Page last updated: 2024-11-13

tenapanor

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Cross-References

ID SourceID
PubMed CID71587953
CHEMBL ID3304485
SCHEMBL ID15267600
MeSH IDM000607773

Synonyms (56)

Synonym
1234423-95-0
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)
tenapanor ,
rdx 5791
azd 1722
tenapanor [usan:inn]
wyd79216a6 ,
azd1722
unii-wyd79216a6
rdx5791
tenapanor [usan]
rdx013 component tenapanor
azd-1722
tenapanor component of rdx-013
tenapanor [inn]
tenapanor component of rdx013
khk-7791
khk7791
tenapanor [who-dd]
rdx-013 component tenapanor
12,15-dioxa-2,7,9-triazaheptadecanamide, 17-(((3-((4s)-6,8-dichloro-1,2,3,4-tetrahydro-2-methyl-4-isoquinolinyl)phenyl)sulfonyl)amino)-n-(2-(2-(2-(((3-((4s)-6,8-dichloro-1,2,3,4-tetrahydro-2-methyl-4-isoquinolinyl)phenyl)sulfonyl)amino)ethoxy)ethoxy)ethyl
tenapanor [mi]
CHEMBL3304485
rdx-5791
SCHEMBL15267600
gtpl8449
1-[2-[2-[2-[[3-[(4s)-6,8-dichloro-2-methyl-3,4-dihydro-1h-isoquinolin-4-yl]phenyl]sulfonylamino]ethoxy]ethoxy]ethyl]-3-[4-[2-[2-[2-[[3-[(4s)-6,8-dichloro-2-methyl-3,4-dihydro-1h-isoquinolin-4-yl]phenyl]sulfonylamino]ethoxy]ethoxy]ethylcarbamoylamino]butyl
DTXSID40154016 ,
mfcd28386333
CS-6273
HY-15991
DB11761
3-((s)-6,8-dichloro-2-methyl-1,2,3,4-tetrahydroisoquinolin-4-yl)-n-(26-((3-((s)-6,8-dichloro-2-methyl-1,2,3,4-tetrahydroisoquinolin-4-yl)phenyl)sulfonamido)-10,17-dioxo-3,6,21,24-tetraoxa-9,11,16,18-tetraazahexacosyl)benzenesulfonamide
BCP24892
azd-1722; azd 1722; azd1722; rdx 5791; rdx-5791; rdx5791
tenapanor free base
1234423-95-0 (free base)
tenapanor; azd1722; rdx5791
EX-A2506
BS-14732
BCP28554
Q17122912
D11652
tenapanor (usan/inn)
us10272079, compound 180
bdbm381823
us10272079, compound 002
AKOS037648586
17-[[[3-[(4s)-6,8-dichloro-1,2,3,4-tetrahydro-2-methyl-4-isoquinolinyl]phenyl]sulfonyl]amino]-n-[2-[2-[2-[[[3-[(4s)-6,8-dichloro-1,2,3,4-tetrahydro-2-methyl-4-isoquinolinyl]phenyl]sulfonyl]amino]ethoxy]ethoxy]ethyl]-8-oxo-12,15-dioxa-2,7,9-triazaheptadeca
A929505
BT178667
EN300-25927897
3-{2-[2-(2-{3-[(4s)-6,8-dichloro-2-methyl-1,2,3,4-tetrahydroisoquinolin-4-yl]benzenesulfonamido}ethoxy)ethoxy]ethyl}-1-{4-[({2-[2-(2-{3-[(4s)-6,8-dichloro-2-methyl-1,2,3,4-tetrahydroisoquinolin-4-yl]benzenesulfonamido}ethoxy)ethoxy]ethyl}carbamoyl)amino]b
dtxcid9076507
tenapanorum
AC-36104

Research Excerpts

Overview

Tenapanor is a first-in-class, non-phosphate binder that inhibits the sodium-hydrogen exchanger 3 or solute carrier family 9 member 3 (SLC9A3) Tenapanor reduces paracellular intestinal phosphate absorption.

