tenapanor Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
5349 1234423-95-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • tenapanor
  • tenapanor hydrochloride
  • RDX5791
  • AZD1722
  • AZD-1722
  • AZD1722-hydrochloride
  • KHK-7791
  • RDX-5791
  • ibsrela
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.
  • Molecular weight: 1145.04
  • Formula: C50H66Cl4N8O10S2
  • CLOGP: 7.53
  • LIPINSKI: 4
  • HAC: 18
  • HDO: 6
  • TPSA: 218
  • ALOGS: -5.59
  • ROTB: 27

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
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)

DiseaseRelationSNOMED_IDDOID
Irritable bowel syndrome characterized by constipation indication 440630006
Gastrointestinal obstruction contraindication 126765001

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (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 strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent 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 strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 50MG BASE IBSRELA ARDELYX INC N211801 Sept. 12, 2019 DISCN TABLET ORAL Sept. 12, 2024 NEW CHEMICAL ENTITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Sodium/hydrogen exchanger 3 Transporter INHIBITOR IC50 9.06 SCIENTIFIC LITERATURE DRUG LABEL

External reference:

IDSource
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:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
IBSRELA HUMAN PRESCRIPTION DRUG LABEL 1 73154-050 TABLET 53.20 mg ORAL NDA 18 sections