General
Preferred name
naloxegol
Synonyms
NALOXEGOL OXALATE ()
AZ-13337019 ()
AZ 13337019 oxalate ()
NKTR-118 oxalate ()
AZ-13337019 oxalate ()
NKTR118 oxalate ()
Movantik ()
Naloxegol (oxalate) ()
NKTR-118 (oxalate) ()
AZ-13337019 (oxalate) ()
NKTR-118-OXALATE ()
Naloxegol oxalate component of movantik ()
Moventig ()
AZ13337019 oxalate ()
NKTR-118 ()
P&D ID
PD009390
CAS
854601-70-0
1354744-91-4
Tags
available
drug
Approved by
EMA
FDA
First approval
2014
Drug indication
Constipation
Opioid-induced constipation
Pain
Drug Status
approved
Max Phase
4.0
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION
Naloxegol oxalate (NKTR-118 oxalate; AZ-13337019 oxalate) is a ¦Ì-opioid-receptor antagonist. Naloxegol oxalate inhibits opioid binding in ¦Ì-opioid receptors in the gastrointestinal tract and effective for alleviating opioid-induced constipation[1][2].
PRICE
67
ROE
Feces: 68% after oral administration.; Urine: 16% after oral administration.
DESCRIPTION
Naloxegol is a PEGylated version of naloxol (α-naloxol PubChem CID 5492271; β-naloxol PubChem CID 5492293). PEGylation reduces the compound's ability to cross the blood-brain barrier, therefore restricting CNS penetration. Naloxegol is termed a peripherally acting μ-opioid receptor antagonist, or PAMORA. The synonyms suffixed with "oxalate " map to the salt as PubChem CID 56959086
(GtoPdb)
DESCRIPTION
Naloxegol oxalate (NKTR-118) is a peripherally-selective opioid antagonist for the treatment of opioid-induced constipation.
(TargetMol Bioactive Compound Library)
DESCRIPTION
Naloxegol is a CYP3A4 enzyme inhibitor. It is also a peripherally-selective opioid antagonist. It is used as the treatment of opioid-induced constipation. lt is a pegylated (polyethylene glycol-modified) derivative of α-naloxol and can be used to reduce opioid-induced symptoms. lt binds to and blocks mu-opioid receptors in the peripheral nervous system. It would reverse the effects of opiate drugs of abuse if it entered the central nervous system. It was approved in 2014 in adult patients with chronic, non-cancer pain. lt was developed by AstraZeneca, licensed from Nektar Therapeutics. It was approved in 2014 in adult patients with chronic, non-cancer pain. It has been listed.
(BOC Sciences Bioactive Compounds)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Compound Sets
18
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
ChEMBL Approved Drugs
ChEMBL Drugs
Drug Repurposing Hub
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
DrugMAP
DrugMAP Approved Drugs
Guide to Pharmacology
MedChem Express Bioactive Compound Library
Natural product-based probes and drugs
NCATS Inxight Approved Drugs
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
40
Molecular Weight
651.36
Hydrogen Bond Acceptors
12
Hydrogen Bond Donors
2
Rotatable Bonds
24
Ring Count
5
Aromatic Ring Count
1
cLogP
1.86
TPSA
126.77
Fraction CSP3
0.76
Chiral centers
5.0
Largest ring
6.0
QED
0.13
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
Opioid Receptor
CYP3A
OPRM1
Pathway
GPCR/G protein
Neuronal Signaling
Metabolism
Indication
constipation
MOA
Opioid Receptor antagonist
Biosynthetic Origin
Alkaloid
Therapeutic Indication
Opioid Induced Constipation
Therapeutic Class
CNS & PNS
Solubility
10 mM in DMSO
Source data
