tenapanor Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 5349 | 1234423-95-0 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
IBSRELA (tenapanor) tablets contain tenapanor hydrochloride as an active ingredient. Tenapanor hydrochloride is a sodium/hydrogen exchanger 3 (NHE3) inhibitor for oral use, an antiporter expressed on the apical surface of the small intestine and colon primarily responsible for the absorption of dietary sodium. In vitro and animal studies indicate its major metabolite, M1, is not active against NHE3. By inhibiting NHE3 on the apical surface of the enterocytes, tenapanor reduces absorption of sodium from the small intestine and colon, resulting in an increase in water secretion into the intestinal lumen, which accelerates intestinal transit time and results in a softer stool consistency.
|
Drug dosage:
None
ADMET properties:
None
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Sept. 12, 2019 | FDA | ARDELYX INC |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
Pharmacologic Action:
None
Drug Use (View source of the data)
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Irritable bowel syndrome characterized by constipation | indication | 440630006 | |
| Gastrointestinal obstruction | contraindication | 126765001 |
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 9.53 | acidic |
| pKa2 | 10.13 | acidic |
| pKa3 | 13.34 | acidic |
| pKa4 | 13.74 | acidic |
| pKa5 | 7.19 | Basic |
| pKa6 | 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 50MG BASE | IBSRELA | ARDELYX INC | N211801 | Sept. 12, 2019 | DISCN | TABLET | ORAL | 9408840 | Dec. 30, 2029 | METHOD OF TREATING IRRITABLE BOWEL SYNDROME WITH CONSTIPATION BY ADMINISTERING TENAPANOR |
| EQ 50MG BASE | IBSRELA | ARDELYX INC | N211801 | Sept. 12, 2019 | DISCN | TABLET | ORAL | 9006281 | May 2, 2030 | METHOD OF TREATING IRRITABLE BOWEL SYNDROME WITH CONSTIPATION BY ADMINISTERING TENAPANOR |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| EQ 50MG BASE | IBSRELA | ARDELYX INC | N211801 | Sept. 12, 2019 | DISCN | TABLET | ORAL | Sept. 12, 2024 | NEW CHEMICAL ENTITY |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Sodium/hydrogen exchanger 3 | Transporter | INHIBITOR | IC50 | 9.06 | SCIENTIFIC LITERATURE | DRUG LABEL |
External reference:
| ID | Source |
|---|---|
| 50605O2ZNS | UNII |
| 1234365-97-9 | SECONDARY_CAS_RN |
| 2199674 | RXNORM |
| 018117 | NDDF |
| d09370 | MMSL |
| 792892003 | SNOMEDCT_US |
| 789705000 | SNOMEDCT_US |
| 71587953 | PUBCHEM_CID |
| DB11761 | DRUGBANK_ID |
| 9652 | INN_ID |
| D11652 | KEGG_DRUG |
| CHEMBL3301627 | ChEMBL_ID |
| CHEMBL3304485 | ChEMBL_ID |
| 8449 | IUPHAR_LIGAND_ID |
| C000599417 | MESH_SUPPLEMENTAL_RECORD_UI |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| IBSRELA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 73154-050 | TABLET | 53.20 mg | ORAL | NDA | 18 sections |