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dibekacin

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Description

Dibekacin: Analog of KANAMYCIN with antitubercular as well as broad-spectrum antimicrobial properties. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

dibekacin : A kanamycin that is kanamycin B lacking the 3- and 4-hydroxy groups on the 2,6-diaminosugar 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 CID470999
CHEMBL ID560976
CHEBI ID37945
SCHEMBL ID49816
MeSH IDM0006245

Synonyms (66)

Synonym
AC-315
(1r,2s,3s,4r,6s)-4,6-diamino-3-[(3-amino-3-deoxy-alpha-d-glucopyranosyl)oxy]-2-hydroxycyclohexyl 2,6-diamino-2,3,4,6-tetradeoxy-alpha-d-erythro-hexopyranoside
SPECTRUM_001398
DKM ,
3',4'-dideoxykanamycin b
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))-2-deoxy-l-streptamine
(1r,2s,3s,4r,6s)-4,6-diamino-3-(3-amino-3-deoxy-alpha-d-glucopyranosyloxy)-2-hydroxycyclohexyl 2,6-diamino-2,3,4,6-tetradeoxy-alpha-d-erythro-hexopyranoside
CHEBI:37945 ,
SPECTRUM5_001613
DKB ,
brn 1441606
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)-2-deoxy-
panamicin
34493-98-6
(2s,3r,4s,5s,6r)-4-amino-2-[(1s,2s,3r,4s,6r)-4,6-diamino-3-[(2r,3r,6s)-3-amino-6-(aminomethyl)tetrahydropyran-2-yl]oxy-2-hydroxy-cyclohexoxy]-6-(hydroxymethyl)tetrahydropyran-3,5-diol
dibekacin
dideoxykanamycin b
KBIO2_007014
KBIO3_002060
KBIOGR_001428
KBIO2_004446
KBIOSS_001878
KBIO2_001878
SPECTRUM3_000960
SPECTRUM2_001528
SPBIO_001316
SPECTRUM4_001074
dibekacinum [inn-latin]
dibekacine [inn-french]
dibekacina [inn-spanish]
einecs 252-064-6
debecacin
kappati
CHEMBL560976
dibekacin (inn)
D07811
(2s,3r,4s,5s,6r)-4-amino-2-[(1s,2s,3r,4s,6r)-4,6-diamino-3-[(2r,3r,6s)-3-amino-6-(aminomethyl)oxan-2-yl]oxy-2-hydroxycyclohexyl]oxy-6-(hydroxymethyl)oxane-3,5-diol
cas-34493-98-6
tox21_111496
dtxcid302915
dtxsid2022915 ,
dibekacina
dibekacinum
dibekacine
45zfo9e525 ,
dibekacin [inn:ban]
unii-45zfo9e525
dibekacin [who-dd]
dibekacin [inn]
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))-2-deoxy-l-streptamine
dibekacin [jan]
dibekacin [mi]
CCG-213771
SCHEMBL49816
CS-4725
JJCQSGDBDPYCEO-XVZSLQNASA-N
HY-B1129
AB01563356_01
AKOS025402025
84D ,
Q3706873
DB13270
NCGC00389765-01
gtpl12134
(2s,3r,4s,5s,6r)-4-amino-2-{[(1s,2s,3r,4s,6r)-4,6-diamino-3-{[(2r,3r,6s)-3-amino-6-(aminomethyl)oxan-2-yl]oxy}-2-hydroxycyclohexyl]oxy}-6-(hydroxymethyl)oxane-3,5-diol
EN300-20000885

Research Excerpts

Overview

Dibekacin is a semisynthetic aminonglycoside derivative of kanamicin B. It has highly activity against most gram-positive and gramnegative bacteria. Dibkacin proved itself to be a new alternative when aminoglycoside antibiotics are indicated.

