Page last updated: 2024-12-08

imidazolidines

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

Cross-References

ID SourceID
PubMed CID449488
CHEBI ID33137
MeSH IDM0461079

Synonyms (18)

Synonym
imidazolidine
504-74-5
CHEBI:33137
AKOS006352062
imidazolidines ,
aee9pl2d22 ,
unii-aee9pl2d22
dihydroimidazol-2-ylidene
WRYCSMQKUKOKBP-UHFFFAOYSA-N
DTXSID2073192
Q5276431
Q3131185
mfcd19216513
imidazolidine, 90% in water
an imidazolidine
CS-0155210
1,3-diazacyclopentane
imidazole, tetrahydro-

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" It is concluded that nilutamide is toxic to isolated rat hepatocytes, as a probable consequence of an oxidative stress due to the redox cycling of this nitroaromatic compound."( Mechanism for the hepatotoxicity of the antiandrogen, nilutamide. Evidence suggesting that redox cycling of this nitroaromatic drug leads to oxidative stress in isolated hepatocytes.
Berson, A; Eugene, D; Fau, D; Fisch, C; Fromenty, B; Pessayre, D, 1992
)
0.28
" All toxic manifestations disappeared after cessation of treatment with Anandron."( Simultaneous liver and lung toxicity related to the nonsteroidal antiandrogen nilutamide (Anandron): a case report.
Cusan, L; Dupont, A; Gomez, JL; Labrie, F; Tremblay, M, 1992
)
0.28
" Since uninterrupted administration of the antiandrogen is of the outmost importance for the successful therapy of prostatic cancer, the availability of a compound such as flutamide that has no side effect other than those due to hypoandrogenicity should greatly facilitate compliance by the patients and the success of the treatment."( Ocular toxicity of Anandron in patients treated for prostatic cancer.
Dupont, A; Harnois, C; Labrie, F; Malenfant, M, 1986
)
0.27
"Acrolein, a highly cytotoxic aldehyde, is a metabolic by-product of the antineoplastic agent cyclophosphamide and is responsible for the development of hemorrhagic cystitis, a serious side effect of cyclophosphamide therapy."( Aldose reductase-catalyzed reduction of acrolein: implications in cyclophosphamide toxicity.
Hunsaker, LA; Kolb, NS; Vander Jagt, DL, 1994
)
0.29
" Nilutamide was well tolerated in the long term with no increase in the incidence of drug specific adverse events."( Long-term efficacy and safety of nilutamide plus castration in advanced prostate cancer, and the significance of early prostate specific antigen normalization. International Anandron Study Group.
De Reijke, TM; Debruyne, FM; Dijkman, GA; Janknegt, RA, 1997
)
0.3
" Also, body weight, skin and hair texture, and behavioural pattern (food and water intake and activity) did not reflect any toxic reaction in host mice at this optimum dose."( Evaluation of toxicity of beta-tethymustine, a new anticancer compound, in mice.
Bhattacharya, B; Bhattacharya, S; Dutta, S; Ghosh, M; Sadhu, U; Sanyal, U, 1999
)
0.3
" Adverse drug reactions were observed in 20."( Efficacy and safety of imidapril in patients with essential hypertension: a double-blind comparison with captopril.
Chen, MF; Chiang, FT; Chien, KL; Huang, PJ; Lai, LP, 2001
)
0.31
" ACE-inhibitor related adverse effects (cough, vertigo, headache, pruritus, tachycardia, orthostatic dysregulation or nausea) were observed in 38 patients (< 2%)."( [Efficiency and safety of ACE-inhibiting imidapril in patients with essential hypertension].
Klein, W; Maier, R; Stoschitzky, K; Zweiker, R, 2002
)
0.31
" However, therapeutic effects of nilutamide are overshadowed by the occurrence of several adverse reactions mediated by toxic mechanism(s), which remain(s) poorly investigated."( Reduction of nilutamide by NO synthases: implications for the adverse effects of this nitroaromatic antiandrogen drug.
Ask, K; Boucher, JL; Camus, P; Casse, L; Dijols, S; Frapart, YM; Giroud, C; Kim, KS; Mansuy, D; Sari, MA; Stuehr, DJ, 2003
)
0.32
" We have shown earlier that aldose reductase (AR) besides reducing glucose to sorbitol, efficiently reduces various toxic lipid-derived aldehydes, generated under oxidative stress, with K(m) in the physiological range."( Aldose reductase prevents aldehyde toxicity in cultured human lens epithelial cells.
Ansari, NH; Pladzyk, A; Ramana, KV; Srivastava, SK, 2006
)
0.33
" Of the total 13 adverse events (n = 12), 11 were mild, 2 were moderate, and none were severe, and only 5 were considered by the investigator as possibly related to treatment."( The safety, tolerability, pharmacokinetics, and pharmacodynamics of single oral doses of RO5068760, an MEK inhibitor, in healthy volunteers: assessment of target suppression.
Barrett, J; Blotner, S; Busse-Reid, R; DeSchepper, S; Deutsch, J; Goelzer, P; Lee, L; Niu, H; Peck, R; Rueger, R; Weissgerber, G, 2010
)
0.36
" Nausea and vomiting were the most common adverse events reported in Nilutamide group."( Efficacy and Safety of Nilutamide in Patients with Metastatic Prostate Cancer who Underwent Orchiectomy: A Systematic Review and Metaanalysis.
Chhabra, M; Rashid, M; Shamshavali, K, 2019
)
0.51
" Safety was assessed by adverse events (AEs), laboratory tests, and electrocardiograms."( Pharmacokinetics, Safety, and Antiviral Effects of Multiple Doses of the Respiratory Syncytial Virus (RSV) Fusion Protein Inhibitor, JNJ-53718678, in Infants Hospitalized With RSV Infection: A Randomized Phase 1b Study.
Baraldi, E; Epalza, C; Ferrero, F; Huntjens, D; Martinón-Torres, F; McFadyen, K; Remmerie, B; Rojo, P; Rusch, S; Stevens, M; Vingerhoets, J, 2020
)
0.56
" We also determined maximum tolerated doses (MTD) and no observed adverse effect levels (NOAEL) after intramuscular (i."( A systematic evaluation of the cucurbit[7]uril pharmacokinetics and toxicity after a single dose and short-term repeated administration in mice.
Andrýs, R; Jošt, P; Lísa, M; Múčková, L; Pejchal, J; Zdarova Karasova, J, 2022
)
0.72
" CB[7] also prevents the formation of toxic oligomers and inhibits seed-catalyzed fibril proliferation."( Cucurbit[7]uril Inhibits Islet Amyloid Polypeptide Aggregation by Targeting N Terminus Hot Segments and Attenuates Cytotoxicity.
Gremer, L; Hamilton, AD; Hoyer, W; Magzoub, M; Maity, D; Oh, Y, 2022
)
0.72

