naloxegol 🐶 Veterinary Use | 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: -0.18
  • LIPINSKI: 2
  • HAC: 12
  • HDO: 2
  • TPSA: 126.77
  • ALOGS: -4.06
  • ROTB: 24

  • Status: ONP

  • 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 196.80 24.24 62 2231 27132 63459597
Withdrawal syndrome 97.93 24.24 34 2259 19963 63466766
Abdominal pain 79.33 24.24 73 2220 293383 63193346
Hyperhidrosis 64.50 24.24 43 2250 107793 63378936
Drug screen positive 51.57 24.24 14 2279 3615 63483114
Diarrhoea 39.24 24.24 82 2211 715284 62771445
Chills 38.06 24.24 32 2261 113346 63373383
Nausea 29.58 24.24 82 2211 854389 62632340
Intentional product misuse 28.65 24.24 21 2272 60896 63425833
Pain 26.50 24.24 72 2221 740556 62746173
Vomiting 24.75 24.24 59 2234 559558 62927171

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 85.31 29.11 31 1298 19803 34935799
Withdrawal syndrome 51.75 29.11 19 1310 12436 34943166
Abdominal pain 44.92 29.11 42 1287 163576 34792026
Hyperhidrosis 43.48 29.11 30 1299 75662 34879940
Pain 38.76 29.11 43 1286 204632 34750970
Agranulocytosis 36.83 29.11 18 1311 23803 34931799

FDA Adverse Event Reporting System (Geriatric)

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 140.21 23.17 50 2592 34668 79707078
Withdrawal syndrome 69.60 23.17 28 2614 26826 79714920
Abdominal pain 61.88 23.17 70 2572 389499 79352247
Hyperhidrosis 52.51 23.17 42 2600 151450 79590296
Nausea 36.25 23.17 90 2552 957106 78784640
Diarrhoea 34.59 23.17 84 2558 880405 78861341
Pain 32.95 23.17 72 2570 703730 79038016
Vomiting 28.76 23.17 66 2576 665762 79075984
Agranulocytosis 28.37 23.17 18 2624 45012 79696734

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC A06AH03 ALIMENTARY TRACT AND METABOLISM
DRUGS FOR CONSTIPATION
DRUGS FOR CONSTIPATION
Peripheral opioid receptor antagonists
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
FDA MoA N0000000154 Opioid Antagonists
CHEBI has role CHEBI:35488 central nervous system depressants
CHEBI has role CHEBI:50137 mu-opioid receptor antagonists
CHEBI has role CHEBI:90755 antidote to opioid overdose
FDA EPC N0000175691 Opioid Antagonist
CHEBI has role CHEBI:75325 cathartics

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Therapeutic opioid induced constipation indication 136801000119102




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

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)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 12.5MG BASE MOVANTIK VALINOR N204760 Sept. 16, 2014 RX TABLET ORAL 7056500 June 29, 2024 TREATMENT OF OPIOID-INDUCED CONSTIPATION
EQ 25MG BASE MOVANTIK VALINOR N204760 Sept. 16, 2014 RX TABLET ORAL 7056500 June 29, 2024 TREATMENT OF OPIOID-INDUCED CONSTIPATION
EQ 12.5MG BASE MOVANTIK VALINOR N204760 Sept. 16, 2014 RX TABLET ORAL 8067431 Dec. 16, 2024 TREATMENT OF OPIOID-INDUCED CONSTIPATION
EQ 25MG BASE MOVANTIK VALINOR N204760 Sept. 16, 2014 RX TABLET ORAL 8067431 Dec. 16, 2024 TREATMENT OF OPIOID-INDUCED CONSTIPATION

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
44T7335BKE UNII
D10375 KEGG_DRUG
1354744-91-4 SECONDARY_CAS_RN
4019852 VANDF
4034135 VANDF
C3700399 UMLSCUI
CHEBI:82975 CHEBI
CHEBI:7459 CHEBI
CHEMBL2219418 ChEMBL_ID
56959087 PUBCHEM_CID
DB09049 DRUGBANK_ID
CHEMBL2219416 ChEMBL_ID
9434 INN_ID
C000589308 MESH_SUPPLEMENTAL_RECORD_UI
7539 IUPHAR_LIGAND_ID
1551777 RXNORM
228769 MMSL
27364 MMSL
30568 MMSL
31169 MMSL
d00311 MMSL
d08289 MMSL
004661 NDDF
015863 NDDF
015864 NDDF
372890007 SNOMEDCT_US
719411008 SNOMEDCT_US
719412001 SNOMEDCT_US
763564001 SNOMEDCT_US
89018006 SNOMEDCT_US
C0027358 UMLSCUI
DB01183 DRUGBANK_ID
1526 INN_ID
D009270 MESH_DESCRIPTOR_UI
5284596 PUBCHEM_CID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
MOVANTIK HUMAN PRESCRIPTION DRUG LABEL 1 0310-1969 TABLET, FILM COATED 12.50 mg ORAL NDA 26 sections
MOVANTIK HUMAN PRESCRIPTION DRUG LABEL 1 0310-1970 TABLET, FILM COATED 25 mg ORAL NDA 26 sections
MOVANTIK HUMAN PRESCRIPTION DRUG LABEL 1 55700-383 TABLET, FILM COATED 25 mg ORAL NDA 27 sections
MOVANTIK HUMAN PRESCRIPTION DRUG LABEL 1 55700-988 TABLET, FILM COATED 25 mg ORAL NDA 26 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 57841-1300 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
MOVANTIK HUMAN PRESCRIPTION DRUG LABEL 1 57841-1301 TABLET, FILM COATED 25 mg ORAL NDA 26 sections
MOVANTIK HUMAN PRESCRIPTION DRUG LABEL 1 82625-8801 TABLET, FILM COATED 12.50 mg ORAL NDA 26 sections
MOVANTIK HUMAN PRESCRIPTION DRUG LABEL 1 82625-8802 TABLET, FILM COATED 25 mg ORAL NDA 26 sections