ExcerptReferenceRelevance
"Tenapanor is a first-in-class, non-phosphate binder that inhibits the sodium-hydrogen exchanger 3 or solute carrier family 9 member 3 (SLC9A3) encoded by the SLC9A3 gene, and blocks paracellular phosphate absorption."( Small Intestinal Phosphate Absorption: Novel Therapeutic Implications.
Jacobs, JW; Rosenbaum, D; Sprague, SM; Yee, J, 2021
)
1.34
"Tenapanor is a novel drug administered as a small tablet, twice daily."( Long-term safety and decrease of pill burden by tenapanor therapy: a phase 3 open-label study in hemodialysis patients with hyperphosphatemia.
Akizawa, T; Fukagawa, M; Koiwa, F; Nakanishi, K; Ohara, M; Sato, Y, 2023
)
1.89
"Tenapanor is a first-in-class, minimally absorbed, small-molecule inhibitor of the gastrointestinal sodium/hydrogen exchanger isoform 3. "( Efficacy of Tenapanor in Treating Patients With Irritable Bowel Syndrome With Constipation: A 12-Week, Placebo-Controlled Phase 3 Trial (T3MPO-1).
Chey, WD; Lembo, AJ; Rosenbaum, DP, 2020
)
2.38
"Tenapanor is a locally acting, minimally absorbed, selective small-molecule inhibitor of the intestinal sodium/hydrogen exchanger 3 (NHE3) that was approved in September 2019 by the U.S."( Tenapanor for constipation-predominant irritable bowel syndrome.
Cash, BD; Siddiqui, S, 2020
)
2.72
"Tenapanor is a nonbinder, sodium/hydrogen exchanger isoform 3 (NHE3) inhibitor that reduces paracellular intestinal phosphate absorption."( Combination treatment with tenapanor and sevelamer synergistically reduces urinary phosphorus excretion in rats.
Chertow, GM; Fung, C; Jiang, Z; King, AJ; Kohler, J; Kumaraswamy, P; Quach, A; Rosenbaum, DP, 2021
)
1.64
"Tenapanor is a first-in-class, minimally absorbed, small-molecule inhibitor of the gastrointestinal sodium/hydrogen exchanger isoform 3. "( Efficacy of Tenapanor in Treating Patients With Irritable Bowel Syndrome With Constipation: A 26-Week, Placebo-Controlled Phase 3 Trial (T3MPO-2).
Chey, WD; Lembo, AJ; Rosenbaum, DP; Yang, Y, 2021
)
2.44
"Tenapanor is an inhibitor of the sodium-proton (Na(+)/H(+)) exchanger NHE3, which plays a prominent role in sodium handling in the gastrointestinal tract and kidney."( Intestinal inhibition of the Na+/H+ exchanger 3 prevents cardiorenal damage in rats and inhibits Na+ uptake in humans.
Bell, N; Carreras, CW; Charmot, D; He, L; Jacobs, JW; Joly, KM; Kohler, J; Koo-McCoy, S; Kozuka, K; Labonte, ED; Leadbetter, MR; Navre, M; Plato, CF; Rosenbaum, DP; Spencer, AG; Tabora, J, 2014
)
1.12
"Tenapanor is a potent inhibitor of Na(+)/H(+) exchanger 3 [NHE3], localized in the apical membrane of intestinal epithelial cells."( Tenapanor hydrochloride for the treatment of constipation-predominant irritable bowel syndrome.
Fichna, J; Wasilewski, A; Zielińska, M, 2015
)
2.58
"Tenapanor is a minimally absorbed small molecule inhibitor of the sodium/hydrogen exchanger isoform 3 that functions in the gut to reduce sodium and phosphate absorption."( Effect of Tenapanor on Serum Phosphate in Patients Receiving Hemodialysis.
Åstrand, M; Block, GA; Chertow, GM; Johansson, S; Knutsson, M; Langkilde, AM; Leonsson-Zachrisson, M; Rosenbaum, DP, 2017
)
1.58
"Tenapanor is a first-in-class, small-molecule inhibitor of the gastrointestinal sodium/hydrogen exchanger NHE3. "( Tenapanor Treatment of Patients With Constipation-Predominant Irritable Bowel Syndrome: A Phase 2, Randomized, Placebo-Controlled Efficacy and Safety Trial.
Chey, WD; Lembo, AJ; Rosenbaum, DP, 2017
)
3.34

Effects

ExcerptReferenceRelevance
"Tenapanor has been shown to improve bowel movement frequency/form and abdominal pain in patients with IBS-C."( Tenapanor for constipation-predominant irritable bowel syndrome.
Cash, BD; Siddiqui, S, 2020
)
2.72

Treatment

Tenapanor increased stool sodium and weight over placebo in patients undergoing hemodialysis. Tenapanor treatment reduced absorption of intestinal sodium and phosphate from the gut in Japanese adults.

ExcerptReferenceRelevance
"Tenapanor treatment increased stool sodium and weight over placebo in patients undergoing hemodialysis. "( Effect of Tenapanor on Interdialytic Weight Gain in Patients on Hemodialysis.
Block, GA; Carlsson, BC; Greasley, PJ; Johansson, SA; Knutsson, M; Leonsson-Zachrisson, M; Rosenbaum, DP; Rydén-Bergsten, T; Stefansson, BV, 2016
)
2.28
"Tenapanor treatment reduced absorption of intestinal sodium and phosphate from the gut in Japanese adults. "( A phase 1 study of the safety, tolerability, pharmacodynamics, and pharmacokinetics of tenapanor in healthy Japanese volunteers.
Johansson, S; Knutsson, M; Leonsson-Zachrisson, M; Rosenbaum, DP, 2017
)
2.12

Toxicity

Diarrhea was the most frequent adverse event (tenapanor b) Adverse events were largely limited to softened stool and a modest increase in bowel movement frequency.

