U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ACHIRAL
Molecular Formula C27H31N7OS
Molecular Weight 501.646
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of FIMASARTAN

SMILES

CCCCC1=NC(C)=C(CC(=S)N(C)C)C(=O)N1CC2=CC=C(C=C2)C3=CC=CC=C3C4=NN=NN4

InChI

InChIKey=AMEROGPZOLAFBN-UHFFFAOYSA-N
InChI=1S/C27H31N7OS/c1-5-6-11-24-28-18(2)23(16-25(36)33(3)4)27(35)34(24)17-19-12-14-20(15-13-19)21-9-7-8-10-22(21)26-29-31-32-30-26/h7-10,12-15H,5-6,11,16-17H2,1-4H3,(H,29,30,31,32)

HIDE SMILES / InChI
Molecular Formula C27H31N7OS
Molecular Weight 501.646
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
Curator's Comment: description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/23811571, http://www.boryung.co.kr/eng/product/mainProduct.do

Fimasartan is a angiotensin II receptor antagonist which was developed in Korea for the treatment of hypertension. The drug is available in different forms: Kanarb, Dukarb (in combination with Amlodipine), Tuvero (in combination with Rosuvastatin). Fimasartan was tested to be effective in Mexican and Russian population and now is being tested in the USA.

Originator

Approval Year

Unknown
139594
Targets

Targets

Primary TargetPharmacologyConditionPotency
Antagonist
2778
 0.13 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8429
KANARB

Approved Use

For the treatment of essential hypertension.

Launch Date

2010
PubMed

PubMed

TitleDatePubMed
Pharmacological characterization of BR-A-657, a highly potent nonpeptide angiotensin II receptor antagonist.
2013
Patents

Patents

20040266800
3
20120264772
3

Sample Use Guides

In Vivo Use Guide
Fimasartan is taken as a single oral dose of 60-mg tablet or a single 30-mg intravenous (IV) infusion.
Route of Administration: Other
In Vitro Use Guide
Rabbit thoracic aorta cells were incubated with different concentrations of fimasartan ((0.1, 1, 10 nM). At those concentrations fimasartan caused nonparallel rightward shifts in the concentration–contractile response curve to Ang II with a significant reduction in the maximal contractile response to 96.6, 47 and 18%, respectively.
Substance Class Chemical
Created
by admin
on Fri Dec 15 16:10:35 GMT 2023
Edited
by admin
on Fri Dec 15 16:10:35 GMT 2023
Record UNII
P58222188P
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
FIMASARTAN
INN   WHO-DD  
INN  
Official Name English
BR1015 component fimasartan
Common Name English
fimasartan [INN]
Common Name English
2-((2-BUTYL-4-METHYL-6-OXO-1-((2'-(1H-TETRAZOL-5-YL)BIPHENYL-4-YL)METHYL)-1,6-DIHYDROPYRIMIDIN-5-YL))-N,N-DIMETHYLTHIOACETAMIDE
Systematic Name English
Fimasartan [WHO-DD]
Common Name English
Classification Tree Code System Code
WHO-ATC C09DA10
Created by admin on Fri Dec 15 16:10:35 GMT 2023 , Edited by admin on Fri Dec 15 16:10:35 GMT 2023
WHO-ATC C09CA10
Created by admin on Fri Dec 15 16:10:35 GMT 2023 , Edited by admin on Fri Dec 15 16:10:35 GMT 2023
NCI_THESAURUS C66930
Created by admin on Fri Dec 15 16:10:35 GMT 2023 , Edited by admin on Fri Dec 15 16:10:35 GMT 2023
Code System Code Type Description
ChEMBL
CHEMBL1951143
Created by admin on Fri Dec 15 16:10:35 GMT 2023 , Edited by admin on Fri Dec 15 16:10:35 GMT 2023
PRIMARY
MESH
C558933
Created by admin on Fri Dec 15 16:10:35 GMT 2023 , Edited by admin on Fri Dec 15 16:10:35 GMT 2023
PRIMARY
EPA CompTox
DTXSID80179460
Created by admin on Fri Dec 15 16:10:35 GMT 2023 , Edited by admin on Fri Dec 15 16:10:35 GMT 2023
PRIMARY
EVMPD
SUB75858
Created by admin on Fri Dec 15 16:10:35 GMT 2023 , Edited by admin on Fri Dec 15 16:10:35 GMT 2023
PRIMARY
SMS_ID
100000137528
Created by admin on Fri Dec 15 16:10:35 GMT 2023 , Edited by admin on Fri Dec 15 16:10:35 GMT 2023
PRIMARY
WIKIPEDIA
Fimasartan
Created by admin on Fri Dec 15 16:10:35 GMT 2023 , Edited by admin on Fri Dec 15 16:10:35 GMT 2023
PRIMARY
PUBCHEM
9870652
Created by admin on Fri Dec 15 16:10:35 GMT 2023 , Edited by admin on Fri Dec 15 16:10:35 GMT 2023
PRIMARY
CAS
247257-48-3
Created by admin on Fri Dec 15 16:10:35 GMT 2023 , Edited by admin on Fri Dec 15 16:10:35 GMT 2023
PRIMARY
FDA UNII
P58222188P
Created by admin on Fri Dec 15 16:10:35 GMT 2023 , Edited by admin on Fri Dec 15 16:10:35 GMT 2023
PRIMARY
INN
8678
Created by admin on Fri Dec 15 16:10:35 GMT 2023 , Edited by admin on Fri Dec 15 16:10:35 GMT 2023
PRIMARY
DRUG CENTRAL
4906
Created by admin on Fri Dec 15 16:10:35 GMT 2023 , Edited by admin on Fri Dec 15 16:10:35 GMT 2023
PRIMARY
NCI_THESAURUS
C81417
Created by admin on Fri Dec 15 16:10:35 GMT 2023 , Edited by admin on Fri Dec 15 16:10:35 GMT 2023
PRIMARY
DRUG BANK
DB09279
Created by admin on Fri Dec 15 16:10:35 GMT 2023 , Edited by admin on Fri Dec 15 16:10:35 GMT 2023
PRIMARY
Related Record Type Details
Structure of FIMASARTAN POTASSIUM TRIHYDRATE
SALT/SOLVATE -> PARENT
Structure of FIMASARTAN POTASSIUM ANHYDROUS
SALT/SOLVATE -> PARENT
TYPE-1 ANGIOTENSIN II RECEPTOR
TARGET -> INHIBITOR
Related Record Type Details
Structure of FIMASARTAN
ACTIVE MOIETY
NIH
NCATS
PRIVACY ACT
ACCESSIBILITY
DISCLAIMER
HHS VULNERABILITY DISCLOSURE
For language access assistance, contact the NCATS Public Information Officer
National Center for Advancing Translational Sciences (NCATS),
6701 Democracy Boulevard, Bethesda MD 20892-4874 • 301-594-8966