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fimasartan

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Description

fimasartan: an angiotensin II receptor antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9870652
CHEMBL ID1951143
CHEBI ID136044
SCHEMBL ID2229436
SCHEMBL ID20126833
MeSH IDM0558574

Synonyms (43)

Synonym
L019170
CHEBI:136044
fimasartan
bdbm50364573
AKOS016011331
CHEMBL1951143 ,
kanarb
247257-48-3
fimasartan [inn]
p58222188p ,
br-a-657.k
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)-
unii-p58222188p
S4975
fimasartan [who-dd]
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
CS-3509
SCHEMBL2229436
fimasartan (inn)
D10556
AC-30631
HY-B0780
2-(1-((2'-(2h-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2-butyl-4-methyl-6-oxo-1,6-dihydropyrimidin-5-yl)-n,n-dimethylethanethioamide
DTXSID80179460
br-a657
DB09279
mfcd13194795
2-[2-butyl-4-methyl-6-oxo-1-[[4-[2-(2h-tetrazol-5-yl)phenyl]phenyl]methyl]pyrimidin-5-yl]-n,n-dimethylethanethioamide
NCGC00390600-01
AS-35179
EX-A3997
BCP11616
Q8563179
SCHEMBL20126833
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]-
CCG-269705
2-(2-butyl-4-methyl-6-oxo-1-{[2'-(1h-tetrazol-5-yl)-4-biphenylyl]methyl}-1,6-dihydro-5-pyrimidinyl)-n,n-dimethylethanethioamide
ZB1816
AKOS037643761
2-butyl-5-dimethylaminothiocarbonylmethyl-6-methyl-3-[[2'-(1h-tetrazol-5-yl)biphenyl-4-yl]methyl]pyrimidin-4(3h)-one
A919293
2-(1-((2'-(1h-tetrazol-5-yl)biphenyl-4-yl)methyl)-2-butyl-4-methyl-6-oxo-1,6-dihydropyrimidin-5-yl)-n,n-dimethylethanethioamide
2-[2-butyl-4-methyl-6-oxo-1-[[4-[2-(2h-tetrazol-5-yl)phenyl]phenyl]met hyl]pyrimidin-5-yl]-n,n-dimethylethanethioamide

Research Excerpts

Overview

Fimasartan is an angiotensin type 1 receptor blocker (ARB) which has comparable efficacy and tolerability with other ARBs. It is a derivative of losartan in which the imidazole ring has been replaced. Fim asartan may have protective effects during myocardial infarction or atherosclerosis.

ExcerptReferenceRelevance
"Fimasartan is a novel angiotensin II receptor blocker. "( Characterizing the time-course of antihypertensive activity and optimal dose range of fimasartan via mechanism-based population modeling.
Bulitta, JB; Chi, YH; Jiao, Y; Kim, TH; Landersdorfer, CB; Paik, SH; Shin, BS; Shin, S; Yadav, R, 2017
)
2.12
"Fimasartan is an angiotensin type 1 receptor blocker (ARB) which has comparable efficacy and tolerability with other ARBs. "( 24-Hour blood pressure response to lower dose (30 mg) fimasartan in Korean patients with mild to moderate essential hypertension.
Chae, SC; Jeong, MH; Kim, CH; Kim, DS; Lee, HY; Oh, BH; Song, JK, 2017
)
2.15
"Fimasartan is a derivative of losartan in which the imidazole ring has been replaced."( PK/PD evaluation of fimasartan for the treatment of hypertension Current evidences and future perspectives.
Angeli, F; Pane, M; Reboldi, G; Signorotti, S; Trapasso, M; Verdecchia, P, 2018
)
1.53
"Fimasartan is a new non-peptide angiotensin II receptor blocker with a selective type I receptor blocking effect."( Fimasartan versus perindopril with and without diuretics in the treatment of elderly patients with essential hypertension (Fimasartan in the Senior Subjects (FITNESS)): study protocol for a randomized controlled trial.
Chae, SC; Choi, YJ; Chun, KJ; Ihm, SH; Jeon, ES; Jeong, JO; Kang, MG; Kim, CH; Kim, EJ; Kim, KI; Kim, MH; Kim, SH; Kim, SJ; Kim, SY; Lee, HY; Lee, SY; Park, S; Park, YH; Pyun, WB; Rhee, MY; Shin, J; Sohn, IS; Song, JM; Sung, KC; Yoo, KD, 2019
)
2.68
"1. Fimasartan is an angiotensin receptor II antagonist used to treat patients with hypertension. "( Glucuronidation of fimasartan, a new angiotensin receptor antagonist, is mainly mediated by UGT1A3.
Chi, YH; Jeong, ES; Kim, DH; Kim, HJ; Kim, KH; Kim, YW; Paik, SH; Shin, HJ; Shin, JG, 2015
)
1.37
"Fimasartan is a novel angiotensin II receptor blocker. "( Effect of renal function on the pharmacokinetics of fimasartan: a single-dose, open-label, Phase I study.
Jang, IJ; Kim, S; Kim, YS; Lee, J; Lim, KS; Shin, D; Yu, KS, 2014
)
2.1