ExcerptReferenceRelevance
" Adverse events were mild or moderate in severity, and were typically gastrointestinal in nature."( Pharmacodynamics, Safety, and Tolerability of the NHE3 Inhibitor Tenapanor: Two Trials in Healthy Volunteers.
Jacobs, JW; Rosenbaum, DP; Yan, A, 2018
)
0.72
" Adverse events were largely limited to softened stool and a modest increase in bowel movement frequency, resulting from increased stool sodium and water content, stemming from tenapanor's mechanism of action."( Efficacy and Safety of Tenapanor in Patients with Hyperphosphatemia Receiving Maintenance Hemodialysis: A Randomized Phase 3 Trial.
Block, GA; Chertow, GM; Rosenbaum, DP; Yan, A, 2019
)
1.02
" Adverse effects were limited to those induced by its known mechanism of action, which increases stool sodium and water content."( Efficacy and Safety of Tenapanor in Patients with Hyperphosphatemia Receiving Maintenance Hemodialysis: A Randomized Phase 3 Trial.
Block, GA; Chertow, GM; Rosenbaum, DP; Yan, A, 2019
)
0.82
" Data on drug-related adverse events (AEs), gastrointestinal AEs and diarrhea were collected to determine the safety of tenapanor."( Efficacy and safety of tenapanor in hemodialysis patients with hyperphosphatemia: A systematic review and meta-analysis of randomized placebo-controlled trials.
Ai, X; Dong, H; Feng, J; Huang, B; Huang, X; Li, J; Li, L; Li, X; Luo, H; Wang, J; Xiao, H; Xue, G; You, S; Zhang, Y, 2023
)
1.43
" Treatment-emergent adverse events (TEAEs) were evaluated in the entire T3MPO-3 safety population and in patients who received a total of ≥52 weeks of tenapanor."( Long-term safety of tenapanor in patients with irritable bowel syndrome with constipation in the T3MPO-3 study.
Chey, WD; Edelstein, S; Fogel, RP; Friedenberg, KA; Lembo, AJ; Rosenbaum, DP; Yang, Y; Zhao, S, 2023
)
1.43
" Diarrhea was the most frequent adverse event, occurring in 135 patients (63."( Long-term safety and decrease of pill burden by tenapanor therapy: a phase 3 open-label study in hemodialysis patients with hyperphosphatemia.
Akizawa, T; Fukagawa, M; Koiwa, F; Nakanishi, K; Ohara, M; Sato, Y, 2023
)
1.17

Dosage Studied

Tenapanor produced generally dose-dependent increases in stool sodium excretion. Two-daily dosing appeared to have a greater effect on sodium absorption. However, Phase III clinical trials are still needed to confirm results.

ExcerptRelevanceReference
" However, Phase III clinical trials are still needed to confirm results obtained in earlier phases and optimize the dose-response for tenapanor, whereas limiting diarrhea, its major adverse effect."( Tenapanor hydrochloride for the treatment of constipation-predominant irritable bowel syndrome.
Fichna, J; Wasilewski, A; Zielińska, M, 2015
)
2.06
"Tenapanor produced generally dose-dependent increases in stool sodium excretion and decreases in urinary sodium excretion versus placebo; in addition, twice-daily dosing appeared to have a greater effect on sodium absorption than once-daily dosing with an equivalent daily dose."( Pharmacodynamics, Safety, and Tolerability of the NHE3 Inhibitor Tenapanor: Two Trials in Healthy Volunteers.
Jacobs, JW; Rosenbaum, DP; Yan, A, 2018
)
2.16
" We measured 24-h urinary phosphorus excretion in male rats assigned to groups dosed orally with vehicle or tenapanor (0."( Combination treatment with tenapanor and sevelamer synergistically reduces urinary phosphorus excretion in rats.
Chertow, GM; Fung, C; Jiang, Z; King, AJ; Kohler, J; Kumaraswamy, P; Quach, A; Rosenbaum, DP, 2021
)
1.13
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Sodium/hydrogen exchanger 3Rattus norvegicus (Norway rat)IC50 (µMol)0.01150.00930.60862.4000AID1341061; AID1411075; AID1893593
Sodium/hydrogen exchanger 3Homo sapiens (human)IC50 (µMol)0.00350.00050.00350.0050AID1341062; AID1411076; AID1893592
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (5)

