Compounds > tenapanor
Page last updated: 2024-08-03 22:28:43

tenapanor

Description

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

Protein Targets (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)
Sodium/hydrogen exchanger 3Rattus norvegicus (Norway rat)IC500.0115AID1341061; AID1411075; AID1893593
Sodium/hydrogen exchanger 3Homo sapiens (human)IC500.0035AID1341062; AID1411076; AID1893592

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 assay2022ACS medicinal chemistry letters, Jul-14, Volume: 13, Issue:7
ISSN: 1948-5875
AID1893646Toxicity in Sprague-Dawley rat assessed as change in aspartate aminotransferase level at 30 mg/kg, po administered for 7 days measured on day 82022ACS medicinal chemistry letters, Jul-14, Volume: 13, Issue:7
ISSN: 1948-5875
AID1893641Drug metabolism in Sprague-Dawley rat at 30 mg/kg, po administered via gavage by LC-MS/MS analysis2022ACS medicinal chemistry letters, Jul-14, Volume: 13, Issue:7
ISSN: 1948-5875
AID1893639Drug metabolism in Sprague-Dawley rat feces at 0.1 mg/kg, po administered via gavage measured after 72 hrs by LC-MS/MS analysis2022ACS medicinal chemistry letters, Jul-14, Volume: 13, Issue:7
ISSN: 1948-5875
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 hrs2022ACS medicinal chemistry letters, Jul-14, Volume: 13, Issue:7
ISSN: 1948-5875
AID1893636Drug recovery in Sprague-Dawley rat feces at 0.1 mg/kg, po administered via gavage measured after 72 hrs by LC-MS/MS analysis2022ACS medicinal chemistry letters, Jul-14, Volume: 13, Issue:7
ISSN: 1948-5875
AID1893643Toxicity in Sprague-Dawley rat assessed as gross pathological changes at 30 mg/kg, po administered for 7 days measured on day 8 by necropsy2022ACS medicinal chemistry letters, Jul-14, Volume: 13, Issue:7
ISSN: 1948-5875
AID1893640Cmax in Sprague-Dawley rat at 30 mg/kg, po administered via gavage by LC-MS/MS analysis2022ACS medicinal chemistry letters, Jul-14, Volume: 13, Issue:7
ISSN: 1948-5875
AID1893647Toxicity in Sprague-Dawley rat assessed as diarrhea at 30 mg/kg, po administered for 7 days2022ACS medicinal chemistry letters, Jul-14, Volume: 13, Issue:7
ISSN: 1948-5875
AID1893644Toxicity in Sprague-Dawley rat assessed as pathological changes at 30 mg/kg, po administered for 7 days measured on day 8 by microscopy2022ACS medicinal chemistry letters, Jul-14, Volume: 13, Issue:7
ISSN: 1948-5875
AID1893645Toxicity in Sprague-Dawley rat assessed as change in alanine aminotransferase level at 30 mg/kg, po administered for 7 days measured on day 82022ACS medicinal chemistry letters, Jul-14, Volume: 13, Issue:7
ISSN: 1948-5875
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 assay2022ACS medicinal chemistry letters, Jul-14, Volume: 13, Issue:7
ISSN: 1948-5875
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 chromatography2022ACS medicinal chemistry letters, Jul-14, Volume: 13, Issue:7
ISSN: 1948-5875
AID1893642Inhibition of human ERG at 10 uM relative to control2022ACS medicinal chemistry letters, Jul-14, Volume: 13, Issue:7
ISSN: 1948-5875