ExcerptReferenceRelevance
"Dibekacin is a semisynthetic aminonglycoside derivative of kanamicin B, with highly activity against most gram-positive and gramnegative bacteria. "( [Comparative activity of dibekacin and several cephalosporins on Pseudomonas aeruginosa].
Aragno, M; Carlone, NA; Cuffini, AM; Forno-Pizzoglio, M,
)
1.88
"Dibekacin is a new aminoglycoside derived semi-synthetically from kanamycin B. "( [In vitro antibacterial activity of dibekacin on staphylococci, streptococci and aerobic Gram negative bacilli].
Deforges, L; Duval, J; Le Soussy, CJ; Van Thoi, J, 1982
)
1.98
"Dibekacin proved itself to be a new alternative when aminoglycoside antibiotics are indicated"( [Therapy of surgical infections with dibekacin. Pharmacokinetic, clinical and bacteriological results].
Primavesi, CA; Sievers, U; von Kobyletzki, D, 1980
)
1.26
"Dibekacin (Orbicin) is a new aminoglycoside antibiotic which chemically differs from tobramycin only by lack of an OH-group. "( [Dibekacin--a novel aminoglycoside antibioticl. Antimicrobial activity and parallel resistance in vitro].
Schassan, HH; Witt, U, 1979
)
2.61

Treatment

ExcerptReferenceRelevance
"Dibekacin-treated animals showed a significant (P less than 0.05) increase in the thresholds of the Preyer pinna reflex and the VIIIth nerve compound action potential in response to sound click stimulation."( Comparative ototoxicity of dibekacin and netilmicin in guinea pigs.
Arpini, A; Forlani, A; Marzanatti, M; Parravicini, L, 1983
)
1.28

Toxicity

The toxic effects of dibekacin sulfate (DKB) in male and female rats were examined in chronic toxicity test (intraperitoneal injection), and the following results were obtained.

ExcerptReferenceRelevance
"The LD50 values of dibekacin to mice were determined following three different methods of administration, namely, intravenous constant infusion, intravenous bolus injection, and intramuscular injection."( Acute toxicity and pharmacokinetics of dibekacin mice.
Fujita, M; Kikai, S; Komiya, I; Murata, S; Tomono, N; Umemura, K, 1981
)
0.86
" (5) Judging from the above-mentioned results, "the maximal non toxic dose" through the intraperitoneal administration to rats of this drug was assumed 20 mg/kg in either sex."( [Toxicological studies on dibekacin for intravenous injection use. I. Subacute toxicity in rats and rabbits (author's transl)].
Hirano, F; Ishiwatari, N; Kawaoto, H; Koeda, T; Kumagai, K; Niizato, T; Odaki, M; Sasaki, H; Suzuki, H; Watanabe, H; Watanuki, T; Yokota, M, 1980
)
0.56
"The toxic effects of dibekacin sulfate (DKB) in male and female rats were examined in chronic toxicity test (intraperitoneal injection), and the following results were obtained."( [Toxicological studies on dibekacin for intravenous injection use. II. Chronic toxicity in rats (author's transl)].
Hirano, F; Ishiwatari, N; Kawaoto, H; Koeda, T; Niizato, T; Odaki, M; Sasaki, H; Senoo, A; Watanabe, H; Watanuki, T; Yokota, M, 1980
)
0.88
" 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
" Vigamox(®) containing moxifloxacin and Tosuflo(®) containing tosufloxacin were more toxic when compared with the other antibiotics."( In vitro assessment of the cytotoxicity of six topical antibiotics to four cultured ocular surface cell lines.
Ayaki, M; Iwasawa, A; Niwano, Y, 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 kidneys accumulated high amounts of dibekacin, and eliminated it with a half-life of about 7 days. The pharmacokinetic test results and the efficacy with severe infections showed dibkacin to be equivalent to the new aminoglycoside antibiotics gentamycin, sisomicin and tobramycin.