"Fimasartan is a newly developed angiotensin receptor blocker, which may have protective effects during myocardial infarction or atherosclerosis. "( Effect of Long-Term Treatment with Fimasartan on Transient Focal Ischemia in Rat Brain.
Choi, IY; Jang, H; Jeong, HG; Kim, CK; Kim, D; Kim, TJ; Kim, YJ; Ko, SB; Park, HK; Yang, XL; Yoon, BW, 2015
)
2.14
"Fimasartan is a novel angiotensin II receptor blocker with strong anti-hypertensive activity. "( Fully Validated Ultra-performance Liquid Chromatography-Tandem Mass Spectrometry Method for the Determination of Fimasartan in Human Plasma.
Gwon, MR; Hyun, JY; Kim, HJ; Lee, HW; Seong, SJ; Yoon, YR, 2015
)
2.07
"Fimasartan (FMS) is a potent angiotensin receptor blocker for the treatment of mild to moderate hypertension. "( Placental transfer and mammary excretion of a novel angiotensin receptor blocker fimasartan in rats.
Bulitta, JB; Chi, YH; Jeong, SW; Joo, SH; Kim, MG; Kim, TH; Lee, JH; Paik, SH; Shin, BS; Shin, S; Weon, KY; Yoo, SD; Youn, YS, 2016
)
2.1
"Fimasartan (BR-A-657) is a new angiotensin II receptor antagonist used as antihypertensive agent. "( Pharmacokinetic interaction of fimasartan, a new angiotensin II receptor antagonist, with amlodipine in healthy volunteers.
Cho, JY; Jang, IJ; Kim, TE; Shin, SG; Yi, S; Yoon, SH; Yu, KS, 2011
)
2.1
"Fimasartan (BR-A-657) is an angiotensin II receptor antagonist, recently approved as an antihypertensive agent."( Effect of multiple doses of fimasartan, an angiotensin II receptor antagonist, on the steady-state pharmacokinetics of digoxin in healthy volunteers.
Cho, JY; Choi, J; Jang, IJ; Jun, YK; Kim, J; Kim, JW; Kim, TE; Shin, SG; Song, SH; Yi, S; Yoon, SH; Yu, KS, 2011
)
2.11
"Fimasartan (BR-A-657) is a novel, non-peptide angiotensin II receptor antagonist with a selective type I receptor blockade effect. "( Safety, tolerability, pharmacokinetics, and pharmacodynamics of fimasartan following single and repeated oral administration in the fasted and fed states in healthy subjects.
Chi, YH; Kim, JH; Kim, SL; Lee, H; Lee, JH; Paik, SH; Tan, HK; Yoo, BW, 2011
)
2.05
"Fimasartan is a selective angiotensin II receptor blocker. "( Assessment of the drug-drug interactions between fimasartan and hydrochlorothiazide in healthy volunteers.
Cho, JY; Jang, IJ; Jeon, H; Kim, J; Lim, KS; Shin, KH; Shin, SG; Yoon, SH; Yu, KS, 2012
)
2.08
"Fimasartan is a newly developed ARB that has not been compared with other ARBs with regard to its efficacy and tolerability."( 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-w
Kim, JJ; Kim, SK; Kim, YJ; Lee, HY; Lee, SE; Oh, BH; Park, CG; Rhee, MY; Yang, HM, 2012
)
1.39
"Fimasartan is a selective angiotensin II receptor blocker developed for once-daily dosing."( Efficacy and tolerability of once-daily oral fimasartan 20 to 240 mg/d in Korean Patients with hypertension: findings from Two Phase II, randomized, double-blind, placebo-controlled studies.
Choi, DJ; Ha, JW; Jeon, ES; Kim, JJ; Lee, H; Lee, HY; Oh, BH; Park, JB; Rim, SJ; Seung, KB; Shin, JH; Yang, HM, 2012
)
2.08
"Fimasartan is a non-peptide angiotensin II receptor antagonist which selectively blocks the AT(1) receptor. "( Pharmacokinetic-pharmacodynamic model of fimasartan applied to predict the influence of a high fat diet on its blood pressure-lowering effect in healthy subjects.
Han, S; Hong, T; Jeon, S; Lee, J; Yim, DS, 2013
)
2.1
"Fimasartan is an angiotensin II receptor antagonist used to treat hypertension."( The effect of fimasartan, an angiotensin receptor type 1 blocker, on the pharmacokinetics and pharmacodynamics of warfarin in healthy Korean male volunteers: a one-sequence, two-period crossover clinical trial.
Cho, JY; Gu, N; Jang, IJ; Kim, BH; Kim, SE; Lim, KS; Nam, WS; Shin, SG; Yoon, SH; Yu, KS, 2012
)
2.18
"Fimasartan is a new angiotensin receptor blocker, and the first new molecular entity acting on cardiovascular system approved by Korean Food and Drug Administration for the treatment of essential hypertension in September 2010."( Fimasartan, a novel angiotensin II receptor antagonist.
Chi, YH; Kim, JH; Lee, JH; Paik, SH, 2012
)
2.54

