Page last updated: 2024-12-07

landiolol

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

Landiolol is a selective beta-1 adrenergic receptor antagonist with a rapid onset and short duration of action. It is synthesized via a multi-step process involving the coupling of a substituted phenyl ring to a chiral alcohol derivative. Landiolol is primarily used as an antihypertensive agent for the rapid control of blood pressure in patients with hypertension. Its short duration of action allows for quick adjustments to dosing based on the patient's response. Studies on landiolol have investigated its efficacy in various clinical settings, including hypertension, acute coronary syndromes, and cardiac surgery. The compound's unique properties make it an attractive option for patients requiring rapid and transient blood pressure control. The rapid onset and short duration of action are key advantages over other beta-blockers, allowing for precise control of blood pressure. Further research continues to explore its potential applications and clinical benefits.'

landiolol: structure given in first source; a highly cardioselective ultra short-acting beta-blocker [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID114905
CHEMBL ID1742466
CHEBI ID135809
SCHEMBL ID121446
MeSH IDM0354483

Synonyms (35)

Synonym
benzenepropanoic acid, 4-(2-hydroxy-3-((2-((4-morpholinylcarbonyl)amino)ethyl)amino)propoxy)-, (2,2-dimethyl-1,3-dioxolan-4-yl)methyl ester, (s-(r*,r*))-
ono-1101
(-)-((s)-2,2-dimethyl-1,3-dioxolan-4-yl)methyl p-((s)-2-hydroxy-3-((2-(4-morpholinecarboxamido)ethyl)amino)propoxy)hydrocinnamate
benzenepropanoic acid, 4-((2s)-2-hydroxy-3-((2-((4-morpholinylcarbonyl)amino)ethyl)amino)propoxy)-, ((4s)-2,2-dimethyl-1,3-dioxolan-4-yl)methyl ester
landiolol
(s-(r*,r*))-(2,2-dimethyl-1,3-dioxolan-4-yl)methyl 4-(2-hydroxy-3-((2-((4-morpholinylcarbonyl)amino)ethyl)amino)propoxy)benzenepropanoate
ono 1101
CHEBI:135809
[(4s)-2,2-dimethyl-1,3-dioxolan-4-yl]methyl 3-[4-[(2s)-2-hydroxy-3-[2-(morpholine-4-carbonylamino)ethylamino]propoxy]phenyl]propanoate
NCGC00182709-01
NCGC00182709-02
133242-30-5
landiolol [usan:inn]
62nwq924lh ,
unii-62nwq924lh
who 7516
ldll600
aop200704
aop-200704
ldll-600
CHEMBL1742466
AKOS015896630
(-)-2,2-dimethyl-1,3-dioxolan-4s-ylmethyl 3-[4-[3-[2-(morpholinocarbonylamino)ethylamino]-2s-hydroxypropoxy]phenyl]propionate
benzenepropanoic acid, 4-[(2s)-2-hydroxy-3-[[2-[(4-morpholinylcarbonyl)amino]ethyl]amino]propoxy]-, [(4s)-2,2-dimethyl-1,3-dioxolan-4-yl]methyl ester
landiolol [inn]
landiolol [who-dd]
landiolol [mi]
landiolol [usan]
[(4s)-2,2-dimethyl-1,3-dioxolan-4-yl]methyl 3-(4-{(2s)-2-hydroxy-3-[{2-[(morpholin-4-ylcarbonyl)amino]ethyl}amino]propoxy}phenyl)propanoate
SCHEMBL121446
DTXSID10158026
DB12212
Q6484656
cid 15034750
EX-A7978

Research Excerpts

Overview

Landiolol is an intravenous, selective beta-1-receptor blocking agent with rapid onset of action and ultra-short half-life. It has a predominant negative chronotropic and only mild negative inotropic effect without significant reduction of blood pressure.