ExcerptReferenceRelevance
" The biological half-life of DKB was prolonged in pretreatment with ABPC and that of ABPC was shortened in pretreatment with DKB."( [Fundamental studies of combination of antibiotics, especially on pharmacokinetics. III. Combination of ampicillin and dibekacin (author's transl)].
Aratani, H; Nakatsuka, M, 1979
)
0.47
" The serum levels of this drug were in proportion to dosage, and the pharmacokinetic parameters were almost the same through the three dosage levels."( Pharmacokinetics of dibekacin after intramuscular administration in man.
Chow, SY; Komiya, I; Nakadori, S; Umemura, K, 1977
)
0.58
" 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
" Comparison of pharmacokinetic parameters (i."( Pharmacokinetics of dibekacin in children with cystic fibrosis.
Courcol, RJ; Delnatte, J; Loeuille, GA; Martin, GR, 1985
)
0.59
"A study was made of the serum levels and of the pharmacokinetic parameters of dibekacin after administration by intravenous infusion at a dose of 2 mg/kg of the drug to rabbits using different infusion times."( Effect of infusion time on the pharmacokinetics of dibekacin in rabbits.
Dominguez-Gil, A; Lanao, JM; Navarro, AS, 1984
)
0.75
"The pharmacokinetic behavior of dibekacin was studied in 8 elderly subjects."( [Pharmacokinetic studies on intravenous drip infusion of dibekacin in elderly subjects without apparent renal failure (author's transl)].
Okada, K; Sawae, Y; Umemura, K, 1982
)
0.79
"The principal pharmacokinetic parameters of dibekacin were studied in five adult subjects with normal renal function after IM and IV injection of a single dose of 1 mg/kg."( [Pharmacokinetics of dibekacin in subjects with normal renal function].
Borsa, F; Humbert, G; Leroy, A; Thauvin, C, 1982
)
0.84
" Renal insufficiency caused a very marked prolongation in the serum half-life of elimination."( [Pharmacokinetics of dibekacin in patients with chronic renal impairment].
Fillastre, JP; Godin, M; Leroy, A; Viotte, G, 1982
)
0.58
" The kidneys accumulated high amounts of dibekacin, and eliminated it with a half-life of about 7 days."( [Animal experiments on the nephrotoxicity, pharmacokinetics and therapeutic efficacy of dibekacin].
Bopp, S; Marre, R; Sack, K; Schulz, E, 1981
)
0.75
" 2) The biological half-life of dibekacin in mice was 24--45 min."( Acute toxicity and pharmacokinetics of dibekacin mice.
Fujita, M; Kikai, S; Komiya, I; Murata, S; Tomono, N; Umemura, K, 1981
)
0.82
" 1) In both rabbits and dogs, the pharmacokinetic constants for the intravenous constant infusion and intramuscular injection were similar to each other, and the serum levels after the intravenous constant infusion for 1 hr were similar to those after the intramuscular injection except the peak time."( Pharmacokinetics of dibekacin in rabbits and dogs.
Fujita, M; Kikai, S; Komiya, I; Murata, S; Tomono, N; Umemura, K, 1981
)
0.59
" The pharmacokinetic test results and the efficacy with severe infections showed dibekacin to be equivalent to the new aminoglycoside antibiotics gentamycin, sisomicin and tobramycin."( [Therapy of surgical infections with dibekacin. Pharmacokinetic, clinical and bacteriological results].
Primavesi, CA; Sievers, U; von Kobyletzki, D, 1980
)
0.76
"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
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35
" 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
"In vivo synergistic effects of cefodizime (CDZM) were investigated in combination with aminoglycosides (AGs), sisomicin (SISO) or dibekacin (DKB) against Pseudomonas aeruginosa in immunocompromised tumour bearing mice."( [Therapeutic efficacy of cefodizime in combination with aminoglycosides against systemic infections caused by Pseudomonas aeruginosa in immunocompromised tumour bearing mice].
Deguchi, K; Furukawa, T; Hyodo, A; Miyake, Y; Uji, T, 1993
)
0.49
" 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
" The absorption rate (AR) was obtained by dividing the concentration of DKB in RC by that in DC."( [Inhibitory effect of nasal mucus on the absorption of drugs through respiratory epithelium].
Hayashi, H, 1990
)
0.28
" 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
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

The pharmacokinetic behavior of dibekacin after intramuscular administration was studied in nine healthy volunteers. 50 patients were treated with a dosage of 150-225 mg dibakacin, administered in three single daily doses. Dibkacin and gentamicin show reproducibly higher renal cortical tissue concentrations than tobramycin in the acute infusion studies and multiple dosing studies.

