Page last updated: 2024-11-05

nafcillin

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

Description

Nafcillin is a beta-lactam antibiotic that is effective against gram-positive bacteria. It is a semisynthetic penicillin derivative that was first synthesized in the 1960s. Nafcillin inhibits the synthesis of peptidoglycan, a major component of bacterial cell walls, leading to bacterial cell lysis. It is primarily used to treat infections caused by Staphylococcus aureus, including skin infections, pneumonia, and endocarditis. Nafcillin is typically administered intravenously or intramuscularly. However, due to the emergence of methicillin-resistant Staphylococcus aureus (MRSA), nafcillin is often not effective against these strains. Nafcillin is studied to understand its mechanism of action, optimize its efficacy, and develop new antibiotics with improved resistance profiles.'

Nafcillin: A semi-synthetic antibiotic related to penicillin. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

nafcillin : A penicillin in which the substituent at position 6 of the penam ring is a (2-ethoxy-1-naphthoyl)amino group. [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 CID8982
CHEMBL ID1443
CHEBI ID7447
SCHEMBL ID47797
MeSH IDM0014418

Synonyms (77)

Synonym
BRD-K18574842-323-03-3
(2s,5r,6r)-6-({[2-(ethyloxy)naphthalen-1-yl]carbonyl}amino)-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid
(2s,5r,6r)-6-[(2-ethoxynaphthalene-1-carbonyl)amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid
4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid, 6-[[(2-ethoxy-1-naphthalenyl)carbonyl]amino]-3,3-dimethyl-7-oxo-, (2s,5r,6r)-
BSPBIO_000825
PRESTWICK2_000843
PRESTWICK3_000843
BPBIO1_000909
C07250
147-52-4
nafcillin
(2-ethoxy-1-naphthalenyl)penicillin
(2-ethoxy-1-naphthyl)penicillin
(2s,5r,6r)-6-[(2-ethoxy-1-naphthoyl)amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid
6-(2-ethoxy-1-naphthamido)penicillanic acid
naphcillin
DB00607
brn 0862393
penicillin, (2-ethoxy-1-naphthalenyl)-
4-thia-1-azabicyclo(3.2.0)heptane-2-carboxylic acid, 6-(((2-ethoxy-1-naphthalenyl)carbonyl)amino)-3,3-dimethyl-7-oxo-, (2s-(2alpha,5alpha,6beta))-
einecs 205-690-9
hsdb 3133
nafcilin-1
nafcillin [inn:ban]
nafcilina [inn-spanish]
nafcillinum [inn-latin]
naphthamidopenicillin
penicillin, (2-ethoxy-1-naphthyl)-
nafcilline [inn-french]
4-thia-1-azabicyclo(3.2.0)heptane-2-carboxylic acid, 6-(2-ethoxy-1-naphthamido)-3,3-dimethyl-7-oxo-
PRESTWICK1_000843
SPBIO_002746
PRESTWICK0_000843
(2s,5r,6r)-6-{[(2-ethoxynaphthalen-1-yl)carbonyl]amino}-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid
nafcilline
CHEBI:7447 ,
nafcilina
6beta-(2-ethoxynaphthalene-1-carboxamido)-2,2-dimethylpenam-3alpha-carboxylic acid
nafcillinum
CHEMBL1443
D08242
nafcillin (inn)
(2s,5r,6r)-6-(2-ethoxynaphthalene-1-amido)-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid
unii-4cnz27m7rv
4cnz27m7rv ,
EPITOPE ID:141583
(2s-(2.alpha.,5.alpha.,6.beta.))-6-(((2-ethoxy-l-naphthalenyl)carbonyl)-amino)-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo(3.2.0)heptane-2-carboxylic acid
nafcillin [mi]
nafcillin [inn]
nafcillin [hsdb]
nafcillin [vandf]
4-thia-1-azabicyclo(3.2.0)heptane-2-carboxylic acid, 6-(((2-ethoxy-1-naphthalenyl)carbonyl)amino)-3,3-dimethyl-7-oxo-, (2s,5r,6r)-
nafcillin [who-dd]
SCHEMBL47797
W-108115
DTXSID8023343 ,
bdbm50103525
(2s,5r,6r)-6-(2-ethoxy-1-naphthamido)-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid
BCP17447
Q1638852
gtpl10942
ethoxynaphthamido penicillin sodium
EN300-24433472
CS-0009511
HY-B0555
AKOS040744845
nafcilina (inn-spanish)
4-thia-1-azabicyclo(3.2.0)heptane-2-carboxylic acid, 6-(((2-ethoxy-1-naphthalenyl)carbonyl)amino)-3,3-dimethyl-7-oxo-, (2s///
(2s-(2alpha,5alpha,6beta))-6-(((2-ethoxy-l-naphthalenyl)carbonyl)-amino)-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo(3.2.0)heptane-2-carboxylic acid
nafcilline (inn-french)
(2s,5r,6r)-6-((2-ethoxy-1-naphthoyl)amino)-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo(3.2.0)heptane-2-carboxylic acid
(2s,5r,6r)-6-(((2-ethoxynaphthalen-1-yl)carbonyl)amino)-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo(3.2.0)heptane-2-carboxylic acid
j01cf06
(2s,5r,6r)-6-((2-ethoxynaphthalene-1-carbonyl)amino)-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo(3.2.0)heptane-2-carboxylic acid
nafcillina
nafcillinum (inn-latin)
dtxcid303343

Research Excerpts

Overview

Nafcillin is an antibiotic used for infections due to penicillin-resistant Staphylococcus aureus. It is a semisyntheticPenicillin that is generally well tolerated with few side effects.

ExcerptReferenceRelevance
"Nafcillin is an antibiotic used for infections due to penicillin-resistant Staphylococcus aureus. "( Nafcillin-induced bullous skin eruption with granulocytopenia in a patient with end-stage renal disease.
Chang, MO; Chang, YS; Chung, S; Kim, MJ; Koh, ES; Park, CW; Shin, SJ, 2012
)
3.26
"Nafcillin is a semisynthetic penicillin that is generally well tolerated with few side effects. "( Nafcillin-associated hepatotoxicity. Report of a case and review of the literature.
Janney, CG; Neuschwander-Tetri, BA; Presti, ME, 1996
)
3.18
"Nafcillin is a widely used penicillinase-resistant penicillin. "( Hepatic and renal dysfunction following nafcillin administration.
Hetsko, CM; Lestico, MR; Vick, KE,
)
1.84

Effects

ExcerptReferenceRelevance
"Nafcillin has been used as adjunctive therapy to clear persistent MRSA bacteremia. "( Nafcillin enhances innate immune-mediated killing of methicillin-resistant Staphylococcus aureus.
Bayer, AS; Dam, Q; Dhand, A; Hensler, ME; Nizet, V; Nonejuie, P; Okumura, CY; Olson, J; Pogliano, J; Sakoulas, G; Thienphrapa, W; Yeaman, MR, 2014
)
3.29

Treatment

Nafcillin treatment was associated with higher rates of both PAD as well as DEEs compared with cefazolin treatment. Treatment with nafcill in combination with vancomycin cleared bloodstream infections within 24 h and sterilized 12/13 spleens.

ExcerptReferenceRelevance
"Nafcillin treatment was associated with higher rates of both PAD as well as DEEs compared with cefazolin treatment. "( Comparative evaluation of the tolerability of cefazolin and nafcillin for treatment of methicillin-susceptible Staphylococcus aureus infections in the outpatient setting.
Hooper, DC; Nelson, SB; Shenoy, ES; Youngster, I, 2014
)
2.09
"Nafcillin treatment is associated with higher rates of adverse events and treatment discontinuation than oxacillin among hospitalized adult patients."( Adverse Events Lead to Drug Discontinuation More Commonly among Patients Who Receive Nafcillin than among Those Who Receive Oxacillin.
Byers, KE; Falcione, BA; He, P; Oleksiuk, LM; Sheridan, KR; Shields, RK; Viehman, JA, 2016
)
1.38
"Four nafcillin-treated prostheses, six silver-pefloxacin-coated grafts, and 11 control grafts were interposed in the infrarenal aorta of dogs and immediately challenged with an intravenous infusion of 1 X 10(7) Staphylococcus aureus."( Simple methods for direct antibiotic protection of synthetic vascular grafts.
Benvenisty, AI; Fox, CL; Modak, S; Nowygrod, R; Reemtsma, K; Voorhees, AB; White, JV, 1984
)
0.72
"Nafcillin pretreatment of donor and recipient strains was used in all subsequent conjugation experiments."( Transposon Tn916 mutagenesis in Bacillus anthracis.
Ivins, BE; Knudson, GB; Leblanc, DJ; Welkos, SL, 1988
)
1
"Treatment with nafcillin (NAF) has been preferred to cefazolin (CFZ)."( A comparison of safety and outcomes with cefazolin versus nafcillin for methicillin-susceptible Staphylococcus aureus bloodstream infections.
Barber, GR; Barron, MA; Fish, DN; Goolsby, TA; Miller, MA; Moine, P; Mueller, SW, 2020
)
1.14
"Treatment with nafcillin in combination with vancomycin cleared bloodstream infections within 24 h and sterilized 12/13 spleens (92%), as well as 8/13 kidneys (62%), following 3 days of treatment."( Successful therapy of experimental endocarditis caused by vancomycin-resistant Staphylococcus aureus with a combination of vancomycin and beta-lactam antibiotics.
Archer, GL; Climo, MW; Fox, PM; Lampen, RJ; Stumpf, KS, 2006
)
0.67

Toxicity

Vancomycin was associated with a significantly greater number of side effects than was ceftriaxone, cefazolin, or oxacillin. 18% of patients who received nafcillin discontinued therapy prematurely due to adverse events.

