Page last updated: 2024-12-04

arbekacin

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Description

arbekacin: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

arbekacin : A kanamycin that is kanamycin B bearing an N-(2S)-4-amino-2-hydroxybutyryl group on the aminocyclitol ring. [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]

Cross-References

ID SourceID
PubMed CID68682
CHEMBL ID426926
CHEBI ID37922
SCHEMBL ID18413
MeSH IDM0100125

Synonyms (43)

Synonym
CHEBI:37922 ,
(2s)-4-amino-n-[(1r,2s,3s,4r,5s)-5-amino-2-(3-amino-3-deoxy-alpha-d-glucopyranosyloxy)-4-(2,6-diamino-2,3,4,6-tetradeoxy-alpha-d-erythro-hexopyranosyloxy)-3-hydroxycyclohexyl]-2-hydroxybutanamide
arbekacin (inn)
D07462
arbekacin
haberacin
arbekacin [inn]
arbekacine [french]
o-3-amino-3-deoxy-alpha-d-glucopyranosyl-(1->4)-o-(2,6-diamino-2,3,4,6-tetradeoxy-alpha-d-erythro-hexopyranosyl-(1->6))-n'-((2s)-4-amino-2-hydroxybutyryl)-2-deoxy-l-streptamine
arbekacinum [latin]
o-3-amino-3-deoxy-alpha-d-glucopyranosyl-(1-4)-o-(2,6-diamino-2,3,4,6-tetradeoxy-alpha-d-erythro-hexopyranosyl-(1-6))-n'-((2s)-4-amino-2-hydroxybutyryl)-2-deoxy-l-streptamine
d-streptamine, o-3-amino-3-deoxy-alpha-d-glucopyranosyl-(1-6)-o-(2,6-diamino-2,3,4,6-tetradeoxy-alpha-d-erythro-hexopyranosyl-(1-4))-n1-(4-amino-2-hydroxy-1-oxobutyl)-2-deoxy-, (s)-
d-streptamine, o-3-amino-3-deoxy-alpha-d-glucopyranosyl-(1-6)-o-(2,6-diamino-2,3,4,6-tetradeoxy-alpha-d-erythro-hexopyranosyl-(1-4))-n(sup 1)-(4-amino-2-hydroxy-1-oxobutyl)-2-deoxy-, (s)-
arbekacina [spanish]
dkb-ahb
(2s)-4-amino-n-[(1r,2s,3s,4r,5s)-5-amino-4-[(2r,3r,6s)-3-amino-6-(aminomethyl)tetrahydropyran-2-yl]oxy-2-[(2s,3r,4s,5s,6r)-4-amino-3,5-dihydroxy-6-(hydroxymethyl)tetrahydropyran-2-yl]oxy-3-hydroxy-cyclohexyl]-2-hydroxy-butanamide
DB06696
butanamide, 4-amino-n-[(1r,2s,3s,4r,5s)-5-amino-2-[(3-amino-3-deoxy-.alpha.-d-glucopyranosyl)oxy]-4-[(2,6-diamino-2,3,4,6-tetradeoxy-.alpha.-d-erythro-hexopyranosyl)oxy]-3-hydroxycyclohexyl]-2-hydroxy-, (2s)-
me-1100
me1100
CHEMBL426926
(2s)-4-amino-n-[(1r,2s,3s,4r,5s)-5-amino-4-[(2r,3r,6s)-3-amino-6-(aminomethyl)oxan-2-yl]oxy-2-[(2s,3r,4s,5s,6r)-4-amino-3,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-3-hydroxycyclohexyl]-2-hydroxybutanamide
arbekacinum
arbekacina
arbekacine
g7v6sli20l ,
unii-g7v6sli20l
gtpl7345
SCHEMBL18413
arbekacin [who-dd]
arbekacin [mi]
o-3-amino-3-deoxy-.alpha.-d-glucopyranosyl-(1->4)-o-(2,6-diamino-2,3,4,6-tetradeoxy-.alpha.-d-erythro-hexopyranosyl-(1->6))-n'-((2s)-4-amino-2-hydroxybutyryl)-2-deoxy-l-streptamine
d-streptamine, o-3-amino-3-deoxy-.alpha.-d-glucopyranosyl-(1->6)-o-(2,6-diamino-2,3,4,6-tetradeoxy-.alpha.-d-erythro-hexopyranosyl-(1->4))-n1-((2s)-4-amino-2-hydroxy-1-oxobutyl)-2-deoxy-
DTXSID8048319
AKOS025149466
(2s)-4-amino-n-[(1r,2s,3s,4r,5s)-5-amino-2-{[(2s,3r,4s,5s,6r)-4-amino-3,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy}-4-{[(2r,3r,6s)-3-amino-6-(aminomethyl)oxan-2-yl]oxy}-3-hydroxycyclohexyl]-2-hydroxybutanamide
84G ,
MKKYBZZTJQGVCD-XTCKQBCOSA-N
(s)-4-amino-n-((1r,2s,3s,4r,5s)-5-amino-2-((2s,3r,4s,5s,6r)-4-amino-3,5-dihydroxy-6-(hydroxymethyl)tetrahydro-2h-pyran-2-yloxy)-4-((2r,3r,6s)-3-amino-6-(aminomethyl)tetrahydro-2h-pyran-2-yloxy)-3-hydroxycyclohexyl)-2-hydroxybutanamide
(2s)-4-amino-n-{(1r,2s,3s,4r,5s)-5-amino-2-[(3-amino-3-deoxy-alpha-d-glucopyranosyl)oxy]-4-[(2,6-diamino-2,3,4,6-tetradeoxy-alpha-d-erythro-hexopyranosyl)oxy]-3-hydroxycyclohexyl}-2-hydroxybutanamide
Q4784668
51025-85-5 (free base)
(s)-4-amino-n-((1r,2s,3s,4r,5s)-5-amino-2-(((2s,3r,4s,5s,6r)-4-amino-3,5-dihydroxy-6-(hydroxymethyl)tetrahydro-2h-pyran-2-yl)oxy)-4-(((2r,3r,6s)-3-amino-6-(aminomethyl)tetrahydro-2h-pyran-2-yl)oxy)-3-hydroxycyclohexyl)-2-hydroxybutanamide

