Naloxegol

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Naloxegol
Naloxegol.svg
Systematic (IUPAC) name
(5α,6α)-17-Allyl-6-[(20-hydroxy-3,6,9,12,15,18-hexaoxaicos-1-yl)oxy]-4,5-epoxymorphinan-3,14-diol
Clinical data
Trade names Movantik
AHFS/Drugs.com entry
Licence data US FDA:link
Pregnancy
category
  • US: C (Risk not ruled out)
Legal status
  • US: Unscheduled
Routes of
administration
Oral
Pharmacokinetic data
Protein binding ~4.2%
Metabolism Hepatic (CYP3A)
Biological half-life 6–11 h
Excretion Feces (68%), urine (16%)
Identifiers
CAS Registry Number 854601-70-0
ATC code A06AH03
PubChem CID: 56959087
ChemSpider 28651656
ChEBI CHEBI:82975
Chemical data
Formula C34H53NO11
Molecular mass 651.785

Naloxegol (INN; NKTR-118), or PEGylated naloxol,[1] trade name Movantik, is a peripherally-selective opioid antagonist developed by AstraZeneca, licensed from Nektar, for the treatment of opioid-induced constipation.[2] It was approved in 2014 in adult patients with chronic, non-cancer pain.[3] Doses of 25 mg were found safe and well tolerated for 52 weeks.[4] Adverse gastrointestinal reactions increased in methadone patients and were sometimes severe.

Naloxegol was previously a schedule 2 drug because of its chemical similarity to opium alkaloids. It was recently reclassified as a legend drug after the FDA concluded that it was not habit-forming.

See also[edit]

References[edit]

  1. ^ Roland Seifert; Thomas Wieland; Raimund Mannhold; Hugo Kubinyi; Gerd Folkers (17 July 2006). G Protein-Coupled Receptors as Drug Targets: Analysis of Activation and Constitutive Activity. John Wiley & Sons. p. 227. ISBN 978-3-527-60695-5. Retrieved 14 May 2012. 
  2. ^ "Nektar | R&D Pipeline | Products in Development | CNS/Pain | Oral Naloxegol (NKTR-118) and Oral NKTR-119". Retrieved 2012-05-14. 
  3. ^ "FDA approves MOVANTIK™ (naloxegol) Tablets C-II for the treatment of opioid-induced constipation in adult patients with chronic non-cancer pain". 16 September 2014. 
  4. ^ "Randomised clinical trial: the long-term safety and tolerability of naloxegol in patients with pain and opioid-induced constipation.". Aliment Pharmacol Ther. Oct 2014. PMID 25112584.