ExcerptReferenceRelevance
"68 patients (from newborns to 18 years of age) were studied prospectively for adverse effects associated with methicillin, nafcillin and oxacillin."( Adverse effects of methicillin, nafcillin and oxacillin in pediatric patients.
DeBolt, SL; Nahata, MC; Powell, DA, 1982
)
0.75
"This study compared adverse drug reactions (ADRs) to oxacillin with those to nafcillin and other antibiotics."( Higher occurrence of hepatotoxicity and rash in patients treated with oxacillin, compared with those treated with nafcillin and other commonly used antimicrobials.
Alvarez, AM; Gomez, MM; Maraqa, NF; Rathore, MH, 2002
)
0.75
" All patients were included in the adverse drug reaction analysis; 1,252 were evaluable for purposes of evaluating treatment efficacy."( Evaluation of the efficacy and safety of outpatient parenteral antimicrobial therapy for infections with methicillin-sensitive Staphylococcus aureus.
Dalovisio, JR; Jiang, X; Tice, AD; Wynn, M, 2005
)
0.33
"Vancomycin was associated with a significantly greater number of side effects than was ceftriaxone, cefazolin, or oxacillin, and nafcillin was associated with a significantly greater number of adverse events than ceftriaxone."( Evaluation of the efficacy and safety of outpatient parenteral antimicrobial therapy for infections with methicillin-sensitive Staphylococcus aureus.
Dalovisio, JR; Jiang, X; Tice, AD; Wynn, M, 2005
)
0.53
"5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects."( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004
)
0.32
"To identify clinical variables associated with CLNAF and nafcillin-related adverse drug reactions (ADRs)."( Patient Variables Associated with Nafcillin Plasma Concentrations and Toxicity.
Alexander, DP; Barker, BC; Benefield, RJ; Gast, CM, 2016
)
0.96
" Adverse drug reactions (ADRs) were defined using the National Institutes of Health, Division of Microbiology and Infectious Diseases criteria and scored for probability of association with nafcillin by using Naranjo criteria."( Patient Variables Associated with Nafcillin Plasma Concentrations and Toxicity.
Alexander, DP; Barker, BC; Benefield, RJ; Gast, CM, 2016
)
0.9
"Nafcillin can be a safe alternative to vancomycin for empirical therapy of LOS among NICU infants who do not have a history of methicillin-resistant S aureus infection or colonization."( Safety and Efficacy of Nafcillin for Empiric Therapy of Late-Onset Sepsis in the NICU.
Conroy, S; Magers, J; Prusakov, P; Sánchez, PJ; Speaks, S, 2022
)
2.47

Pharmacokinetics

Nafcillin is often used for prophylaxis but not pharmacokinetic data are available perioperatively in pediatric patients. The initial serum half-life for nafcillin was 0.5 log10 CFU/g.

ExcerptReferenceRelevance
" Nafcillin is often used for prophylaxis but not pharmacokinetic data are available perioperatively in pediatric patients."( Pharmacokinetics and cerebrospinal fluid concentration of nafcillin in pediatric patients undergoing cerebrospinal fluid shunt placement.
Barson, WJ; Bartkowski, MH; Fan-Havard, P; Kosnik, EJ; Nahata, MC, 1990
)
1.43
"The pharmacokinetic interaction of the monobactam antibiotic aztreonam with cephradine, clindamycin, gentamicin, metronidazole, and nafcillin was investigated in five separate studies in 48 healthy male volunteers."( Pharmacokinetic interaction of aztreonam with other antibiotics.
Adamovics, J; Creasey, WA; Dhruv, R; Platt, TB; Sugerman, AA, 1984
)
0.47
" 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

Compound-Compound Interactions

The in vitro activity of sisomicin and netilmicin alone and in combination with nafcillin, oxacillin and methicillin against 30 strains of enterococci was investigated. The activity of piperacillin/tazobactam,. ampicillin/sulbactam, imipenem and nafcillin alone was compared with vancomycin monotherapy against MRSA.

ExcerptReferenceRelevance
"The in vitro activity of sisomicin and netilmicin alone and in combination with nafcillin, oxacillin and methicillin against 30 strains of enterococci was investigated."( In vitro activity of sisomicin and netilmicin alone and in combination with nafcillin, oxacillin and methicillin against enterococci.
Glotzbecker, C; Watanakunakorn, C, 1978
)
0.71
"The in vitro activity of nafcillin, oxacillin, and methicillin alone and in combination with gentamicin and tobramycin against 30 strains of enterococci was investigated."( Comparative in vitro activity of nafcillin, oxacillin, and methicillin in combination with gentamicin and tobramycin against enterococci.
Glotzbecker, C; Watanakunakorn, C, 1977
)
0.84
"The effectiveness of three semisynthetic, penicillinase-resistant penicillins alone and in combination with gentamicin was tested against 29 clinical isolates of enterococci."( Comparative synergistic activity of nafcillin, oxacillin, and methicillin in combination with gentamicin against.
Glew, RH; Millering, RS; Wennersten, C, 1975
)
0.53
"The activity of piperacillin/tazobactam, ampicillin/sulbactam, imipenem and nafcillin alone and in combination with vancomycin was compared with vancomycin monotherapy against MRSA in test-tube time-kill studies and in infected fibrin clots."( An evaluation of the bactericidal activity of ampicillin/sulbactam, piperacillin/tazobactam, imipenem or nafcillin alone and in combination with vancomycin against methicillin-resistant Staphylococcus aureus (MRSA) in time-kill curves with infected fibrin
Palmer, SM; Rybak, MJ, 1997
)
0.74
" Due to structural and mechanistic similarities between vancomycin and telavancin, we investigated the activity of telavancin combined with nafcillin and imipenem compared to the known synergistic combination of telavancin and gentamicin."( Comparative activities of telavancin combined with nafcillin, imipenem, and gentamicin against Staphylococcus aureus.
Gandhi, RG; Leonard, SN; Patel, MD; Supple, ME, 2013
)
0.84

Bioavailability

ExcerptReferenceRelevance
"The quantitative structure-bioavailability relationship of 232 structurally diverse drugs was studied to evaluate the feasibility of constructing a predictive model for the human oral bioavailability of prospective new medicinal agents."( QSAR model for drug human oral bioavailability.
Topliss, JG; Yoshida, F, 2000
)
0.31

Dosage Studied

Nafcillin is a safe and effective antibiotic for the treatment of infections due to susceptible bacteria. Convenience of vancomycin dosing may not outweigh the potential benefits of nafcillin or cefazolin in MSSA bacteremia.