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" ABK was found less toxic to kidney than VCM, and the toxicity was strengthened by combined treatment with VCM and ABK."( [A study on nephrotoxicity of arbekacin and vancomycin in rats].
Asaoka, H; Niizato, T; Nishiyama, S; Ohnishi, M; Saito, A, 1994
)
0.29
"ABK is an effective and safe antibiotic for the treatment of acquired staphylococcal infection in the neonatal intensive care nursery."( Efficacy and safety of arbekacin for staphylococcal infection in the NICU.
Suzuki, K, 2003
)
0.32
" Incidence of adverse reactions was 38."( The efficacy and safety of high-dose arbekacin sulfate therapy (once-daily treatment) in patients with MRSA infection.
Fukuda, Y; Hashiguchi, K; Imamura, Y; Inoue, Y; Izumikawa, K; Kakeya, H; Kobayashi, T; Kohno, S; Kondo, A; Miyazaki, T; Morinaga, Y; Nakamura, S; Yamamoto, Y; Yanagihara, K, 2012
)
0.38
" There was no increase in the incidence of adverse events."( Clinical efficacy and safety of arbekacin sulfate in patients with MRSA sepsis or pneumonia: a multi-institutional study.
Akiyama, N; Arai, T; Hanaki, H; Higashihara, M; Ichiwata, T; Ikegami, K; Kimura, T; Kobayashi, M; Matsumoto, T; Miyao, N; Nemoto, M; Oda, S; Ohyashiki, K; Otsuka, Y; Soma, K; Sunakawa, K; Suzuki, Y; Totsuka, K; Yokota, H; Yoshida, M; Yukioka, T, 2013
)
0.39
"Arbekacin can be considered as safe and effective alternative to vancomycin in the management of MRSA infections."( A Multicentre, Open label, Randomized, Comparative, Parallel Group, Active-controlled, Phase III Clinical Trial to Evaluate Safety and Efficacy of Arbekacin Sulphate Injection versus Vancomycin Injection in Patients Diagnosed with MRSA Infection.
Agarwal, R; Agrawal, RP; Basu, I; Bhalla, H; Bs, M; Das, C; Deb, AK; Dube, A; Kurlekar, U; Padhye, D; Pawar, R; Shahavi, V; Singh, RM; Srivastava, A; Srivastava, P, 2018
)
0.48

Pharmacokinetics

The bactericidal activities of arbekacin (ABK), vancomycin (VCM), gentamicin (GM) and netilmicin (NTL) in mixed culture with Staphylococcus aureus (MRSA) and Pseudomonas aeruginosa were examined using an in vitro computer programmed pharmacokinetic simulation system. The protective effect of these agents on systemic infection was also examined.

ExcerptReferenceRelevance
" Pharmacokinetic analysis was made in accordance with the two-compartment open model, and 24-hour endogenous creatinine clearance (Ccr) was used as the renal function index."( [Pharmacokinetics of arbekacin in healthy volunteers and patients with renal insufficiency].
Kishi, M; Kumon, H; Mizuno, A; Nasu, Y; Ohmori, H; Tsugawa, M, 1989
)
0.28
"In vitro studies of elimination of arbekacin (HBK), a new aminoglycoside antibiotic, from blood by means of hemodialysis or adsorption with charcoal, and pharmacokinetic studies in patients with renal dysfunction were examined."( [Clinical study of aminoglycosides on renal dysfunction--pharmacokinetics of arbekacin and its elimination effects by hemodialysis and adsorption with charcoal].
Arakawa, S; Fujii, A; Hamada, K; Hara, S; Kamidono, S; Maeda, H; Miyazaki, S, 1989
)
0.28
" Elimination serum half-life increased in relation to the degree of renal impairment, from 2 h in normal subjects to 32 h in patients with creatinine clearance below 10 ml/min."( [Pharmacokinetics of habekacin in patients with chronic renal insufficiency].
Bernadet, P; Fillastre, JP; Humbert, G; Josse, S; Leroy, A; Moulin, B, 1987
)
0.27
" The elimination half-life in serum increased in relation to the degree of renal impairment, from 2 h in normal subjects to 32 h in patients with creatinine clearances of less than 10 ml/min."( Pharmacokinetics of habekacin in patients with renal insufficiency.
Bernadet, P; Fillastre, JP; Humbert, G; Josse, S; Leroy, A; Moulin, B, 1987
)
0.27
"The bactericidal activities of arbekacin (ABK), vancomycin (VCM), gentamicin (GM) and netilmicin (NTL) in mixed culture with Staphylococcus aureus (MRSA) and Pseudomonas aeruginosa were examined using an in vitro computer programmed pharmacokinetic simulation system and also the protective effect of these agents on systemic infection in neutropenic mice was examined."( [Evaluation of bactericidal activity of arbekacin in mixed culture with MRSA and Pseudomonas aeruginosa using an in vitro pharmacokinetic simulation system].
Goto, S; Sugano, T; Takada, T; Takase, Y; Tsuji, A; Yamaguchi, K; Yoshida, T, 1994
)
0.29
" Maximum serum concentration (Cmax), serum half-life (T1/2 beta) and urinary recovery rate (0-48 hours) after single administration of 200 mg of ABK, were 13."( [Evaluation of once-daily administration of arbekacin. Experimental study and determination of pharmacokinetic properties in man].
Araake, M; Mitomi, N; Niizato, T; Shimizu, K; Totsuka, K, 1994
)
0.29
"The objective of the present study was to determine pharmacokinetic variables and to characterize a new initial dosing regimen of arbekacin (ABK) for preterm and term newborn infants."( Pharmacokinetics and dosing of arbekacin in preterm and term newborn infants.
Matsuzaki, T; Suzuki, K; Tanikawa, K, 2003
)
0.32
" Population pharmacokinetic studies were performed to determine the optimal dosage regimens for three types of antibiotics: an aminoglycoside, arbekacin; a glycopeptide, vancomycin; and a carbapenem, panipenem."( Population pharmacokinetics of arbekacin, vancomycin, and panipenem in neonates.
Kimura, T; Kubo, H; Matsuura, N; Shimada, S; Sunakawa, K; Yago, K, 2004
)
0.32
"We inoculated an in vitro pharmacodynamic model simultaneously with clinical isolates of methicillin-resistant Staphylococcus aureus and an enterocin-producing enterococcus (vancomycin-resistant Enterococcus faecalis, ampicillin susceptible) at 7 log10 CFU/ml to examine enterocin effects and antimicrobial activity on staphylococci."( Impact of Enterococcus faecalis on the bactericidal activities of arbekacin, daptomycin, linezolid, and tigecycline against methicillin-resistant Staphylococcus aureus in a mixed-pathogen pharmacodynamic model.
Chin, JN; LaPlante, KL; Leuthner, KD; Rybak, MJ, 2006
)
0.33
" In total, 1,581 serum arbekacin concentrations were measured (primarily from routine patient care) and used to perform the present pharmacokinetic analysis."( Population pharmacokinetics of Arbekacin in patients infected with methicillin-resistant Staphylococcus aureus.
Aikawa, N; Kaku, M; Morita, K; Sato, R; Shimizu, K; Tanigawara, Y, 2006
)
0.33
" Since we have reported the population pharmacokinetic parameters for arbekacin in the preceding paper (Y."( Pharmacokinetic-pharmacodynamic relationship of arbekacin for treatment of patients infected with methicillin-resistant Staphylococcus aureus.
Aikawa, N; Kaku, M; Sato, R; Shimizu, K; Tanigawara, Y, 2006
)
0.33
" A pharmacokinetic model with three compartments (1, central; 2, peripheral; 3, filtrate-dialysate side hemofilter) accurately reflected the concentration-time data for both plasma and filtrate-dialysate."( Pharmacokinetics and pharmacodynamics of once-daily arbekacin during continuous venovenous hemodiafiltration in critically ill patients.
Ikawa, K; Ikeda, K; Morikawa, N; Suyama, H; Yamanoue, T, 2009
)
0.35
"Once a day of arbekacin (ABK) administrations based on a new object of peak concentration setting on 9-20 microg/mL were performed to 14 neonates."( [Evaluation of once a day of arbekacin administration to neonates as a new object of peak concentration].
Kinoshita, D, 2010
)
0.36
"The efficacy of arbekacin in patients with MRSA infections is influenced by the peak concentration (Cpeak)/MIC ratio (≧8)."( Population pharmacokinetics of arbekacin in different infectious disease settings and evaluation of dosing regimens.
Hagihara, M; Hamada, Y; Hirai, J; Kato, H; Koizumi, Y; Matsuura, K; Mikamo, H; Nishiyama, N; Sakanashi, D; Suematsu, H; Yamagishi, Y, 2016
)
0.43
" In the pharmacokinetic study, the C max in the 30 mg/mL ME1100 treatment group in the epithelial lining fluid (ELF) and plasma was 31."( Efficacy and pharmacokinetics of ME1100, a novel optimized formulation of arbekacin for inhalation, compared with amikacin in a murine model of ventilator-associated pneumonia caused by Pseudomonas aeruginosa.
Hasegawa, H; Izumikawa, K; Kaku, N; Kosai, K; Miyazaki, T; Morinaga, Y; Mukae, H; Takeda, K; Uno, N; Yanagihara, K, 2017
)
0.46
" The objective of these analyses was to develop a population pharmacokinetic model to describe the arbekacin concentration-time profile in plasma and epithelial lining fluid (ELF) following ME1100 administration."( Population Pharmacokinetic Analyses for Arbekacin after Administration of ME1100 Inhalation Solution.
Ambrose, PG; Bhavnani, SM; Kondo, K; Koresawa, T; Lakota, EA; Rubino, CM; Sato, N, 2019
)
0.51
" However, the influence of the physiology of patients with FN on the pharmacokinetic (PK) parameters of ABK remains unclear."( Increased Arbekacin Clearance in Patients With Febrile Neutropenia.
Chuma, M; Hamada, T; Hatta, Y; Imai, T; Iriyama, N; Iwabuchi, S; Kimura, T; Matsumoto, C; Miura, K; Nakagawa, M; Nakayama, T; Suzuki, S; Takahashi, H; Takei, M; Tochikura, N; Uchino, Y, 2020
)
0.56