ExcerptReferenceRelevance
"Landiolol is an intravenous, selective beta-1-receptor blocking agent with rapid onset of action and ultra-short half-life that has a predominant negative chronotropic and only mild negative inotropic effect without significant reduction of blood pressure."( The application of landiolol in the cardiovascular and intensive care
Fejér, C; Gellér, L; Kiss, B; Kovács, E; Merkely, B; Pilecky, D; Radics, P; Ruzsa, Z; Straub, É; Zima, E, 2022
)
1.77
"Landiolol is a new-generation beta-blocker with fast onset and short half-life."( Comparison of landiolol and amiodarone for the treatment of new-onset atrial fibrillation after cardiac surgery (FAAC) trial: study protocol for a randomized controlled trial.
Besnier, E; Briant, AR; Caspersen, E; Denisenko, A; Descamps, R; Fellahi, JL; Fischer, MO; Gaudard, P; Guinot, PG; Hanouz, JL; Lorne, E; Mahjoub, Y; Mongardon, N; Moussa, MD; Oilleau, JF; Parienti, JJ; Paul, LPS; Rozec, B; Tomadesso, C, 2023
)
1.99
"Landiolol is an ultra-short-acting beta-antagonist known to prevent postoperative atrial fibrillation."( Association Between Intraoperative Landiolol Use and In-Hospital Mortality After Coronary Artery Bypass Grafting: A Nationwide Observational Study in Japan.
Fushimi, K; Ikumi, S; Iwasaki, Y; Kaiho, Y; Nakajima, M; Ohbe, H; Sasabuchi, Y; Yamauchi, M; Yasunaga, H, 2023
)
1.91
"Landiolol is an ultrashort-acting beta-blocker with high beta-1 receptor affinity and less blood pressure-lowering properties than other beta-blockers available for intravenous use in Germany. "( Cost-Effectiveness Analysis of Landiolol, an Ultrashort-Acting Beta-Blocker, for Prevention of Postoperative Atrial Fibrillation for the Germany Health Care System.
Heringlake, M; Walter, E, 2020
)
2.29
"Landiolol is a recently innovated ultra-short-acting beta-blocker with 251-fold β1/β2 selectivity, which was originally indicated only to control peri-operative supra-ventricular tachyarrhythmia by 2013 in Japan."( Novel rate control strategy with landiolol in patients with cardiac dysfunction and atrial fibrillation.
Imamura, T; Kinugawa, K, 2020
)
1.56
"Landiolol hydrochloride is a novel, ultra-short-acting β-blocker recently developed in Japan."( Effects of landiolol hydrochloride on intractable tachyarrhythmia after pediatric cardiac surgery.
Abe, M; Hiramatsu, Y; Horigome, H; Kanemoto, S; Sakakibara, Y; Takahashi-Igari, M; Tokunaga, C, 2013
)
1.5
"Landiolol (Onoact(®)) is an intravenously administered, ultra short-acting β1-blocker with an elimination half-life of 3-4 min and ≈8-fold greater cardioselectivity than esmolol in vitro. "( Landiolol: a review of its use in intraoperative and postoperative tachyarrhythmias.
Plosker, GL, 2013
)
3.28
"Landiolol is an ultra-short-acting β-blocker that appears to be more cardioselective and less toxic than esmolol. "( Pharmacokinetics, pharmacodynamics, and safety of landiolol hydrochloride in healthy Chinese subjects.
Hua, W; Huang, M; Wang, H; Wang, M; Zhang, Q; Zhou, W, 2014
)
2.1
"Landiolol hydrochloride is an intravenous β1-blocker with a very short half-life."( Dose-finding study of landiolol hydrochloride: a short-acting β1-blocker for controlling heart rate during coronary computed-tomography angiography in Japan.
Hamada, C; Hara, K; Hirano, M; Iino, M; Ikari, Y; Jinzaki, M; Kuribayashi, S, 2013
)
1.43
"Landiolol is an ultra-short acting beta-blocker, and some randomized controlled trials of landiolol administration for the prevention of POAF have been conducted in Japan."( Perioperative landiolol administration reduces atrial fibrillation after cardiac surgery: A meta-analysis of randomized controlled trials.
Hamasaki, T; Kitakaze, M; Sakamoto, A, 2014
)
1.48
"Landiolol is an ultra-short-acting β1-selective blocker whose effect on tachyarrhythmia after TCPC is unclear."( Effects of landiolol on refractory tachyarrhythmia after total cavopulmonary connection: a retrospective, observational, cohort study.
Fujita, Y; Miyake, K; Miyazu, M; Sento, Y; Sobue, K; Tomita, M; Yoshimura, S; Yoshizawa, S, 2016
)
1.55
"Landiolol is a more recent addition."( Comparison of the β-Adrenergic Receptor Antagonists Landiolol and Esmolol: Receptor Selectivity, Partial Agonism, and Pharmacochaperoning Actions.
Freissmuth, M; Nanoff, C; Nasrollahi-Shirazi, S; Sucic, S; Yang, Q, 2016
)
1.41
"Landiolol hydrochloride is a newly developed ultra short-acting selective beta1-blocker with a half-life of approximately 4 minutes."( [Clinical evaluation of landiolol hydrochloride, an ultra short-acting beta-blocker].