Pharmacokinetics

ExcerptReferenceRelevance
" Elimination half-life tended to be longer in males than in females."( Sorbinil pharmacokinetics in male and female elderly volunteers.
Petrie, JC; Scott, AK; Webster, J, 1987
)
0.27
" The plasma decay of Anandron after the absorption phase was biexponential in all patients, with the terminal phase half-life ranging from 23."( Pharmacokinetics of Anandron in patients with advanced carcinoma of the prostate.
Bertagna, C; Creaven, PJ; Huben, R; Pendyala, L; Tremblay, D, 1988
)
0.27
"In order to obtain a rational explanation and analytical method of the unique pharmacokinetic behaviors of imidapril and imidaprilat in human, a new pharmacokinetic model was designed by introducing a saturable-reversible angiotensin I converting enzyme (ACE)-imidaprilat binding process and a linear imidapril-imidaprilat conversion process."( A saturable tissue-angiotensin I converting enzyme (ACE) binding model for the pharmacokinetic analysis of imidapril, a new ACE inhibitor, and its active metabolite in human.
Mizobe, M; Noda, K; Tagawa, K, 1995
)
0.29
"The possible influence of impaired liver function on the pharmacokinetic disposition of imidapril, a novel prodrug type angiotensin-converting enzyme (ACE) inhibitor, and its active metabolite, imidaprilat, was investigated."( Pharmacokinetics of imidapril and its active metabolite imidaprilat following single dose and during steady state in patients with impaired liver function.
Hoogkamer, JF; Kirch, W; Kleinbloesem, CH; Lankhaar, G; Nokhodian, A; Ouwerkerk, MJ; Ungethüm, W, 1997
)
0.3
" However, the slower biotransformation did not result in statistically significant differences in Cmax and AUC for either imidapril or its active metabolite following repeated administration."( Pharmacokinetics of imidapril and its active metabolite imidaprilat following single dose and during steady state in patients with impaired liver function.
Hoogkamer, JF; Kirch, W; Kleinbloesem, CH; Lankhaar, G; Nokhodian, A; Ouwerkerk, MJ; Ungethüm, W, 1997
)
0.3
"Imidapril is regarded as an ACE inhibitor of which the pharmacokinetic disposition is only slightly affected in patients with impaired liver function."( Pharmacokinetics of imidapril and its active metabolite imidaprilat following single dose and during steady state in patients with impaired liver function.
Hoogkamer, JF; Kirch, W; Kleinbloesem, CH; Lankhaar, G; Nokhodian, A; Ouwerkerk, MJ; Ungethüm, W, 1997
)
0.3
"To investigate the potential pharmacokinetic and pharmacodynamic interaction between imidapril and digoxin."( Pharmacokinetic and pharmacodynamic interaction trial after repeated oral doses of imidapril and digoxin in healthy volunteers.
Harder, S; Thürmann, PA, 1997
)
0.3
" Cmax was 19."( Pharmacokinetic and pharmacodynamic interaction trial after repeated oral doses of imidapril and digoxin in healthy volunteers.
Harder, S; Thürmann, PA, 1997
)
0.3
" Body weight-adjusted Cmax did not differ between genders."( Effect of age and gender on azimilide pharmacokinetics after a single oral dose of azimilide dihydrochloride.
Agnew, J; Bao, J; Bryson, P; Comer, P; Corey, A; Griffith, S; Li, J, 1997
)
0.3
"To investigate the pharmacokinetic profile of the ACE-inhibitor imidapril in 10 hypertensive patients after a first single dose (10 mg) and after 28 days therapy with imidapril 10 mg once daily."( Single dose and steady state pharmacokinetics and pharmacodynamics of the ACE-inhibitor imidapril in hypertensive patients.
Harder, S; Thürmann, PA; Ungethüm, W, 1998
)
0.3
"In this group of hypertensive patients, the pharmacokinetic profile and the drop in ACE-activity as well as in blood pressure seen after a single dose of imidapril and at steady state were similar."( Single dose and steady state pharmacokinetics and pharmacodynamics of the ACE-inhibitor imidapril in hypertensive patients.
Harder, S; Thürmann, PA; Ungethüm, W, 1998
)
0.3
" However, Cmax and AUC for both imidapril and imidaprilat were significantly higher in patients with severe renal impairment than in healthy volunteers."( Pharmacokinetics of imidapril and its active metabolite imidaprilat following single dose and during steady state in patients with chronic renal failure.
Hoogkamer, JF; Kirch, W; Kleinbloesem, CH; Lankhaar, G; Nokhodian, A; Ouwerkerk, MJ; Ungethüm, W, 1998
)
0.3
" Unconfounded pharmacodynamic estimates required inclusion of circadian QTc variation in the pharmacodynamic model."( Pharmacokinetics and pharmacodynamics following intravenous doses of azimilide dihydrochloride.
Agnew, J; Brum, J; Corey, A; Parekh, N; Valentine, S; Williams, M, 1999
)
0.3
"2 L/kg (23%), and terminal exponential half-life = 78."( Azimilide pharmacokinetics following intravenous and oral administration of a solution and capsule formulation.
Agnew, JR; Corey, AE; Nesbitt, JD; Powell, JH; Thompson, GA; Valentine, SN; Wagner, DL, 1999
)
0.3
"This article provides a summary of the pharmacodynamic properties of major antiandrogens as well as an extensive review of their tolerability."( Antiandrogens: a summary review of pharmacodynamic properties and tolerability in prostate cancer therapy.
De Angelis, M; De Benedetto, G; Migliari, R; Murru, M; Muscas, G; Verdacchi, T, 1999
)
0.3
"The pharmacokinetic and dynamic interactions of the angiotensin-converting enzyme (ACE) inhibitor imidapril with other therapeutic principles used in hypertension and heart failure were evaluated."( Pharmacokinetic and dynamic interactions of the angiotensin-converting enzyme inhibitor imidapril with hydrochlorothiazide, bisoprolol and nilvadipine.