ExcerptRelevanceReference
" In the second group, the dosage of each antibiotic necessary to induce apnea is sought."( [Neuromuscular inhibition of new aminoglycoside antibiotics].
Baltar, I; Esplugues, J; Marti, JL; Orts, A, 1979
)
0.26
"Pharmacokinetic behavior of dibekacin after intramuscular administration was studied in nine healthy volunteers by cross over administrations of three dosage levels (1 mg(pot."( Pharmacokinetics of dibekacin after intramuscular administration in man.
Chow, SY; Komiya, I; Nakadori, S; Umemura, K, 1977
)
0.87
" 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
" After having given their written informed consent, 50 patients were treated with a dosage of 150-225 mg dibekacin, administered in three single daily doses."( [Therapy of urinary tract infections with dibekacin].
Kuber, W; Loebenstein, T; Maier, U, 1983
)
0.74
" In special paragraphs the intrinsic ototoxic potential of the newer aminoglycoside antibiotics, the influence of the dosage and route of administration, of renal function, preexisting hearing disturbances, individual and familial sensitivity, pregnancy, newborn age and the combination with sound exposure, diuretics and cephalosporins are considered."( Drug-induced sudden hearing loss and vestibular disturbances.
Federspil, P, 1981
)
0.26
" Comparatively, kanamycin has a major ototoxic effect when it is administrated at the same dosage during the same period of time."( [Experimental study of the intrauterine ototoxicity of dibekacin].
Marot, M; Uziel, A, 1982
)
0.51
" After repetitive dosing a distinct tendency to accumulation (highest renal concentration: 330 microgram/g) could be detected."( [Animal experiments on the nephrotoxicity, pharmacokinetics and therapeutic efficacy of dibekacin].
Bopp, S; Marre, R; Sack, K; Schulz, E, 1981
)
0.48
" Dibekacin and gentamicin show reproducibly higher renal cortical tissue concentrations than tobramycin in both the acute infusion studies and multiple dosing studies."( Dibekacin intrarenal distribution characteristics and renal cortical elution kinetics. Comparison with gentamicin and tobramycin.
Bryant, HH; Carter, GG; Herbst, DV; Stout, RL; Walker, G; Whelton, A,
)
2.48
" From the calculated pharmacokinetic parameters, a dosage regimen for this kind of patient is proposed."( Disposition of Dibekacin in patients undergoing haemodialysis.
Campillo, JA; Dominguez-Gil, A; Lanao, JM; Martin, A; Rubio, F, 1980
)
0.61
" In this latter group, otitis media was induced by injecting glycerin into the middle ear clefts 1 months after birth, and the degree of inflammation was varied by administering or withholding antibiotics (cefamandole and dibekacin) and adjusting the dosage regimen."( The relationship between the degree of chronic middle ear inflammation and tympanic bulla pneumatization in the pig as animal model.
Ikarashi, F; Nakano, Y; Okura, T, 1994
)
0.47
" 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
" Depending on the intended indication and dosing regimen, PPL can delay or stop development of a compound in the drug discovery process."( Evaluation of a published in silico model and construction of a novel Bayesian model for predicting phospholipidosis inducing potential.
Gehlhaar, D; Greene, N; Johnson, TO; Pelletier, DJ; Tilloy-Ellul, A,
)
0.13
" 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 (2)

RoleDescription
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.
[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 (1)

ClassDescription
kanamycins
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (2)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
AR proteinHomo sapiens (human)Potency31.06340.000221.22318,912.5098AID743040; AID743042; AID743054
estrogen nuclear receptor alphaHomo sapiens (human)Potency11.88320.000229.305416,493.5996AID743079
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (57)