Compound-Compound Interactions

ExcerptReferenceRelevance
" Arbekacin may prove useful when used in combination with vancomycin in treating infections caused by gentamicin-resistant MRSA."( In-vitro activity of arbekacin alone and in combination with vancomycin against gentamicin- and methicillin-resistant Staphylococcus aureus.
Chow, JW; Kariyama, R; Kumon, H; You, I; Zervos, MJ, 2000
)
0.31

Bioavailability

ExcerptReferenceRelevance
" A bioavailability term was included for the inhalational route of administration, which was estimated to be 19."( Population Pharmacokinetic Analyses for Arbekacin after Administration of ME1100 Inhalation Solution.
Ambrose, PG; Bhavnani, SM; Kondo, K; Koresawa, T; Lakota, EA; Rubino, CM; Sato, N, 2019
)
0.51

Dosage Studied

Once-daily dosing can improve the therapeutic efficacy of arbekacin. A trough arbekACin concentration of <2 μg/mL can reduce the risk of nephrotoxicity.

ExcerptRelevanceReference
" In conclusion, if it could be necessary to use habekacin and to prefer this aminoglycoside to gentamicin from an antibacterial activity point of view it is necessary to keep in mind that this drug is potentially nephrotoxic and that the dosage had to be strictly respected."( [Habekacin: a new aminoglycoside. Study of nephrotoxicity in rats in comparison with gentamicin, netilmicin and amikacin].
Fillastre, JP; Morin, JP; Olier, B; Thomas, N, 1988
)
0.27
" Cumulative drug dose-response curves were obtained for three different muscles in 24 rabbits."( Neuromuscular blocking effects of the aminoglycoside antibiotics arbekacin, astromicin, isepamicin and netilmicin on the diaphragm and limb muscles in the rabbit.
Hashimoto, Y; Kato, M; Liu, M, 2001
)
0.31
"The objective of the present study was to determine pharmacokinetic variables and to characterize a new initial dosing regimen of arbekacin (ABK) for preterm and term newborn infants."( Pharmacokinetics and dosing of arbekacin in preterm and term newborn infants.
Matsuzaki, T; Suzuki, K; Tanikawa, K, 2003
)
0.32
" The new initial dosing regimen was determined based on these data."( Pharmacokinetics and dosing of arbekacin in preterm and term newborn infants.
Matsuzaki, T; Suzuki, K; Tanikawa, K, 2003
)
0.32
" The new dosing regimen is 5 mg/kg every 48 h, 5 mg/kg every 24 h, and 4 mg/kg every 24 h for PE, PL, and T, respectively."( Pharmacokinetics and dosing of arbekacin in preterm and term newborn infants.
Matsuzaki, T; Suzuki, K; Tanikawa, K, 2003
)
0.32
"With the new dosing regimen, more infants achieved serum ABK levels within the optimal range than the conventional one."( Pharmacokinetics and dosing of arbekacin in preterm and term newborn infants.
Matsuzaki, T; Suzuki, K; Tanikawa, K, 2003
)
0.32
" At 72 h, ABK or VAN alone produced equivalent bacterial reductions regardless of dosing frequency and GEN resistance."( Efficacies of vancomycin, arbekacin, and gentamicin alone or in combination against methicillin-resistant Staphylococcus aureus in an in vitro infective endocarditis model.
Choi, JH; Choi, SM; Chun, HS; Kang, MW; Lee, DG; Shin, WS; Yim, DS; Yoo, JH, 2003
)
0.32
"Immature renal function in neonates requires antibiotic dosage adjustment."( Population pharmacokinetics of arbekacin, vancomycin, and panipenem in neonates.
Kimura, T; Kubo, H; Matsuura, N; Shimada, S; Sunakawa, K; Yago, K, 2004
)
0.32
" In this study, the authors investigated the pharmacokinetics of ABK based on therapeutic drug monitoring (TDM), in order to establish an effective dosage regimen with minimal adverse reactions in MRSA infected newborns and infants."( Dosage regimen of arbekacin for methicillin-resistant Staphylococcus aureus infection in newborns and infants.
Ebisu, R; Minowa, H; Takahashi, Y; Uchida, Y; Yoshida, K; Yoshioka, A, 2004
)
0.32
" Morphological studies using scanning electron microscopy and histochemical staining demonstrated that an effective dosage of arbekacin induced dramatic changes in the biofilm membranous structure as well as in the inflammatory response, resulting in eradication of the biofilm structure and resolution of inflammation."( Effect of arbekacin on a methicillin-resistant Staphylococcus aureus-induced biofilm in a rat model.
Morikawa, K; Nonaka, M; Torii, I; Yoshikawa, Y, 2004
)
0.32
" Proper use and dosage is required, and is based on patient background and the conditions of infection, among other factors."( [Analysis of factors in selecting anti-methicillin-resistant Staphylococcus aureus drugs by doctors].
Aoyama, T; Hayashi, H; Matsumoto, Y; Matsuzaki, T; Saito, A, 2008
)
0.35
" The purpose of this study is to evaluate the clinical application of serum cystatin C as a marker of GFR to determine the initial dosage of arbekacin, an antibiotic primarily excreted via the kidneys."( Evaluation of the clinical application of cystatin C, a new marker of the glomerular filtration rate, for the initial dose-setting of arbekacin.
Araki, H; Inoue, T; Murase, M; Nishimiya, T; Otsuka, T; Suemaru, K; Tanaka, A, 2008
)
0.35
"These results suggest that serum cystatin C is a useful marker of GFR for determining the initial dosage of arbekacin, especially in patients with moderate impairment of renal function."( Evaluation of the clinical application of cystatin C, a new marker of the glomerular filtration rate, for the initial dose-setting of arbekacin.