Belz, GG; Breithaupt-Grögler, K; Meurer-Witt, B; Ungethüm, W, 2001
)
0.31
" Plasma concentrations of imidaprilat and H were followed up to 48 h, those of B and N up to 24 h and area under the concentration time curve (AUC), maximum plasma concentration (Cmax) and time to Cmax (tmax) were determined."( Pharmacokinetic and dynamic interactions of the angiotensin-converting enzyme inhibitor imidapril with hydrochlorothiazide, bisoprolol and nilvadipine.
Belz, GG; Breithaupt-Grögler, K; Meurer-Witt, B; Ungethüm, W, 2001
)
0.31
"The combination of imidapril with a diuretic, beta-adrenoceptor antagonist or calcium-channel blocker seems a reasonable and safe treatment option when striving for additive pharmacodynamic effects not accompanied by relevant pharmacokinetic interactions."( Pharmacokinetic and dynamic interactions of the angiotensin-converting enzyme inhibitor imidapril with hydrochlorothiazide, bisoprolol and nilvadipine.
Belz, GG; Breithaupt-Grögler, K; Meurer-Witt, B; Ungethüm, W, 2001
)
0.31
"Pharmacokinetic (PK) and pharmacodynamic (PD) models for azimilide were developed and validated with sparse blood sampling and QTc interval data obtained during three clinical trials of azimilide for prevention of supraventricular arrhythmia recurrence."( A population pharmacokinetic-pharmacodynamic analysis and model validation of azimilide.
Agnew, JR; Grasela, TH; Ludwig, EA; Phillips, L; Thompson, GA, 2001
)
0.31
" The pharmacokinetic and pharmacodynamic changes observed upon coadministration were small and are not expected to be clinically important."( Influence of coadministration on the pharmacokinetics of azimilide dihydrochloride and digoxin.
Agnew, JR; Corey, AE; Moehrke, W; Parekh, N; Powell, JH; Thompson, GA; Toothaker, RD; Valentine, SN, 2005
)
0.33
" Pharmacokinetic (PK) plasma samples are generally taken from a parallel group of animals to avoid disruption of the behavioral pharmacodynamic (PD) endpoint."( Evaluation of an innovative population pharmacokinetic-based design for behavioral pharmacodynamic endpoints.
Laird, JM; Lessard, E; Martino, G; Viberg, A, 2012
)
0.38
"5% of free form of fidarestat may be pharmacologically active and the Cmax for free fidarestat was found to be 80."( Plasma protein binding, pharmacokinetics, tissue distribution and CYP450 biotransformation studies of fidarestat by ultra high performance liquid chromatography-high resolution mass spectrometry.
Banerjee, SK; Bhandi, MM; Borkar, RM; Dubey, AP; Nandekar, PP; Sangamwar, AT; Srinivas, R, 2015
)
0.42
" Therefore, the method described is sensitive, linear, precise and specific enough to determine PT-31 in preclinical pharmacokinetic investigations."( Development and validation of a UHPLC-MS/MS bioanalytical method to quantify in plasma the analgesic candidate PT-31 following a preliminary pharmacokinetic study in rats.
Bessegato, TC; Buqui, GA; Dalla Costa, T; Galdino, SL; Lopes, NP; Niehues, M; Pitta, IR, 2016
)
0.43
" Here, we report the pharmacokinetics, the population pharmacokinetic modeling, and the safety and tolerability of JNJ-53718678 from the first-in-human, double-blind, randomized, placebo-controlled phase I study."( Population Pharmacokinetic Modeling of JNJ-53718678, a Novel Fusion Inhibitor for the Treatment of Respiratory Syncytial Virus: Results from a Phase I, Double-Blind, Randomized, Placebo-Controlled First-in-Human Study in Healthy Adult Subjects.
Brochot, A; Huntjens, DRH; Ouwerkerk-Mahadevan, S; Rusch, S; Stevens, M; Verloes, R, 2017
)
0.46
" A population pharmacokinetic model was developed and validated."( Population Pharmacokinetic Modeling of JNJ-53718678, a Novel Fusion Inhibitor for the Treatment of Respiratory Syncytial Virus: Results from a Phase I, Double-Blind, Randomized, Placebo-Controlled First-in-Human Study in Healthy Adult Subjects.
Brochot, A; Huntjens, DRH; Ouwerkerk-Mahadevan, S; Rusch, S; Stevens, M; Verloes, R, 2017
)
0.46
"A population pharmacokinetic model that describes the concentration data well with good precision of all parameter estimates was developed and validated."( Population Pharmacokinetic Modeling of JNJ-53718678, a Novel Fusion Inhibitor for the Treatment of Respiratory Syncytial Virus: Results from a Phase I, Double-Blind, Randomized, Placebo-Controlled First-in-Human Study in Healthy Adult Subjects.
Brochot, A; Huntjens, DRH; Ouwerkerk-Mahadevan, S; Rusch, S; Stevens, M; Verloes, R, 2017
)
0.46
" Sparse pharmacokinetic samples were assessed using population pharmacokinetics modeling."( Pharmacokinetics, Safety, and Antiviral Effects of Multiple Doses of the Respiratory Syncytial Virus (RSV) Fusion Protein Inhibitor, JNJ-53718678, in Infants Hospitalized With RSV Infection: A Randomized Phase 1b Study.
Baraldi, E; Epalza, C; Ferrero, F; Huntjens, D; Martinón-Torres, F; McFadyen, K; Remmerie, B; Rojo, P; Rusch, S; Stevens, M; Vingerhoets, J, 2020
)
0.56
" Pharmacokinetic parameters were similar at the highest doses for cohorts 1-3 (area under the plasma concentration-time curve from time of administration up to 24 hours postdosing at day 7: 35 840, 34 980, and 39 627 ng × hour/mL, respectively)."( Pharmacokinetics, Safety, and Antiviral Effects of Multiple Doses of the Respiratory Syncytial Virus (RSV) Fusion Protein Inhibitor, JNJ-53718678, in Infants Hospitalized With RSV Infection: A Randomized Phase 1b Study.
Baraldi, E; Epalza, C; Ferrero, F; Huntjens, D; Martinón-Torres, F; McFadyen, K; Remmerie, B; Rojo, P; Rusch, S; Stevens, M; Vingerhoets, J, 2020
)
0.56

