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naloxegol 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| opioid receptor antagonists/agonists related to normorphine | 4832 | 854601-70-0 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A peripherally acting opioid receptor antagonist specific for mu-opioid receptors. Used to decrease the constipating effects of opioids.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 25 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BA (Bioavailability) | 2 % |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 0.536 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 25.003 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 1.384 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 7.674 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 56.920 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 77.740 | % | High | 1 |
| herg | hERG pIC50 | 4.446 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 1.762 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 38.548 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 64.320 | % | High | 1 |
| kinase-safety-class | ACVR2B,AXL,BRAF,BTK,CAMK2D,CDK5,CDK9,EIF2AK3,ERBB2,GRK2,ITK,MAPK7,MAPKAPK2,NTRK2,PDK1,PDK2,PRKDC,TEK,TGFBR1 | 19 | |||
| kinase-selectivity-class | AXL,BRAF,GRK2,MAP2K6,TEK | 5 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 4.539 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 8.222 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 56.580 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 7.586 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 63.150 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 21.478 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 80.180 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 60.600 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 939.723 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Sept. 16, 2014 | FDA | ASTRAZENECA PHARMS | |
| Sept. 25, 2014 | EMA |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Drug withdrawal syndrome | 209.34 | 24.97 | 65 | 3025 | 28658 | 90596699 |
| Withdrawal syndrome | 99.64 | 24.97 | 35 | 3055 | 22489 | 90602868 |
| Abdominal pain | 67.76 | 24.97 | 75 | 3015 | 395646 | 90229711 |
| Drug screen positive | 61.41 | 24.97 | 16 | 3074 | 3741 | 90621616 |
| Hyperhidrosis | 59.81 | 24.97 | 44 | 3046 | 136261 | 90489096 |
| Diarrhoea | 47.82 | 24.97 | 101 | 2989 | 939089 | 89686268 |
| Chills | 39.40 | 24.97 | 34 | 3056 | 131947 | 90493410 |
| Nausea | 27.13 | 24.97 | 91 | 2999 | 1110225 | 89515132 |
FDA Adverse Event Reporting System (Male)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Drug withdrawal syndrome | 81.04 | 28.70 | 31 | 1682 | 21518 | 42598104 |
| Agranulocytosis | 51.69 | 28.70 | 25 | 1688 | 30587 | 42589035 |
| Withdrawal syndrome | 47.54 | 28.70 | 19 | 1694 | 14756 | 42604866 |
| Abdominal pain | 40.99 | 28.70 | 44 | 1669 | 190427 | 42429195 |
| Hyperhidrosis | 37.14 | 28.70 | 30 | 1683 | 90482 | 42529140 |
| Drug screen positive | 31.18 | 28.70 | 10 | 1703 | 4121 | 42615501 |
| Pain | 30.58 | 28.70 | 43 | 1670 | 244805 | 42374817 |
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Drug withdrawal syndrome | 141.94 | 22.07 | 52 | 3691 | 38002 | 110547554 |
| Withdrawal syndrome | 61.51 | 22.07 | 27 | 3716 | 31353 | 110554203 |
| Abdominal pain | 51.08 | 22.07 | 74 | 3669 | 512915 | 110072641 |
| Hyperhidrosis | 43.93 | 22.07 | 42 | 3701 | 187256 | 110398300 |
| Ischaemic stroke | 42.89 | 22.07 | 23 | 3720 | 41240 | 110544316 |
| Agranulocytosis | 41.71 | 22.07 | 26 | 3717 | 61734 | 110523822 |
| Diarrhoea | 37.31 | 22.07 | 103 | 3640 | 1139402 | 109446154 |
| Nausea | 31.25 | 22.07 | 102 | 3641 | 1235588 | 109349968 |
| Pain | 25.13 | 22.07 | 80 | 3663 | 954875 | 109630681 |
| Drug screen positive | 24.76 | 22.07 | 9 | 3734 | 6401 | 110579155 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| 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 |
| FDA EPC | N0000175691 | Opioid Antagonist |
| CHEBI has role | CHEBI:35488 | central nervous system depressant |
| CHEBI has role | CHEBI:50137 | μ-opioid receptor antagonist |
| CHEBI has role | CHEBI:90755 | antidote to opioid poisoning |
| CHEBI has role | CHEBI:75325 | cathartic |
| CHEBI has role | CHEBI:35480 | analgesic |
| CHEBI has role | CHEBI:50503 | laxative |
Related Drugs by ATC class:
A06AH Peripheral opioid receptor antagonists 4 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Therapeutic opioid induced constipation | indication | 136801000119102 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (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:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Mu-type opioid receptor | GPCR | ANTAGONIST | DRUG LABEL | DRUG LABEL |
External reference:
| ID | Source |
|---|---|
| 44T7335BKE | UNII |
| D10375 | KEGG_DRUG |
| 1354744-91-4 | SECONDARY_CAS_RN |
| 4019852 | VANDF |
| 4034135 | VANDF |
| C3700399 | UMLSCUI |
| CHEBI:82975 | 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 |
| 5284596 | PUBCHEM_CID |
| 1526 | INN_ID |
| D009270 | MESH_DESCRIPTOR_UI |
| CHEBI:7459 | CHEBI |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| 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 | 57841-1301 | 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 |