ExcerptRelevanceReference
" Results from this study indicate that nafcillin is a safe and effective antibiotic for the treatment of infections due to susceptible bacteria in the dosage tested."( Clinical and pharmacokinetic evaluation of nafcillin in infants and children.
Feldman, WE; Nelson, JD; Stanberry, LR, 1978
)
0.79
"Data on 40 patients with Staphylococcus aureus endocarditis treated with appropriate antibiotics in adequate dosage at the University of Cincinnati Medical Center hospitals between January 1961 and June 1975 were analyzed."( Prognostic factors in Staphylococcus aureus endocarditis and results of therapy with a penicillin and gentamicin.
Baird, IM; Watanakunakorn, C,
)
0.13
" Therefore, no modification of the usual nafcillin dosage is necessary when using this drug in hemodialysis patients."( Pharmacokinetics of nafcillin in patients with renal failure.
Diaz, CR; Kane, JG; Parker, RH; Pelsor, FR, 1977
)
0.85
" Thus, an alternative dosage regimen of cefadroxil should be considered in the future studies."( Cefadroxil kinetics and dynamics in a pediatric patient with acute osteomyelitis.
Jackson, DS; Nahata, MC; Powell, DA, 1990
)
0.28
"To evaluate the cost-effectiveness of cefotaxime sodium at a dosage of 12 g/day vs nafcillin sodium and tobramycin sulfate for the treatment of serious infection, the hospital and physician charges of patients enrolled in a prospective, randomized, clinical trial were analyzed."( Cefotaxime vs nafcillin and tobramycin for the treatment of serious infection. Comparative cost-effectiveness.
Holloway, JJ; Lietman, PS; Moore, RD; Smith, CR, 1986
)
0.86
" His prothrombin time ranged between 14 and 17 s (control, 12 s) despite an increase in his warfarin dosage to 25 mg/d."( Warfarin resistance with nafcillin therapy.
Evans, HJ; Qureshi, GD; Reinders, TP; Somori, GJ, 1984
)
0.57
" Infected rabbits were treated with nafcillin, clindamycin, chloramphenicol, or no drug (control) for up to 11 days; dosage was designed so that peak antibiotic serum concentration/minimal inhibitory concentration ratios were approximately 50."( Laboratory tests for defining bactericidal activity as predictors of antibiotic efficacy in the treatment of endocarditis due to Staphylococcus aureus in rabbits.
Fass, RJ, 1984
)
0.54
" Therefore, the purpose of this study was to compare the effectiveness of standard once per day dosing of oral levofloxacin with a standard parenteral antibiotic regimen (nafcillin four times daily) for the treatment of experimental MSSA osteomyelitis in rabbits."( Comparative evaluation of oral levofloxacin and parenteral nafcillin in the treatment of experimental methicillin-susceptible Staphylococcus aureus osteomyelitis in rabbits.
Calhoun, JH; Mader, JT; Shirtliff, ME, 2001
)
0.75
" The findings of these studies collectively suggest that once-daily dosing of telavancin may provide an effective approach for the treatment of clinically relevant infections with gram-positive organisms."( Pharmacodynamics of telavancin (TD-6424), a novel bactericidal agent, against gram-positive bacteria.
Hegde, SS; Judice, JK; Kaniga, K; McCullough, J; Obedencio, G; Pace, J; Reyes, N; Shaw, JP; Skinner, R; Thomas, R; Vanasse, N; Wiens, T, 2004
)
0.32
" Human therapeutic dosing regimens for nafcillin, daptomycin, vancomycin, linezolid, and gentamicin were simulated."( Impact of high-inoculum Staphylococcus aureus on the activities of nafcillin, vancomycin, linezolid, and daptomycin, alone and in combination with gentamicin, in an in vitro pharmacodynamic model.
LaPlante, KL; Rybak, MJ, 2004
)
0.83
" His warfarin dosage had to be increased to a maximum of 88 mg/week to achieve a therapeutic INR."( Interaction between warfarin and nafcillin: case report and review of the literature.
Epplen, K; Foruhari, F; Frey, RJ; Kim, KY, 2007
)
0.62
" Convenience of vancomycin dosing may not outweigh the potential benefits of nafcillin or cefazolin in the treatment of MSSA bacteremia."( Comparative effectiveness of nafcillin or cefazolin versus vancomycin in methicillin-susceptible Staphylococcus aureus bacteremia.
Cosgrove, SE; Furuno, JP; Harris, AD; Johnson, JK; McGregor, JC; Perencevich, EN; Sakoulas, G; Schweizer, ML; Shardell, MD; Thom, KA, 2011
)
0.89
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (1)

RoleDescription
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
penicillinAny member of the group of substituted penams containing two methyl substituents at position 2, a carboxylate substituent at position 3 and a carboxamido group at position 6.
penicillin allergenAny penicillin which causes the onset of an allergic reaction.
[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 (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Solute carrier family 22 member 8Mus musculus (house mouse)IC50 (µMol)34.90003.02003.02003.0200AID1209730
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Molecular Functions (1)

Processvia Protein(s)Taxonomy
organic anion transmembrane transporter activitySolute carrier family 22 member 8Mus musculus (house mouse)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (1)

Processvia Protein(s)Taxonomy
basolateral plasma membraneSolute carrier family 22 member 8Mus musculus (house mouse)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (169)

