Tenapanor

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Tenapanor
Names
Trade namesIbsrela
Other namesTenapanor hydrochloride
  • 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)
Clinical data
Drug classNHE3 inhibitors
Pregnancy
category
  • US: N (Not classified yet)
Routes of
use		By mouth
External links
AHFS/Drugs.comMonograph
Legal
License data
Legal status
Chemical and physical data
FormulaC50H66Cl4N8O10S2
Molar mass1145.04 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, is a medication used to treat irritable bowel syndrome with constipation (IBS-C).[1] It is taken by mouth.[1]

Common side effects include diarrhea, abdominal swelling, and lightheadedness.[1] Use in pregnancy and breastfeeding is believed to be safe.[1] It acts by blocking the sodium-proton exchanger NHE3 there by decreasing the uptake of sodium by the intestines.[1]

Tenapanor was approved for medical use in the United States in 2019.[1] As of 2021; however, it is not yet in pharmacies.[2] As of 2021 it is not approved in Europe or the United Kingdom.[3]

Medical uses

It is used for irritable bowel syndrome with constipation (IBS-C).[4]

Dosage

It is usually taken at a dose of 50 mg two times per day.[1]

Mechanism of action

Proposed mechanism of action of tenapanor in individuals with IBS-C[5]

In terms of the mode of action of Tenapanor we find that it binds to and inhibits NHE3. This inhibition reduces the loss of sodium ions out of the gut, as a consequence the gut attracts and retains water.[5]

History

The U.S. Food and Drug Administration (FDA) considers it to be a first-in-class medication.[6]

References

  1. ↑ 1.0 1.1 1.2 1.3 1.4 1.5 1.6 "Tenapanor Monograph for Professionals". Drugs.com. Archived from the original on 27 January 2021. Retrieved 25 September 2021.
  2. ↑ "Ibsrela Prices and Ibsrela Coupons - GoodRx". GoodRx. Retrieved 25 September 2021.
  3. ↑ "Tenapanor". SPS - Specialist Pharmacy Service. 26 May 2017. Archived from the original on 23 July 2017. Retrieved 25 September 2021.
  4. ↑ "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.Public Domain This article incorporates text from this source, which is in the public domain.
  5. ↑ 5.0 5.1 Singh, Prashant; Sayuk, Gregory S.; Rosenbaum, David P.; Edelstein, Susan; Kozuka, Kenji; Chang, Lin (10 April 2024). "An Overview of the Effects of Tenapanor on Visceral Hypersensitivity in the Treatment of Irritable Bowel Syndrome with Constipation". Clinical and Experimental Gastroenterology. 17: 87–96. doi:10.2147/CEG.S454526. Archived from the original on 16 May 2024. Retrieved 14 May 2024.
  6. ↑ "New Drug Therapy Approvals 2019". U.S. Food and Drug Administration. 31 December 2019. Archived from the original on 16 September 2020. Retrieved 15 September 2020.

External links

Identifiers:
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