Araki, H; Inoue, T; Murase, M; Nishimiya, T; Otsuka, T; Suemaru, K; Tanaka, A, 2008
)
0.35
" However, despite the low CCR, even the maintenance ABK dosage for normal CCR did not elevate the highest serum level (C(max)) to the effective range in the patient group."( Recommended dose of arbekacin, an aminoglycoside against methicillin-resistant Staphylococcus aureus, does not achieve desired serum concentration in critically ill patients with lowered creatinine clearance.
Aibiki, M; Fukuoka, N, 2008
)
0.35
" The present results hypothesize that adjustment of antibiotic dosing according to CCR further lowers C(max) in critically ill patients with reduced CCR."( Recommended dose of arbekacin, an aminoglycoside against methicillin-resistant Staphylococcus aureus, does not achieve desired serum concentration in critically ill patients with lowered creatinine clearance.
Aibiki, M; Fukuoka, N, 2008
)
0.35
" Our findings suggest that PEGylation of N-WASP181-200 is a useful strategy for reducing dosage of the concomitant with which to decrease renal accumulation in the kidney, leading to prevention of aminoglycoside-induced nephrotoxicity."( Effect of PEGylation of N-WASP181-200 on the inhibitory potency for renal aminoglycoside accumulation.
Fujii, K; Nagai, J; Sawada, T; Takano, M; Yumoto, R, 2009
)
0.35
"This study examined the pharmacokinetics of arbekacin during continuous venovenous hemodiafiltration (CVVHDF) and assessed the pharmacodynamics to consider arbekacin dosage adaptation in CVVHDF."( Pharmacokinetics and pharmacodynamics of once-daily arbekacin during continuous venovenous hemodiafiltration in critically ill patients.
Ikawa, K; Ikeda, K; Morikawa, N; Suyama, H; Yamanoue, T, 2009
)
0.35
"769, n = 35), which suggested the usefulness of the dosage design."( [Evaluation of once a day of arbekacin administration to neonates as a new object of peak concentration].
Kinoshita, D, 2010
)
0.36
" In conclusion, we recommend the initial dose of ABK at 5-6 mg/kg or higher and the dosage regimen should be adjusted to achieve C (peak) at 10-15 μg/mL or higher in the treatment of patients with pneumonia or sepsis caused by MRSA."( Clinical efficacy and safety of arbekacin sulfate in patients with MRSA sepsis or pneumonia: a multi-institutional study.
Akiyama, N; Arai, T; Hanaki, H; Higashihara, M; Ichiwata, T; Ikegami, K; Kimura, T; Kobayashi, M; Matsumoto, T; Miyao, N; Nemoto, M; Oda, S; Ohyashiki, K; Otsuka, Y; Soma, K; Sunakawa, K; Suzuki, Y; Totsuka, K; Yokota, H; Yoshida, M; Yukioka, T, 2013
)
0.39
" First, although the daily dose of 150-200 mg was approved in Japan, recent PK-PD studies revealed that higher serum concentration is required to achieve better clinical efficacy and several findings concerning the usefulness of higher dosage regimen have obtained recently."( Clinical practice guidelines for therapeutic drug monitoring of arbekacin: a consensus review of the Japanese Society of Chemotherapy and the Japanese Society of Therapeutic Drug Monitoring.
Hamada, Y; Igarashi, M; Kasahara, K; Kimura, M; Kimura, T; Kobayashi, M; Matsumoto, K; Mikamo, H; Mochizuki, T; Nishi, Y; Ohmagari, N; Okada, K; Seki, M; Takahashi, Y; Takakura, S; Takesue, Y; Tanigawara, Y; Tokimatsu, I, 2014
)
0.4
" This study was to evaluate the pharmacokinetics of arbekacin in different infectious diseases and to evaluate its dosing regimens."( Population pharmacokinetics of arbekacin in different infectious disease settings and evaluation of dosing regimens.
Hagihara, M; Hamada, Y; Hirai, J; Kato, H; Koizumi, Y; Matsuura, K; Mikamo, H; Nishiyama, N; Sakanashi, D; Suematsu, H; Yamagishi, Y, 2016
)
0.43
" As ABK has a narrow therapeutic concentration window, the dosage must be adjusted via therapeutic drug monitoring."( Increased Arbekacin Clearance in Patients With Febrile Neutropenia.
Chuma, M; Hamada, T; Hatta, Y; Imai, T; Iriyama, N; Iwabuchi, S; Kimura, T; Matsumoto, C; Miura, K; Nakagawa, M; Nakayama, T; Suzuki, S; Takahashi, H; Takei, M; Tochikura, N; Uchino, Y, 2020
)
0.56
" Although therapeutic drug monitoring (TDM) is recommended during arbekacin treatment, little evidence for the target exposure and once-daily dosing has been reported."( Evaluation of once-daily dosing and target concentrations in therapeutic drug monitoring for arbekacin: A meta-analysis.
Fujii, S; Mayumi, T; Oda, K; Takesue, Y; Yamamoto, T, 2021
)
0.62
" Once-daily dosing significantly reduced the risk of treatment failure (RR = 0."( Evaluation of once-daily dosing and target concentrations in therapeutic drug monitoring for arbekacin: A meta-analysis.
Fujii, S; Mayumi, T; Oda, K; Takesue, Y; Yamamoto, T, 2021
)
0.62
"Once-daily dosing can improve the therapeutic efficacy of arbekacin, and a trough arbekacin concentration of <2 μg/mL can reduce the risk of nephrotoxicity."( Evaluation of once-daily dosing and target concentrations in therapeutic drug monitoring for arbekacin: A meta-analysis.
Fujii, S; Mayumi, T; Oda, K; Takesue, Y; Yamamoto, T, 2021
)
0.62
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (4)