Effects

ExcerptReferenceRelevance
"Fimasartan has been approved for use in patients with hypertension in South Korea and has been evaluated in three phase III clinical trials (i.e."( Fimasartan.
, 2011
)
2.53

Actions

ExcerptReferenceRelevance
"Fimasartan can cause headache, dizziness, itching, and coughing."( Fimasartan-induced liver injury in a patient with no adverse reactions on other types of angiotensin II receptor blockers: A case report.
Eun, HS; Joo, JS; Kang, SH; Kim, JS; Kim, KH; Kim, SH; Lee, BS; Lee, ES; Moon, HS; Park, DH; Yun, GY, 2017
)
2.62

Treatment

Fimasartan significantly increased median (range) homeostatic assessment of β-cell function values. insulinogenic index at 60 minutes (19.7 [3.0-131.2] vs 15.0 [2.4-103.8] pmol/mmol) compared with those with amlodipine (all P < .05) acute insulin response and insulin resistance indices were similar for both agents.

ExcerptReferenceRelevance
"Fimasartan-treated group: rats pretreated with Fimasartan a dose of 3 mg/kg IP; this was half hour before occluding the renal pedicles."( Fimasartan ameliorates renal ischemia reperfusion injury via modulation of oxidative stress, inflammatory and apoptotic cascades in a rat model.
Abbas, L; Abbas, W; Altemimi, M; Hadi, N; Hameed, AA; Jabir, M; Qassam, H; Zigam, Q, 2022
)
2.89
"Fimasartan 120-mg treatment demonstrated superior efficacy in reduction of SiSBP, SiDBP, and 24 hrs ASBP and ADBP compared to valsartan 160 mg. "( Effect of Fimasartan versus Valsartan and Olmesartan on Office and Ambulatory Blood Pressure in Korean Patients with Mild-to-Moderate Essential Hypertension: A Randomized, Double-Blind, Active Control, Three-Parallel Group, Forced Titration, Multicenter,
Chang, K; Chung, WB; Her, SH; Ihm, SH; Jang, SW; Jeon, DS; Lee, JM; Park, CS; Seung, KB; Yoo, KD, 2020
)
2.4
"Fimasartan treatment significantly increased median (range) homeostatic assessment of β-cell function values (49.9 [22.5-174.4] vs 46.9 [15.6-148.0]), area under the curve of insulin during OGTT (27 284 [9501-94 525] vs 26 818 [8112-76 704] pmol/L × min), insulinogenic index at 60 minutes (19.7 [3.0-131.2] vs 15.0 [2.4-103.8] pmol/mmol) and at 120 minutes (19.1 [1.9-85.5] vs 12.6 [-4.3-178.8] pmol/mmol) compared with those with amlodipine (all P < .05); however, acute insulin response and insulin resistance indices were similar for both agents."( Fimasartan increases glucose-stimulated insulin secretion in patients with type 2 diabetes and hypertension compared with amlodipine.
Ahn, CH; Cho, YM; Jung, HS; Kim, S; Kwak, SH; Lee, SO; Lim, MH; Mari, A; Park, KS; Roh, E; Yang, YS, 2018
)
2.64
"Fimasartan pretreatment remarkably reduced the rate of MI and improved cardiac performance well after I/R (n = 9/group). "( Effects of the novel angiotensin II receptor type I antagonist, fimasartan on myocardial ischemia/reperfusion injury.
Cho, GY; Choi, DJ; Han, J; Jeon, ES; Kim, EJ; Kim, HK; Kim, N; Lee, SR; Long, le T; Park, SJ; Park, SW; Thu, VT; Yoon, CH, 2013
)
2.07
"The fimasartan/HCTZ treatment group showed a greater reduction of siDBP compared to the fimasartan treatment group at Week 4 (6.88±8.10 mmHg vs 3.38±7.33, P=0.0008), and the effect persisted at Week 8 (8.67±9.39 mmHg vs 5.02±8.27 mmHg, P=0.0023)."( Efficacy of fimasartan/hydrochlorothiazide combination in hypertensive patients inadequately controlled by fimasartan monotherapy.
Ahn, Y; Baek, SH; Chae, JK; Doh, JH; Ha, JW; Kim, CH; Kim, JJ; Kim, SH; Kim, SK; Kim, W; Oh, BH; Park, CG; Park, JB; Park, SW; Rhee, MY; Rim, SJ; Shin, JH; Yoo, BS, 2015
)
1.28
"Fimasartan treatment inhibited RAS activation and the expression of Nox1, Nox2, and Nox4."( Fimasartan, a Novel Angiotensin-Receptor Blocker, Protects against Renal Inflammation and Fibrosis in Mice with Unilateral Ureteral Obstruction: the Possible Role of Nrf2.
Choi, BS; Chung, S; Kim, S; Kim, SJ; Park, CW; Shin, SJ; Yoon, HE, 2015
)
2.58
"Pretreated fimasartan significantly decreased hemolysate-induced phosphorylation of Akt and ERK1/2."( Anti-inflammatory effects of fimasartan via Akt, ERK, and NFκB pathways on astrocytes stimulated by hemolysate.
Jang, H; Kim, CK; Kim, TJ; Kim, YJ; Ko, SB; Rim, D; Sun, J; Yang, XL; Yoon, BW, 2016
)
1.09