Compound-Compound Interactions

ExcerptReferenceRelevance
"The in vitro effects of Bay k 4999 in combination with gentamicin, tobramycin, amikacin sisomicin and netilmicin in bacteriostatic (MIC) and bactericidal (MBC) concentrations were compared using the checkerboard dilution technique against 20 different strains of Pseudomonas aeruginosa, Escherichia coli, Klebsiella pneumoniae and indole-positive-negative Proteus species."( In vitro efficacy of Bay k 4999, a new ureido-penicillin, in combination with aminoglycosides against Pseudomonas aeruginosa, Escherichia coli, Klebsiella pneumoniae and Proteus strains.
Daschner, FD; Langmaack, H; Steffens, A, 1979
)
0.26
" Multicenter trials will be necessary to delineate the place of LHRH agonist alone or LHRH agonist combined with an antiandrogen in the treatment of prostatic cancer."( Preliminary results on the clinical efficacy and safety of androgen inhibition by an LHRH agonist alone or combined with an antiandrogen in the treatment of prostatic carcinoma.
Faure, N; Fazekas, AT; Jean, C; Laroche, B; Lemay, A; Plante, R; Robert, G; Roy, R; Thabet, M, 1983
)
0.27

Bioavailability

ExcerptReferenceRelevance
" This method was very useful for use in pharmacokinetic and bioavailability studies of the three metabolites of imidapril in humans."( Determination of three metabolites of a new angiotensin-converting enzyme inhibitor, imidapril, in plasma and urine by gas chromatography-mass spectrometry using multiple ion detection.
Banno, K; Horimoto, S; Mabuchi, M; Matsuoka, M, 1992
)
0.28
" In the rat, bioavailability by the oral route was complete."( Pharmacokinetics and metabolism of nilutamide.
Creaven, PJ; Pendyala, L; Tremblay, D, 1991
)
0.28
" The estimated potency of aldose reductase inhibition for each of the three drugs in this study was significantly discrepant from the in vitro studies indicating the complicated nature of the bioavailability of a pharmaceutical agent in vivo, especially where pharmacologically active metabolites of a given drug are involved."( In vivo pharmacokinetics of aldose reductase inhibitors: 3-fluoro-3-deoxy-D-glucose NMR studies in rat brains.
Kwee, IL; Nakada, T, 1989
)
0.28
" The nonsteroid flutamide is a prodrug converted to the active metabolite, hydroxyflutamide; anandron is well absorbed on oral administration of an active dose and intact compound disappears slowly from plasma."( Pharmacology of an antiandrogen, anandron, used as an adjuvant therapy in the treatment of prostate cancer.
Fiet, J; Moguilewsky, M; Raynaud, JP; Tournemine, C, 1986
)
0.27
" When the plasma pharmacokinetics of radioactivity and unchanged drug after the first single dose were compared with that during steady state, AUC0-12h of unchanged Anandron during steady state was significantly higher than the AUC0-infinity after the first single dose, suggesting that the plasma clearance of Anandron is lowered upon chronic administration of the drug, assuming that the bioavailability is constant."( Pharmacokinetics of Anandron in patients with advanced carcinoma of the prostate.
Bertagna, C; Creaven, PJ; Huben, R; Pendyala, L; Tremblay, D, 1988
)
0.27
" Bioavailability of TA-606 was 11 times higher than that of 606A in Sprague-Dawley rats, with consistent hypotensive potencies in spontaneously hypertensive rats (SHRs)."( Pharmacologic profile of TA-606, a novel angiotensin II-receptor antagonist in the rat.
Hashimoto, Y; Hayashida, K; Kaji, H; Kurosawa, Y; Minami, K; Murata, S; Narita, H; Ohashi, R, 1998
)
0.3
" In this paper we report the discovery and characterization of (R)-5-(4-bromobenzyl)-3-(3, 5-dichlorophenyl)-1,5-dimethylimidazolidine-2,4-dione (BIRT 377), an orally bioavailable small molecule that interacts specifically with LFA-1 via noncovalent binding to the CD11a chain and prevents LFA-1 from binding to its ligand, ICAM-1."( Cutting edge: a small molecule antagonist of LFA-1-mediated cell adhesion.