Kasuya, S; Kikuchi, C; Saito, N; Tanaka, S, 2008
)
1.37
"Landiolol is an ultra-short-acting beta(1)-adrenergic receptor blocking agent that is used for both perioperative and postoperative patients with tachycardia during general anesthesia. "( Validation of HPLC-UV methods for quantitatively determining landiolol and its major metabolite in human blood.
Hashimoto, Y; Miyata, Y; Nago, S; Shibakawa, K; Tsunekawa, M, 2009
)
2.04
"Landiolol hydrochloride is a newly developed cardioselective, ultra short-acting beta(1)-adrenergic receptor blocking agent used for perioperative arrhythmia control. "( Population pharmacokinetics of landiolol hydrochloride in healthy subjects.
Hasegawa, C; Hashimoto, Y; Honda, N; Kasai, H; Kikawa, S; Kitagawa, J; Kunisawa, T; Miyata, Y; Nakade, S; Ohno, T; Tanigawara, Y; Yamauchi, A, 2008
)
2.07
"Landiolol is a newly developed ultrashort-acting beta-adrenoceptor antagonist with a half-life of 3 min that is eight times more cardioselective than esmolol."( Effect of low-dose landiolol, an ultrashort-acting beta-blocker, on postoperative atrial fibrillation after CABG surgery.
Fujiwara, H; Kawamura, T; Namai, A; Sakurai, M, 2009
)
1.4
"Landiolol is a recently developed, selective short-acting beta1-antagonist. "( The efficacy of landiolol for suppressing the hyperdynamic response following laryngoscopy and tracheal intubation: a systematic review.
Furuya, H; Inoue, S; Kawaguchi, M; Tanaka, Y, 2009
)
2.14
"Landiolol is a new ultra-short-acting beta 1-selective adrenoreceptor antagonist, which is metabolized rapidly by plasma cholinesterase (PCHE). "( Metoclopramide does not prolong duration of action of landiolol attenuating the hemodynamic response to induction of anesthesia and tracheal intubation.
Abe, R; Furuya, H; Inoue, S; Kawaguchi, M; Kobayashi, H, 2010
)
2.05
"Landiolol is an ultra-short-acting β-blocker that has less effect on blood pressure, but little is known about its efficacy and safety for patients with AMI undergoing primary percutaneous coronary intervention (PCI)."( Randomized study on the efficacy and safety of landiolol, an ultra-short-acting β1-adrenergic blocker, in patients with acute myocardial infarction undergoing primary percutaneous coronary intervention.
Abe, N; Hanada, K; Higuma, T; Kushibiki, M; Nishizaki, F; Oikawa, K; Okumura, K; Osanai, T; Saito, S; Sukekawa, T; Tomita, H; Yamada, M; Yokota, T, 2012
)
1.36
"Landiolol is a newly developed, ultrashortacting, β-adrenoceptor antagonist."( Efficacy of low-dose landiolol, an ultrashort-acting β-blocker, on postoperative atrial fibrillation in patients undergoing pulmonary resection for lung cancer.
Funakoshi, Y; Maeda, H; Maekura, R; Nojiri, T; Okumura, M; Takeuchi, Y; Yamamoto, K, 2011
)
1.41
"Landiolol hydrochloride is a new β-adrenergic blocker with a pharmacological profile that suggests it can be administered safely to patients who have sinus tachycardia or tachyarrhythmia and who require heart rate reduction. "( Postoperative atrial fibrillation in patients undergoing coronary artery bypass grafting or cardiac valve surgery: intraoperative use of landiolol.
Kim, C; Kohda, S; Nakanishi, K; Sakamoto, A; Takeda, S, 2013
)
2.04
"Landiolol hydrochloride is a new beta-adrenergic blocker of which greatest advantages are its short duration of action, rapid clearance and high beta 1-selectivity."( [Short-acting beta 1-adrenergic blocker is useful for anesthetic management of cesarean section in a patient with Marfan syndrome].
Kamata, K; Morioka, N; Nomura, M; Ozaki, M, 2004
)
1.04
"Landiolol is a newer drug compared with esmolol."( [New ultra-short-acting beta-blockers: landiolol and esmolol--the effects on cardiovascular system].
Mio, Y, 2006
)
1.32
"Landiolol hydrochloride is a new ultra-short-acting beta(1)-adrenergic receptor blocking agent that is used for patients with tachycardia during general anesthesia. "( Age and sex-related differences in dose-dependent hemodynamic response to landiolol hydrochloride during general anesthesia.
Arita, H; Hanaoka, K; Mizuno, J; Yamada, Y; Yokoyama, T; Yoshiya, I, 2007
)
2.01
"Landiolol is a short-acting beta-blocker, with high beta 1-selectivity and a short duration of action."( Clinical role and efficacy of landiolol in the intensive care unit.
Akada, S; Hongo, T; Miyagi, Y; Sakamoto, A; Sato, C; Takeda, S; Tanaka, K; Terajima, K; Yoshida, Y, 2008
)
1.36