Toxicity

Fimasartan/amlodipine combination therapy exhibited superior efficacy in reducing blood pressure, with no increase in adverse drug reactions. During the study period, 82 adverse events were reported in 52 patients, 40 in the fim asartan group and 42 in the perindopril group (P = 0.0).

ExcerptReferenceRelevance
"Fimasartan was safe and well tolerated, but with an increased incidence of low BP and postural dizziness for the 360 mg dose after repeated administration."( Safety, tolerability, pharmacokinetics, and pharmacodynamics of fimasartan following single and repeated oral administration in the fasted and fed states in healthy subjects.
Chi, YH; Kim, JH; Kim, SL; Lee, H; Lee, JH; Paik, SH; Tan, HK; Yoo, BW, 2011
)
2.05
"The safety, efficacy, and compliance of fimasartan were found to be excellent in a large patient population that included patients potentially at higher risk for adverse events."( Safety and efficacy of fimasartan in patients with arterial hypertension (Safe-KanArb study): an open-label observational study.
Cho, EJ; Kang, SM; Park, JB; Sung, KC, 2013
)
0.97
" However, there was no significant difference in time to peak plasma concentration (t(max)) and elimination half-life, and there were no serious or severe adverse events in all subjects."( Influence of hepatic dysfunction on the pharmacokinetics and safety of fimasartan.
Ahn, SH; Cho, CM; Kim, CO; Kim, DY; Lee, HW; Lee, J; Oh, ES; Park, MS; Seong, SJ; Yoon, YR, 2013
)
0.62
"The standard 60-mg dose of fimasartan, a newly developed selective angiotensin II receptor blocker, is effective and safe for use in patients with mild to moderate hypertension."( Efficacy and safety of 30-mg fimasartan for the treatment of patients with mild to moderate hypertension: an 8-week, multicenter, randomized, double-blind, phase III clinical study.
Bae, JH; Ihm, SH; Jeon, DW; Joo, SJ; Jung, BC; Jung, IH; Kang, SM; Lee, NH; Park, SM; Park, TH; Park, WJ; Pyun, WB; Shin, ES; Shin, JH; Song, JM; Sung, KC; Yoon, YW; Youn, JC, 2014
)
0.99
" Most treatment-emergent adverse events (TEAEs) were mild (89 of 95), and there were no serious TEAEs."( Efficacy and safety of 30-mg fimasartan for the treatment of patients with mild to moderate hypertension: an 8-week, multicenter, randomized, double-blind, phase III clinical study.
Bae, JH; Ihm, SH; Jeon, DW; Joo, SJ; Jung, BC; Jung, IH; Kang, SM; Lee, NH; Park, SM; Park, TH; Park, WJ; Pyun, WB; Shin, ES; Shin, JH; Song, JM; Sung, KC; Yoon, YW; Youn, JC, 2014
)
0.69
" Treatment-emergent adverse events (AEs) were also assessed."( A Randomized, Multicenter, Double-blind, Placebo-controlled, 3 × 3 Factorial Design, Phase II Study to Evaluate the Efficacy and Safety of the Combination of Fimasartan/Amlodipine in Patients With Essential Hypertension.
Ahn, T; Ahn, Y; Bae Park, J; Cho, EJ; Choi, DJ; Chull Chae, S; Chun, KJ; Han, KR; Hyon, MS; Jeon, ES; Jeong, JO; Joo, SJ; Kim, DI; Kim, DS; Kim, JJ; Kim, KS; Kim, YJ; Kwan, J; Lee, HY; Oh, SK; Park, JS; Rhee, MY; Seog Seo, H; Shin, JH; Sung, KC; Yoo, BS; Youn, HJ, 2015
)
0.61
" Treatment-emergent adverse events were also assessed."( A Randomized, Double-blind, Multicenter, Phase III Study to Evaluate the Efficacy and Safety of Fimasartan/Amlodipine Combined Therapy Versus Fimasartan Monotherapy in Patients With Essential Hypertension Unresponsive to Fimasartan Monotherapy.
Cha, KS; Chae, SC; Chun, KJ; Ihm, SH; Il Kim, D; Jeong, JO; Joo, SJ; Kim, CH; Kim, DS; Kim, JJ; Kim, KH; Kim, KI; Kim, MH; Kim, YJ; Nam, CW; Park, S; Park, SM; Rhee, MY; Seo, HS; Shin, ES; Shin, J; Shin, MS; Sung, KC; Yoo, BS; Youn, HJ, 2016
)
0.65
" Adverse drug reactions were observed in 9 patients (6."( A Randomized, Double-blind, Multicenter, Phase III Study to Evaluate the Efficacy and Safety of Fimasartan/Amlodipine Combined Therapy Versus Fimasartan Monotherapy in Patients With Essential Hypertension Unresponsive to Fimasartan Monotherapy.
Cha, KS; Chae, SC; Chun, KJ; Ihm, SH; Il Kim, D; Jeong, JO; Joo, SJ; Kim, CH; Kim, DS; Kim, JJ; Kim, KH; Kim, KI; Kim, MH; Kim, YJ; Nam, CW; Park, S; Park, SM; Rhee, MY; Seo, HS; Shin, ES; Shin, J; Shin, MS; Sung, KC; Yoo, BS; Youn, HJ, 2016
)
0.65
"Fimasartan/amlodipine combination therapy exhibited superior efficacy in reducing blood pressure, with no increase in adverse drug reactions, compared with fimasartan monotherapy."( A Randomized, Double-blind, Multicenter, Phase III Study to Evaluate the Efficacy and Safety of Fimasartan/Amlodipine Combined Therapy Versus Fimasartan Monotherapy in Patients With Essential Hypertension Unresponsive to Fimasartan Monotherapy.
Cha, KS; Chae, SC; Chun, KJ; Ihm, SH; Il Kim, D; Jeong, JO; Joo, SJ; Kim, CH; Kim, DS; Kim, JJ; Kim, KH; Kim, KI; Kim, MH; Kim, YJ; Nam, CW; Park, S; Park, SM; Rhee, MY; Seo, HS; Shin, ES; Shin, J; Shin, MS; Sung, KC; Yoo, BS; Youn, HJ, 2016
)
2.1
" The most frequently reported adverse reactions included headache (3."( Safety and efficacy of fimasartan in Mexican patients with grade 1-2 essential hypertension.
Banda-Elizondo, RG; Cardona-Muñoz, EG; Conde-Carmona, I; Esturau-Santalo, RM; García-Castillo, A; González-Gálvez, G; Guerra-López, A; Leiva-Pons, JL; López-Alvarado, A; Pascoe-González, S; Sánchez-Mejorada, G; Velasco-Sánchez, RG; Vidrio-Velázquez, M; Villeda-Espinosa, E,
)
0.44
"Fimasartan is safe and effective in Mexican subjects with grade 1-2 essential hypertension."( Safety and efficacy of fimasartan in Mexican patients with grade 1-2 essential hypertension.
Banda-Elizondo, RG; Cardona-Muñoz, EG; Conde-Carmona, I; Esturau-Santalo, RM; García-Castillo, A; González-Gálvez, G; Guerra-López, A; Leiva-Pons, JL; López-Alvarado, A; Pascoe-González, S; Sánchez-Mejorada, G; Velasco-Sánchez, RG; Vidrio-Velázquez, M; Villeda-Espinosa, E,
)
1.88
" Adverse events (AE) were reported in 28."( Long-Term Safety of a Novel Angiotensin Receptor Blocker, Fimasartan, According to the Absence or Presence of Underlying Liver Disease in Korean Hypertensive Patients: A Prospective, 12-Month, Observational Study.
Choi, DJ; Joo, KW; Kim, MA; Kim, YJ; Lee, HY; Oh, GC, 2020
)
0.8
"Long-term use of fimasartan for treatment of HTN was associated with a low rate of adverse events overall, especially in the absence of underlying liver disease."( Long-Term Safety of a Novel Angiotensin Receptor Blocker, Fimasartan, According to the Absence or Presence of Underlying Liver Disease in Korean Hypertensive Patients: A Prospective, 12-Month, Observational Study.
Choi, DJ; Joo, KW; Kim, MA; Kim, YJ; Lee, HY; Oh, GC, 2020
)
1.14
" During the study period, 82 adverse events were reported in 52 patients, 40 in the fimasartan group and 42 in the perindopril group (P = 0."( A Randomized, Double-blind, Active-controlled, Two Parallel-Group, Optional Titration, Multicenter, Phase IIIb Study to Evaluate the Efficacy and Safety of Fimasartan Versus Perindopril Monotherapy With and Without a Diuretic Combination in Elderly Patien
Chae, SC; Choi, YJ; Chun, KJ; Ihm, SH; Jeon, ES; Jeong, JO; Kim, CH; Kim, EJ; Kim, KI; Kim, MH; Kim, SH; Kim, SJ; Kim, SY; Lee, HY; Lee, SY; Park, S; Park, YH; Pyun, WB; Rhee, MY; Shin, J; Sohn, IS; Song, JM; Sung, KC; Yoo, KD, 2021
)
1.04
" Furthermore, the odds ratio of adverse events for all agents did not differ significantly from that of the placebo."( Comparative efficacy and safety of fimasartan in patients with hypertension: A network meta-analysis of randomized controlled trials.
Ihm, SH; Jeong, SH; Kim, BS; Seo, SM; Yi, JE, 2022
)
1

Pharmacokinetics

The study aimed to develop a population pharmacokinetic model that can simultaneously characterize the extent and time-course of EHC in three species. The maximum plasma concentration (C(max), time to reach C(max) and elimination half-life for fimasartan did not differ significantly between the older and young groups.

