Discovery of naldemedine: A potent and orally available opioid receptor antagonist for treatment of opioid-induced adverse effects.

Author: GotoYoshihisa, HagaNobuhiro, HaraShinichiro, HasegawaTsuyoshi, InagakiMasanao, KaiHiroyuki, KanemasaToshiyuki, KoikeKatsumi, KumeMasaharu, NakamuraTakashi, OonishiShuuichi, TamuraYoshinori

Paper Details 
Original Abstract of the Article :
Structure-activity relationship studies of several morphinan derivatives were conducted to obtain dual antagonists for μ- and δ-opioid receptors. We discovered peripherally restricted dual antagonists for μ/δ-opioid receptors as a new chemotype with a morphinan scaffold, which are orally available a...See full text at original site
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引用元:
https://doi.org/10.1016/j.bmcl.2018.11.007

データ提供:米国国立医学図書館(NLM)

A New Weapon in the Fight Against Opioid-Induced Side Effects

Opioids are powerful pain relievers, but they can also cause unpleasant side effects such as constipation and vomiting. This study focuses on the discovery of naldemedine, a potent and orally available opioid receptor antagonist, for the treatment of opioid-induced adverse effects. The authors describe the development of naldemedine as a potential drug candidate, highlighting its unique properties and potential benefits for patients.

Targeting the Roots of Opioid Side Effects

The study emphasizes the importance of developing new therapies to manage the side effects of opioid medications. Naldemedine, a peripherally restricted dual antagonist for μ/δ-opioid receptors, offers a promising solution for reducing opioid-induced constipation and emesis/vomiting without interfering with the analgesic effects of morphine. This research highlights the potential of targeted therapies to improve patient outcomes and enhance the overall benefits of opioid pain management.

Improving Opioid Safety and Efficacy

This study offers a new tool in the arsenal for managing opioid-induced side effects. Naldemedine, with its unique properties and targeted action, holds the promise of improving patient outcomes and enhancing the safety and efficacy of opioid pain management. This research encourages further investigation into the potential of naldemedine as a valuable treatment option for patients experiencing opioid-induced adverse effects.

Dr.Camel's Conclusion

This study showcases the power of scientific innovation in addressing the challenges associated with opioid pain management. Naldemedine, a novel drug with a targeted mechanism of action, holds the promise of reducing opioid-induced side effects and improving patient outcomes. This research is a testament to the ongoing efforts to develop safer and more effective pain management strategies.

Date :
  1. Date Completed 2019-11-04
  2. Date Revised 2022-08-16
Further Info :

Pubmed ID

30446313

DOI: Digital Object Identifier

10.1016/j.bmcl.2018.11.007

Related Literature

SNS
PICO Info
in preparation
Languages

English

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