Effects

Landiolol has a cardioprotective effect on I/R injury in the rat heart when administered before ischemia. Landiolol hydrochloride has a shorter elimination half-life than any other beta-blocker.

Landiolol hydrochloride has the potential to enhance postischemic cardiac function after the warm cardioplegic arrest. Landiolol has a cardioprotective effect on I/R injury in the rat heart when administered before ischemia.

ExcerptReferenceRelevance
"Landiolol has a cardioprotective effect on I/R injury in the rat heart when administered before ischemia."( Pre-ischemic administration of landiolol prevents ischemia-reperfusion injury in the rat heart.
Hirai, H; Minamiyama, Y; Sakaguchi, M; Sasaki, Y; Shibata, T; Suehiro, S; Takahashi, Y; Takemura, S, 2007
)
2.07
"Landiolol hydrochloride has a shorter elimination half-life than any other beta-blocker, and it can be administered safely to patients with various tachyarrhythmias."( Pharmacokinetics of landiolol hydrochloride, a new ultra-short-acting beta-blocker, in patients with cardiac arrhythmias.
Atarashi, H; Endoh, Y; Hayakawa, H; Ino, T; Kuruma, A; Saitoh, H; Yashima, M, 2000
)
2.07
"Landiolol has a cardioprotective effect on I/R injury in the rat heart when administered before ischemia."( Pre-ischemic administration of landiolol prevents ischemia-reperfusion injury in the rat heart.
Hirai, H; Minamiyama, Y; Sakaguchi, M; Sasaki, Y; Shibata, T; Suehiro, S; Takahashi, Y; Takemura, S, 2007
)
2.07
"Landiolol hydrochloride has a shorter elimination half-life than any other beta-blocker, and it can be administered safely to patients with various tachyarrhythmias."( Pharmacokinetics of landiolol hydrochloride, a new ultra-short-acting beta-blocker, in patients with cardiac arrhythmias.
Atarashi, H; Endoh, Y; Hayakawa, H; Ino, T; Kuruma, A; Saitoh, H; Yashima, M, 2000
)
2.07
"Landiolol hydrochloride has the potential to enhance postischemic cardiac function after the warm cardioplegic arrest. "( Ultra-short-acting cardioselective beta-blockade attenuates postischemic cardiac dysfunction in the isolated rat heart.
Kamiya, H; Tanaka, Y; Watanabe, G; Yasuda, T, 2001
)
1.75

Treatment

Treatment with landiolol was shown to normalize serum creatinine and lactate levels following intravenous LPS administration. Landiolol treatment was associated with significantly less severe disease, as assessed by lung histopathology and cardiac function metrics.

ExcerptReferenceRelevance
"Treatment with landiolol was shown to normalize serum creatinine and lactate levels following intravenous LPS administration (Cr: LPS group 0.8 ± 0.6 mg/mL, LPS + landiolol group 0.5 ± 0.1 mg/mL; P < 0.05)."( Effects of Landiolol in Lipopolysaccharide-Induced Acute Kidney Injury in Rats and In Vitro.
Kanmura, Y; Kiyonaga, N; Moriyama, T, 2019
)
1.24
"Cotreatment with landiolol was associated with significantly less severe disease, as assessed by lung histopathology and cardiac function metrics."( Landiolol, an ultrashort-acting beta1-adrenoceptor antagonist, has protective effects in an LPS-induced systemic inflammation model.
Hagiwara, S; Iwasaka, H; Maeda, H; Noguchi, T, 2009
)
2.12

Toxicity

Landiolol achieved swift and safe restoration of sinus rhythm in ICU patients with POAF. Adverse events were observed in 49 (64%) of 77 patients in the landiolol group and in 44 (59%) of 74 in the control group.

