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plecanatide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| peptides and glycopeptides | 5208 | 467426-54-6 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Plecanatide is structurally related to human uroguanylin, and similar to uroguanylin, plecanatide functions as a guanylate cyclase-C (GC-C) agonist. Both plecanatide and its active metabolite bind to GC-C and act locally on the luminal surface of the intestinal epithelium. Activation of GC-C results in an increase in both intracellular and extracellular concentrations of cyclic guanosine monophosphate (cGMP). Elevation of intracellular cGMP stimulates secretion of chloride and bicarbonate into the intestinal lumen, mainly through activation of the cystic fibrosis transmembrane conductance regulator (CFTR) ion channel, resulting in increased intestinal fluid and accelerated transit.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 3 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Bocci G, Oprea TI, Benet LZ |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
None
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 19, 2017 | FDA | SYNERGY PHARMS INC |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | A06AX07 | ALIMENTARY TRACT AND METABOLISM DRUGS FOR CONSTIPATION DRUGS FOR CONSTIPATION Other drugs for constipation |
| MeSH PA | D000074268 | Guanylyl Cyclase C Agonists |
| MeSH PA | D005765 | Gastrointestinal Agents |
| MeSH PA | D020536 | Enzyme Activators |
| FDA MoA | N0000185499 | Guanylate Cyclase Activators |
| FDA EPC | N0000185500 | Guanylate Cyclase-C Agonist |
| CHEBI has role | CHEBI:50503 | laxative |
| CHEBI has role | CHEBI:53784 | antispasmodic drug |
Related Drugs by ATC class:
A06AX Other drugs for constipation 7 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Chronic idiopathic constipation | indication | 82934008 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 3.25 | acidic |
| pKa2 | 3.45 | acidic |
| pKa3 | 3.97 | acidic |
| pKa4 | 4.37 | acidic |
| pKa5 | 11.74 | acidic |
| pKa6 | 12.37 | acidic |
| pKa7 | 12.62 | acidic |
| pKa8 | 12.7 | acidic |
| pKa9 | 13.22 | acidic |
| pKa10 | 13.36 | acidic |
| pKa11 | 13.36 | acidic |
| pKa12 | 13.57 | acidic |
| pKa13 | 13.71 | acidic |
| pKa14 | 13.79 | acidic |
| pKa15 | 7.52 | 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 |
|---|---|---|---|---|---|---|---|---|---|---|
| 3MG | TRULANCE | SALIX | N208745 | Jan. 19, 2017 | RX | TABLET | ORAL | 9610321 | Sept. 15, 2031 | CHRONIC IDIOPATHIC CONSTIPATION |
| 3MG | TRULANCE | SALIX | N208745 | Jan. 19, 2017 | RX | TABLET | ORAL | 9610321 | Sept. 15, 2031 | IRRITABLE BOWEL SYNDROME WITH CONSTIPATION |
| 3MG | TRULANCE | SALIX | N208745 | Jan. 19, 2017 | RX | TABLET | ORAL | 9919024 | Sept. 15, 2031 | CHRONIC IDIOPATHIC CONSTIPATION |
| 3MG | TRULANCE | SALIX | N208745 | Jan. 19, 2017 | RX | TABLET | ORAL | 9919024 | Sept. 15, 2031 | IRRITABLE BOWEL SYNDROME WITH 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 |
|---|---|---|---|---|---|---|---|---|---|
| Heat-stable enterotoxin receptor | Enzyme | AGONIST | EC50 | 6.72 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
| Tumor necrosis factor | Cytokine | Kd | 8.42 | CHEMBL | |||||
| Tumor necrosis factor ligand superfamily member 11 | Cytokine | IC50 | 6 | CHEMBL | |||||
| Tumor necrosis factor receptor superfamily member 1A | Membrane receptor | IC50 | 4.66 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 7IK8Z952OK | UNII |
| 4036439 | VANDF |
| C3711911 | UMLSCUI |
| CHEBI:750504 | CHEBI |
| CHEMBL2103867 | ChEMBL_ID |
| 70693500 | PUBCHEM_CID |
| DB13170 | DRUGBANK_ID |
| D09948 | KEGG_DRUG |
| CHEMBL2105240 | ChEMBL_ID |
| 9367 | INN_ID |
| C584575 | MESH_SUPPLEMENTAL_RECORD_UI |
| 9069 | IUPHAR_LIGAND_ID |
| 725134000 | SNOMEDCT_US |
| 763544006 | SNOMEDCT_US |
| 250462 | MMSL |
| 32292 | MMSL |
| d08521 | MMSL |
| 017076 | NDDF |
| 1873752 | RXNORM |
| 7IK8Z952OK | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Trulance Immediate release | HUMAN PRESCRIPTION DRUG LABEL | 1 | 65649-003 | TABLET | 3 mg | ORAL | NDA | 26 sections |