RoleDescription
antimicrobial agentA substance that kills or slows the growth of microorganisms, including bacteria, viruses, fungi and protozoans.
protein synthesis inhibitorA compound, usually an anti-bacterial agent or a toxin, which inhibits the synthesis of a protein.
antibacterial agentA substance (or active part thereof) that kills or slows the growth of bacteria.
antibacterial drugA drug used to treat or prevent bacterial infections.
[role 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]

Drug Classes (2)

ClassDescription
kanamycins
aminoglycoside
[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]

Pathways (1)

PathwayProteinsCompounds
Arbekacin Action Pathway14

Protein Targets (1)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency12.57970.005612.367736.1254AID624044
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (95)

Assay IDTitleYearJournalArticle
AID299406Antibacterial activity against methicillin-resistant Staphylococcus aureus by agar dilution method2007Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13
Synthesis and antibacterial activity of 5-deoxy-5-episubstituted arbekacin derivatives.
AID564685Antimicrobial activity against multidrug-resistant Klebsiella pneumoniae isolates by microdilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
ACHN-490, a neoglycoside with potent in vitro activity against multidrug-resistant Klebsiella pneumoniae isolates.
AID560599Antimicrobial activity against Escherichia coli JM109 transformant harboring pSTV28 plasmid expressing aac(6')-Iaf wild type gene by microdilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
AAC(6')-Iaf, a novel aminoglycoside 6'-N-acetyltransferase from multidrug-resistant Pseudomonas aeruginosa clinical isolates.
AID310090Antibacterial activity against methicillin-resistant Staphylococcus aureus MF4902007Bioorganic & medicinal chemistry letters, Nov-15, Volume: 17, Issue:22
Effect of varying the 4''-position of arbekacin derivatives on antibacterial activity against MRSA and Pseudomonas aeruginosa.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID276898Antibacterial activity against gentamycin and arbekacin-resistant Staphylococcus aureus RN4220/pMF490 expressing AAC(6')-APH(2'') enzyme by twofold agar dilution method2006Bioorganic & medicinal chemistry letters, Dec-15, Volume: 16, Issue:24
Synthesis and antibacterial activity of novel neamine derivatives.
AID560590Antimicrobial activity against Pseudomonas aeruginosa isolate IMCJ798 by microdilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
AAC(6')-Iaf, a novel aminoglycoside 6'-N-acetyltransferase from multidrug-resistant Pseudomonas aeruginosa clinical isolates.
AID66574Antibacterial activity was determined against clinically isolated vancomycin-B resistant enterococci (VRE) strains (10 strains)2003Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6
Synthesis and structure-activity relationships of 5-amino-6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-8-methylquinolonecarboxylic acid antibacterials having fluorinated 7-[(3R)-3-(1-aminocyclopropan-1-yl)pyrrolidin-1-yl] substituents.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID456045Antibacterial activity against vancomycin-resistant Enterococcus faecalis after 18 hrs by twofold microbroth dilution method2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Design, synthesis and biological evaluations of novel 7-[3-(1-aminocycloalkyl)pyrrolidin-1-yl]-6-desfluoro-8-methoxyquinolones with potent antibacterial activity against multi-drug resistant Gram-positive bacteria.
AID456044Antibacterial activity against penicillin-intermediate resistant Streptococcus pneumoniae after 18 hrs by twofold microbroth dilution method2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Design, synthesis and biological evaluations of novel 7-[3-(1-aminocycloalkyl)pyrrolidin-1-yl]-6-desfluoro-8-methoxyquinolones with potent antibacterial activity against multi-drug resistant Gram-positive bacteria.
AID66576Antibacterial activity was determined against clinically isolated vancomycin-A resistant enterococci (VRE) strains (33 strains)2003Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6
Synthesis and structure-activity relationships of 5-amino-6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-8-methylquinolonecarboxylic acid antibacterials having fluorinated 7-[(3R)-3-(1-aminocyclopropan-1-yl)pyrrolidin-1-yl] substituents.
AID520875Antibacterial activity against methicillin-resistant mecA-positive Staphylococcus saprophyticus isolates isolated from genitourinary tracts of acute cystitis patient after 24 hrs at 35 degC by agar dilution method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Methicillin-resistant Staphylococcus saprophyticus isolates carrying staphylococcal cassette chromosome mec have emerged in urogenital tract infections.
AID310096Antibacterial activity against Pseudomonas aeruginosa isolates2007Bioorganic & medicinal chemistry letters, Nov-15, Volume: 17, Issue:22
Effect of varying the 4''-position of arbekacin derivatives on antibacterial activity against MRSA and Pseudomonas aeruginosa.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID299401Antibacterial activity against methicillin-resistant Staphylococcus aureus MSC03571 by agar dilution method2007Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13
Synthesis and antibacterial activity of 5-deoxy-5-episubstituted arbekacin derivatives.
AID520872Antibacterial activity against methicillin-resistant mecA-positive Staphylococcus saprophyticus isolate TSU67 isolated from genitourinary tracts of acute cystitis patient after 24 hrs at 35 degC by agar dilution method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Methicillin-resistant Staphylococcus saprophyticus isolates carrying staphylococcal cassette chromosome mec have emerged in urogenital tract infections.
AID299403Antibacterial activity against Pseudomonas aeruginosa PAO1 by agar dilution method2007Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13
Synthesis and antibacterial activity of 5-deoxy-5-episubstituted arbekacin derivatives.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID310095Antibacterial activity against Pseudomonas aeruginosa GN3152007Bioorganic & medicinal chemistry letters, Nov-15, Volume: 17, Issue:22
Effect of varying the 4''-position of arbekacin derivatives on antibacterial activity against MRSA and Pseudomonas aeruginosa.
AID299404Antibacterial activity against Pseudomonas aeruginosa GN315 by agar dilution method2007Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13
Synthesis and antibacterial activity of 5-deoxy-5-episubstituted arbekacin derivatives.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID299402Antibacterial activity against Escherichia coli NIH JC2 by agar dilution method2007Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13
Synthesis and antibacterial activity of 5-deoxy-5-episubstituted arbekacin derivatives.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID560598Antimicrobial activity against Escherichia coli JM109 transformant harboring pSTV28 plasmid by microdilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
AAC(6')-Iaf, a novel aminoglycoside 6'-N-acetyltransferase from multidrug-resistant Pseudomonas aeruginosa clinical isolates.
AID523398Antimicrobial activity against amikacin-susceptible Nocardia farcinica IFM 10152 harboring 16s rRNA A1408G mutant after 5 days by broth microdilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Homozygous triplicate mutations in three 16S rRNA genes responsible for high-level aminoglycoside resistance in Nocardia farcinica clinical isolates from a Canada-wide bovine mastitis epizootic.
AID299400Antibacterial activity against methicillin-resistant Staphylococcus aureus MF490 by agar dilution method2007Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13
Synthesis and antibacterial activity of 5-deoxy-5-episubstituted arbekacin derivatives.
AID456043Antibacterial activity against ciprofloxacin, methicillin-resistant Staphylococcus aureus after 18 hrs by twofold microbroth dilution method2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Design, synthesis and biological evaluations of novel 7-[3-(1-aminocycloalkyl)pyrrolidin-1-yl]-6-desfluoro-8-methoxyquinolones with potent antibacterial activity against multi-drug resistant Gram-positive bacteria.
AID520868Antibacterial activity against methicillin-resistant mecA-positive Staphylococcus saprophyticus isolate TSU28 isolated from genitourinary tracts of acute cystitis patient after 24 hrs at 35 degC by agar dilution method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Methicillin-resistant Staphylococcus saprophyticus isolates carrying staphylococcal cassette chromosome mec have emerged in urogenital tract infections.
AID276903Antibacterial activity against Pseudomonas aeruginosa GN3054 expressing AAC(3)-I by twofold agar dilution method2006Bioorganic & medicinal chemistry letters, Dec-15, Volume: 16, Issue:24
