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
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
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/22864732Curator'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
Sources: https://www.ncbi.nlm.nih.gov/pubmed/22864732
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
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL2094256 Sources: https://www.ncbi.nlm.nih.gov/pubmed/23811571 |
0.13 nM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | KANARB Approved UseFor the treatment of essential hypertension. Launch Date2010 |
PubMed
Title | Date | PubMed |
---|---|---|
Pharmacokinetic interaction of fimasartan, a new angiotensin II receptor antagonist, with amlodipine in healthy volunteers. | 2011 Jun |
|
Simultaneous determination of fimasartan, a novel antihypertensive agent, and its active metabolite in rat plasma by liquid chromatography-tandem mass spectrometry. | 2011 Nov |
|
Efficacy and tolerability of fimasartan, a new angiotensin receptor blocker, compared with losartan (50/100 mg): a 12-week, phase III, multicenter, prospective, randomized, double-blind, parallel-group, dose escalation clinical trial with an optional 12-week extension phase in adult Korean patients with mild-to-moderate hypertension. | 2012 Mar |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/26272450
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
Sources: https://www.ncbi.nlm.nih.gov/pubmed/23811571
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.
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100000168911
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1402813-38-0
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NON-SPECIFIC STOICHIOMETRY |
PARENT (SALT/SOLVATE)
SUBSTANCE RECORD