Bormann, BJ; Jeanfavre, DD; Kelly, TA; Kishimoto, KM; Mainolfi, EA; McNeil, DW; Nabozny, GH; Reilly, PL; Rothlein, R; Woska, JR; Zinter, R, 1999
)
0.3
"This study investigated the relative oral bioavailability of azimilide dihydrochloride following administration in the fed (high-fat meal) and fasted states."( Comparative oral bioavailability of azimilide dihydrochloride in the fed and fasted states.
Agnew, JR; Corey, AE; Nesbitt, JD; Powell, JH; Thompson, GA; Valentine, SN; Wagner, DL, 2000
)
0.31
" The aim of this study was to investigate whether increasing the viscosity of a topical aldose reductase inhibitor suspension increases the lenticular bioavailability of the inhibitor and whether such a formulation can arrest sugar cataract formation."( Topical aldose reductase inhibitor formulations for effective lens drug delivery in a rat model for sugar cataracts.
Babb, T; Blessing, K; Kador, PF; Kompella, UB; Koushik, K; Randazzo, J; Takamura, Y; Zhu, W, 2007
)
0.34
" Thus, the knowledge about the characteristic and site-specific expression of CES1 and CES2 in rat intestine will help to predict the oral bioavailability of ester prodrugs."( Identification of carboxylesterases expressed in rat intestine and effects of their hydrolyzing activity in predicting first-pass metabolism of ester prodrugs.
Gao, J; Liu, D; Liu, Y; Ren, X; Xu, Y; Zhang, C, 2011
)
0.37
"The present study provides proof-of-concept regarding the expectedly high enzymatic stability of primaquinederived imidazolidin-4-ones, imidazoquines, formerly developed as alternatives to the parent antimalarial with potentially improved oral bioavailability [J."( Comparative analysis of in vitro rat liver metabolism of the antimalarial primaquine and a derived imidazoquine.
Fernandes, I; Gomes, P; Mateus, N; Moreira, R; Vale, N, 2012
)
0.38
" Compared with the intraperitoneal injection, the relative oral bioavailability of the NIT2011 was 27."( Synthesis, radioprotective activity and pharmacokinetics characteristic of a new stable nitronyl nitroxyl radical-NIT2011.
Cheng, M; Cheng, Y; Gao, P; Jia, Y; Lu, C; Sun, X; Wang, H; Zhou, S, 2013
)
0.39
" In mice, LEI-101 had excellent oral bioavailability reaching high concentrations in the kidney and liver with minimal penetration into the brain."( The novel, orally available and peripherally restricted selective cannabinoid CB2 receptor agonist LEI-101 prevents cisplatin-induced nephrotoxicity.
Baggelaar, M; Cao, Z; Cinar, R; Erdelyi, K; Fezza, F; Hansen, T; Heitman, L; Ignatowska-Janlowska, B; Kunos, G; Lichtman, A; Maccarrone, M; Mukhopadhyay, P; Pacher, P; Ruben, M; Soethoudt, M; Van der Stelt, M; van Gils, N; Wilkerson, J, 2016
)
0.43
" The present study evaluates the effect of a reduction in particle size assessed by homogenization, sonication, and homogenization plus sonication on the bioavailability of imidazolidinedione (IZ), an antimalarial compound with known causal prophylactic activity and radical cure of relapsing malaria."( Improving Relative Bioavailability of Oral Imidazolidinedione by Reducing Particle Size Using Homogenization and Ultra-Sonication.
Aylor, S; Black, C; Li, Q; Potter, B; Sousa, J; Vuong, C; Xie, L; Zeng, Q; Zhang, J, 2019
)
0.51
" This publication covers the medicinal chemistry efforts resulting in the identification of JNJ-53718678, an orally bioavailable RSV inhibitor that was shown to be efficacious in a phase 2a challenge study in healthy adult subjects and that is currently being evaluated in hospitalized infants and adults."( Discovery of 3-({5-Chloro-1-[3-(methylsulfonyl)propyl]-1
Battles, MB; Cooymans, L; Demin, S; Hu, L; Jonckers, THM; Koul, A; Kwanten, L; McLellan, JS; Raboisson, P; Roymans, D; Tahri, A; Van den Berg, J; Vendeville, S; Vos, A, 2020
)
0.56