Assay IDTitleYearJournalArticle
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
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1119390Antibacterial activity against kanamycin-resistant Pseudomonas aeruginosa GN315 expressing AAC(6') enzyme2012MedChemComm, Apr-01, Volume: 3, Issue:4
Understanding and overcoming aminoglycoside resistance caused by N-6'-acetyltransferase.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1119389Antibacterial activity against kanamycin-resistant Escherichia coli K-12 R5 expressing AAC(6') enzyme2012MedChemComm, Apr-01, Volume: 3, Issue:4
Understanding and overcoming aminoglycoside resistance caused by N-6'-acetyltransferase.
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.
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.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID523067Activity of Aminoglycoside 2'-phosphotransferase 2a using ATP/GTP as second substrate by spectrophotometric assay2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Mutant APH(2'')-IIa enzymes with increased activity against amikacin and isepamicin.
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.
AID523072Ratio of Kcat to Km for Aminoglycoside 2'-phosphotransferase 2a R92H/D268N mutant using ATP/GTP as second substrate by spectrophotometric assay2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Mutant APH(2'')-IIa enzymes with increased activity against amikacin and isepamicin.
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.
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.
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.
AID523069Activity of Aminoglycoside 2'-phosphotransferase 2a R92H/D268N mutant using ATP/GTP as second substrate by spectrophotometric assay2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Mutant APH(2'')-IIa enzymes with increased activity against amikacin and isepamicin.
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID522930Antibacterial activity against Escherichia coli JM83 harboring pHF022 containing aminoglycoside 2''-2a phosphotransferase R92H/D268N mutant by broth microdilution method2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Mutant APH(2'')-IIa enzymes with increased activity against amikacin and isepamicin.
AID588220Literature-mined public compounds from Kruhlak et al phospholipidosis modelling dataset2008Toxicology mechanisms and methods, , Volume: 18, Issue:2-3
Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models.
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]
AID588208Literature-mined public compounds from Lowe et al phospholipidosis modelling dataset2010Molecular pharmaceutics, Oct-04, Volume: 7, Issue:5
Predicting phospholipidosis using machine learning.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
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]
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.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
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.
AID522933Antibacterial activity against Escherichia coli JM83 harboring pHF022 containing aminoglycoside 2''-2a D268N mutant by broth microdilution method2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Mutant APH(2'')-IIa enzymes with increased activity against amikacin and isepamicin.
AID522931Antibacterial activity against Escherichia coli JM83 harboring pHF022 containing aminoglycoside 2''-2a phosphotransferase R92H mutant by broth microdilution method2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Mutant APH(2'')-IIa enzymes with increased activity against amikacin and isepamicin.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
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]
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]
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
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.
AID523068Activity of Aminoglycoside 2'-phosphotransferase 2a N196D/D268N mutant using ATP/GTP as second substrate by spectrophotometric assay2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Mutant APH(2'')-IIa enzymes with increased activity against amikacin and isepamicin.
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
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.
AID540237Phospholipidosis-positive literature compound observed in rat
AID523070Ratio of Kcat to Km for Aminoglycoside 2'-phosphotransferase 2a using ATP/GTP as second substrate by spectrophotometric assay2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Mutant APH(2'')-IIa enzymes with increased activity against amikacin and isepamicin.
AID523071Ratio of Kcat to Km for Aminoglycoside 2'-phosphotransferase 2a N196D/D268N mutant using ATP/GTP as second substrate by spectrophotometric assay2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Mutant APH(2'')-IIa enzymes with increased activity against amikacin and isepamicin.
AID522929Antibacterial activity against Escherichia coli JM83 harboring pHF022 containing aminoglycoside 2''-2a phosphotransferase N196D/D268N mutant by broth microdilution method2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Mutant APH(2'')-IIa enzymes with increased activity against amikacin and isepamicin.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID523066Antibacterial activity against Escherichia coli JM83 harboring empty pHF022 vector by broth microdilution method2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Mutant APH(2'')-IIa enzymes with increased activity against amikacin and isepamicin.
AID522928Antibacterial activity against Escherichia coli JM83 producing aminoglycoside 2''-2a phosphotransferase by broth microdilution method2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Mutant APH(2'')-IIa enzymes with increased activity against amikacin and isepamicin.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID522932Antibacterial activity against Escherichia coli JM83 harboring pHF022 containing aminoglycoside 2''-2a N196D mutant by broth microdilution method2010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Mutant APH(2'')-IIa enzymes with increased activity against amikacin and isepamicin.
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]
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (478)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990212 (44.35)18.7374
1990's115 (24.06)18.2507
2000's84 (17.57)29.6817
2010's60 (12.55)24.3611
2020's7 (1.46)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 33.68

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

MetricThis Compound (vs All)
Research Demand Index33.68 (24.57)
Research Supply Index6.28 (2.92)
Research Growth Index4.31 (4.65)
Search Engine Demand Index51.07 (26.88)
Search Engine Supply Index2.10 (0.95)

This Compound (33.68)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials33 (6.57%)5.53%
Reviews20 (3.98%)6.00%
Case Studies32 (6.37%)4.05%
Observational0 (0.00%)0.25%
Other417 (83.07%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (1)

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
[information is prepared from clinicaltrials.gov, extracted Sep-2024]