Assay IDTitleYearJournalArticle
AID574305Antimicrobial activity against wild type hospital-acquired methicillin-resistant Staphylococcus aureus N315 serotype USA100 by microdilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Staphylococcus aureus PBP4 is essential for beta-lactam resistance in community-acquired methicillin-resistant strains.
AID495881Antibacterial activity against methicillin-resistant Staphylococcus aureus COL2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Ceftobiprole is superior to vancomycin, daptomycin, and linezolid for treatment of experimental endocarditis in rabbits caused by methicillin-resistant Staphylococcus aureus.
AID574293Antimicrobial activity against community-acquired pbp4::pbp4-deficient Staphylococcus aureus MW2 serotype USA400 by microdilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Staphylococcus aureus PBP4 is essential for beta-lactam resistance in community-acquired methicillin-resistant strains.
AID570772Antimicrobial activity against community-acquired pbp4-deficient Staphylococcus aureus MW2 serotype USA400 by microdilution method relative to wild type2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Staphylococcus aureus PBP4 is essential for beta-lactam resistance in community-acquired methicillin-resistant strains.
AID283163Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL2639 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID558781Antibacterial activity against acrB-deficient Salmonella enterica NKS422 harboring acrEF gene by CLSI method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
H-NS modulates multidrug resistance of Salmonella enterica serovar Typhimurium by repressing multidrug efflux genes acrEF.
AID323805Reduction in bioluminescent methicillin-sensitive Staphylococcus aureus Xen29 in immunocompetent CD1 mouse with peritonitis at 100 mg/kg, sc after 5 hrs relative to control2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Rapid bactericidal activity of daptomycin against methicillin-resistant and methicillin-susceptible Staphylococcus aureus peritonitis in mice as measured with bioluminescent bacteria.
AID588218FDA HLAED, lactate dehydrogenase (LDH) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID283171Decrease in biofilm formation of Staphylococcus lugdunensis assessed as percent biofilm forming isolates2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
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]
AID524387Antibacterial activity against Escherichia coli NKE1365 harboring deletion mutation in acrB and mdtABC protein2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Effect of NlpE overproduction on multidrug resistance in Escherichia coli.
AID1209731Drug uptake by mouse OAT3 expressed in CHO cells at 100 uM after 25 mins by HPLC/UV detection method2013Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
Organic anion transporter 3 interacts selectively with lipophilic β-lactam antibiotics.
AID201180Minimum inhibitory concentration against heteroresistant strain of Staphylococcus aureus 430 in the absence of NaCl1993Journal of medicinal chemistry, Jul-09, Volume: 36, Issue:14
Discovery and structure-activity relationship of a series of 1-carba-1-dethiacephems exhibiting activity against methicillin-resistant Staphylococcus aureus.
AID570770Antimicrobial activity against wild type hospital-acquired methicillin-resistant vancomycin-intermediate Staphylococcus aureus Mu50 serotype USA100 by microdilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Staphylococcus aureus PBP4 is essential for beta-lactam resistance in community-acquired methicillin-resistant strains.
AID523001Cytotoxicity against human 5637 cells assessed as mild induction of cell death by trypan blue exclusion assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Persistence of uropathogenic Escherichia coli in the face of multiple antibiotics.
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID558778Antibacterial activity against tolC-deficient Salmonella enterica NKS174 by CLSI method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
H-NS modulates multidrug resistance of Salmonella enterica serovar Typhimurium by repressing multidrug efflux genes acrEF.
AID283158Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL2492 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID588216FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID283169Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL5258 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID201181Minimum inhibitory concentration against methicillin-resistant Staphylococcus aureus 430 (MRSA) in vitro using trypticase soy broth (TSB)1993Journal of medicinal chemistry, Jul-09, Volume: 36, Issue:14
Discovery and structure-activity relationship of a series of 1-carba-1-dethiacephems exhibiting activity against methicillin-resistant Staphylococcus aureus.
AID279084Antibacterial activity against methicillin-resistant Staphylococcus aureus MBT 5040 in CF1 mouse assessed as kidney infection after 7 days2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Lysostaphin-resistant variants of Staphylococcus aureus demonstrate reduced fitness in vitro and in vivo.
AID524390Antibacterial activity against Escherichia coli NKE1316 harboring deletion mutation in acrB, acrD and mdtABC protein2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Effect of NlpE overproduction on multidrug resistance in Escherichia coli.
AID524398Antibacterial activity against methicillin-susceptible beta-lactamase negative Staphylococcus aureus using 5x10'7 CFU/ml high inoculum after 24 hrs by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Determination of an inoculum effect with various cephalosporins among clinical isolates of methicillin-susceptible Staphylococcus aureus.
AID283168Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL5256 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID574301Antimicrobial activity against wild type hospital-acquired methicillin-resistant Staphylococcus aureus COL serotype USA500 by microdilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Staphylococcus aureus PBP4 is essential for beta-lactam resistance in community-acquired methicillin-resistant strains.
AID588219FDA HLAED, gamma-glutamyl transferase (GGT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID524397Antibacterial activity against methicillin-susceptible beta-lactamase positive Staphylococcus aureus using 5x10'7 CFU/ml high inoculum after 24 hrs by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Determination of an inoculum effect with various cephalosporins among clinical isolates of methicillin-susceptible Staphylococcus aureus.
AID524260Antibacterial activity against Escherichia coli NKE96 harboring deletion mutation in acrB protein2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Effect of NlpE overproduction on multidrug resistance in Escherichia coli.
AID423908Antibacterial activity against exponential growth culture of methicillin-sensitive Staphylococcus aureus ATCC 29213 grown for 2 hrs in MHBc by broth microdilution method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Bactericidal action of daptomycin against stationary-phase and nondividing Staphylococcus aureus cells.
AID323782Antimicrobial activity against bioluminescent methicillin-susceptible Staphylococcus aureus Xen292007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Rapid bactericidal activity of daptomycin against methicillin-resistant and methicillin-susceptible Staphylococcus aureus peritonitis in mice as measured with bioluminescent bacteria.
AID588215FDA HLAED, alkaline phosphatase increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID570769Antimicrobial activity against hospital-acquired pbp4-deficient Staphylococcus aureus N315 serotype USA100 by microdilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Staphylococcus aureus PBP4 is essential for beta-lactam resistance in community-acquired methicillin-resistant strains.
AID1209735Inhibition of mouse OAT3 expressed in CHO cells assessed as inhibition of fluorescein uptake at 500 uM over 20 mins relative to untreated-control2013Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
Organic anion transporter 3 interacts selectively with lipophilic β-lactam antibiotics.
AID660262Ratio of MIC for wild type Escherichia coli TG1 to MIC for acrB-deficient Escherichia coli KAM3 by two-fold serial dilution method2012European journal of medicinal chemistry, Jun, Volume: 52Computational analysis of structure-based interactions and ligand properties can predict efflux effects on antibiotics.
AID323787Antibacterial activity against methicillin-susceptible Staphylococcus aureus Xen29 infected neutropenic CD1 mouse assessed as mouse survival at 50 mg/kg, sc after 24 hrs2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Rapid bactericidal activity of daptomycin against methicillin-resistant and methicillin-susceptible Staphylococcus aureus peritonitis in mice as measured with bioluminescent bacteria.
AID323783Antimicrobial activity against bioluminescent methicillin-resistant Staphylococcus aureus Xen12007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Rapid bactericidal activity of daptomycin against methicillin-resistant and methicillin-susceptible Staphylococcus aureus peritonitis in mice as measured with bioluminescent bacteria.
AID588214FDA HLAED, liver enzyme composite activity2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID588217FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID324355Drug level in rat serum at 25 mg/kg, im2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Lysostaphin in treatment of neonatal Staphylococcus aureus infection.
AID323826Reduction in bioluminescent methicillin-sensitive Staphylococcus aureus Xen29 in neutropenic CD1 mouse with peritonitis at 100 mg/kg, sc after 5 hrs relative to control2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Rapid bactericidal activity of daptomycin against methicillin-resistant and methicillin-susceptible Staphylococcus aureus peritonitis in mice as measured with bioluminescent bacteria.
AID201183Minimum inhibitory concentration against sensitive strain of Staphylococcus aureus 446 in 4% of NaCl1993Journal of medicinal chemistry, Jul-09, Volume: 36, Issue:14
Discovery and structure-activity relationship of a series of 1-carba-1-dethiacephems exhibiting activity against methicillin-resistant Staphylococcus aureus.
AID283149Antimicrobial susceptibility of Staphylococcus lugdunensis isolates by broth microdilution method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID424043Bactericidal activity against 24 hrs cold-arrested exponential growth culture of methicillin-sensitive Staphylococcus aureus ATCC 29213 grown for 2 hrs in MHBc at 2 ug/mL incubated at 37 degC after 2 hrs by time kill study2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Bactericidal action of daptomycin against stationary-phase and nondividing Staphylococcus aureus cells.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' 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]
AID574290Antimicrobial activity against community-acquired pbp3-deficient Staphylococcus aureus MW2 serotype USA400 by microdilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Staphylococcus aureus PBP4 is essential for beta-lactam resistance in community-acquired methicillin-resistant strains.
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]
AID279085Antibacterial activity against methicillin-resistant Staphylococcus aureus MBT 5040 and Staphylococcus aureus MBT 5040-LysoR co-infected in CF1 mouse assessed as kidney infection after 7 days2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Lysostaphin-resistant variants of Staphylococcus aureus demonstrate reduced fitness in vitro and in vivo.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID524262Antibacterial activity against Escherichia coli NKE155 harboring deletion mutation in acrB protein and plasmid expressing nlpE gene2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Effect of NlpE overproduction on multidrug resistance in Escherichia coli.
AID323824Reduction in bioluminescent methicillin-sensitive Staphylococcus aureus Xen29 in neutropenic CD1 mouse with peritonitis at 100 mg/kg, sc after 3 hrs relative to control2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Rapid bactericidal activity of daptomycin against methicillin-resistant and methicillin-susceptible Staphylococcus aureus peritonitis in mice as measured with bioluminescent bacteria.
AID524382Antibacterial activity against Escherichia coli NKE160 harboring deletion mutation in acrB protein and vector expressing tolC gene2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Effect of NlpE overproduction on multidrug resistance in Escherichia coli.
AID574299Antimicrobial activity against community-acquired pbp4-deficient Staphylococcus aureus USA300 by microdilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Staphylococcus aureus PBP4 is essential for beta-lactam resistance in community-acquired methicillin-resistant strains.
AID558779Antibacterial activity against tolC-deficient Salmonella enterica NKS419 harboring hns gene by CLSI method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
H-NS modulates multidrug resistance of Salmonella enterica serovar Typhimurium by repressing multidrug efflux genes acrEF.
AID29812Oral bioavailability in human2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