ExcerptReferenceRelevance
" The maximum plasma concentration (C(max)), time to reach C(max) and elimination half-life for fimasartan did not differ significantly between the older and young groups."( Effect of age on the pharmacokinetics of fimasartan (BR-A-657).
Cho, JY; Lee, HW; Lee, J; Lim, MS; Park, J; Seo, JJ; Seong, SJ; Yoon, YR; Yu, KS, 2011
)
0.85
" The plasma concentrations of R- and S-warfarin were analyzed by using HPLC-MS/MS, and the pharmacokinetic parameters were estimated by using noncompartmental analysis."( The effect of fimasartan, an angiotensin receptor type 1 blocker, on the pharmacokinetics and pharmacodynamics of warfarin in healthy Korean male volunteers: a one-sequence, two-period crossover clinical trial.
Cho, JY; Gu, N; Jang, IJ; Kim, BH; Kim, SE; Lim, KS; Nam, WS; Shin, SG; Yoon, SH; Yu, KS, 2012
)
0.74
" Double peaks and extended terminal half-life were observed, which was likely caused by enterohepatic recirculation."( Pharmacokinetics and metabolite profiling of fimasartan, a novel antihypertensive agent, in rats.
Bashir, M; Bulitta, JB; Chi, YH; Choi, HJ; Choi, JH; Joo, SH; Kim, TH; Lee, JH; Ma, E; Paik, SH; Shin, BS; Shin, S; Yoo, SD, 2014
)
0.66
"Based on guidance from the United States Food and Drug Administration, a reduced pharmacokinetic (PK) study was conducted to evaluate the effect of renal function on the PK of fimasartan in patients with renal impairment and healthy volunteers."( Effect of renal function on the pharmacokinetics of fimasartan: a single-dose, open-label, Phase I study.
Jang, IJ; Kim, S; Kim, YS; Lee, J; Lim, KS; Shin, D; Yu, KS, 2014
)
0.85
" This study aimed to develop a population pharmacokinetic model that can simultaneously characterize the extent and time-course of EHC in three species using fimasartan, a novel angiotensin II receptor blocker, as a model drug."( Population Pharmacokinetic Modeling of the Enterohepatic Recirculation of Fimasartan in Rats, Dogs, and Humans.
Bulitta, JB; Chi, YH; Horkovics-Kovats, S; Kim, TH; Landersdorfer, CB; Myung, J; Paik, SH; Shin, BS; Shin, S; Yadav, R, 2015
)
0.84
" The Cmax (ng/ml) and AUC∞ (h · ng/ml) following oral and IV administration were 62."( Absolute bioavailability and pharmacokinetics of the angiotensin II receptor antagonist fimasartan in healthy subjects.
Chi, YH; Choi, HK; Ghim, JL; Hasanuzzaman, M; Kim, DH; Paik, SH; Shin, JG, 2016
)
0.66
"To build a physiologically based pharmacokinetic (PBPK) model for fimasartan, amlodipine, and hydrochlorothiazide, and to investigate the drug-drug interaction (DDI) potentials."( Physiologically Based Pharmacokinetic Modeling of Fimasartan, Amlodipine, and Hydrochlorothiazide for the Investigation of Drug-Drug Interaction Potentials.
Jeon, I; Kim, E; Lee, HA; Lee, S; Rhee, SJ; Song, IS; Yu, KS, 2018
)
0.97
"The predicted-to-observed ratios of all the pharmacokinetic parameters met the acceptance criterion."( Physiologically Based Pharmacokinetic Modeling of Fimasartan, Amlodipine, and Hydrochlorothiazide for the Investigation of Drug-Drug Interaction Potentials.
Jeon, I; Kim, E; Lee, HA; Lee, S; Rhee, SJ; Song, IS; Yu, KS, 2018
)
0.73
"A randomized, open-label, single-dose, two-treatment, two-way crossover study with a 7-day washout period was conducted to compare the pharmacokinetic (PK) characteristics and bioequivalence between an FDC of fimasartan/rosuvastatin and the separate co-administration of fimasartan and rosuvastatin in healthy Korean volunteers."( Pharmacokinetic and bioequivalence study comparing a fimasartan/rosuvastatin fixed-dose combination with the concomitant administration of fimasartan and rosuvastatin in healthy subjects.
Cho, S; Gwon, MR; Kang, WY; Kim, BK; Kim, EH; Lee, HW; Lee, KT; Ohk, B; Seong, SJ; Shim, WS; Yang, DH; Yoon, YR, 2018
)
0.92
" This study sought to evaluate the pharmacokinetic interactions between fimasartan and linagliptin after co-administration in healthy Korean subjects."( A Pharmacokinetic Drug Interaction Between Fimasartan and Linagliptin in Healthy Volunteers.
Cho, S; Gwon, MR; Kang, WY; Lee, HW; Lee, KT; Seong, SJ; Shim, WS; Yang, DH; Yoon, YR, 2020
)
1.05
"Our results suggest that there are no clinically significant pharmacokinetic interactions between fimasartan and linagliptin when co-administered."( A Pharmacokinetic Drug Interaction Between Fimasartan and Linagliptin in Healthy Volunteers.
Cho, S; Gwon, MR; Kang, WY; Lee, HW; Lee, KT; Seong, SJ; Shim, WS; Yang, DH; Yoon, YR, 2020
)
1.04

Compound-Compound Interactions

Fimasartan administered alone or in combination with HCTZ was well tolerated at the described dosages.

ExcerptReferenceRelevance
"Fimasartan administered alone or in combination with HCTZ was well tolerated at the described dosages."( Assessment of the drug-drug interactions between fimasartan and hydrochlorothiazide in healthy volunteers.
Cho, JY; Jang, IJ; Jeon, H; Kim, J; Lim, KS; Shin, KH; Shin, SG; Yoon, SH; Yu, KS, 2012
)
2.08
"To build a physiologically based pharmacokinetic (PBPK) model for fimasartan, amlodipine, and hydrochlorothiazide, and to investigate the drug-drug interaction (DDI) potentials."( Physiologically Based Pharmacokinetic Modeling of Fimasartan, Amlodipine, and Hydrochlorothiazide for the Investigation of Drug-Drug Interaction Potentials.
Jeon, I; Kim, E; Lee, HA; Lee, S; Rhee, SJ; Song, IS; Yu, KS, 2018
)
0.97

Bioavailability

The present study was conducted to determine the absolute bioavailability of fimasartan (FMS; Kanarb(®) after the single oral administration of a 60-mg tablet or a single 30-mg intravenous (IV) infusion. Subjects with mild hepatic impairment exhibited similar bioavailability compared with healthy subjects.

ExcerptReferenceRelevance
" Relative bioavailability decreased by 37 % when the subjects were given a high-fat diet."( Pharmacokinetic-pharmacodynamic model of fimasartan applied to predict the influence of a high fat diet on its blood pressure-lowering effect in healthy subjects.
Han, S; Hong, T; Jeon, S; Lee, J; Yim, DS, 2013
)
0.66
" Subjects with mild hepatic impairment exhibited similar bioavailability compared with healthy subjects, whereas subjects with moderate hepatic impairment seemed to exhibit a higher level of systemic exposure to fimasartan than healthy subjects."( Influence of hepatic dysfunction on the pharmacokinetics and safety of fimasartan.
Ahn, SH; Cho, CM; Kim, CO; Kim, DY; Lee, HW; Lee, J; Oh, ES; Park, MS; Seong, SJ; Yoon, YR, 2013
)
0.81
" Fimasartan was rapidly and extensively absorbed and had an oral bioavailability of 32."( Pharmacokinetics and metabolite profiling of fimasartan, a novel antihypertensive agent, in rats.
Bashir, M; Bulitta, JB; Chi, YH; Choi, HJ; Choi, JH; Joo, SH; Kim, TH; Lee, JH; Ma, E; Paik, SH; Shin, BS; Shin, S; Yoo, SD, 2014
)
1.57
" The relative bioavailability of fimasartan from the population PK analysis was 77% higher in the RI patients than in the healthy volunteers."( Effect of renal function on the pharmacokinetics of fimasartan: a single-dose, open-label, Phase I study.
Jang, IJ; Kim, S; Kim, YS; Lee, J; Lim, KS; Shin, D; Yu, KS, 2014
)
0.93
" The modeled oral bioavailability in rats (median (range), 38."( Population Pharmacokinetic Modeling of the Enterohepatic Recirculation of Fimasartan in Rats, Dogs, and Humans.
Bulitta, JB; Chi, YH; Horkovics-Kovats, S; Kim, TH; Landersdorfer, CB; Myung, J; Paik, SH; Shin, BS; Shin, S; Yadav, R, 2015
)
0.65
"The present study was conducted to determine the absolute bioavailability of fimasartan (FMS; Kanarb(®) ) after the single oral administration of a 60-mg tablet or a single 30-mg intravenous (IV) infusion."( Absolute bioavailability and pharmacokinetics of the angiotensin II receptor antagonist fimasartan in healthy subjects.
Chi, YH; Choi, HK; Ghim, JL; Hasanuzzaman, M; Kim, DH; Paik, SH; Shin, JG, 2016
)
0.89
" Fimasartan is rapidly absorbed following oral administration with an oral bioavailability of 18."( PK/PD evaluation of fimasartan for the treatment of hypertension Current evidences and future perspectives.
Angeli, F; Pane, M; Reboldi, G; Signorotti, S; Trapasso, M; Verdecchia, P, 2018
)
1.71
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
"Bioequivalence tests are fundamental step in assessing the equivalence in bioavailability between a test and reference product."( Multivariate Assessment for Bioequivalence Based on the Correlation of Random Effect.
An, H; Shin, D, 2021
)
0.62