Synthesis and antibacterial activity of novel neamine derivatives.
AID310094Antibacterial activity against Pseudomonas aeruginosa N1012007Bioorganic & medicinal chemistry letters, Nov-15, Volume: 17, Issue:22
Effect of varying the 4''-position of arbekacin derivatives on antibacterial activity against MRSA and Pseudomonas aeruginosa.
AID310091Antibacterial activity against methicillin-resistant Staphylococcus aureus MSC035712007Bioorganic & medicinal chemistry letters, Nov-15, Volume: 17, Issue:22
Effect of varying the 4''-position of arbekacin derivatives on antibacterial activity against MRSA and Pseudomonas aeruginosa.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID276901Antibacterial activity against Pseudomonas aeruginosa PAO1 by twofold agar dilution method2006Bioorganic & medicinal chemistry letters, Dec-15, Volume: 16, Issue:24
Synthesis and antibacterial activity of novel neamine derivatives.
AID283222Antimicrobial activity against Escherichia coli XL1-Blue [pBluescript 2 SK(+)2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Coproduction of novel 16S rRNA methylase RmtD and metallo-beta-lactamase SPM-1 in a panresistant Pseudomonas aeruginosa isolate from Brazil.
AID456046Antibacterial activity against vancomycin-resistant Enterococcus faecium after 18 hrs by twofold microbroth dilution method2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Design, synthesis and biological evaluations of novel 7-[3-(1-aminocycloalkyl)pyrrolidin-1-yl]-6-desfluoro-8-methoxyquinolones with potent antibacterial activity against multi-drug resistant Gram-positive bacteria.
AID206650Antibacterial activity was determined against clinically isolated Levofloxacin-methicillin resistant Staphylococcus aureus (LVFX-r MRSA) strains (74 strains)2003Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6
Synthesis and structure-activity relationships of 5-amino-6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-8-methylquinolonecarboxylic acid antibacterials having fluorinated 7-[(3R)-3-(1-aminocyclopropan-1-yl)pyrrolidin-1-yl] substituents.
AID534774Antimicrobial activity against Acinetobacter baumannii-calcoaceticus obtained from war-wounded patient2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
In vitro activity of the aminoglycoside antibiotic arbekacin against Acinetobacter baumannii-calcoaceticus isolated from war-wounded patients at Walter Reed Army Medical Center.
AID310097Antibacterial activity against methicillin resistant Staphylococcus aureus isolates2007Bioorganic & medicinal chemistry letters, Nov-15, Volume: 17, Issue:22
Effect of varying the 4''-position of arbekacin derivatives on antibacterial activity against MRSA and Pseudomonas aeruginosa.
AID428869Antibacterial activity against Escherichia coli isolate ARS3 carrying pARS3 by agar dilution method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Novel plasmid-mediated 16S rRNA m1A1408 methyltransferase, NpmA, found in a clinically isolated Escherichia coli strain resistant to structurally diverse aminoglycosides.
AID534775Antimicrobial activity against Acinetobacter baumannii-calcoaceticus obtained from war-wounded patient assessed as zone of inhibition at 128 ug/ml by disk diffusion method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
In vitro activity of the aminoglycoside antibiotic arbekacin against Acinetobacter baumannii-calcoaceticus isolated from war-wounded patients at Walter Reed Army Medical Center.
AID520874Antibacterial activity against methicillin-resistant mecA-positive Staphylococcus saprophyticus isolate TSU90 isolated from genitourinary tracts of acute cystitis patient after 24 hrs at 35 degC by agar dilution method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Methicillin-resistant Staphylococcus saprophyticus isolates carrying staphylococcal cassette chromosome mec have emerged in urogenital tract infections.
AID1895487Antibacterial activity against methicillin resistant Staphylococcus aureus incubated for 24 hrs by broth microdilution method2021European journal of medicinal chemistry, Nov-15, Volume: 224Synthetic access to thiolane-based therapeutics and biological activity studies.
AID276900Antibacterial activity against Escherichia coli NIH JC2 by twofold agar dilution method2006Bioorganic & medicinal chemistry letters, Dec-15, Volume: 16, Issue:24
Synthesis and antibacterial activity of novel neamine derivatives.
AID310093Antibacterial activity against Pseudomonas aeruginosa PA012007Bioorganic & medicinal chemistry letters, Nov-15, Volume: 17, Issue:22
Effect of varying the 4''-position of arbekacin derivatives on antibacterial activity against MRSA and Pseudomonas aeruginosa.
AID523405Antimicrobial activity against amikacin-susceptible Nocardia farcinica IFM 10152 after 3 days by broth microdilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Homozygous triplicate mutations in three 16S rRNA genes responsible for high-level aminoglycoside resistance in Nocardia farcinica clinical isolates from a Canada-wide bovine mastitis epizootic.
AID520423Antibacterial activity against methicillin-resistant mecA-positive Staphylococcus saprophyticus isolate TSU18 isolated from genitourinary tracts of acute cystitis patient after 24 hrs at 35 degC by agar dilution method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Methicillin-resistant Staphylococcus saprophyticus isolates carrying staphylococcal cassette chromosome mec have emerged in urogenital tract infections.
AID560592Antimicrobial activity against multidrug resistant Pseudomonas aeruginosa isolate IMCJ2S1 by microdilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
AAC(6')-Iaf, a novel aminoglycoside 6'-N-acetyltransferase from multidrug-resistant Pseudomonas aeruginosa clinical isolates.
AID1503974Mutation read through activity in READ mouse on C57/BL6 background expressing premature termination codon TGA-containing mouse dystrophin gene exon 23 nucleotide sequence gene exon 23 assessed as ratio of luciferase activity to beta-galactosidase activity2017ACS medicinal chemistry letters, Oct-12, Volume: 8, Issue:10
Structure-Activity Relationship Study of Leucyl-3-
AID428873Antibacterial activity against Escherichia coli JM109 carrying pMCL210 by agar dilution method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Novel plasmid-mediated 16S rRNA m1A1408 methyltransferase, NpmA, found in a clinically isolated Escherichia coli strain resistant to structurally diverse aminoglycosides.
AID206629Antibacterial activity was determined against clinically isolated Levofloxacin-methicillin resistant Staphylococcus aureus (LVFX-r MRSA) strains (74 strains)2003Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6
Synthesis and structure-activity relationships of 5-amino-6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-8-methylquinolonecarboxylic acid antibacterials having fluorinated 7-[(3R)-3-(1-aminocyclopropan-1-yl)pyrrolidin-1-yl] substituents.
AID520869Antibacterial activity against methicillin-resistant mecA-positive Staphylococcus saprophyticus isolate TSU33 isolated from genitourinary tracts of acute cystitis patient after 24 hrs at 35 degC by agar dilution method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Methicillin-resistant Staphylococcus saprophyticus isolates carrying staphylococcal cassette chromosome mec have emerged in urogenital tract infections.
AID534776Cmax in war-wounded patient infected with Acinetobacter baumannii-calcoacetius at 2 to 3 mg/kg/day2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
In vitro activity of the aminoglycoside antibiotic arbekacin against Acinetobacter baumannii-calcoaceticus isolated from war-wounded patients at Walter Reed Army Medical Center.
AID276897Antibacterial activity against Staphylococcus aureus RN4220/pCR1948 expressing AAC(6')-APH(2'') enzyme by twofold agar dilution method2006Bioorganic & medicinal chemistry letters, Dec-15, Volume: 16, Issue:24
Synthesis and antibacterial activity of novel neamine derivatives.
AID310092Antibacterial activity against Escherichia coli NIH JC22007Bioorganic & medicinal chemistry letters, Nov-15, Volume: 17, Issue:22
Effect of varying the 4''-position of arbekacin derivatives on antibacterial activity against MRSA and Pseudomonas aeruginosa.
AID560593Antimicrobial activity against rifampin-resistant Pseudomonas aeruginosa ATCC 27853 by microdilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
AAC(6')-Iaf, a novel aminoglycoside 6'-N-acetyltransferase from multidrug-resistant Pseudomonas aeruginosa clinical isolates.