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.
AID283159Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL2526 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID283155Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL856 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID283167Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL5254 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID524394Antibacterial activity against Escherichia coli NKE1355 harboring deletion mutation in acrB protein and plasmid expressing BAD gene in presence of increasing concentration of arabinose2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Effect of NlpE overproduction on multidrug resistance in Escherichia coli.
AID283165Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL2664 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
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
AID323825Reduction in bioluminescent methicillin-sensitive Staphylococcus aureus Xen29 in neutropenic CD1 mouse with peritonitis at 100 mg/kg, sc after 4 hrs relative to control2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Rapid bactericidal activity of daptomycin against methicillin-resistant and methicillin-susceptible Staphylococcus aureus peritonitis in mice as measured with bioluminescent bacteria.
AID201184Minimum inhibitory concentration against sensitive strain of Staphylococcus aureus 446 in the absence of NaCl1993Journal of medicinal chemistry, Jul-09, Volume: 36, Issue:14
Discovery and structure-activity relationship of a series of 1-carba-1-dethiacephems exhibiting activity against methicillin-resistant Staphylococcus aureus.
AID574304Antimicrobial activity against hospital-acquired pbp3/4-deficient Staphylococcus aureus COL serotype USA500 by microdilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Staphylococcus aureus PBP4 is essential for beta-lactam resistance in community-acquired methicillin-resistant strains.
AID524392Antibacterial activity against Escherichia coli NKE1369 harboring deletion mutation in acrB, acrD, mdtABC protein and plasmid expressing nlpE gene2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Effect of NlpE overproduction on multidrug resistance in Escherichia coli.
AID201182Minimum inhibitory concentration against methicillin-resistant Staphylococcus aureus 430 (MRSA) in vitro using trypticase soy broth (TSB) with 4% NaCl1993Journal of medicinal chemistry, Jul-09, Volume: 36, Issue:14
Discovery and structure-activity relationship of a series of 1-carba-1-dethiacephems exhibiting activity against methicillin-resistant Staphylococcus aureus.
AID524396Antibacterial activity against methicillin-susceptible beta-lactamase negative Staphylococcus aureus using 5x10'5 CFU/ml standard inoculum after 24 hrs by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Determination of an inoculum effect with various cephalosporins among clinical isolates of methicillin-susceptible Staphylococcus aureus.
AID283160Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL2554 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID524386Antibacterial activity against Escherichia coli NKE157 harboring deletion mutation in acrB, acrD protein and plasmid expressing nlpE gene2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Effect of NlpE overproduction on multidrug resistance in Escherichia coli.
AID201185Minimum inhibitory concentration against homoresistant strain of Staphylococcus aureus 447 in 4% of NaCl1993Journal of medicinal chemistry, Jul-09, Volume: 36, Issue:14
Discovery and structure-activity relationship of a series of 1-carba-1-dethiacephems exhibiting activity against methicillin-resistant Staphylococcus aureus.
AID524395Antibacterial activity against methicillin-susceptible beta-lactamase positive Staphylococcus aureus using 5x10'5 CFU/ml standard inoculum after 24 hrs by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Determination of an inoculum effect with various cephalosporins among clinical isolates of methicillin-susceptible Staphylococcus aureus.
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID323785Antibacterial activity against methicillin-susceptible Staphylococcus aureus Xen29 infected nonneutropenic CD1 mouse assessed as mouse survival at 50 mg/kg, sc after 7 days2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Rapid bactericidal activity of daptomycin against methicillin-resistant and methicillin-susceptible Staphylococcus aureus peritonitis in mice as measured with bioluminescent bacteria.
AID283172Effect on biofilm formation of Staphylococcus lugdunensis assessed as percent non-biofilm forming isolates2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID283161Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL2588 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID524384Antibacterial activity against Escherichia coli NKE126 harboring deletion mutation in acrB and acrD protein2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Effect of NlpE overproduction on multidrug resistance in Escherichia coli.
AID19006Calculated membrane partition coefficient (Kmemb)2004Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7
Surface activity profiling of drugs applied to the prediction of blood-brain barrier permeability.
AID575169Inhibition of acrAB AcrAB-TolC-mediated Nile Red efflux in Escherichia coli K-12 3-AG100 overexpressing acrAB AcrAB-TolC assessed as time needed for 50% efflux after energization with 50 mM glucose at 1000 uM by spectrofluorometric assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Optimized Nile Red efflux assay of AcrAB-TolC multidrug efflux system shows competition between substrates.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID570771Antimicrobial activity against hospital-acquired pbp4-deficient Staphylococcus aureus Mu50 serotype USA100 by microdilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Staphylococcus aureus PBP4 is essential for beta-lactam resistance in community-acquired methicillin-resistant strains.
AID524385Antibacterial activity against Escherichia coli NKE156 harboring deletion mutation in acrB protein and vector expressing acrD gene2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Effect of NlpE overproduction on multidrug resistance in Escherichia coli.
AID1209730Inhibition of mouse OAT3 expressed in CHO cells assessed as inhibition of fluorescein uptake over 20 mins2013Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
Organic anion transporter 3 interacts selectively with lipophilic β-lactam antibiotics.
AID524263Antibacterial activity against Escherichia coli NKE127 harboring deletion mutation in acrB and cpxAR protein2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Effect of NlpE overproduction on multidrug resistance in Escherichia coli.
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]
AID574289Antimicrobial activity against wild type community-acquired methicillin-resistant Staphylococcus aureus MW2 serotype USA400 by microdilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Staphylococcus aureus PBP4 is essential for beta-lactam resistance in community-acquired methicillin-resistant strains.
AID524266Antibacterial activity against Escherichia coli NKE128 harboring deletion mutation in acrB and tolC protein2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Effect of NlpE overproduction on multidrug resistance in Escherichia coli.
AID323804Reduction in bioluminescent methicillin-sensitive Staphylococcus aureus Xen29 in immunocompetent CD1 mouse at 100 mg/kg, sc after 4 hrs relative to control2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Rapid bactericidal activity of daptomycin against methicillin-resistant and methicillin-susceptible Staphylococcus aureus peritonitis in mice as measured with bioluminescent bacteria.
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.
AID29359Ionization constant (pKa)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID583433Antimicrobial activity against beta-lactam-resistant and chromosomal mecA deficient Staphylococcus aureus CRB harboring PBP4 E183A F241R, GdpP N182K and AcrB I960V mutant genes selected after 21 days of serial passage in ceftobiprole2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
A mecA-negative strain of methicillin-resistant Staphylococcus aureus with high-level β-lactam resistance contains mutations in three genes.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID558780Antibacterial activity against acrEF-deficient Salmonella enterica NKS176 by CLSI method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
H-NS modulates multidrug resistance of Salmonella enterica serovar Typhimurium by repressing multidrug efflux genes acrEF.
AID524265Antibacterial activity against Escherichia coli NKE159 harboring deletion mutation in acrB, cpxAR protein and plasmid expressing nlpE gene2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Effect of NlpE overproduction on multidrug resistance in Escherichia coli.
AID681774TP_TRANSPORTER: inhibition of PAH uptake (PAH: 2 uM, Nafcillin: 2000 uM) in Xenopus laevis oocytes1999The Journal of pharmacology and experimental therapeutics, Aug, Volume: 290, Issue:2
The interaction and transport of beta-lactam antibiotics with the cloned rat renal organic anion transporter 1.
AID660265Antimicrobial activity against wild type Escherichia coli expressing AcrAB-TolC efflux pump2012European journal of medicinal chemistry, Jun, Volume: 52Computational analysis of structure-based interactions and ligand properties can predict efflux effects on antibiotics.
AID524264Antibacterial activity against Escherichia coli NKE158 harboring deletion mutation in acrB protein and vector expressing cpxAR gene2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Effect of NlpE overproduction on multidrug resistance in Escherichia coli.
AID1209732Drug uptake by mouse OAT3 expressed in CHO cells at 100 uM after 25 mins by HPLC/UV detection method in presence of probenecid2013Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
Organic anion transporter 3 interacts selectively with lipophilic β-lactam antibiotics.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1209734Inhibition of mouse OAT1 expressed in CHO cells assessed as inhibition of fluorescein uptake at 500 uM over 20 mins relative to untreated-control2013Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
Organic anion transporter 3 interacts selectively with lipophilic β-lactam antibiotics.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1209736Inhibition of human OAT3 expressed in CHO cells assessed as inhibition of fluorescein uptake at 500 uM over 20 mins relative to untreated-control2013Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
Organic anion transporter 3 interacts selectively with lipophilic β-lactam antibiotics.
AID523004Antibacterial activity against uropathogenic Escherichia coli UTI89 assessed as degradation of preexisting biofilm after 24 hrs by microscopy2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Persistence of uropathogenic Escherichia coli in the face of multiple antibiotics.
AID540211Fraction unbound 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.
AID27167Delta logD (logD6.5 - logD7.4)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID283164Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL2640 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID323831Antibacterial activity against methicillin-susceptible Staphylococcus aureus Xen29 infected neutropenic CD1 mouse assessed as mortality at 100 mg/kg, po after 4 days2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Rapid bactericidal activity of daptomycin against methicillin-resistant and methicillin-susceptible Staphylococcus aureus peritonitis in mice as measured with bioluminescent bacteria.
AID279082Antibacterial activity against methicillin-resistant Staphylococcus aureus Col in CF1 mouse assessed as kidney infection after 7 days2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Lysostaphin-resistant variants of Staphylococcus aureus demonstrate reduced fitness in vitro and in vivo.
AID574298Antimicrobial activity against wild type community-acquired methicillin-resistant Staphylococcus aureus USA300 by microdilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Staphylococcus aureus PBP4 is essential for beta-lactam resistance in community-acquired methicillin-resistant strains.
AID660263Ratio of MIC for wild type Salmonella typhimurium SH5014 to MIC for Salmonella typhimurium SH7616 harboring missense mutation in acrA/acrB gene by two-fold serial dilution method2012European journal of medicinal chemistry, Jun, Volume: 52Computational analysis of structure-based interactions and ligand properties can predict efflux effects on antibiotics.
AID323803Reduction in bioluminescent methicillin-sensitive Staphylococcus aureus Xen29 in immunocompetent CD1 mouse with peritonitis at 100 mg/kg, sc after 3 hrs relative to control2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Rapid bactericidal activity of daptomycin against methicillin-resistant and methicillin-susceptible Staphylococcus aureus peritonitis in mice as measured with bioluminescent bacteria.