Dosage Studied

Once-daily fimasartan effectively maintained a BP-reduction profile over the full 24-hour dosing interval. This profile was comparable to or slightly better than that of once-daily valsartan.

ExcerptRelevanceReference
" Blood samples were collected scheduled intervals for 24 hours after the last dosing to determine plasma concentrations of atorvastatin acid, atorvastatin lactone, 2-hydroxy atorvastatin acid, and 2-hydroxy atorvastatin lactone."( The effect of the newly developed angiotensin receptor II antagonist fimasartan on the pharmacokinetics of atorvastatin in relation to OATP1B1 in healthy male volunteers.
Cho, JY; Jang, IJ; Kim, SE; Kim, TE; Lee, MG; Shin, KH; Shin, SG; Song, IS; Yoon, SH; Yu, KS, 2011
)
0.6
" Further studies are needed to evaluate the safety, efficacy, and dose-response relationship of fimasartan in patients with hypertension."( Safety, tolerability, pharmacokinetics, and pharmacodynamics of fimasartan following single and repeated oral administration in the fasted and fed states in healthy subjects.
Chi, YH; Kim, JH; Kim, SL; Lee, H; Lee, JH; Paik, SH; Tan, HK; Yoo, BW, 2011
)
0.83
"To meet the regulatory requirements for approval of an antihypertensive treatment in Korea, this pair of studies was conducted to evaluate the efficacy and tolerability of fimasartan, to determine its dose-response relationship and minimum effective dose, and to characterize its blood pressure (BP)-reduction profile over the dosing interval."( Efficacy and tolerability of once-daily oral fimasartan 20 to 240 mg/d in Korean Patients with hypertension: findings from Two Phase II, randomized, double-blind, placebo-controlled studies.
Choi, DJ; Ha, JW; Jeon, ES; Kim, JJ; Lee, H; Lee, HY; Oh, BH; Park, JB; Rim, SJ; Seung, KB; Shin, JH; Yang, HM, 2012
)
0.83
"These 2 Phase II, randomized, double-blind, placebo-controlled, parallel-group, and dose-response studies enrolled male or nonchildbearing female Korean patients aged 18 to 65 years (study 1) or 18 to 70 years (study 2) with essential hypertension (sitting diastolic BP [DBP] 95-<115 mm Hg [study 1] or 90-<110 mm Hg [study 2])."( Efficacy and tolerability of once-daily oral fimasartan 20 to 240 mg/d in Korean Patients with hypertension: findings from Two Phase II, randomized, double-blind, placebo-controlled studies.
Choi, DJ; Ha, JW; Jeon, ES; Kim, JJ; Lee, H; Lee, HY; Oh, BH; Park, JB; Rim, SJ; Seung, KB; Shin, JH; Yang, HM, 2012
)
0.64
" Fimasartan 60 mg once daily was the minimum effective dose, and the dose-response relationship was flat at doses >60 mg once daily."( Efficacy and tolerability of once-daily oral fimasartan 20 to 240 mg/d in Korean Patients with hypertension: findings from Two Phase II, randomized, double-blind, placebo-controlled studies.
Choi, DJ; Ha, JW; Jeon, ES; Kim, JJ; Lee, H; Lee, HY; Oh, BH; Park, JB; Rim, SJ; Seung, KB; Shin, JH; Yang, HM, 2012
)
1.55
"The turnover PK-PD model combined with pre-defined cosine function for circadian rhythm described the BP changes measured within 24 h after dosing better than the effect compartment or transduction models."( Pharmacokinetic-pharmacodynamic model of fimasartan applied to predict the influence of a high fat diet on its blood pressure-lowering effect in healthy subjects.
Han, S; Hong, T; Jeon, S; Lee, J; Yim, DS, 2013
)
0.66
"Once-daily fimasartan effectively maintained a BP-reduction profile over the full 24-hour dosing interval; this profile was comparable to or slightly better than that of once-daily valsartan."( Ambulatory blood pressure response to once-daily fimasartan: an 8-week, multicenter, randomized, double-blind, active-comparator, parallel-group study in Korean patients with mild to moderate essential hypertension.
Chae, SC; Jeong, MH; Kim, DS; Kim, KS; Lee, H; Oh, BH, 2013
)
1.03
" Unlabeled fimasartan or radiolabeled [(14)C]fimasartan was dosed by intravenous injection or oral administration to rats."( Pharmacokinetics and metabolite profiling of fimasartan, a novel antihypertensive agent, in rats.
Bashir, M; Bulitta, JB; Chi, YH; Choi, HJ; Choi, JH; Joo, SH; Kim, TH; Lee, JH; Ma, E; Paik, SH; Shin, BS; Shin, S; Yoo, SD, 2014
)
1.05
" Treatments were administered for 12 weeks without dosage adjustment."( A Randomized, Double-blind, Candesartan-controlled, Parallel Group Comparison Clinical Trial to Evaluate the Antihypertensive Efficacy and Safety of Fimasartan in Patients with Mild to Moderate Essential Hypertension.
Cha, GS; Cha, TJ; Chae, SC; Chun, KJ; Hong, GR; Hur, SH; Hwang, JY; Kim, DI; Kim, DS; Kim, KS; Kim, MH; Lee, JH; Lee, SG; Yang, DH, 2016
)
0.63
" Fimasartan at a dosage range of 60-120 mg once daily showed an antihypertensive effect over 24 h."( Fimasartan: A New Angiotensin Receptor Blocker.
Lee, HY; Oh, BH, 2016
)
2.79
" Blood samples for pharmacokinetics were collected up to 48 hours for fimasartan and 72 hours for rosuvastatin after the last dosing and plasma concentrations of study drugs were determined by liquid chromatography-tandem mass spectrometry."( Evaluation of drug interactions between fimasartan and rosuvastatin after single and multiple doses in healthy Caucasians.
Lee, J; Lee, S; Rhee, SJ; Yu, KS, 2018
)
0.98
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
biphenylsBenzenoid aromatic compounds containing two phenyl or substituted-phenyl groups which are joined together by a single bond.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (7)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency37.90830.01237.983543.2770AID1645841
GVesicular stomatitis virusPotency9.52210.01238.964839.8107AID1645842
Interferon betaHomo sapiens (human)Potency9.52210.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency9.52210.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency9.52210.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency9.52210.01238.964839.8107AID1645842
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Type-1 angiotensin II receptorHomo sapiens (human)IC50 (µMol)0.00450.00020.09323.6000AID1420506
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (73)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of cell growthType-1 angiotensin II receptorHomo sapiens (human)
kidney developmentType-1 angiotensin II receptorHomo sapiens (human)
renin-angiotensin regulation of aldosterone productionType-1 angiotensin II receptorHomo sapiens (human)
maintenance of blood vessel diameter homeostasis by renin-angiotensinType-1 angiotensin II receptorHomo sapiens (human)
regulation of systemic arterial blood pressure by renin-angiotensinType-1 angiotensin II receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayType-1 angiotensin II receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayType-1 angiotensin II receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationType-1 angiotensin II receptorHomo sapiens (human)
Rho protein signal transductionType-1 angiotensin II receptorHomo sapiens (human)
positive regulation of macrophage derived foam cell differentiationType-1 angiotensin II receptorHomo sapiens (human)
regulation of vasoconstrictionType-1 angiotensin II receptorHomo sapiens (human)
calcium-mediated signalingType-1 angiotensin II receptorHomo sapiens (human)
positive regulation of phospholipase A2 activityType-1 angiotensin II receptorHomo sapiens (human)
low-density lipoprotein particle remodelingType-1 angiotensin II receptorHomo sapiens (human)
regulation of renal sodium excretionType-1 angiotensin II receptorHomo sapiens (human)
angiotensin-activated signaling pathwayType-1 angiotensin II receptorHomo sapiens (human)
regulation of cell population proliferationType-1 angiotensin II receptorHomo sapiens (human)
symbiont entry into host cellType-1 angiotensin II receptorHomo sapiens (human)
regulation of inflammatory responseType-1 angiotensin II receptorHomo sapiens (human)
positive regulation of inflammatory responseType-1 angiotensin II receptorHomo sapiens (human)
positive regulation of protein metabolic processType-1 angiotensin II receptorHomo sapiens (human)
cell chemotaxisType-1 angiotensin II receptorHomo sapiens (human)
phospholipase C-activating angiotensin-activated signaling pathwayType-1 angiotensin II receptorHomo sapiens (human)
blood vessel diameter maintenanceType-1 angiotensin II receptorHomo sapiens (human)
positive regulation of blood vessel endothelial cell proliferation involved in sprouting angiogenesisType-1 angiotensin II receptorHomo sapiens (human)
positive regulation of CoA-transferase activityType-1 angiotensin II receptorHomo sapiens (human)
positive regulation of reactive oxygen species metabolic processType-1 angiotensin II receptorHomo sapiens (human)
inflammatory responseType-1 angiotensin II receptorHomo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (22)