Dosage Studied

ExcerptRelevanceReference
" Seven had received nilutamide at the recommended dosage of 150 mg/day, and one had received twice that amount."( Nilutamide pneumonitis: a report on eight patients.
Braud, ML; Camus, P; Coudert, B; Foucher, P; Gabez, P; Lacroix, S; Mabille, JP; Pfitzenmeyer, P; Piard, F, 1992
)
0.28
" Following oral administration of 14C-labeled imidapril and 6366 A to rats, plasma concentrations of radioactivity were much higher after [N-methyl-14C]-imidapril dosing than after [N-methyl-14C]-6366 A dosing at all time points."( Metabolic fate of the new angiotensin-converting enzyme inhibitor imidapril in animals. 1st communication: absorption, pharmacokinetics and excretion in rats and dogs.
Endo, M; Kohno, M; Otsuka, M; Takaiti, O; Yamada, Y, 1992
)
0.28
" Examination of the time course of plasma radioactivity after the single and multiple (7 and 14 times) oral administration revealed that the Cmax and AUCO-24 h values slightly, but significantly, increased according to repeated dosing and the beta-phase of the t1/2 of disappearance became longer after consecutive dosing."( Metabolic fate of the new angiotensin-converting enzyme inhibitor imidapril in animals. 3rd communication: tissue accumulation after consecutive oral administration of [N-methyl-14C]-imidapril in rats.
Endo, M; Kohno, M; Otsuka, M; Suzuki, T; Takaiti, O; Yamada, Y, 1992
)
0.28
" In studies in 12 patients with advanced (Stage D) prostatic carcinoma, single-dose kinetics after 14C-nilutamide and kinetics with repetitive twice-daily dosing of two to seven weeks were measured."( Pharmacokinetics and metabolism of nilutamide.
Creaven, PJ; Pendyala, L; Tremblay, D, 1991
)
0.28
" On the basis of these results, it is unlikely that sorbinil administered at a dosage of 250 mg daily for 3 years has a clinically important effect on the course of retinopathy in adults with insulin-dependent diabetes of moderate duration."( A randomized trial of sorbinil, an aldose reductase inhibitor, in diabetic retinopathy. Sorbinil Retinopathy Trial Research Group.
, 1990
)
0.28
" Chronic dosing with sorbinil (150 mg/kg x 5) induced 2-hydroxylation of the drug, the 0-24 hr urinary excretion of 2HSB increasing from 17."( Drug-protein conjugates--XVI. Studies of sorbinil metabolism: formation of 2-hydroxysorbinil and unstable protein conjugates.
Maggs, JL; Park, BK, 1988
)
0.27
"5 micrograms/ml) were attained within approximately 2 weeks from the initiation of twice daily dosing of Anandron."( Pharmacokinetics of Anandron in patients with advanced carcinoma of the prostate.
Bertagna, C; Creaven, PJ; Huben, R; Pendyala, L; Tremblay, D, 1988
)
0.27
" In diabetic rats with severe hyperglycemia, oral sorbinil (5 mg/kg) dramatically reduced (80-90%) sorbitol levels in tissues without affecting blood glucose; the RBC dose-response curve was similar to that in lens and sciatic nerve."( Red blood cell sorbitol as an indicator of polyol pathway activity. Inhibition by sorbinil in insulin-dependent diabetic subjects.
Aldinger, CE; Leavengood, H; Malone, JI; O'Brien, MM; Page, MG; Peterson, MJ, 1984
)
0.27
"0% after the lower and higher dosage of furazlocillin, with significant inter- and intrasubject variability."( The pharmacokinetics of furazlocillin in healthy humans.
Förster, D; Gau, W; Gundert-Remy, U; Hinderling, PH, 1983
)
0.27
" Various pharmacokinetic parameters were estimated by the simultaneous curve fitting method using the plasma concentration data and the urinary excretion data of imidapril and imidaprilat in a multiple dosing study of healthy human volunteers."( A saturable tissue-angiotensin I converting enzyme (ACE) binding model for the pharmacokinetic analysis of imidapril, a new ACE inhibitor, and its active metabolite in human.
Mizobe, M; Noda, K; Tagawa, K, 1995
)
0.29
" Rats dosed orally (100 mg/kg) were fully protected from VF."( Efficacy of the class III antiarrhythmic agent azimilide in rodent models of ventricular arrhythmia.
Brooks, RR; Carpenter, JF; Maynard, AE; Miller, KE, 1996
)
0.29
" It was found that at the same dosage of 10 mg/kg/day, both AL01576 and AL04114 completely prevented all morphological and biochemical changes in the lenses of naphthalene-fed rats."( Inhibition of naphthalene cataract in rats by aldose reductase inhibitors.
Lou, MF; Xu, GT; York, B; Zigler, S, 1996
)
0.29
"Plasma imidapril concentrations after single and, although less pronounced, after repeated dosing were higher in the liver disease patients, whereas imidaprilat concentrations were lower."( Pharmacokinetics of imidapril and its active metabolite imidaprilat following single dose and during steady state in patients with impaired liver function.
