TASOSARTAN

Details

Stereochemistry	ACHIRAL
Molecular Formula	C23H21N7O
Molecular Weight	411.4591
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC1=NC(C)=C2CCC(=O)N(CC3=CC=C(C=C3)C4=CC=CC=C4C5=NN=NN5)C2=N1

InChI

InChIKey=ADXGNEYLLLSOAR-UHFFFAOYSA-N

InChI=1S/C23H21N7O/c1-14-18-11-12-21(31)30(23(18)25-15(2)24-14)13-16-7-9-17(10-8-16)19-5-3-4-6-20(19)22-26-28-29-27-22/h3-10H,11-13H2,1-2H3,(H,26,27,28,29)

HIDE SMILES / InChI

Molecular Formula	C23H21N7O
Molecular Weight	411.4591
Charge	0
Count

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

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/?term=11046101

Tasosartan is a long-acting angiotensin II (AngII) receptor blocker. Tasosartan is infrequently in the treatment of hypertension and heart failure. The manufacturer withdrew it from FDA review after phase III clinical trials showed elevated transaminases. Tasosartan blocks the renin-angiotensin-aldosterone system (RAAS) at the level of the AT1 receptor that mediates most, if not all, of the important actions of Ang II. Tasosartan binds reversibly to the AT1 receptors in vascular smooth muscle and the adrenal gland. As angiotensin II is a vasoconstrictor, which also stimulates the synthesis and release of aldosterone, blockage of its effects results in decreases in systemic vascular resistance.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Type-1 angiotensin II receptor 41 Target ID: CHEMBL227 Sources: https://www.ncbi.nlm.nih.gov/pubmed/12113820	Antagonist 2849

Conditions

Condition	Modality	Targets	Highest Phase	Product
Hypertension 575 Sources: https://www.ncbi.nlm.nih.gov/pubmed/9878944	Primary		Phase III 665	Unknown Approved Use Unknown
Heart failure 106 Sources: https://www.ncbi.nlm.nih.gov/pubmed/10487332	Primary		Phase III 665	Unknown Approved Use Unknown

C_max

Value	Dose	Co-administered	Analyte	Population
874.1 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10709151/	50 mg 1 times / day multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered:		TASOSARTAN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
1596 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11046101/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:		TASOSARTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN

AUC

Value	Dose	Co-administered	Analyte	Population
1190.4 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10709151/	50 mg 1 times / day multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered:		TASOSARTAN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

T_1/2

Value	Dose	Analyte	Population
7 h REVIEW https://pubmed.ncbi.nlm.nih.gov/9438775/		TASOSARTAN unknown	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN
5.3 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11046101/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	TASOSARTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
5.2 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11046101/	50 mg single, intravenous dose: 50 mg route of administration: Intravenous experiment type: SINGLE co-administered:	TASOSARTAN plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN

Doses

Dose	Population	Adverse events
300 mg 1 times / day steady-state, oral Highest studied dose Dose: 300 mg, 1 times / day Route: oral Route: steady-state Dose: 300 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/9607384/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/9607384/	Disc. AE: abdominal pain, ALT increased... AEs leading to discontinuation/dose reduction: abdominal pain (1 patient) ALT increased (1 patient) AST increased (1 patient) migraine (5 patients) myocardial ischemia (1 patient) cerebral ischemia (1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/9607384/

AEs

AE	Significance	Dose	Population
ALT increased	1 patient Disc. AE	300 mg 1 times / day steady-state, oral Highest studied dose Dose: 300 mg, 1 times / day Route: oral Route: steady-state Dose: 300 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/9607384/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/9607384/
AST increased	1 patient Disc. AE	300 mg 1 times / day steady-state, oral Highest studied dose Dose: 300 mg, 1 times / day Route: oral Route: steady-state Dose: 300 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/9607384/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/9607384/
abdominal pain	1 patient Disc. AE	300 mg 1 times / day steady-state, oral Highest studied dose Dose: 300 mg, 1 times / day Route: oral Route: steady-state Dose: 300 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/9607384/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/9607384/
cerebral ischemia	1 patient Disc. AE	300 mg 1 times / day steady-state, oral Highest studied dose Dose: 300 mg, 1 times / day Route: oral Route: steady-state Dose: 300 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/9607384/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/9607384/
myocardial ischemia	1 patient Disc. AE	300 mg 1 times / day steady-state, oral Highest studied dose Dose: 300 mg, 1 times / day Route: oral Route: steady-state Dose: 300 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/9607384/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/9607384/
migraine	5 patients Disc. AE	300 mg 1 times / day steady-state, oral Highest studied dose Dose: 300 mg, 1 times / day Route: oral Route: steady-state Dose: 300 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/9607384/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/9607384/

PubMed

Title	Date	PubMed
Novel human metabolites of the angiotensin-II antagonist tasosartan and their pharmacological effects.	2002-08-05	12113820
Pharmacology of AT1-receptor blockers.	2001	11683476
Tasosartan, enoltasosartan, and angiotensin II receptor blockade: the confounding role of protein binding.	2000-11	11046101

Patents

Sample Use Guides

In Vivo Use Guide

Single doses of tasosartan (100 mg p.o. and 50 mg i.v) was compared in 12 healthy subjects in a randomized, double blind studies.

Route of Administration: Other

In Vitro Use Guide

Unknown

Substance Class	Chemical Created by `admin` on `Mon Mar 31 18:58:11 GMT 2025` Edited by `admin` on `Mon Mar 31 18:58:11 GMT 2025`
Record UNII	48G92V856H
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

TASOSARTAN

Official Name

English

ANA-756

Preferred Name

English

TASOSARTAN [MI]

Common Name

English

Tasosartan [WHO-DD]

Common Name

English

WAY-ANA-756

Code

English

TASOSARTAN [USAN]

Common Name

English

tasosartan [INN]

Common Name

English

TASOSARTAN [MART.]

Common Name

English

5,8-DIHYDRO-2,4-DIMETHYL-8-((2'-(1H-TETRAZOL-5-YL)(1,1'-BIPHENYL)-4-YL)METHYL)PYRIDO(2,3-D)PYRIMIDIN-7(6H)-ONE

Systematic Name

English

Classification Tree Code System Code

NCI_THESAURUS

C66930