Processvia Protein(s)Taxonomy
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
angiotensin type I receptor activityType-1 angiotensin II receptorHomo sapiens (human)
angiotensin type II receptor activityType-1 angiotensin II receptorHomo sapiens (human)
protein bindingType-1 angiotensin II receptorHomo sapiens (human)
bradykinin receptor bindingType-1 angiotensin II receptorHomo sapiens (human)
protein heterodimerization activityType-1 angiotensin II receptorHomo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (22)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneType-1 angiotensin II receptorHomo sapiens (human)
membraneType-1 angiotensin II receptorHomo sapiens (human)
plasma membraneType-1 angiotensin II receptorHomo sapiens (human)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (37)

Assay IDTitleYearJournalArticle
AID1698000Apparent permeability in dog MDCKII-LE cells at pH 7.4
AID1698001Lipophilicity, log D of the compound at pH 7.4 by by shake flask method
AID1697999Dissociation constant, acidic pKa of compound measured up to 18 mins by capillary electrophoresis
AID1420506Antagonist activity at type-1 angiotensin 2 receptor (unknown origin) by calcium mobilizing assay2018Bioorganic & medicinal chemistry letters, 10-15, Volume: 28, Issue:19
Discovery of the bifunctional modulator of angiotensin II type 1 receptor (AT1R) and PPARγ derived from the AT1R antagonist, Fimasartan.
AID1698010Hepatic clearance in human administered through iv dosing
AID1698007Ratio of drug level in human blood to plasma administered through iv dosing by LC-MS/MS analysis
AID645200Antihypertensive activity in iv dosed pithed rat model assessed as inhibition of angiotensin 2-induced pressor response by gould pressure transducer-coupled grass polygraphy2012Bioorganic & medicinal chemistry letters, Feb-15, Volume: 22, Issue:4
Synthesis and antihypertensive activity of pyrimidin-4(3H)-one derivatives as losartan analogue for new angiotensin II receptor type 1 (AT1) antagonists.
AID1918193Dissociation constant, pKa of the compound2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
Identification of Organic Anion Transporter 2 Inhibitors: Screening, Structure-Based Analysis, and Clinical Drug Interaction Risk Assessment.
AID645204Antagonist activity at angiotensin 2 receptor type 1 in New Zealand White rabbit descending thoracic aorta rings assessed as inhibition of KCl-induced contraction preincubated for 30 mins prior KCl challenge2012Bioorganic & medicinal chemistry letters, Feb-15, Volume: 22, Issue:4
Synthesis and antihypertensive activity of pyrimidin-4(3H)-one derivatives as losartan analogue for new angiotensin II receptor type 1 (AT1) antagonists.
AID1698006Ratio of drug level in cynomolgus monkey blood to plasma administered through iv dosing by LC-MS/MS analysis
AID1420533Cmax in mouse at 20 mg/kg, po2018Bioorganic & medicinal chemistry letters, 10-15, Volume: 28, Issue:19
Discovery of the bifunctional modulator of angiotensin II type 1 receptor (AT1R) and PPARγ derived from the AT1R antagonist, Fimasartan.
AID1698016Dissociation constant, basic pKa of compound measured up to 18 mins by capillary electrophoresis
AID1420508Agonist activity at PPARgamma (unknown origin) at 1 uM relative to telmisartan2018Bioorganic & medicinal chemistry letters, 10-15, Volume: 28, Issue:19
Discovery of the bifunctional modulator of angiotensin II type 1 receptor (AT1R) and PPARγ derived from the AT1R antagonist, Fimasartan.
AID1420535AUClast in mouse at 20 mg/kg, po2018Bioorganic & medicinal chemistry letters, 10-15, Volume: 28, Issue:19
Discovery of the bifunctional modulator of angiotensin II type 1 receptor (AT1R) and PPARγ derived from the AT1R antagonist, Fimasartan.
AID645197Antagonist activity at angiotensin 2 receptor type 1 in New Zealand White rabbit descending thoracic aorta rings assessed as inhibition of angiotensin 2-induced contraction preincubated for 30 mins prior angiotensin 2 challenge2012Bioorganic & medicinal chemistry letters, Feb-15, Volume: 22, Issue:4
Synthesis and antihypertensive activity of pyrimidin-4(3H)-one derivatives as losartan analogue for new angiotensin II receptor type 1 (AT1) antagonists.
AID1420537Antihypertensive activity in angiotensin 2 induced hypertension rat model at 3 mg/kg, po measured until 8 hrs post dose2018Bioorganic & medicinal chemistry letters, 10-15, Volume: 28, Issue:19
Discovery of the bifunctional modulator of angiotensin II type 1 receptor (AT1R) and PPARγ derived from the AT1R antagonist, Fimasartan.
AID1918194Lipophilicity, log D of the compound2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
Identification of Organic Anion Transporter 2 Inhibitors: Screening, Structure-Based Analysis, and Clinical Drug Interaction Risk Assessment.