Hoogkamer, JF; Kirch, W; Kleinbloesem, CH; Lankhaar, G; Nokhodian, A; Ouwerkerk, MJ; Ungethüm, W, 1997
)
0.3
" Dosing adjustments based on either age or gender are not required."( Effect of age and gender on azimilide pharmacokinetics after a single oral dose of azimilide dihydrochloride.
Agnew, J; Bao, J; Bryson, P; Comer, P; Corey, A; Griffith, S; Li, J, 1997
)
0.3
" Assuming that each modality is equally effective, emphasis should be placed on increasing patient tolerance and compliance by the use of long-acting, nontoxic treatments with simple dosing regimens and minimal side effects."( Androgen deprivation for prostatic carcinoma: a rationale for choosing components.
Chatelain, C; Fourcade, RO, 1998
)
0.3
" Dose-response curves were analyzed for 5alpha-dihydrotestosterone, the most active androgen in normal prostate, and androstenedione, a major androgen derived from the adrenals."( Functional characterization of mutant androgen receptors from androgen-independent prostate cancer.
Balk, SP; Bubley, GJ; Fenton, MA; Fertig, AM; Kolvenbag, G; Shuster, TD; Taplin, ME, 1997
)
0.3
" Bicalutamide is available in a convenient one tablet, once-a-day dosing regimen, is at least as effective as flutamide and is better tolerated in terms of diarrhea."( Which is the optimal antiandrogen for use in combined androgen blockade of advanced prostate cancer? The transition from a first- to second-generation antiandrogen.
Sarosdy, MF, 1999
)
0.3
" At a dosage of 125 mg once daily, azimilide significantly increased the time to first symptomatic recurrence of atrial fibrillation/flutter."( Azimilide.
Clemett, D; Markham, A, 2000
)
0.31
" Patients received oral azimilide (100 mg in SVA-1 and SVA-3, 35 or 75 mg in SVA-2, and 125 mg in SVA-4) or matching placebo twice daily for 3 days (loading period), followed by once-daily dosing (maintenance period)."( Antiarrhythmic effects of azimilide in paroxysmal supraventricular tachycardia: efficacy and dose-response.
Connolly, SJ; Marcello, SR; Page, RL; Pritchett, EL; Schnell, DJ; Wilkinson, WE, 2002
)
0.31
"Since azimilide blood concentrations are essentially unaffected by renal function, an a priori dosage regimen adjustment is not required in patients with renal impairment."( Effect of severe renal impairment on the pharmacokinetics of azimilide following single dose oral administration.
Agnew, JR; Corey, AE; Parekh, NJ; Powell, JH; Thompson, GA; Valentine, SN, 2002
)
0.31
" Exploiting these observations, we have designed and validated an assay that allows us to measure receptor occupancy in vitro on monkey and human peripheral blood leukocytes and ex vivo in whole blood from monkeys dosed with small molecule LFA-1 antagonists."( Small molecule LFA-1 antagonists compete with an anti-LFA-1 monoclonal antibody for binding to the CD11a I domain: development of a flow-cytometry-based receptor occupancy assay.
Caviness, GO; Fogal, SE; Giblin, PA; Jeanfavre, DD; Kelly, TA; Kishimoto, TK; Kroe, RR; Last-Barney, K; Mainolfi, EA; Panzenbeck, MJ; Reilly, PL; Rothlein, R; Woska, JR, 2003
)
0.32
" In the present study, we investigated the dose-response effect of an aldose reductase (AR) inhibitor, fidarestat, on retinal vascular changes in the retinas of streptozotocin (STZ)-induced diabetic rats."( Long-term treatment with fidarestat suppresses the development of diabetic retinopathy in STZ-induced diabetic rats.
Jomori, T; Kato, N; Nakayama, Y; Suzuki, T; Yashima, S,
)
0.13
" Based on these results, no a priori dosage adjustment is required in subjects with mild to moderate hepatic impairment."( Effect of mild and moderate hepatic impairment on azimilide pharmacokinetics following single dose oral administration.
Agnew, JR; Corey, AE; King, EC; Parekh, NJ; Powell, JH; Thompson, GA, 2004
)
0.32
"Twenty-four-hour ambulatory blood pressure monitoring (ABPM) provides the most accurate efficacy assessment of an antihypertensive agent throughout a 24-hour dosing interval."( A multicentre, 12-week study of imidapril and candesartan cilexetil in patients with mild to moderate hypertension using ambulatory blood pressure monitoring.
Alegría, E; Gonzalez-Juanatey, JR; Marquez, E; Olivan, J; Palma-Gamiz, JL; Pêgo, M; Pujol, M; Sagastagoitia-Gorostiza, JD, 2007
)
0.34
"Imidapril in once-daily doses of up to 20mg was shown to be at least as effective as candesartan cilexetil given in once-daily doses of up to 16 mg in reducing BP throughout the entire 24-hour dosing interval."( A multicentre, 12-week study of imidapril and candesartan cilexetil in patients with mild to moderate hypertension using ambulatory blood pressure monitoring.