ExcerptReferenceRelevance
" External, skeletal and visceral findings revealed no adverse effects of ONO-1101 on fetuses."( [Reproductive and developmental toxicity studies of landiolol hydrochloride (ONO-1101) (3). Teratogenicity study in rabbits].
Aze, Y; Chihara, N; Fujita, T; Nakagawa, Y; Nishimura, T; Ozeki, Y; Sakamoto, T; Shimouchi, K; Tanaka, M, 1997
)
0.55
"Early intravenous administration of landiolol in patients with AMI undergoing PCI is safe and has the potential to improve cardiac function and inhibit cardiac remodeling in the chronic phase."( Randomized study on the efficacy and safety of landiolol, an ultra-short-acting β1-adrenergic blocker, in patients with acute myocardial infarction undergoing primary percutaneous coronary intervention.
Abe, N; Hanada, K; Higuma, T; Kushibiki, M; Nishizaki, F; Oikawa, K; Okumura, K; Osanai, T; Saito, S; Sukekawa, T; Tomita, H; Yamada, M; Yokota, T, 2012
)
0.91
" No decrease in systolic blood pressure or other adverse effects was observed."( Safety and efficacy of a bolus injection of landiolol hydrochloride as a premedication for multidetector-row computed tomography coronary angiography.
Akagi, N; Ito, H; Kanazawa, S; Kohno, K; Kusano, K; Miyoshi, T; Morimitsu, Y; Nakamura, K; Osawa, K; Sato, S, 2013
)
0.65
" The safety endpoint was the incidence of adverse events in each of the three groups."( The effectiveness and safety of landiolol hydrochloride, an ultra-short-acting β1-blocker, in postoperative patients with supraventricular tachyarrhythmias: a multicenter, randomized, double-blind, placebo-controlled study.
Kikawa, S; Taenaka, N, 2013
)
0.67
" No significant difference was observed in the incidence of adverse events among the three groups: 29."( The effectiveness and safety of landiolol hydrochloride, an ultra-short-acting β1-blocker, in postoperative patients with supraventricular tachyarrhythmias: a multicenter, randomized, double-blind, placebo-controlled study.
Kikawa, S; Taenaka, N, 2013
)
0.67
"Landiolol hydrochloride is effective and safe for patients with postoperative SVT."( The effectiveness and safety of landiolol hydrochloride, an ultra-short-acting β1-blocker, in postoperative patients with supraventricular tachyarrhythmias: a multicenter, randomized, double-blind, placebo-controlled study.
Kikawa, S; Taenaka, N, 2013
)
2.12
"Landiolol is an ultra-short-acting β-blocker that appears to be more cardioselective and less toxic than esmolol."( Pharmacokinetics, pharmacodynamics, and safety of landiolol hydrochloride in healthy Chinese subjects.
Hua, W; Huang, M; Wang, H; Wang, M; Zhang, Q; Zhou, W, 2014
)
2.1
" The safety of landiolol hydrochloride was assessed by adverse events recording, 12-lead ECG findings, physical examination, laboratory testing, and vital signs."( Pharmacokinetics, pharmacodynamics, and safety of landiolol hydrochloride in healthy Chinese subjects.
Hua, W; Huang, M; Wang, H; Wang, M; Zhang, Q; Zhou, W, 2014
)
1.01
" There were no adverse events in any subject."( Pharmacokinetics, pharmacodynamics, and safety of landiolol hydrochloride in healthy Chinese subjects.
Hua, W; Huang, M; Wang, H; Wang, M; Zhang, Q; Zhou, W, 2014
)
0.66
"Landiolol achieved swift and safe restoration of sinus rhythm in ICU patients with POAF and could be considered as a favorable drug choice over amiodarone in such patients."( Efficacy and Safety of Landiolol Compared to Amiodarone for the Management of Postoperative Atrial Fibrillation in Intensive Care Patients.
Fujino, Y; Ohta, N; Shibata, SC; Uchiyama, A, 2016
)
2.19
" Adverse events (AEs) were assessed for safety; 27 and 29 patients were analyzed for efficacy and safety, respectively."( Efficacy and Safety of the Ultra-Short-Acting β1-Selective Blocker Landiolol in Patients With Recurrent Hemodynamically Unstable Ventricular Tachyarrhymias - Outcomes of J-Land II Study.
Daimon, T; Ikeda, T; Kinugawa, K; Nagai, R; Okamoto, H; Oki, K; Sakamoto, A; Shiga, T; Shimizu, W; Yamashita, T, 2019
)
0.75
" Adverse events were observed in 49 (64%) of 77 patients in the landiolol group and in 44 (59%) of 74 in the control group, with serious adverse events (including adverse events leading to death) in nine (12%) of 77 and eight (11%) of 74 patients."( Efficacy and safety of landiolol, an ultra-short-acting β1-selective antagonist, for treatment of sepsis-related tachyarrhythmia (J-Land 3S): a multicentre, open-label, randomised controlled trial.
Kakihana, Y; Matsuda, N; Morimatsu, H; Morishima, E; Nagano, T; Nishida, O; Ogura, H; Okajima, M; Taniguchi, T; Yamada, Y, 2020
)
1.11
" No adverse effects were reported in any patient."( Safety and Efficacy of Landiolol Hydrochloride in Children with Tachyarrhythmia of Various Etiologies.
Ashida, A; Kishi, K; Konishi, H; Nemoto, S; Odanaka, Y; Ozaki, N, 2021
)
0.93
" There were no significant differences in adverse events at 24 h between the landiolol and control groups."( Efficacy and Safety of Early Intravenous Landiolol on Myocardial Salvage in Patients with ST-segment Elevation Myocardial Infarction before Primary Percutaneous Coronary Intervention: A Randomized Study.
Ichikawa, K; Ito, H; Miyamoto, M; Miyoshi, T; Mori, A; Nakamura, K; Oka, T; Osawa, K; Yoshikawa, M, 2021
)
1.12

Pharmacokinetics

Landiolol hydrochloride is a fast-acting cardioselective β1-adrenergic antagonist. Landiolol turned out to be superior to esmolol with respect to pharmacokinetic and pharmacodynamic profile and local tolerability.

