Tenapanor

Tenapanor, used in form of tenapanor hydrochloride and sold under the brand name Ibsrela, is a treatment for adults with a disease of the gut called irritable bowel syndrome with constipation commonly referred to as IBS-C.[3]

Tenapanor
Clinical data
Trade namesIbsrela
Other namestenapanor hydrochloride
AHFS/Drugs.comMonograph
License data
Routes of
administration		By mouth
Drug classNHE3 inhibitors
ATC code
Legal status
Legal status
Identifiers
IUPAC name
  • N,N'-(10,17,-dioxo-3,6,21,24-tetraoxa-9,11,16,18-tetraazahexacosane-1,26-diyl)bis([(4S)-6,8-dichloro-2-methyl-1,2,3,4-tetrahydroisoquinolin-4-yl]benzenesulfonamide)
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.243.471
Chemical and physical data
FormulaC50H66Cl4N8O10S2
Molar mass1145.04 g·mol−1
3D model (JSmol)
SMILES
  • CN1C[C@H](C2=C(C1)C(=CC(=C2)Cl)Cl)C3=CC(=CC=C3)S(=O)(=O)NCCOCCOCCNC(=O)NCCCCNC(=O)NCCOCCOCCNS(=O)(=O)C4=CC=CC(=C4)[C@@H]5CN(CC6=C5C=C(C=C6Cl)Cl)C
InChI
  • InChI=1S/C50H66Cl4N8O10S2/c1-61-31-43(41-27-37(51)29-47(53)45(41)33-61)35-7-5-9-39(25-35)73(65,66)59-15-19-71-23-21-69-17-13-57-49(63)55-11-3-4-12-56-50(64)58-14-18-70-22-24-72-20-16-60-74(67,68)40-10-6-8-36(26-40)44-32-62(2)34-46-42(44)28-38(52)30-48(46)54/h5-10,25-30,43-44,59-60H,3-4,11-24,31-34H2,1-2H3,(H2,55,57,63)(H2,56,58,64)/t43-,44-/m0/s1
  • Key:DNHPDWGIXIMXSA-CXNSMIOJSA-N

Tenapanor is a drug developed by Ardelyx, which acts as an inhibitor of the sodium-proton exchanger NHE3. This antiporter protein is found in the kidney and intestines, and normally acts to regulate the levels of sodium absorbed and secreted by the body. When administered orally, tenapanor selectively inhibits sodium uptake in the intestines, limiting the amount absorbed from food, and thereby reduces levels of sodium in the body.[4] This may make it useful in the treatment of chronic kidney disease and hypertension, both of which are exacerbated by excess sodium in the diet.[5]

It was approved for medical use in the United States in 2019.[6][3][7] The U.S. Food and Drug Administration (FDA) considers it to be a first-in-class medication.[8]

References
  1. "Summary Basis of Decision (SBD) for Ibsrela". Health Canada. Retrieved 29 May 2022.
  2. "Regulatory Decision Summary - Ibsrela". Health Canada. 23 October 2014. Retrieved 4 June 2022.
  3. "Drug Trials Snapshots: Ibsrela". U.S. Food and Drug Administration (FDA). 27 September 2019. Archived from the original on 19 November 2019. Retrieved 18 November 2019. This article incorporates text from this source, which is in the public domain.
  4. Spencer AG, Labonte ED, Rosenbaum DP, Plato CF, Carreras CW, Leadbetter MR, Kozuka K, Kohler J, Koo-McCoy S, He L, Bell N, Tabora J, Joly KM, Navre M, Jacobs JW, Charmot D (2014). "Intestinal inhibition of the na+/h+ exchanger 3 prevents cardiorenal damage in rats and inhibits na+ uptake in humans". Sci Transl Med. 6 (227): 227ra36. doi:10.1126/scitranslmed.3007790. PMID 24622516. S2CID 10741924.
  5. Spencer AG, Labonte ED, Rosenbaum DP, Plato CF, Carreras CW, Leadbetter MR, Kozuka K, Kohler J, Koo-McCoy S, He L, Bell N, Tabora J, Joly KM, Navre M, Jacobs JW, Charmot D (March 2014). "Intestinal inhibition of the Na+/H+ exchanger 3 prevents cardiorenal damage in rats and inhibits Na+ uptake in humans". Sci Transl Med. 6 (227): 227ra36. doi:10.1126/scitranslmed.3007790. PMID 24622516. S2CID 10741924.
  6. "Ibsrela (tenapanor) FDA Approval History". Drugs.com. 12 September 2019. Retrieved 19 November 2019.
  7. "Drug Approval Package: Ibsrela". U.S. Food and Drug Administration (FDA). 19 November 2019. Archived from the original on 19 November 2019. Retrieved 18 November 2019.
  8. "New Drug Therapy Approvals 2019". U.S. Food and Drug Administration. 31 December 2019. Retrieved 15 September 2020.
  • "Tenapanor". Drug Information Portal. U.S. National Library of Medicine (NLM).


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