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- Q15708351 subject Q52309.
- Q15708351 subject Q8376869.
- Q15708351 subject Q8702225.
- Q15708351 subject Q9056368.
- Q15708351 subject Q9134654.
- Q15708351 abstract "Naloxegol (INN; PEGylated naloxol; trade names Movantik and Moventig) is a peripherally-selective opioid antagonist developed by AstraZeneca, licensed from Nektar, for the treatment of opioid-induced constipation. It was approved in 2014 in adult patients with chronic, non-cancer pain. Doses of 25 mg were found safe and well tolerated for 52 weeks. When given concomitantly with opioid analgesics, naloxegol reduced constipation-related side effects, while maintaining comparable levels of analgesia.Chemically, naloxegol is a pegylated (polyethylene glycol-modified) derivative of α-naloxol. Specifically, the 5-α-hydroxyl group of α-naloxol is connected via an ether linkage to the free hydroxyl group of a monomethoxy-terminated n=7 oligomer of PEG, shown extending at the lower left of the molecule image at right. The "n=7" defines the number of two-carbon ethylenes, and so the chain length, of the attached PEG chain, and the "monomethoxy" indicates that the terminal hydroxyl group of the PEG is "capped" with a methyl group. The pegylation of the 5-α-hydroxyl side chain of naloxol prevents the drug from crossing the blood-brain barrier (BBB). As such, it can be considered the antithesis of the peripherally-acting opiate loperamide which is utilized as an opiate-targeting anti-diarrheal agent that does not cause traditional opiate side-effects due to its inability to accumulate in the central nervous system in normal subjects. Naloxegol was previously a Schedule II drug in the United States because of its chemical similarity to opium alkaloids, but was recently reclassified as a prescription drug after the FDA concluded that the impermeability of the blood-brain barrier to this compound made it non-habit-forming, and so without the potential for abuse -- specifically, naloxegol was officially decontrolled on 23. January 2015. As an opiate antagonist, it is not expected to be capable of inducing the euphoria and anxiolytic effects which are generally cited as the desirable effects of commonly abused opiates (all of which are opiate agonists) if it were to cross the BBB; it would in fact reverse the effects of opiate drugs of abuse if it entered the central nervous system.".
- Q15708351 atcPrefix "A06".
- Q15708351 atcSuffix "AH03".
- Q15708351 casNumber "854601-70-0".
- Q15708351 chEBI "82975".
- Q15708351 iupacName "(5α,6α)-4,5-epoxy-6-(3,6,9,12,15,18,21-heptaoxadocos-1-yloxy)-17-(2-propen-1-yl)morphinan-3,14-diol".
- Q15708351 pubchem "56959087".
- Q15708351 thumbnail Naloxegol.svg?width=300.
- Q15708351 wikiPageWikiLink Q103230.
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- Q15708351 wikiPageWikiLink Q410083.
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- Q15708351 wikiPageWikiLink Q4914025.
- Q15708351 wikiPageWikiLink Q5014970.
- Q15708351 wikiPageWikiLink Q52309.
- Q15708351 wikiPageWikiLink Q62903.
- Q15708351 wikiPageWikiLink Q682252.
- Q15708351 wikiPageWikiLink Q6960846.
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- Q15708351 wikiPageWikiLink Q824258.
- Q15708351 wikiPageWikiLink Q8376869.
- Q15708351 wikiPageWikiLink Q866317.
- Q15708351 wikiPageWikiLink Q8702225.
- Q15708351 wikiPageWikiLink Q898317.
- Q15708351 wikiPageWikiLink Q9056368.
- Q15708351 wikiPageWikiLink Q908096.
- Q15708351 wikiPageWikiLink Q9134654.
- Q15708351 wikiPageWikiLink Q928770.
- Q15708351 atcPrefix "A06".
- Q15708351 atcSuffix "AH03".
- Q15708351 casNumber "854601".
- Q15708351 chebi "82975".
- Q15708351 iupacName "-45".
- Q15708351 pubchem "56959087".
- Q15708351 type ChemicalSubstance.
- Q15708351 type Drug.
- Q15708351 type ChemicalObject.
- Q15708351 type Thing.
- Q15708351 type Q8386.
- Q15708351 comment "Naloxegol (INN; PEGylated naloxol; trade names Movantik and Moventig) is a peripherally-selective opioid antagonist developed by AstraZeneca, licensed from Nektar, for the treatment of opioid-induced constipation. It was approved in 2014 in adult patients with chronic, non-cancer pain. Doses of 25 mg were found safe and well tolerated for 52 weeks.".
- Q15708351 label "Naloxegol".
- Q15708351 depiction Naloxegol.svg.