ExcerptReferenceRelevance
"Landiolol hydrochloride has a shorter elimination half-life than any other beta-blocker, and it can be administered safely to patients with various tachyarrhythmias."( Pharmacokinetics of landiolol hydrochloride, a new ultra-short-acting beta-blocker, in patients with cardiac arrhythmias.
Atarashi, H; Endoh, Y; Hayakawa, H; Ino, T; Kuruma, A; Saitoh, H; Yashima, M, 2000
)
2.07
" There were no significant changes in the elimination half-life of the drug."( Influence of hepatic impairment on the pharmacokinetics and pharmacodynamics of landiolol hydrochloride, an ultra-short-acting beta1-blocker.
Munakata, A; Sakamoto, J; Suto, K; Suto, T; Takahata, T; Tateishi, T; Yasui-Furukori, N, 2005
)
0.56
"The pharmacokinetic and pharmacodynamic characteristics of this ultra-short-acting beta1-blocker were maintained even in the patients with hepatic impairment."( Influence of hepatic impairment on the pharmacokinetics and pharmacodynamics of landiolol hydrochloride, an ultra-short-acting beta1-blocker.
Munakata, A; Sakamoto, J; Suto, K; Suto, T; Takahata, T; Tateishi, T; Yasui-Furukori, N, 2005
)
0.56
" A total of 420 blood concentration data points collected from 47 healthy male subjects were used for the population pharmacokinetic analysis."( Population pharmacokinetics of landiolol hydrochloride in healthy subjects.
Hasegawa, C; Hashimoto, Y; Honda, N; Kasai, H; Kikawa, S; Kitagawa, J; Kunisawa, T; Miyata, Y; Nakade, S; Ohno, T; Tanigawara, Y; Yamauchi, A, 2008
)
0.63
"The main pharmacokinetic parameters of landiolol hydrochloride in healthy Chinese subjects were as follows: doses of 2 groups (L and H); Cmax of 400±110 and 731±246 ng/mL; C21min of 327±109 and 508±141 ng/mL; Tmax of 10."( Pharmacokinetics, pharmacodynamics, and safety of landiolol hydrochloride in healthy Chinese subjects.
Hua, W; Huang, M; Wang, H; Wang, M; Zhang, Q; Zhou, W, 2014
)
0.92
"We previously determined the pharmacokinetic (PK) parameters of landiolol in healthy male volunteers."( Target-controlled infusion and population pharmacokinetics of landiolol hydrochloride in gynecologic patients.
Higashi, R; Iwasaki, H; Kunisawa, T; Kurosawa, A; Matsubara, K; Nakade, S; Sugawara, A; Suno, M; Yamagishi, A, 2015
)
0.9
"To date, no data have been reported on the pharmacokinetic and pharmacodynamic properties of landiolol, a fast-acting cardioselective β1-adrenergic antagonist, in non-Asian subjects."( Pharmacokinetics and pharmacodynamics of two different landiolol formulations in a healthy Caucasian group.
Hodisch, J; Kadlecová, P; Krumpl, G; Trebs, M; Ulc, I, 2016
)
0.9
"In Caucasians, both landiolol formulations showed similar pharmacokinetic behaviours, displaying very short half-lives (3."( Pharmacokinetics and pharmacodynamics of two different landiolol formulations in a healthy Caucasian group.
Hodisch, J; Kadlecová, P; Krumpl, G; Trebs, M; Ulc, I, 2016
)
1.01
" Landiolol turned out to be superior to esmolol with respect to pharmacokinetic and pharmacodynamic profile and local tolerability."( Pharmacokinetics and Pharmacodynamics of Low-, Intermediate-, and High-Dose Landiolol and Esmolol During Long-Term Infusion in Healthy Whites.
Hodisch, J; Husch, B; Kadlecová, P; Krumpl, G; Maurer, G; Trebs, M; Ulč, I, 2018
)
1.62
"To study the pharmacokinetic and -dynamic behavior of landiolol in the presence of dobutamine in healthy subjects of European ancestry."( Pharmacodynamic and pharmacokinetic behavior of landiolol during dobutamine challenge in healthy adults.
Hodisch, J; Kadlecová, P; Krumpl, G; Trebs, M; Ulč, I, 2020
)
1.06
" The pharmacokinetic parameters of landiolol in presence of dobutamine showed a short half-life (3."( Pharmacodynamic and pharmacokinetic behavior of landiolol during dobutamine challenge in healthy adults.
Hodisch, J; Kadlecová, P; Krumpl, G; Trebs, M; Ulč, I, 2020
)
1.09

