Tenapanor

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Tenapanor
Tenapanor.svg
Clinical data
Trade names Ibsrela, Xphozah, others
Other namesTenapanor hydrochloride
AHFS/Drugs.com Monograph
License data
Routes of
administration 		By mouth
Drug class NHE3 inhibitors
ATC code
Legal status
Legal status
Identifiers
  • 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 InfoCard 100.243.471 OOjs UI icon edit-ltr-progressive.svg
Chemical and physical data
Formula C50H66Cl4N8O10S2
Molar mass 1145.04 g·mol−1
3D model (JSmol)
  • 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=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, sold under the brand name Ibsrela among others, is a medication used for the treatment of adults with a disease of the gut called irritable bowel syndrome with constipation commonly referred to as IBS-C. [3] [5] It is used in form of tenapanor hydrochloride. [3] It is also used in the treatment of hyperphosphatemia associated with chronic kidney disease. [4] Tenapanor is a sodium hydrogen exchanger 3 (NHE3) inhibitor. [4]

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. [6] 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. [7]

It was approved for medical use in the United States in September 2019. [3] [8] [5] [9] The U.S. Food and Drug Administration (FDA) considers it to be a first-in-class medication. [10] In October 2023, tenapanor was approved by the FDA for the treatment of hyperphosphatemia. [11]

References

  1. ↑ "Summary Basis of Decision (SBD) for Ibsrela". Health Canada. 23 October 2014. Archived from the original on 30 May 2022. Retrieved 29 May 2022.
  2. ↑ "Regulatory Decision Summary - Ibsrela". Health Canada. 23 October 2014. Archived from the original on 13 November 2021. Retrieved 4 June 2022.
  3. 1 2 3 4 "Ibsrela- tenapanor hydrochloride tablet". DailyMed. 14 April 2022. Archived from the original on 19 October 2023. Retrieved 19 October 2023.
  4. 1 2 3 "Xphozah 10 MG- tenapanor tablet, film coated; Xphozah 20 MG- tenapanor tablet, film coated; Xphozah 30 MG- tenapanor tablet, film coated". DailyMed. 17 October 2023. Retrieved 10 November 2023.
  5. 1 2 "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.PD-icon.svg This article incorporates text from this source, which is in the public domain .
  6. ↑ Spencer AG, Labonte ED, Rosenbaum DP, Plato CF, Carreras CW, Leadbetter MR, et al. (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.
  7. ↑ Spencer AG, Labonte ED, Rosenbaum DP, Plato CF, Carreras CW, Leadbetter MR, et al. (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.
  8. ↑ "Ibsrela (tenapanor) FDA Approval History". Drugs.com. 12 September 2019. Archived from the original on 28 November 2020. Retrieved 19 November 2019.
  9. ↑ "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.
  10. ↑ "New Drug Therapy Approvals 2019". U.S. Food and Drug Administration (FDA). 31 December 2019. Archived from the original on 16 September 2020. Retrieved 15 September 2020.
  11. ↑ "US FDA approves Ardelyx's kidney disease-related drug". Reuters. 18 October 2023. Archived from the original on 24 October 2023. Retrieved 24 October 2023.


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