TENAPANOR HYDROCHLORIDE

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C50H66Cl4N8O10S2.2ClH
Molecular Weight	1217.971
Optical Activity	UNSPECIFIED
Defined Stereocenters	2 / 2
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

SMILES

Cl.Cl.CN1C[C@@H](C2=CC=CC(=C2)S(=O)(=O)NCCOCCOCCNC(=O)NCCCCNC(=O)NCCOCCOCCNS(=O)(=O)C3=CC(=CC=C3)[C@@H]4CN(C)CC5=C4C=C(Cl)C=C5Cl)C6=C(C1)C(Cl)=CC(Cl)=C6

InChI

InChIKey=VFRAXTZDILCRKY-OWRGXFNZSA-N

InChI=1S/C50H66Cl4N8O10S2.2ClH/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);2*1H/t43-,44-;;/m0../s1

HIDE SMILES / InChI

Molecular Formula	ClH
Molecular Weight	36.461
Charge	0
Count	MOL RATIO 2 MOL RATIO (average)

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Molecular Formula	C50H66Cl4N8O10S2
Molecular Weight	1145.049
Charge	0
Count	MOL RATIO 1 MOL RATIO (average)

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	2 / 2
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description

Tenapanor is an inhibitor of the sodium-proton (Na(+)/H(+)) exchanger NHE3 and reduces sodium absorption in the GI tract, thus increasing intestinal fluid. Ardelyx has completed Phase 3 development of tenapanor for the treatment of irritable bowel syndrome with constipation (IBS-C) and submitted a new drug application to the U.S. Food and Drug Administration for the treatment of patients with IBS-C. In addition, tenapanor successfully completed phase III clinical trial for the treatment of hyperphosphatemia in people with end-stage renal disease who are on dialysis and RDX013, a potassium secretagogue program for the potential treatment of high potassium, or hyperkalemia, a problem among certain patients with kidney and/or heart disease.

Originator

Approval Year

Doses

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Dose	Population	Adverse events
50 mg 2 times / day multiple, oral Recommended	unhealthy, adult n = 1203	Disc. AE: Diarrhea...
90 mg 2 times / day steady, oral Highest studied dose	healthy, mean 29.3 years n = 12	Other AEs: Diarrhea, Abdominal pain...
180 mg single, oral Highest studied dose	healthy, mean 37.5 years n = 6
60 mg 2 times / day steady, oral Highest studied dose	healthy, mean 37.5 years n = 12	Other AEs: Diarrhea...
50 mg 2 times / day multiple, oral Recommended	unhealthy, mean 45 years n = 307	Disc. AE: Diarrhea...

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AEs

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AE	Significance	Dose	Population
Diarrhea	6.5% Disc. AE	50 mg 2 times / day multiple, oral Recommended	unhealthy, adult n = 1203
Abdominal pain	1 patient	90 mg 2 times / day steady, oral Highest studied dose	healthy, mean 29.3 years n = 12
Headache	1 patient	90 mg 2 times / day steady, oral Highest studied dose	healthy, mean 29.3 years n = 12
Diarrhea	3 patients	90 mg 2 times / day steady, oral Highest studied dose	healthy, mean 29.3 years n = 12
Diarrhea	1 patient	60 mg 2 times / day steady, oral Highest studied dose	healthy, mean 37.5 years n = 12

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Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1,737	inhibitor 1,767 substrate 1,037	inhibitor 1,852 substrate 1,217	inhibitor 1,612

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
P-gp 1,461 BCRP 699 Cav1.2 45 CYP1A2 1,524 CYP2B6 810 CYP2C8 911 CYP2C19 1,478 OATP1B1 788 OATP1B3 706 OAT1 599 OAT3 642 OCT2 647 MATE1 306 MATE2 263 CYP3A4/5 278	BCRP 561 OATP1B1 406 OATP1B3 350 CYP3A5 395 CYP1A2 1,054 CYP2A6 543 CYP2B6 664 CYP2C8 693 CYP2C19 991 CYP2E1 667	CYP1A2 701 CYP2B6 547 CYP3A4/5 124

Drug as perpetrator

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Target	Modality	Activity
BCRP 773	inhibitor 3,277	no
CYP1A2 1,692	inducer 1,573	no
CYP1A2 1,692	inhibitor 3,277	no
CYP2B6 1,001	inducer 1,573	no
CYP2B6 1,001	inhibitor 3,277	no

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Drug as victim

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Target	Modality	Activity	Metabolite	Clinical evidence
CYP3A4 1,737	substrate 3,367	minor	M1 13	yes (co-administration study)
BCRP 561	substrate 3,367	no
CYP2E1 667	substrate 3,367	no
OATP1B1 406	substrate 3,367	no
OATP1B3 350	substrate 3,367	no

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Tox targets

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Target	Modality	Activity	Metabolite	Clinical evidence
Cav1.2 49	inhibitor 1,626
hERG 1,647	inhibitor 1,626

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Sourcing

Sourcing

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Vendor/Aggregator	ID	URL
AA Blocks	AA00A0DO	https://www.aablocks.com/goods/Goods/detail?id=AA00A0DO
AbMole Bioscience	M7572	http://www.abmole.com/products/tenapanor.html
Adooq BioScience	A14011	https://www.adooq.com/tenapanor.html
Ambeed	A984988	https://www.ambeed.com/products/1234423-95-0.html
BioChemPartner	BCP24892	http://www.biochempartner.com/1234423-95-0-BCP24892

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PubMed

Title	Date	PubMed
No data available in table

Patents

Sample Use Guides

In Vivo Use Guide

twice-daily oral tenapanor (3, 10, or 30 mg [the latter down-titrated, if needed]) for 8 weeks

Route of Administration: Oral

Substance Class	Chemical
Record UNII	50605O2ZNS
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

TENAPANOR HYDROCHLORIDE

Official Name

English

TENAPANOR HYDROCHLORIDE [JAN]

Common Name

English

TENAPANOR HYDROCHLORIDE [ORANGE BOOK]

Common Name

English

TENAPANOR HYDROCHLORIDE [MI]

Common Name

English

RDX5791

Code

English

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Classification Tree

Code System

Code

Pharmacologic Substance

NCI_THESAURUS

C78276

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Code System

Code

Type

Description

NCI_THESAURUS

C152556

PRIMARY

DAILYMED

50605O2ZNS

PRIMARY

ChEMBL

CHEMBL3304485

PRIMARY

FDA UNII

50605O2ZNS

PRIMARY

PUBCHEM

78131177

PRIMARY

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SMILES

InChI

Originator

Approval Year

Doses

AEs

Overview

OverviewOther

Drug as perpetrator​

Drug as victim

Tox targets

Sourcing

PubMed

Patents

Sample Use Guides

Drug as perpetrator