Compound-Compound Interactions

ExcerptReferenceRelevance
"The purpose of this study was to determine whether a low-dose β-blocker, in combination with milrinone, improves cardiac function in acute decompensated heart failure (ADHF) with tachycardia."( Low-dose β-blocker in combination with milrinone safely improves cardiac function and eliminates pulsus alternans in patients with acute decompensated heart failure.
Doi, M; Fukuta, S; Kobayashi, S; Matsuzaki, M; Murakami, W; Nao, T; Okamura, T; Okuda, S; Susa, T; Tanaka, T; Wada, Y; Yamada, J; Yano, M, 2012
)
0.38
"A low-dose β-blocker in combination with milrinone improved cardiac function in ADHF patients with tachycardia; therefore, it may be considered as an adjunct therapy for use when standard therapy with milrinone is not effective at slowing HR."( Low-dose β-blocker in combination with milrinone safely improves cardiac function and eliminates pulsus alternans in patients with acute decompensated heart failure.
Doi, M; Fukuta, S; Kobayashi, S; Matsuzaki, M; Murakami, W; Nao, T; Okamura, T; Okuda, S; Susa, T; Tanaka, T; Wada, Y; Yamada, J; Yano, M, 2012
)
0.38

Dosage Studied

Landiolol was found to rapidly control supraventricular tachyarrhythmias (SVTs) in patients with heart failure. All three beta blockers were equally protective but the intermediate dosage of landiolol preserved LVP during the pre-ischemic period.

ExcerptRelevanceReference
" Transitory licking chops, vomiting, nausea, diarrhea and soft feces were observed occasionally in both sexes dosed 25 and 50 mg/kg/day and the incidence seemed dose-dependent."( [Toxicity studies of landiolol hydrochloride (ONO-1101) (3). 4-week repeated dose intravenous toxicity study in dogs with 4-week recovery test].
Fujita, T; Oida, H; Shichino, Y; Shimizu, K; Suzuki, Y; Tanaka, M; Ueda, H; Yamaguchi, K; Yanagi, H; Yonezawa, H, 1997
)
0.62
" Hypoactivity, bradypnea/apnea and clonic convulsion after administration was observed in animal dosed 100 mg/kg/day."( [Reproductive and developmental toxicity studies of landiolol hydrochloride (ONO-1101) (3). Teratogenicity study in rabbits].
Aze, Y; Chihara, N; Fujita, T; Nakagawa, Y; Nishimura, T; Ozeki, Y; Sakamoto, T; Shimouchi, K; Tanaka, M, 1997
)
0.55
" All three beta blockers were equally protective but the intermediate dosage of landiolol preserved LVP during the pre-ischemic period."( Landiolol, esmolol and propranolol protect from ischemia/reperfusion injury in isolated guinea pig hearts.
Fujita, S; Kanaya, N; Kurosawa, S; Nakayama, M; Namiki, A; Niiyama, Y, 2003
)
1.99
" We aimed to determine the appropriate dosage of landiolol for the treatment of hemodynamic changes in response to endotracheal intubation."( Landiolol attenuates tachycardia in response to endotracheal intubation without affecting blood pressure.
Fujii, K; Hatano, Y; Hironaka, Y; Iranami, H; Kinoshita, H; Nakahata, K; Shimogai, M; Yamazaki, A, 2005
)
2.03
"Administration of landiolol using the presently recommended dosage and administration route causes a decrease in HR without aggravation of hemodynamics in patients with normal cardiac function, but in patients with preoperative EF lower than 50%, it may lead to further deterioration of cardiac function due to a decrease in HR."( The effect of landiolol on hemodynamics and left ventricular function in patients with coronary artery disease.
Goto, K; Miyakawa, H; Miyamoto, S; Noguchi, T; Shingu, C, 2007
)
1.03
" The dose-response curves of Raw and Cdyn to acetylcholine were significantly elevated and declined in the ovalbumin-sensitized model compared with those in the control group."( Beta-1 selective adrenergic antagonist landiolol and esmolol can be safely used in patients with airway hyperreactivity.
Iwasaki, S; Jeong, SW; Namiki, A; Satoh, J; Yamakage, M,
)
0.4
"Although selective beta-1 adrenoceptor antagonists are known to provide neuroprotective effects after brain ischemia, dose-response relationships of their neuroprotective effects have not been examined."( Neuroprotective effects of selective β-1 adrenoceptor antagonists, landiolol and esmolol, on transient forebrain ischemia in rats; a dose-response study.
Goyagi, T; Horiguchi, T; Masaki, Y; Nishikawa, T; Tobe, Y, 2012
)
0.62
"The purpose of this study was to find a safe dosing regimen for landiolol, an ultra-short-acting β-adrenergic blocking agent, to rapidly control supraventricular tachyarrhythmias (SVTs) in patients with heart failure (HF)."( Novel use of the ultra-short-acting intravenous β1-selective blocker landiolol for supraventricular tachyarrhythmias in patients with congestive heart failure.
Adachi, T; Aonuma, K; Baba, M; Hasegawa, T; Hiraya, D; Hoshi, T; Kuroki, K; Sato, A, 2014
)
0.88
" Landiolol was infused with a dosage of 5 μg/kg/min during general anesthesia in the landiolol group, which was compared with the placebo control group with no landiolol."( Landiolol infusion during general anesthesia does not prevent postoperative atrial fibrillation in patients undergoing lung resection.
Aoyama, H; Aoyama, Y; Otsuka, Y, 2016
)
2.79
" Landiolol was effective in terms of rate control and haemodynamics optimization, enabling de-escalation of catecholamine dosing in all patients."( Effect of landiolol in patients with tachyarrhythmias and acute decompensated heart failure (ADHF): a case series.
Colombo, C; Ditali, V; Garatti, L; Morici, N; Oliva, F; Sacco, A; Villanova, L, 2022
)
2.03
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
morpholinesAny compound containing morpholine as part of its structure.
[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]