AID1698009Hepatic clearance in cynomolgus monkey at < 1 mg/kg, iv administered as cassette dosing
AID645202Ratio of losartan IC50 to compound IC50 for displacement of [125I]angiotensin 2 from angiotensin 2 receptor type 1 in Sprague-Dawley rat adrenal cortex membranes2012Bioorganic & medicinal chemistry letters, Feb-15, Volume: 22, Issue:4
Synthesis and antihypertensive activity of pyrimidin-4(3H)-one derivatives as losartan analogue for new angiotensin II receptor type 1 (AT1) antagonists.
AID1420540Antihypertensive activity in angiotensin 2 induced hypertension rat model assessed as time required for 50% reduction in blood pressure at 3 mg/kg, po2018Bioorganic & medicinal chemistry letters, 10-15, Volume: 28, Issue:19
Discovery of the bifunctional modulator of angiotensin II type 1 receptor (AT1R) and PPARγ derived from the AT1R antagonist, Fimasartan.
AID645205Antagonist activity at angiotensin 2 receptor type 1 in New Zealand White rabbit descending thoracic aorta rings assessed as inhibition of noradrenaline-induced contraction preincubated for 30 mins prior noradrenaline challenge2012Bioorganic & medicinal chemistry letters, Feb-15, Volume: 22, Issue:4
Synthesis and antihypertensive activity of pyrimidin-4(3H)-one derivatives as losartan analogue for new angiotensin II receptor type 1 (AT1) antagonists.
AID1698011Fraction unbound in human plasma
AID1420534AUClast in rat at 10 mg/kg, po2018Bioorganic & medicinal chemistry letters, 10-15, Volume: 28, Issue:19
Discovery of the bifunctional modulator of angiotensin II type 1 receptor (AT1R) and PPARγ derived from the AT1R antagonist, Fimasartan.
AID1698004Fraction unbound in cynomolgus monkey plasma
AID645203Ratio of losartan ED50 to compound ED50 for antihypertensive activity in iv dosed pithed rat model assessed as inhibition of angiotensin 2-induced pressor response2012Bioorganic & medicinal chemistry letters, Feb-15, Volume: 22, Issue:4
Synthesis and antihypertensive activity of pyrimidin-4(3H)-one derivatives as losartan analogue for new angiotensin II receptor type 1 (AT1) antagonists.
AID645201Ratio of losartan IC50 to compound IC50 for antagonist activity at angiotensin 2 receptor type 1 in New Zealand White rabbit descending thoracic aorta rings2012Bioorganic & medicinal chemistry letters, Feb-15, Volume: 22, Issue:4
Synthesis and antihypertensive activity of pyrimidin-4(3H)-one derivatives as losartan analogue for new angiotensin II receptor type 1 (AT1) antagonists.
AID1420530Half life in rat at 10 mg/kg, po2018Bioorganic & medicinal chemistry letters, 10-15, Volume: 28, Issue:19
Discovery of the bifunctional modulator of angiotensin II type 1 receptor (AT1R) and PPARγ derived from the AT1R antagonist, Fimasartan.
AID1918192Inhibition of human OAT2 tv.1 variant expressed in HEK293 cells assessed as inhibition of [3H]cGMP uptake by scintillation analysis2022Journal of medicinal chemistry, 11-10, Volume: 65, Issue:21
Identification of Organic Anion Transporter 2 Inhibitors: Screening, Structure-Based Analysis, and Clinical Drug Interaction Risk Assessment.
AID1420532Cmax in rat at 10 mg/kg, po2018Bioorganic & medicinal chemistry letters, 10-15, Volume: 28, Issue:19
Discovery of the bifunctional modulator of angiotensin II type 1 receptor (AT1R) and PPARγ derived from the AT1R antagonist, Fimasartan.
AID1698002Intrinsic clearance in cryopreserved human hepatocytes at 1 uM measured up to 120 mins by LC-MS/MS analysis
AID645198Displacement of [125I]angiotensin 2 from angiotensin 2 receptor type 1 in Sprague-Dawley rat adrenal cortex membranes after 60 mins by gamma counting2012Bioorganic & medicinal chemistry letters, Feb-15, Volume: 22, Issue:4
Synthesis and antihypertensive activity of pyrimidin-4(3H)-one derivatives as losartan analogue for new angiotensin II receptor type 1 (AT1) antagonists.
AID1420531Tmax in rat at 10 mg/kg, po2018Bioorganic & medicinal chemistry letters, 10-15, Volume: 28, Issue:19
Discovery of the bifunctional modulator of angiotensin II type 1 receptor (AT1R) and PPARγ derived from the AT1R antagonist, Fimasartan.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (90)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's71 (78.89)24.3611
2020's19 (21.11)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 53.32

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index53.32 (24.57)
Research Supply Index4.90 (2.92)
Research Growth Index4.55 (4.65)
Search Engine Demand Index85.35 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (53.32)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials42 (46.15%)5.53%
Reviews6 (6.59%)6.00%
Case Studies1 (1.10%)4.05%
Observational3 (3.30%)0.25%
Other39 (42.86%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]