naldemedine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| opioid receptor antagonists/agonists related to normorphine | 5220 | 916072-89-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Naldemedine is an opioid antagonist with binding affinities for mu-, delta-, and kappa-opioid receptors. Naldemedine functions as a peripherally-acting mu-opioid receptor antagonist in tissues such as the gastrointestinal tract, thereby decreasing the constipating effects of opioids.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.20 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| S (Water solubility) | 1.14 mg/mL | Bocci G, Oprea TI, Benet LZ |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Bocci G, Oprea TI, Benet LZ |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Feb. 18, 2019 | EMA | SHIONOGI B.V. | |
| March 23, 2017 | FDA | SHIONOGI INC |
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 |
|---|---|---|---|---|---|---|
| Malignant neoplasm progression | 68.01 | 41.87 | 27 | 624 | 82094 | 63406277 |
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 |
|---|---|---|---|---|---|---|
| Interstitial lung disease | 79.22 | 34.85 | 37 | 877 | 65245 | 34890772 |
| Malignant neoplasm progression | 52.36 | 34.85 | 31 | 883 | 88015 | 34868002 |
| Delirium | 41.36 | 34.85 | 21 | 893 | 43970 | 34912047 |
| Hepatic function abnormal | 41.20 | 34.85 | 21 | 893 | 44342 | 34911675 |
| Diarrhoea | 38.97 | 34.85 | 49 | 865 | 389863 | 34566154 |
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 |
|---|---|---|---|---|---|---|
| Interstitial lung disease | 110.72 | 35.01 | 51 | 1557 | 112549 | 79630231 |
| Malignant neoplasm progression | 95.69 | 35.01 | 49 | 1559 | 135941 | 79606839 |
| Hepatic function abnormal | 68.25 | 35.01 | 32 | 1576 | 73075 | 79669705 |
| Delirium | 60.86 | 35.01 | 31 | 1577 | 84596 | 79658184 |
| Diarrhoea | 43.25 | 35.01 | 69 | 1539 | 880420 | 78862360 |
| Immune-mediated enterocolitis | 36.44 | 35.01 | 10 | 1598 | 4820 | 79737960 |
| Decreased appetite | 35.75 | 35.01 | 39 | 1569 | 342379 | 79400401 |
| Platelet count decreased | 35.15 | 35.01 | 30 | 1578 | 194634 | 79548146 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | A06AH05 | ALIMENTARY TRACT AND METABOLISM DRUGS FOR CONSTIPATION DRUGS FOR CONSTIPATION Peripheral opioid receptor antagonists |
| FDA MoA | N0000000154 | Opioid Antagonists |
| FDA EPC | N0000175691 | Opioid Antagonist |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Therapeutic opioid induced constipation | indication | 136801000119102 | |
| Gastrointestinal obstruction | contraindication | 126765001 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 5.64 | acidic |
| pKa2 | 9.8 | acidic |
| pKa3 | 11.9 | acidic |
| pKa4 | 13.58 | acidic |
| pKa5 | 6.59 | Basic |
Orange Book patent data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| EQ 0.2MG BASE | SYMPROIC | BDSI | N208854 | March 23, 2017 | RX | TABLET | ORAL | RE46375 | Oct. 5, 2026 | TREATMENT OF OPIOID-INDUCED CONSTIPATION |
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 | Ki | 8.95 | IUPHAR | DRUG LABEL | |||
| Delta-type opioid receptor | GPCR | ANTAGONIST | Ki | 9.04 | IUPHAR |
External reference:
| ID | Source |
|---|---|
| 03KSI6WLXH | UNII |
| 1345728-04-2 | SECONDARY_CAS_RN |
| 4036929 | VANDF |
| C4325235 | UMLSCUI |
| CHEMBL2105755 | ChEMBL_ID |
| 54732242 | PUBCHEM_CID |
| DB11691 | DRUGBANK_ID |
| D10188 | KEGG_DRUG |
| CHEMBL3039508 | ChEMBL_ID |
| 9484 | INN_ID |
| 9150 | IUPHAR_LIGAND_ID |
| 259144 | MMSL |
| 32868 | MMSL |
| d08609 | MMSL |
| 017143 | NDDF |
| 017144 | NDDF |
| 733465009 | SNOMEDCT_US |
| 763565000 | SNOMEDCT_US |
| 1876597 | RXNORM |
| C000620491 | MESH_SUPPLEMENTAL_RECORD_UI |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| SYMPROIC | HUMAN PRESCRIPTION DRUG LABEL | 1 | 59385-041 | TABLET | 0.20 mg | ORAL | NDA | 28 sections |
| SYMPROIC | HUMAN PRESCRIPTION DRUG LABEL | 1 | 59385-041 | TABLET | 0.20 mg | ORAL | NDA | 28 sections |