Processvia Protein(s)Taxonomy
monoatomic ion transportSodium/hydrogen exchanger 3Homo sapiens (human)
regulation of intracellular pHSodium/hydrogen exchanger 3Homo sapiens (human)
sodium ion import across plasma membraneSodium/hydrogen exchanger 3Homo sapiens (human)
proton transmembrane transportSodium/hydrogen exchanger 3Homo sapiens (human)
potassium ion transmembrane transportSodium/hydrogen exchanger 3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (6)

Processvia Protein(s)Taxonomy
protein bindingSodium/hydrogen exchanger 3Homo sapiens (human)
sodium:proton antiporter activitySodium/hydrogen exchanger 3Homo sapiens (human)
PDZ domain bindingSodium/hydrogen exchanger 3Homo sapiens (human)
phosphatidylinositol bindingSodium/hydrogen exchanger 3Homo sapiens (human)
identical protein bindingSodium/hydrogen exchanger 3Homo sapiens (human)
potassium:proton antiporter activitySodium/hydrogen exchanger 3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (9)

Processvia Protein(s)Taxonomy
early endosomeSodium/hydrogen exchanger 3Homo sapiens (human)
plasma membraneSodium/hydrogen exchanger 3Homo sapiens (human)
brush borderSodium/hydrogen exchanger 3Homo sapiens (human)
cell surfaceSodium/hydrogen exchanger 3Homo sapiens (human)
apical plasma membraneSodium/hydrogen exchanger 3Homo sapiens (human)
brush border membraneSodium/hydrogen exchanger 3Homo sapiens (human)
early endosome membraneSodium/hydrogen exchanger 3Homo sapiens (human)
recycling endosome membraneSodium/hydrogen exchanger 3Homo sapiens (human)
extracellular exosomeSodium/hydrogen exchanger 3Homo sapiens (human)
apical plasma membraneSodium/hydrogen exchanger 3Homo sapiens (human)
plasma membraneSodium/hydrogen exchanger 3Homo sapiens (human)
brush border membraneSodium/hydrogen exchanger 3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (14)

Assay IDTitleYearJournalArticle
AID1893593Inhibition of rat NHE3 expressed in opossum kidney cells assessed as reduction in Na-HEPES buffer-mediated pH recovery in presence of NEH1 inhibitor ethyl isopropyl amiloride by BCECF-AM dye based fluorescence assay
AID1893646Toxicity in Sprague-Dawley rat assessed as change in aspartate aminotransferase level at 30 mg/kg, po administered for 7 days measured on day 8
AID1893641Drug metabolism in Sprague-Dawley rat at 30 mg/kg, po administered via gavage by LC-MS/MS analysis
AID1893639Drug metabolism in Sprague-Dawley rat feces at 0.1 mg/kg, po administered via gavage measured after 72 hrs by LC-MS/MS analysis
AID1893633In vivo inhibition of NEH3 in Sprague-Dawley rat assessed as increase in fecal water content at 0.1 to 3 mg/kg, po administered via gavage measured after 6 hrs
AID1893636Drug recovery in Sprague-Dawley rat feces at 0.1 mg/kg, po administered via gavage measured after 72 hrs by LC-MS/MS analysis
AID1893643Toxicity in Sprague-Dawley rat assessed as gross pathological changes at 30 mg/kg, po administered for 7 days measured on day 8 by necropsy
AID1893640Cmax in Sprague-Dawley rat at 30 mg/kg, po administered via gavage by LC-MS/MS analysis
AID1893647Toxicity in Sprague-Dawley rat assessed as diarrhea at 30 mg/kg, po administered for 7 days
AID1893644Toxicity in Sprague-Dawley rat assessed as pathological changes at 30 mg/kg, po administered for 7 days measured on day 8 by microscopy
AID1893645Toxicity in Sprague-Dawley rat assessed as change in alanine aminotransferase level at 30 mg/kg, po administered for 7 days measured on day 8
AID1893592Inhibition of human NHE3 expressed in opossum kidney cells assessed as reduction in Na-HEPES buffer-mediated pH recovery in presence of NEH1 inhibitor ethyl isopropyl amiloride by BCECF-AM dye based fluorescence assay
AID1893632In vivo inhibition of NEH3 in Sprague-Dawley rat assessed as reduction in sodium excretion in urine at 0.1 to 3 mg/kg, po administered via gavage measured after 16 hrs by ion chromatography
AID1893642Inhibition of human ERG at 10 uM relative to control
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (41)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's21 (51.22)24.3611
2020's20 (48.78)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 227.86

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index227.86 (24.57)
Research Supply Index4.06 (2.92)
Research Growth Index4.68 (4.65)
Search Engine Demand Index433.36 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (227.86)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials16 (39.02%)5.53%
Reviews14 (34.15%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other11 (26.83%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]