Alegría, E; Gonzalez-Juanatey, JR; Marquez, E; Olivan, J; Palma-Gamiz, JL; Pêgo, M; Pujol, M; Sagastagoitia-Gorostiza, JD, 2007
)
0.34
" Using the same dosing regimen, only perindopril inhibited the brain ACE activities by more than 50%, whereas imidapril and enalapril showed much less potent effects."( Effect of a centrally active angiotensin-converting enzyme inhibitor, perindopril, on cognitive performance in a mouse model of Alzheimer's disease.
Kanda, T; Nagata, Y; Shirakura, S; Suzuki, N; Takahashi, S; Takayama, M; Uchida, S; Yamada, K, 2010
)
0.36
" Representative compounds 8e and 9c showed good causal prophylactic activity in Rhesus monkeys dosed 30 mg/kg/day for 3 consecutive days by IM, delayed patency for 19-21 days and 54-86 days, respectively, as compared to the untreated control."( New imidazolidinedione derivatives as antimalarial agents.
Kozar, MP; Lin, AJ; Luong, T; Melendez, V; Sathunuru, R; Zhang, L, 2011
)
0.37
" The proposed methods were successfully applied to the pharmaceutical dosage form containing the investigated compound without any interference from the excipients."( UV derivative spectrophotometric and RP-HPLC methods for determination of imidapril hydrochloride in tablets and for its stability assessment in solid state.
Kolasa, K; Regulska, K; Stanisz, B,
)
0.13
" Imidapril had a superior effect for preventing ventricular remodeling characterized by fibrosis and collagen accumulation in left ventricle compared with ramipril in the moderate and large MI groups, even though the dosage used in this study was too small to reduce systemic blood pressure."( A comparison between imidapril and ramipril on attenuation of ventricular remodeling after myocardial infarction.
Hirata, Y; Isobe, M; Nagai, R; Ogawa, M; Suzuki, J; Watanabe, R, 2012
)
0.38
" A refined dosing strategy was applied for a muscarinic agonist, AZD6088, using the rat spinal nerve ligation heat hyperalgesia model."( Evaluation of an innovative population pharmacokinetic-based design for behavioral pharmacodynamic endpoints.
Laird, JM; Lessard, E; Martino, G; Viberg, A, 2012
)
0.38
" Thus, NIT2011 has potential in being developed as an oral dosage form, safe and effective radioprotective agent."( Synthesis, radioprotective activity and pharmacokinetics characteristic of a new stable nitronyl nitroxyl radical-NIT2011.
Cheng, M; Cheng, Y; Gao, P; Jia, Y; Lu, C; Sun, X; Wang, H; Zhou, S, 2013
)
0.39
" No mutagenic effect was observed confirming that the presence of DKP in IMD final dosage form has no impact on cancer initiation."( Is there any association between imidapril hydrochloride stability profile under dry air conditions and cancer initiation?
Murias, M; Regulska, K; Regulski, M; Stanisz, B, 2013
)
0.39
" Both 27 and 48 demonstrated robust activity in the acute rat monoiodoacetate-induced osteoarthritis model of pain, and subchronic dosing of 48 showed a shift to a lower EC50 over 7 days."( Substituted Indazoles as Nav1.7 Blockers for the Treatment of Pain.
Daanen, JF; DeGoey, DA; El-Kouhen, OF; Fricano, MM; Frost, JM; Ghoreishi-Haack, N; Gum, RJ; Hsieh, GC; Kort, ME; Lundgaard, GL; Matulenko, MA; Neelands, T; Pai, M; Shi, L; Zhan, C; Zhang, XF, 2016
)
0.43
" Steady-state conditions were reached on day 2 of the 8-day dosing regimen."( Population Pharmacokinetic Modeling of JNJ-53718678, a Novel Fusion Inhibitor for the Treatment of Respiratory Syncytial Virus: Results from a Phase I, Double-Blind, Randomized, Placebo-Controlled First-in-Human Study in Healthy Adult Subjects.
Brochot, A; Huntjens, DRH; Ouwerkerk-Mahadevan, S; Rusch, S; Stevens, M; Verloes, R, 2017
)
0.46
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (3)

ClassDescription
saturated organic heteromonocyclic parent
imidazolidines
azacycloalkane
[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 (1,611)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990328 (20.36)18.7374
1990's391 (24.27)18.2507
2000's483 (29.98)29.6817
2010's326 (20.24)24.3611
2020's83 (5.15)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 7.03

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

MetricThis Compound (vs All)
Research Demand Index7.03 (24.57)
Research Supply Index7.52 (2.92)
Research Growth Index4.56 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (7.03)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials186 (11.16%)5.53%
Reviews122 (7.32%)6.00%
Case Studies38 (2.28%)4.05%
Observational1 (0.06%)0.25%
Other1,319 (79.17%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]