AID574292Antimicrobial activity against community-acquired pbp3/4-deficient Staphylococcus aureus MW2 serotype USA400 by microdilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Staphylococcus aureus PBP4 is essential for beta-lactam resistance in community-acquired methicillin-resistant strains.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID522869Antibacterial activity against uropathogenic Escherichia coli UTI89 infected in human 5637 cells assessed as decrease in intracellular bacterial level at 1200 to 1600 ug/ml after 12 hrs by serial dilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Persistence of uropathogenic Escherichia coli in the face of multiple antibiotics.
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID524393Antibacterial activity against Escherichia coli NKE1359 harboring deletion mutation in acrB protein and plasmid expressing BADnlpE gene in presence of increasing concentration of arabinose2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Effect of NlpE overproduction on multidrug resistance in Escherichia coli.
AID583431Antimicrobial activity against methicillin-resistant and tetracycline-sensitive Staphylococcus aureus COLn2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
A mecA-negative strain of methicillin-resistant Staphylococcus aureus with high-level β-lactam resistance contains mutations in three genes.
AID323830Antibacterial activity against methicillin-resistant Staphylococcus aureus Xen1 infected neutropenic CD1 mouse assessed as mortality at 100 mg/kg, po after 4 days2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Rapid bactericidal activity of daptomycin against methicillin-resistant and methicillin-susceptible Staphylococcus aureus peritonitis in mice as measured with bioluminescent bacteria.
AID574291Antimicrobial activity against community-acquired pbp4-deficient Staphylococcus aureus MW2 serotype USA400 by microdilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Staphylococcus aureus PBP4 is essential for beta-lactam resistance in community-acquired methicillin-resistant strains.
AID524383Antibacterial activity against Escherichia coli NKE161 harboring deletion mutation in acrB protein, vector expressing tolC gene and plasmid expressing nlpE gene2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Effect of NlpE overproduction on multidrug resistance in Escherichia coli.
AID524389Antibacterial activity against Escherichia coli NKE1367 harboring deletion mutation in acrB, mdtABC protein and plasmid expressing nlpE gene2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Effect of NlpE overproduction on multidrug resistance in Escherichia coli.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID283170Increase in biofilm formation of Staphylococcus lugdunensis assessed as percent biofilm forming isolates2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID524388Antibacterial activity against Escherichia coli NKE1366 harboring deletion mutation in acrB and vector expressing mdtABC gene2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Effect of NlpE overproduction on multidrug resistance in Escherichia coli.
AID574303Antimicrobial activity against hospital-acquired pbp4-deficient Staphylococcus aureus COL serotype USA500 by microdilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Staphylococcus aureus PBP4 is essential for beta-lactam resistance in community-acquired methicillin-resistant strains.
AID283157Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL2414 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
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.
AID424042Bactericidal activity against 1 hr cold-arrested exponential growth culture of methicillin-sensitive Staphylococcus aureus ATCC 29213 grown for 2 hrs in MHBc at 2 ug/mL incubated at 0 degC by time kill study2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Bactericidal action of daptomycin against stationary-phase and nondividing Staphylococcus aureus cells.
AID574294Antimicrobial activity against wild type community-acquired methicillin-resistant Staphylococcus aureus MW2 ex serotype USA400 by microdilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Staphylococcus aureus PBP4 is essential for beta-lactam resistance in community-acquired methicillin-resistant strains.
AID583432Antimicrobial activity against methicillin-, tetracycline-susceptible and chromosomal mecA deficient Staphylococcus aureus COLnex2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
A mecA-negative strain of methicillin-resistant Staphylococcus aureus with high-level β-lactam resistance contains mutations in three genes.
AID28681Partition coefficient (logD6.5)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID283174Decrease in biofilm formation of Staphylococcus epidermidis RP62A2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
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.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID283166Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL5204 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID558782Antibacterial activity against acrB-deficient Salmonella enterica NKS416 harboring acrEF, hns gene by CLSI method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
H-NS modulates multidrug resistance of Salmonella enterica serovar Typhimurium by repressing multidrug efflux genes acrEF.
AID283156Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL2394 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID323829Protection against methicillin-susceptible Staphylococcus aureus Xen29 infection in nonneutropenic CD1 mouse at 100 mg/kg, po after 7 days2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Rapid bactericidal activity of daptomycin against methicillin-resistant and methicillin-susceptible Staphylococcus aureus peritonitis in mice as measured with bioluminescent bacteria.
AID575170Inhibition of acrAB AcrAB-TolC-mediated Nile Red efflux in Escherichia coli K-12 3-AG100 overexpressing acrAB AcrAB-TolC assessed as time needed for 50% efflux after energization with 50 mM glucose at 200 uM by spectrofluorometric assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Optimized Nile Red efflux assay of AcrAB-TolC multidrug efflux system shows competition between substrates.
AID323790Antibacterial activity against methicillin-resistant Staphylococcus aureus Xen1 infected neutropenic CD1 mouse assessed as mortality at 100 mg/kg, po within 24 hrs2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Rapid bactericidal activity of daptomycin against methicillin-resistant and methicillin-susceptible Staphylococcus aureus peritonitis in mice as measured with bioluminescent bacteria.
AID570773Antimicrobial activity against community-acquired pbp4-deficient Staphylococcus aureus USA300 by microdilution method relative to wild type2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Staphylococcus aureus PBP4 is essential for beta-lactam resistance in community-acquired methicillin-resistant strains.
AID323799Reduction in bioluminescent methicillin-sensitive Staphylococcus aureus Xen29 in immunocompetent CD1 mouse with peritonitis at 100 mg/kg, sc relative to control2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Rapid bactericidal activity of daptomycin against methicillin-resistant and methicillin-susceptible Staphylococcus aureus peritonitis in mice as measured with bioluminescent bacteria.
AID558776Antibacterial activity against acrB-deficient Salmonella enterica NKS175 by CLSI method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
H-NS modulates multidrug resistance of Salmonella enterica serovar Typhimurium by repressing multidrug efflux genes acrEF.
AID279083Antibacterial activity against methicillin-resistant Staphylococcus aureus Col and Staphylococcus aureus Col-LysoR co-infected in CF1 mouse assessed as kidney infection after 7 days2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Lysostaphin-resistant variants of Staphylococcus aureus demonstrate reduced fitness in vitro and in vivo.
AID323828Reduction in bioluminescent methicillin-sensitive Staphylococcus aureus Xen29 in neutropenic CD1 mouse with peritonitis at 100 mg/kg, sc after 2 hrs relative to control2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Rapid bactericidal activity of daptomycin against methicillin-resistant and methicillin-susceptible Staphylococcus aureus peritonitis in mice as measured with bioluminescent bacteria.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID574295Antimicrobial activity against community-acquired pbp3-deficient Staphylococcus aureus MW2 ex serotype USA400 by microdilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Staphylococcus aureus PBP4 is essential for beta-lactam resistance in community-acquired methicillin-resistant strains.
AID323786Antibacterial activity against methicillin-resistant Staphylococcus aureus Xen1 infected neutropenic CD1 mouse assessed as mouse survival at 50 mg/kg, sc after 24 hrs2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Rapid bactericidal activity of daptomycin against methicillin-resistant and methicillin-susceptible Staphylococcus aureus peritonitis in mice as measured with bioluminescent bacteria.
AID323791Antibacterial activity against methicillin-susceptible Staphylococcus aureus Xen29 infected neutropenic CD1 mouse assessed as mortality at 100 mg/kg, po within 24 hrs2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Rapid bactericidal activity of daptomycin against methicillin-resistant and methicillin-susceptible Staphylococcus aureus peritonitis in mice as measured with bioluminescent bacteria.
AID283162Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL2622 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID574297Antimicrobial activity against community-acquired pbp3/4-deficient Staphylococcus aureus MW2 ex serotype USA400 by microdilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Staphylococcus aureus PBP4 is essential for beta-lactam resistance in community-acquired methicillin-resistant strains.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID201186Minimum inhibitory concentration against homoresistant strain of Staphylococcus aureus 447 in the absence of NaCl1993Journal of medicinal chemistry, Jul-09, Volume: 36, Issue:14
Discovery and structure-activity relationship of a series of 1-carba-1-dethiacephems exhibiting activity against methicillin-resistant Staphylococcus aureus.
AID283173Decrease in biofilm formation of Staphylococcus aureus SA1132007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID574296Antimicrobial activity against community-acquired pbp4-deficient Staphylococcus aureus MW2 ex serotype USA400 by microdilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Staphylococcus aureus PBP4 is essential for beta-lactam resistance in community-acquired methicillin-resistant strains.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID155838Tested against penicillin binding protein 2a (PBP2a) enzyme.1993Journal of medicinal chemistry, Jul-09, Volume: 36, Issue:14
Discovery and structure-activity relationship of a series of 1-carba-1-dethiacephems exhibiting activity against methicillin-resistant Staphylococcus aureus.
AID574302Antimicrobial activity against hospital-acquired pbp3-deficient Staphylococcus aureus COL serotype USA500 by microdilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Staphylococcus aureus PBP4 is essential for beta-lactam resistance in community-acquired methicillin-resistant strains.
AID558777Antibacterial activity against acrB-deficient Salmonella enterica NKS291 harboring hns gene by CLSI method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
H-NS modulates multidrug resistance of Salmonella enterica serovar Typhimurium by repressing multidrug efflux genes acrEF.
AID558775Antibacterial activity against Salmonella enterica ATCC 14028 by CLSI method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
H-NS modulates multidrug resistance of Salmonella enterica serovar Typhimurium by repressing multidrug efflux genes acrEF.
AID201179Minimum inhibitory concentration against heteroresistant strain of Staphylococcus aureus 430 in 4% of NaCl1993Journal of medicinal chemistry, Jul-09, Volume: 36, Issue:14
Discovery and structure-activity relationship of a series of 1-carba-1-dethiacephems exhibiting activity against methicillin-resistant Staphylococcus aureus.
AID523002Cytotoxicity against human 5637 cells assessed as mild induction of cell death by LDH release assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Persistence of uropathogenic Escherichia coli in the face of multiple antibiotics.
AID524261Antibacterial activity against Escherichia coli NKE154 harboring vector expressing acrB deletion mutant2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Effect of NlpE overproduction on multidrug resistance in Escherichia coli.
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]
AID524391Antibacterial activity against Escherichia coli NKE1368 harboring deletion mutation in acrB, acrD and vector expressing mdtABC gene2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Effect of NlpE overproduction on multidrug resistance in Escherichia coli.
AID574300Antimicrobial activity against community-acquired pbp4::pbp4-deficient Staphylococcus aureus USA300 by microdilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Staphylococcus aureus PBP4 is essential for beta-lactam resistance in community-acquired methicillin-resistant strains.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (600)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990379 (63.17)18.7374
1990's81 (13.50)18.2507
2000's68 (11.33)29.6817
2010's60 (10.00)24.3611
2020's12 (2.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 59.26