AID520870Antibacterial activity against methicillin-resistant mecA-positive Staphylococcus saprophyticus isolate TSU47 isolated from genitourinary tracts of acute cystitis patient after 24 hrs at 35 degC by agar dilution method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Methicillin-resistant Staphylococcus saprophyticus isolates carrying staphylococcal cassette chromosome mec have emerged in urogenital tract infections.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID299405Antibacterial activity against Pseudomonas aeruginosa N101 by agar dilution method2007Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13
Synthesis and antibacterial activity of 5-deoxy-5-episubstituted arbekacin derivatives.
AID276895Antibacterial activity against Staphylococcus aureus RN4220 by twofold agar dilution method2006Bioorganic & medicinal chemistry letters, Dec-15, Volume: 16, Issue:24
Synthesis and antibacterial activity of novel neamine derivatives.
AID276902Antibacterial activity against Pseudomonas aeruginosa GN4925 expressing AAC(6')-Ib by twofold agar dilution method2006Bioorganic & medicinal chemistry letters, Dec-15, Volume: 16, Issue:24
Synthesis and antibacterial activity of novel neamine derivatives.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID428872Antibacterial activity against Escherichia coli JM109 carrying pMCL-BE by agar dilution method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Novel plasmid-mediated 16S rRNA m1A1408 methyltransferase, NpmA, found in a clinically isolated Escherichia coli strain resistant to structurally diverse aminoglycosides.
AID428870Antibacterial activity against Escherichia coli CSH-2 carrying Escherichia coli ARS3 pARS3 by agar dilution method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Novel plasmid-mediated 16S rRNA m1A1408 methyltransferase, NpmA, found in a clinically isolated Escherichia coli strain resistant to structurally diverse aminoglycosides.
AID299399Antibacterial activity against Staphylococcus aureus 209P JC1 by agar dilution method2007Bioorganic & medicinal chemistry letters, Jul-01, Volume: 17, Issue:13
Synthesis and antibacterial activity of 5-deoxy-5-episubstituted arbekacin derivatives.
AID208626Antibacterial activity was determined against clinically isolated penicillin resistant Streptococcus pneumoniae (PRSP) strains (50 strains)2003Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6
Synthesis and structure-activity relationships of 5-amino-6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-8-methylquinolonecarboxylic acid antibacterials having fluorinated 7-[(3R)-3-(1-aminocyclopropan-1-yl)pyrrolidin-1-yl] substituents.
AID560600Antimicrobial activity against Escherichia coli JM109 transformant harboring pSTV28 plasmid expressing aac(6')-Iaf (TTG-ATG) mutant gene by microdilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
AAC(6')-Iaf, a novel aminoglycoside 6'-N-acetyltransferase from multidrug-resistant Pseudomonas aeruginosa clinical isolates.
AID276896Antibacterial activity against Staphylococcus aureus RN4220/pMS520 expressing AAD(4')-I enzyme by twofold agar dilution method2006Bioorganic & medicinal chemistry letters, Dec-15, Volume: 16, Issue:24
Synthesis and antibacterial activity of novel neamine derivatives.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID564686Antimicrobial activity against beta lactamase KPC-producing Klebsiella pneumoniae isolates by microdilution method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
ACHN-490, a neoglycoside with potent in vitro activity against multidrug-resistant Klebsiella pneumoniae isolates.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID310089Antibacterial activity against Staphylococcus aureus 209P JC-12007Bioorganic & medicinal chemistry letters, Nov-15, Volume: 17, Issue:22
Effect of varying the 4''-position of arbekacin derivatives on antibacterial activity against MRSA and Pseudomonas aeruginosa.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID276899Antibacterial activity against gentamycin and arbekacin-resistant Staphylococcus aureus MF490 expressing AAD(4'), AAC(6')-APH(2'') enzymes by twofold agar dilution method2006Bioorganic & medicinal chemistry letters, Dec-15, Volume: 16, Issue:24
Synthesis and antibacterial activity of novel neamine derivatives.
AID523397Antimicrobial activity against amikacin-susceptible Nocardia farcinica IFM 10152 harboring 16s rRNA A1408G mutant after 3 days by broth microdilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Homozygous triplicate mutations in three 16S rRNA genes responsible for high-level aminoglycoside resistance in Nocardia farcinica clinical isolates from a Canada-wide bovine mastitis epizootic.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID283220Antimicrobial activity against Pseudomonas aeruginosa PA09052007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Coproduction of novel 16S rRNA methylase RmtD and metallo-beta-lactamase SPM-1 in a panresistant Pseudomonas aeruginosa isolate from Brazil.
AID283221Antimicrobial activity against Escherichia coli XL1-Blue pPA95S292007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Coproduction of novel 16S rRNA methylase RmtD and metallo-beta-lactamase SPM-1 in a panresistant Pseudomonas aeruginosa isolate from Brazil.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID523396Antimicrobial activity against amikacin-resistant Nocardia farcinica IFM 10580 after 3 days by broth microdilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Homozygous triplicate mutations in three 16S rRNA genes responsible for high-level aminoglycoside resistance in Nocardia farcinica clinical isolates from a Canada-wide bovine mastitis epizootic.
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID208611Antibacterial activity was determined against clinically isolated penicillin resistant Streptococcus pneumoniae (PRSP) strains (50 strains)2003Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6
Synthesis and structure-activity relationships of 5-amino-6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-8-methylquinolonecarboxylic acid antibacterials having fluorinated 7-[(3R)-3-(1-aminocyclopropan-1-yl)pyrrolidin-1-yl] substituents.
AID560591Antimicrobial activity against Pseudomonas aeruginosa isolate IMCJ799 by microdilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
AAC(6')-Iaf, a novel aminoglycoside 6'-N-acetyltransferase from multidrug-resistant Pseudomonas aeruginosa clinical isolates.
AID520873Antibacterial activity against methicillin-resistant mecA-positive Staphylococcus saprophyticus isolate TSU69 isolated from genitourinary tracts of acute cystitis patient after 24 hrs at 35 degC by agar dilution method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Methicillin-resistant Staphylococcus saprophyticus isolates carrying staphylococcal cassette chromosome mec have emerged in urogenital tract infections.
AID66572Antibacterial activity was determined against clinically isolated vancomycin-A resistant enterococci (VRE) strains (33 strains)2003Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6
Synthesis and structure-activity relationships of 5-amino-6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-8-methylquinolonecarboxylic acid antibacterials having fluorinated 7-[(3R)-3-(1-aminocyclopropan-1-yl)pyrrolidin-1-yl] substituents.
AID428871Antibacterial activity against Escherichia coli CSH-2 by agar dilution method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Novel plasmid-mediated 16S rRNA m1A1408 methyltransferase, NpmA, found in a clinically isolated Escherichia coli strain resistant to structurally diverse aminoglycosides.
AID534771Antimicrobial activity against Acinetobacter baumannii-calcoaceticus obtained from war-wounded patient assessed as susceptible isolates2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
In vitro activity of the aminoglycoside antibiotic arbekacin against Acinetobacter baumannii-calcoaceticus isolated from war-wounded patients at Walter Reed Army Medical Center.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID567091Drug absorption in human assessed as human intestinal absorption rate2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Prediction of drug intestinal absorption by new linear and non-linear QSPR.
AID520871Antibacterial activity against methicillin-resistant mecA-positive Staphylococcus saprophyticus isolate TSU57 isolated from genitourinary tracts of acute cystitis patient after 24 hrs at 35 degC by agar dilution method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Methicillin-resistant Staphylococcus saprophyticus isolates carrying staphylococcal cassette chromosome mec have emerged in urogenital tract infections.
AID66578Antibacterial activity was determined against clinically isolated vancomycin-B resistant enterococci (VRE) strains (10 strains)2003Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6
Synthesis and structure-activity relationships of 5-amino-6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-8-methylquinolonecarboxylic acid antibacterials having fluorinated 7-[(3R)-3-(1-aminocyclopropan-1-yl)pyrrolidin-1-yl] substituents.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (260)

