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

Details

Stereochemistry ACHIRAL
Molecular Formula C27H30N7OS.K
Molecular Weight 539.737
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of FIMASARTAN POTASSIUM ANHYDROUS

SMILES

[K+].CCCCC1=NC(C)=C(CC(=S)N(C)C)C(=O)N1CC2=CC=C(C=C2)C3=CC=CC=C3C4=NN=N[N-]4

InChI

InChIKey=OCKQGXSJNJCCDO-UHFFFAOYSA-N
InChI=1S/C27H30N7OS.K/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;/q-1;+1

HIDE SMILES / InChI

Molecular Formula K
Molecular Weight 39.0983
Charge 1
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

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.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
0.13 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
KANARB

Approved Use

For the treatment of essential hypertension.

Launch Date

1.28329921E12
PubMed

PubMed

TitleDatePubMed
Pharmacokinetic interaction of fimasartan, a new angiotensin II receptor antagonist, with amlodipine in healthy volunteers.
2011 Jun
Effect of age on the pharmacokinetics of fimasartan (BR-A-657).
2011 Nov
Fimasartan, a novel angiotensin II receptor antagonist.
2012 Jul
Pharmacological characterization of BR-A-657, a highly potent nonpeptide angiotensin II receptor antagonist.
2013
Safety and efficacy of fimasartan in patients with arterial hypertension (Safe-KanArb study): an open-label observational study.
2013 Feb
Effect of renal function on the pharmacokinetics of fimasartan: a single-dose, open-label, Phase I study.
2014
The Efficacy of Fimasartan for Cardiovascular Events and Metabolic Syndrome (K-MetS Study): Rationale, Design and Participant Characteristics.
2014 May
Cardioprotective effect of fimasartan, a new angiotensin receptor blocker, in a porcine model of acute myocardial infarction.
2015 Jan
Patents

Sample Use Guides

Fimasartan is taken as a single oral dose of 60-mg tablet or a single 30-mg intravenous (IV) infusion.
Route of Administration: Other
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 Sat Dec 16 10:50:37 UTC 2023
Edited
by admin
on Sat Dec 16 10:50:37 UTC 2023
Record UNII
T2ICP7GBBN
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
FIMASARTAN POTASSIUM ANHYDROUS
Common Name English
5-PYRIMIDINEETHANETHIOAMIDE, 2-BUTYL-1,6-DIHYDRO-N,N,4-TRIMETHYL-6-OXO-1-((2'-(2H-TETRAZOL-5-YL)(1,1'-BIPHENYL)-4-YL)METHYL)-, POTASSIUM SALT (1:1)
Systematic Name English
Code System Code Type Description
FDA UNII
T2ICP7GBBN
Created by admin on Sat Dec 16 10:50:37 UTC 2023 , Edited by admin on Sat Dec 16 10:50:37 UTC 2023
PRIMARY
SMS_ID
100000168911
Created by admin on Sat Dec 16 10:50:37 UTC 2023 , Edited by admin on Sat Dec 16 10:50:37 UTC 2023
PRIMARY
PUBCHEM
71465067
Created by admin on Sat Dec 16 10:50:37 UTC 2023 , Edited by admin on Sat Dec 16 10:50:37 UTC 2023
PRIMARY
CAS
1402813-38-0
Created by admin on Sat Dec 16 10:50:37 UTC 2023 , Edited by admin on Sat Dec 16 10:50:37 UTC 2023
NON-SPECIFIC STOICHIOMETRY
Related Record Type Details
SOLVATE->ANHYDROUS
PARENT -> SALT/SOLVATE