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

MetricThis Compound (vs All)
Research Demand Index59.26 (24.57)
Research Supply Index6.51 (2.92)
Research Growth Index4.31 (4.65)
Search Engine Demand Index101.32 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (59.26)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials29 (4.50%)5.53%
Reviews34 (5.28%)6.00%
Case Studies173 (26.86%)4.05%
Observational1 (0.16%)0.25%
Other407 (63.20%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (14)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Prospective Randomized Study to Compare Clinical Outcomes in Patients With Osteomyelitis Treated With Intravenous Antibiotics Versus Intravenous Antibiotics With an Early Switch to Oral Antibiotics [NCT02099240]Early Phase 111 participants (Actual)Interventional2014-03-06Terminated(stopped due to Not enough patient enrollment and lack of staffing)
Dalbavancin For The Treatment Of Gram Positive Osteomyelitis Or Joint Infections Including Prosthetic Hip Or Knee Infections [NCT03426761]Phase 441 participants (Actual)Interventional2018-01-25Completed
Dalbavancin as an Option for Treatment of S. Aureus Bacteremia (DOTS): A Phase 2b, Multicenter, Randomized, Open-Label, Assessor-Blinded Superiority Study to Compare the Efficacy and Safety of Dalbavancin to Standard of Care Antibiotic Therapy for the Com [NCT04775953]Phase 2200 participants (Actual)Interventional2021-04-22Active, not recruiting
A Phase 2, Randomized, Double-Blind, Parallel-Group, Multinational Trial of Intravenous Televancin (TD-6424) for Treatment of Uncomplicated Staphylococcus Aureus Bacteremia [NCT00062647]Phase 260 participants (Actual)Interventional2003-08-31Completed
A Multi-Center, Randomized, Open-Label, Comparative Study to Assess the Safety and Efficacy of a Treatment Algorithm to Reduce the Use of Vancomycin in Adult Patients With Blood Stream Infections Due to Staphylococci [NCT01191840]Phase 2509 participants (Actual)Interventional2011-02-28Completed
A Prospective, Multicenter, Randomized, Evaluator-blinded, Comparator-controlled Study to Describe the Safety and Efficacy of Daptomycin for the Treatment of Complicated Skin and Skin Structure Infections (cSSSI) and Staphylococcus Aureus Bacteremia Among [NCT01104662]Phase 492 participants (Actual)Interventional2010-04-19Terminated(stopped due to Cubist has reached an agreement with the FDA that enrollment in the DAP-RENSE-08-05 study can stop.)
A Phase 2 Randomized Study Investigating the Safety, Efficacy and Pharmacokinetics of Daptomycin 6 mg/kg and 8 mg/kg Versus Comparator in the Treatment of Subjects Undergoing Surgical Standard of Care for Osteomyelitis Associated With an Infected Prosthet [NCT00428844]Phase 275 participants (Actual)Interventional2007-06-26Completed
An Evaluation of the Safety, Efficacy and Pharmacokinetics of Daptomycin in Pediatric Subjects Aged One to Seventeen Years With Complicated Skin and Skin Structure Infections Caused by Gram-Positive Pathogens [NCT00711802]Phase 4396 participants (Actual)Interventional2008-07-23Completed
Pharmacokinetics of Understudied Drugs Administered to Children Per Standard of Care [NCT01431326]3,520 participants (Actual)Observational2011-11-30Completed
[NCT01756924]Phase 214 participants (Actual)Interventional2012-12-31Terminated(stopped due to This study has been terminated; alternative study designs are being considered. Fusidic acid remains available under an Expanded Access Protocol.)
Are Long Term Prophylactic Antibiotics Useful With Antibiotic Impregnated External Ventricular Drains (EVDs)? [NCT05001750]Phase 184 participants (Anticipated)Interventional2021-06-14Recruiting
A Phase 3, Multicenter, Double-Blind, Randomized, Comparator Controlled Trial of the Safety and Efficacy of Dalbavancin Versus Active Comparator in Pediatric Subjects With Acute Hematogenous Osteomyelitis of the Long Bones Known or Suspected to be Due to [NCT02344511]Phase 30 participants (Actual)Interventional2016-03-31Withdrawn
A Multicenter, Randomized, Double-Blinded Comparative Study to Evaluate the Efficacy, Safety, and Pharmacokinetics of Daptomycin Versus Active Comparator in Pediatric Subjects With Acute Hematogenous Osteomyelitis Due to Gram-Positive Organisms [NCT01922011]Phase 3149 participants (Actual)Interventional2013-09-13Completed
A Phase 3 Multicenter, Randomized, Open-label, Clinical Trial of Telavancin Versus Standard Intravenous Therapy in the Treatment of Subjects With Staphylococcus Aureus Bacteremia Including Infective Endocarditis [NCT02208063]Phase 3121 participants (Actual)Interventional2014-12-31Terminated(stopped due to Halted due to lack of statistical power. No safety concerns identified.)
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00062647 (1) [back to overview]Clinical Response (Cure, Failure, or Indeterminate) as Determined by the Investigator Based the Presence or Absence of Clinical Signs and Symptoms Associated With Bacteremia, Metastatic Complications, or Positive Culture at the Test of Cure Evaluation
NCT00428844 (6) [back to overview]Any Creatine Phosphokinase (CPK) Elevation > 500 Units Per Liter (U/L)
NCT00428844 (6) [back to overview]Pharmacokinetic Parameter: Area Under the Concentration-time Curve During a Dosing Interval at Steady State (AUCss)
NCT00428844 (6) [back to overview]Pharmacokinetic Parameter: Maximum Plasma Concentration (Cmax)
NCT00428844 (6) [back to overview]Microbiological Response
NCT00428844 (6) [back to overview]Overall Clinical Outcome
NCT00428844 (6) [back to overview]Safety - Notable Laboratory Abnormalities
NCT00711802 (3) [back to overview]Pharmacokinetics (PK): Area Under the Plasma Concentration-Time Curve for Daptomycin From 0 to the Last Sampling Time Point (AUC[0-t])
NCT00711802 (3) [back to overview]Percentage of Participants With an Overall Therapeutic Response at Test of Cure Visit
NCT00711802 (3) [back to overview]Percentage of Participants With Treatment-Emergent Adverse Events (TEAEs)
NCT01104662 (2) [back to overview]Number of Participants With Treatment-emergent Creatine Phosphokinase (CPK) Elevations Through End of Therapy/Early Termination (EOT/ET)
NCT01104662 (2) [back to overview]Overall Therapeutic Outcome at Test of Cure (TOC)/Safety Visit
NCT01191840 (5) [back to overview]Cure Rate
NCT01191840 (5) [back to overview]Number of Participants That Changed From Vancomycin to Another Study Antibiotic Due to an Adverse Event
NCT01191840 (5) [back to overview]Number of Participants With Adverse Events Leading to Study Drug Withdrawal
NCT01191840 (5) [back to overview]Number of Participants With Serious Adverse Events
NCT01191840 (5) [back to overview]Antibiotic Days by Treatment Group
NCT01922011 (13) [back to overview]Number of Participants With 1 or More Adverse Events (AEs)
NCT01922011 (13) [back to overview]Number of Participants With 1 or More Serious Adverse Events (SAEs)
NCT01922011 (13) [back to overview]Percentage of Participants With Clinical Improvement in the 3 General Categories of Pain, Inflammation, and Limb Function Based on the Investigator's Overall Assessment of Severity of Each of the Symptom Categories.
NCT01922011 (13) [back to overview]Percentage of Participants With Clinical Improvement Measured as a Composite End Point of Pain, Inflammation, Limb Function, Body Temperature, and C-reactive Protein at End-of IV (EOIV) Therapy Visit.
NCT01922011 (13) [back to overview]Plasma Concentration of Daptomycin at 15 Minutes to 1 Hour After the End of IV Infusion
NCT01922011 (13) [back to overview]Plasma Concentration of Daptomycin at 2 to 3 Hours After the End of IV Infusion
NCT01922011 (13) [back to overview]Plasma Concentration of Daptomycin at 4 to 5 Hours After the End of IV Infusion
NCT01922011 (13) [back to overview]Plasma Concentration of Daptomycin at the End of IV Infusion
NCT01922011 (13) [back to overview]Concentration of Serum Creatine Kinase (CK)
NCT01922011 (13) [back to overview]Percentage of Participants With a Clinical Cure Categorized by Baseline Pathogen at Test of Cure
NCT01922011 (13) [back to overview]Percentage of Participants With a Favorable Clinical Outcome
NCT01922011 (13) [back to overview]Percentage of Participants With a Favorable Microbiological Response Categorized by Baseline Pathogen at Test of Cure
NCT01922011 (13) [back to overview]Percentage of Participants With Sustained Clinical Improvement
NCT02208063 (4) [back to overview]Investigator Clinical Response (Success or Failure) at EOT in the Microbiological All-treated (mAT) Population
NCT02208063 (4) [back to overview]Number of Participants With a Clinical Outcome of Cure at Test of Cure (TOC)
NCT02208063 (4) [back to overview]Number of Participants With an Investigator Clinical Outcome of Cure at TOC in the Microbiological All-treated (mAT) Population
NCT02208063 (4) [back to overview]Number of Participants With the Development of a New Metastatic Foci of S. Aureus Infection at Test of Cure (TOC) in the Microbiological All-treated (mAT) Populations

