP3A inhibitor increases naldemsine exposure; coadministration with a strong CYP 3A inducer decreases its exposure.
Naldemedine for the Use of Management of Opioid Induced Constipation.
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Naldemedine is an FDA-approved, once-daily oral tablet that counteracts this side effect of opioid-induced constipation by antagonizing mu, kappa, and delta-opioid receptors and has been shown to be safe and effective.
Naldemedine: A New Option for OIBD
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The available data suggest that naldemedine is a valid treatment option for OIBD, as it is a well-tolerated drug that alleviates constipation without affecting analgesia or causing symptoms of opioid withdrawal.
Opioid-Induced Constipation in Oncological Patients: New Strategies of Management
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Traditional recommended therapies are appraised and compared with the latest pharmacological developments, and whether naloxegol is more efficacious by its comparison directly with first-line treatments, including laxatives is addressed.

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