naloxegol Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
opioid receptor antagonists/agonists related to normorphine 4832 854601-70-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • moventig
  • naloxegol oxalate
  • movantik
  • naloxegol
  • NKTR-118
A peripherally acting opioid receptor antagonist specific for mu-opioid receptors. Used to decrease the constipating effects of opioids.
  • Molecular weight: 651.79
  • Formula: C34H53NO11
  • CLOGP: 0.16
  • LIPINSKI: 2
  • HAC: 12
  • HDO: 2
  • TPSA: 126.77
  • ALOGS: -4.06
  • ROTB: 24

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
25 mg O

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Sept. 25, 2014 EMA
Sept. 16, 2014 FDA ASTRAZENECA PHARMS

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Drug withdrawal syndrome 196.02 27.24 62 1642 27322 46657036
Withdrawal syndrome 89.18 27.24 31 1673 18103 46666255
Abdominal pain 75.31 27.24 64 1640 229967 46454391
Hyperhidrosis 63.95 27.24 40 1664 89268 46595090
Constipation 53.89 27.24 47 1657 174050 46510308
Drug screen positive 50.47 27.24 14 1690 3877 46680481
Chills 42.51 27.24 32 1672 96000 46588358
Diarrhoea 41.24 27.24 73 1631 559529 46124829
Pain 34.76 27.24 62 1642 476886 46207472
Intentional product misuse 30.89 27.24 20 1684 47108 46637250
Nausea 27.52 27.24 70 1634 687384 45996974

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Drug withdrawal syndrome 86.29 34.63 30 945 19779 29931724
Withdrawal syndrome 52.64 34.63 18 957 11232 29940271
Hyperhidrosis 48.56 34.63 29 946 67061 29884442
Abdominal pain 46.62 34.63 37 938 135617 29815886
Constipation 45.80 34.63 34 941 112872 29838631
Pain 44.74 34.63 40 935 172601 29778902

Pharmacologic Action:

SourceCodeDescription
ATC A06AH03 ALIMENTARY TRACT AND METABOLISM
DRUGS FOR CONSTIPATION
DRUGS FOR CONSTIPATION
Peripheral opioid receptor antagonists
FDA MoA N0000000154 Opioid Antagonists
FDA EPC N0000175691 Opioid Antagonist
MeSH PA D002491 Central Nervous System Agents
MeSH PA D009292 Narcotic Antagonists
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D018689 Sensory System Agents
CHEBI has role CHEBI:50137 mu-opioid receptor antagonists
CHEBI has role CHEBI:75325 cathartics

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Therapeutic opioid induced constipation indication 136801000119102

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.69 acidic
pKa2 8.06 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Mu-type opioid receptor GPCR ANTAGONIST DRUG LABEL DRUG LABEL

External reference:

IDSource
D10375 KEGG_DRUG
1354744-91-4 SECONDARY_CAS_RN
4034135 VANDF
C3858036 UMLSCUI
CHEBI:82975 CHEBI
CHEMBL2219416 ChEMBL_ID
CHEMBL2219418 ChEMBL_ID
DB09049 DRUGBANK_ID
C000589308 MESH_SUPPLEMENTAL_RECORD_UI
7539 IUPHAR_LIGAND_ID
9434 INN_ID
44T7335BKE UNII
56959087 PUBCHEM_CID
1551777 RXNORM
228769 MMSL
30568 MMSL
31169 MMSL
d08289 MMSL
015863 NDDF
015864 NDDF
719411008 SNOMEDCT_US
719412001 SNOMEDCT_US
763564001 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
MOVANTIK HUMAN PRESCRIPTION DRUG LABEL 1 55700-383 TABLET, FILM COATED 25 mg ORAL NDA 27 sections
MOVANTIK HUMAN PRESCRIPTION DRUG LABEL 1 57841-1300 TABLET, FILM COATED 12.50 mg ORAL NDA 26 sections
MOVANTIK HUMAN PRESCRIPTION DRUG LABEL 1 57841-1301 TABLET, FILM COATED 25 mg ORAL NDA 26 sections