TimeframeStudies, This Drug (%)All Drugs %
pre-199022 (8.46)18.7374
1990's94 (36.15)18.2507
2000's82 (31.54)29.6817
2010's53 (20.38)24.3611
2020's9 (3.46)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials26 (9.85%)5.53%
Reviews17 (6.44%)6.00%
Case Studies19 (7.20%)4.05%
Observational0 (0.00%)0.25%
Other202 (76.52%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (5)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Randomized, Open-Label Phase 1b Study of ME1100 Inhalation Solution Plus Best Available Therapy in the Treatment of Mechanically Ventilated Subjects With Bacterial Pneumonia [NCT02459158]Phase 125 participants (Actual)Interventional2015-09-30Completed
A Randomized, Double-Blind, Placebo-Controlled, Single Ascending Dose Study to Assess the Safety, Tolerability, and Pharmacokinetics of ME1100 Inhalation Solution (Arbekacin Inhalation Solution) Administered to Healthy Volunteers [NCT01907776]Phase 156 participants (Actual)Interventional2013-07-31Completed
Phase II Study of Nonsense Readthrough Compound NPC-14 (Arbekacin Sulfate) to Explore Safety, Tolerability, and Efficacy in Duchenne Muscular Dystrophy Patients (NORTH POLE DMD Study) [NCT01918384]Phase 221 participants (Anticipated)Interventional2013-08-31Active, not recruiting
An Open-label, Single Dose Study to Assess Intrapulmonary Pharmacokinetics of ME1100 Inhalation Solution Administered to Healthy Volunteers [NCT01961830]Phase 142 participants (Actual)Interventional2013-09-30Completed
Arbekacin Treatment of Adult Patients With Infections Caused by Multidrug-resistant Bacteria [NCT01659515]0 participants Expanded AccessNo longer available
[information is prepared from clinicaltrials.gov, extracted Sep-2024]