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

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%
SubstanceStudiesClassesRolesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
niacinamide
2
pyridine alkaloid;
pyridinecarboxamide;
vitamin B3		anti-inflammatory agent;
antioxidant;
cofactor;
EC 2.4.2.30 (NAD(+) ADP-ribosyltransferase) inhibitor;
EC 3.5.1.98 (histone deacetylase) inhibitor;
Escherichia coli metabolite;
geroprotector;
human urinary metabolite;
metabolite;
mouse metabolite;
neuroprotective agent;
Saccharomyces cerevisiae metabolite;
Sir2 inhibitor		201820195.5medium000020
lubiprostone
2
201820205.0medium000020
indican
1
beta-D-glucoside;
exopolysaccharide;
indolyl carbohydrate		202020204.0low000010
arginine vasopressin
1
vasopressincardiovascular drug;
hematologic agent;
mitogen		201820186.0low000010
enalapril
1
dicarboxylic acid monoester;
dipeptide		antihypertensive agent;
EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor;
geroprotector;
prodrug		2014201410.0low100010
phosphorus
9
monoatomic phosphorus;
nonmetal atom;
pnictogen		macronutrient201520234.6high600045
plecanatide
2
201820205.0medium000020
ConditionIndicatedStudiesFirst YearLast YearAverage AgeRelationship StrengthTrialspre-19901990's2000's2010'spost-2020
Abdominal Pain0
3
201720214.7low300021
Albuminuria0
1
2014201410.0low100010
Blood Pressure, High0
2
201620187.0low000020
Calcification, Pathologic0
1
201520159.0low000010
Calcinosis0
1
201520159.0low000010
Cardiovascular Diseases0
1
201620168.0low000010
Chronic Disease0
1
202020204.0low000010
Chronic Illness0
1
202020204.0low000010
Chronic Kidney Diseases0
11
201420215.6low300083
Chronic Kidney Failure0
5
201620225.0low300041
Colicky Pain0
3
201720214.7low300021
Colitis, Mucous0
13
201520234.4medium300094
Colonic Inertia0
11
201520234.2low300074
Constipation1
11
201520234.2low300074
Cystic Fibrosis0
1
202220222.0low000001
Cystic Fibrosis of Pancreas0
1
202220222.0low000001
Diarrhea0
7
201620234.4low600043
Disease Models, Animal0
3
201420159.3low100030
Electrolytes0
1
2014201410.0low100010
Hyperphosphatemia1
14
201720233.5medium600068
Hypertension0
2
201620187.0low000020
Hypertrophy0
1
2014201410.0low100010
Intestinal Obstruction0
1
202220222.0low000001
Irritable Bowel Syndrome1
13
201520234.4medium300094
Kidney Calculi0
1
201820186.0low000010
Kidney Diseases0
1
201820186.0low000010
Kidney Failure, Chronic0
5
201620225.0low300041
Kidney Stones0
1
201820186.0low000010
Renal Insufficiency, Chronic0
11
201420215.6low300083
Uremia0
1
202020204.0low000010
Vascular Calcification0
1
202020204.0low000010
Weight Gain0
1
201620168.0low100010

Safety/Toxicity (7)

ArticleYear
Long-term safety and decrease of pill burden by tenapanor therapy: a phase 3 open-label study in hemodialysis patients with hyperphosphatemia.
Scientific reports, , 11-04, Volume: 13, Issue:1		2023
Long-term safety of tenapanor in patients with irritable bowel syndrome with constipation in the T3MPO-3 study.
Neurogastroenterology and motility, , Volume: 35, Issue:11		2023
Efficacy and safety of tenapanor in hemodialysis patients with hyperphosphatemia: A systematic review and meta-analysis of randomized placebo-controlled trials.
Therapeutic apheresis and dialysis : official peer-reviewed journal of the International Society for Apheresis, the Japanese Society for Apheresis, the Japanese Society for Dialysis Therapy, , Volume: 27, Issue:5		2023
Efficacy and Safety of Tenapanor in Patients with Hyperphosphatemia Receiving Maintenance Hemodialysis: A Randomized Phase 3 Trial.
Journal of the American Society of Nephrology : JASN, , Volume: 30, Issue:4		2019
Pharmacodynamics, Safety, and Tolerability of the NHE3 Inhibitor Tenapanor: Two Trials in Healthy Volunteers.
Clinical drug investigation, , Volume: 38, Issue:4		2018
Tenapanor Treatment of Patients With Constipation-Predominant Irritable Bowel Syndrome: A Phase 2, Randomized, Placebo-Controlled Efficacy and Safety Trial.
The American journal of gastroenterology, , Volume: 112, Issue:5		2017
A phase 1 study of the safety, tolerability, pharmacodynamics, and pharmacokinetics of tenapanor in healthy Japanese volunteers.
Clinical and experimental nephrology, , Volume: 21, Issue:3		2017

Pharmacokinetics (3)

ArticleYear
Pharmacodynamics, Safety, and Tolerability of the NHE3 Inhibitor Tenapanor: Two Trials in Healthy Volunteers.
Clinical drug investigation, , Volume: 38, Issue:4		2018
Effect of Food Intake on the Pharmacodynamics of Tenapanor: A Phase 1 Study.
Clinical pharmacology in drug development, , Volume: 6, Issue:5		2017
A phase 1 study of the safety, tolerability, pharmacodynamics, and pharmacokinetics of tenapanor in healthy Japanese volunteers.
Clinical and experimental nephrology, , Volume: 21, Issue:3		2017

Dosage (4)

ArticleYear
Combination treatment with tenapanor and sevelamer synergistically reduces urinary phosphorus excretion in rats.
American journal of physiology. Renal physiology, , 01-01, Volume: 320, Issue:1		2021
Efficacy of Secretagogues in Patients With Irritable Bowel Syndrome With Constipation: Systematic Review and Network Meta-analysis.
Gastroenterology, , Volume: 155, Issue:6		2018
Pharmacodynamics, Safety, and Tolerability of the NHE3 Inhibitor Tenapanor: Two Trials in Healthy Volunteers.
Clinical drug investigation, , Volume: 38, Issue:4		2018
Tenapanor hydrochloride for the treatment of constipation-predominant irritable bowel syndrome.
Expert opinion on investigational drugs, , Volume: 24, Issue:8		2015

Interactions (1)

ArticleYear
Preclinical and Healthy Volunteer Studies of Potential Drug-Drug Interactions Between Tenapanor and Phosphate Binders.
Clinical pharmacology in drug development, , Volume: 6, Issue:5		2017