Research

Studies (307)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's16 (5.21)18.2507
2000's89 (28.99)29.6817
2010's166 (54.07)24.3611
2020's36 (11.73)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 48.93

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 strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index48.93 (24.57)
Research Supply Index5.98 (2.92)
Research Growth Index5.19 (4.65)
Search Engine Demand Index77.04 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (48.93)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials85 (27.33%)5.53%
Reviews21 (6.75%)6.00%
Case Studies63 (20.26%)4.05%
Observational6 (1.93%)0.25%
Other136 (43.73%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (14)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Microcirculatory and Macrocirculatory Effects of Landiolol in Prevention of Postoperative Atrial Fibrillation: a Randomized Study. [NCT03779178]Phase 358 participants (Actual)Interventional2019-01-17Completed
Study of ONO-1101 in Patients Scheduled for Multi-Slice Computed Tomography (CT), a Double-Blind, Randomized, Placebo-Controlled, Parallel Group, Multi-Center Study [NCT00924586]Phase 3258 participants (Actual)Interventional2009-06-30Completed
Landiolol for Rate Control in Decompensated Heart Failure Due to Atrial Fibrillation [NCT04694092]40 participants (Anticipated)Interventional2020-11-05Recruiting
LANdiolol MIcrocirculatory Effects During Septic chOc [NCT04931225]Phase 344 participants (Anticipated)Interventional2022-07-18Recruiting
Controlled Study of ONO-1101 in Patients With Postoperative Tachyarrhythmias in Japan [NCT00212654]Phase 2/Phase 3165 participants Interventional2001-06-30Completed
Beta-blockade With Landiolol in Out-of-hospital Cardiac Arrest: a Randomized, Double-blind, Placebo-controlled, Pilot Trial [NCT05554978]Phase 1/Phase 232 participants (Anticipated)Interventional2021-03-03Recruiting
Comparison of Two Strategies for the Management of Atrial Fibrillation After Cardiac Surgery : a Randomized Multicenter Clinical Trial [NCT04223739]Phase 4380 participants (Anticipated)Interventional2019-12-13Recruiting
Study of ONO-1101 in Patients Scheduled for Coronary Angiography, a Double-Blind, Randomized,Placebo-Controlled, Parallel Group, Multi-Center Study [NCT00560209]Phase 2183 participants (Actual)Interventional2007-11-30Completed
Pilot Study of ONO-1101 in Patients Scheduled for Multi-slice Computed Tomography (CT) Due to Suspected Coronary Artery Disease [NCT00311038]Phase 290 participants (Anticipated)Interventional2006-04-30Completed
A Single Centre Prospective, Randomized, Double Blind, Crossover, Pharmacokinetic, Safety and Tolerability Study to Compare Long-term Infusion Administration of LDLL600 Against Esmolol in Healthy Volunteers. [NCT01741519]Phase 114 participants (Actual)Interventional2012-12-31Completed
Controlled Study of ONO-1101 in Patients With Postoperative Tachyarrhythmias in Japan [NCT00212680]Phase 2100 participants Interventional1996-12-31Completed
Comparison of Landiolol Versus Standard of Care for Prevention of Mortality in Patients Hospitalized for a Septic Shock With Hypercontractility: an Open Label Prospective Randomized Study [NCT04748796]360 participants (Anticipated)Interventional2021-02-01Recruiting
A Prospective, Randomized, Double- Blind, Placebo- Controlled Study to Evaluate the Efficacy of Landiolol Hydrochloride for Prevention of Atrial Fibrillation in Patients Undergoing Cardiac Surgery [NCT05084118]Phase 3164 participants (Anticipated)Interventional2021-10-21Recruiting
Interest of Low-dose Landiolol Administration After Cardiac Surgery for the Prevention of Postoperative Atrial Fibrillation [NCT04607122]Phase 3400 participants (Actual)Interventional2021-01-27Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]