Clinical Response (Cure, Failure, or Indeterminate) as Determined by the Investigator Based the Presence or Absence of Clinical Signs and Symptoms Associated With Bacteremia, Metastatic Complications, or Positive Culture at the Test of Cure Evaluation

Outcomes in this exploratory study were compared for noninferiority though no specific margin was justified. The 95% CI for the difference was -35.5 to 31.9; further statistical evaluation is not warranted owing to the small sample size. (NCT00062647)
Timeframe: 12 weeks after start of treatment

,
Interventionparticipants (Number)
CuredFailure
Standard Therapy81
Telavancin71

[back to top]

Any Creatine Phosphokinase (CPK) Elevation > 500 Units Per Liter (U/L)

Number of subjects with CPK >500 U/L between Day 3 and 7 days following the last dose of study medication (Day 7P) as measured by the central laboratory. (NCT00428844)
Timeframe: From the 3rd day of therapy to 1 week post last dose (approximately week 7)

InterventionParticipants (Number)
Daptomycin 6 mg/kg4
Daptomycin 8 mg/kg5
Comparator2

[back to top]

Pharmacokinetic Parameter: Area Under the Concentration-time Curve During a Dosing Interval at Steady State (AUCss)

The pharmacokinetic (PK) parameters of daptomycin at steady state for the 6 mg/kg and 8 mg/kg dose groups. On treatment day 4, PK samples for daptomycin levels were to be obtained prior to start of daptomycin infusion (0 hr) and at 0.5 hr (end of infusion), 1-1.5 hr, 3-5 hr, 8-12 hr, and 24 hr after the start of daptomycin infusion. (NCT00428844)
Timeframe: Day 4 (steady state)

Interventionµg•hr/mL (Median)
Daptomycin 6 mg/kg499
Daptomycin 8 mg/kg821

[back to top]

Pharmacokinetic Parameter: Maximum Plasma Concentration (Cmax)

The pharmacokinetic (PK) parameters of daptomycin at steady state for the 6 mg/kg and 8 mg/kg dose groups. On treatment day 4, PK samples for daptomycin levels were to be obtained prior to start of daptomycin infusion (0 hr) and at 0.5 hr (end of infusion), 1-1.5 hr, 3-5 hr, 8-12 hr, and 24 hr after the start of daptomycin infusion. (NCT00428844)
Timeframe: Day 4 (steady state)

Interventionµg/mL (Median)
Daptomycin 6 mg/kg59.1
Daptomycin 8 mg/kg92.3

[back to top]

Microbiological Response

Sponsor's assessment of subject-level microbiological response at the test-of-cure visit for the modified Intent-to-Treat (mITT) population. (NCT00428844)
Timeframe: Approximately 6 weeks post last dose (approximately week 12)

,,
InterventionParticipants (Number)
SuccessFailureNon-evaluable
Comparator867
Daptomycin 6 mg/kg1284
Daptomycin 8 mg/kg1238

[back to top]

Overall Clinical Outcome

The sponsor determined overall clinical outcome based on blinded review of clinical, microbiological, and radiological response of the subject including, but not limited to, clinical signs and symptoms of PJI, microbiological assessments, radiographic findings, and surgical procedures performed. Subjects were a success if both clinical and microbiological responses were success. A subject who failed to respond clinically or microbiologically was a failure. If microbiological response was non-evaluable and/or clinical evaluation at TOC was not performed, the subject was non-evaluable. (NCT00428844)
Timeframe: Approximately 6 weeks post last dose (approximately week 12)

,,
InterventionParticipants (Number)
SuccessFailureNonevaluable
Comparator8112
Daptomycin 6 mg/kg13101
Daptomycin 8 mg/kg1382

[back to top]

Safety - Notable Laboratory Abnormalities

Summary of Notable Laboratory Abnormalities - description of the proportion of subjects within each treatment group that had clinical laboratory values outside the reference range. (NCT00428844)
Timeframe: From the 1st day of therapy to maximum of 23 weeks post last dose (up to maximum of week 30)

,,
InterventionParticipants (Number)
Hematocrit (<30%, >60%)Hemoglobin (<9,>19 g/dL)Red Blood Cell (Female <2.5,>6.0; Male <3.0, >6.5)White Blood Cell (<2, >20 x 10^9/L)Platelets (<40, >450 x 10^9/L)Albumin (<3, >6 g/dL)Alkaline Phosphatase (>1350 U/L)Alanine aminotransferase (>235 U/L)Aspartate aminotransferase (>185 U/L)Total bilirubin (>2.2 mg/dL)Blood Urea Nitrogen (>50 mg/dL)Creatinine (Female >2.0; Male>2.8 mg/dL)
Comparator151230104000012
Daptomycin 6 mg/kg121021137001021
Daptomycin 8 mg/kg101040134000000

[back to top]

Pharmacokinetics (PK): Area Under the Plasma Concentration-Time Curve for Daptomycin From 0 to the Last Sampling Time Point (AUC[0-t])

"Participants who volunteered for PK sampling had a blood sample collected for analysis at the following time points:~Age Group 1; Day 3: Predose, 0.25 hour (hr), 1 hr, 4 hr, and12 hr postdose. Age Group 2; Day 3: Predose, 0.25 hr, 1 hr, 6 hr, and 10 hr postdose. Age Group 3; Day 1, 2, or 3: Predose, 0.25 hr, 1 hr, 6 hr, and 8 hr postdose. Age Group 4; Day 1, 2, or 3: 0, 1, 2, 4, and 6 hr relative to end of infusion." (NCT00711802)
Timeframe: Predose and 5 timepoints according to age group (up to 12 hours postdose)

Interventionmicrogram*hour per milliliter (μg*hr/mL) (Mean)
Age Group 1: Daptomycin318
Age Group 2: DaptomycinNA
Age Group 3: Daptomycin318
Age Group 4: Daptomycin466

[back to top]

Percentage of Participants With an Overall Therapeutic Response at Test of Cure Visit

"The assessment of therapeutic response was determined by comparing a participant's signs and symptoms at the test of cure visit (up to 14 days after last dose) to those recorded at baseline. Participants were classified as Success or Failure by combining their clinical and microbiological efficacy responses. Resolution of clinically significant signs and symptoms associated with the skin infection present at study baseline was considered Success by the Investigator. These participants were deemed both clinically cured and microbiologically eradicated. For participants whose clinical course could not be clearly defined as improved, a clinical outcome of Failure was rendered. In addition, if it was determined that the primary site of infection required additional antibiotic treatment, the assessment of clinical response was Failure. If the Investigator was unable to determine a response because the participant was lost to follow-up, the assessment was Unable to evaluate." (NCT00711802)
Timeframe: Baseline through 14 days after last dose of study drug

,,,,,,,
Interventionpercentage of participants (Number)
Clinical successClinical failureUnable to evaluate
Age Group 1: Daptomycin95.904.1
Age Group 1: Standard of Care (SOC)91.92.75.4
Age Group 2: Daptomycin90.42.76.9
Age Group 2: SOC92.107.9
Age Group 3: Daptomycin82.71.216.1
Age Group 3: SOC76.2023.8
Age Group 4: Daptomycin80.0020.0
Age Group 4: SOC86.7013.3

[back to top]

Percentage of Participants With Treatment-Emergent Adverse Events (TEAEs)

"A TEAE was defined as any treatment-emergent adverse event (AE) that occurred from the time of first dose of the study drug through the last study evaluation or pre-existing adverse AEs that were aggravated in severity or frequency during the dosing period. The percentage of participants with at least 1 TEAE, with at least one drug-related AE (drug-related included possibly related or related as deemed by the Investigator; it also included events if causality was missing), and who discontinued from treatment due to a TEAE is presented. A summary of serious and other non-serious adverse events regardless of causality is located in the Reported Adverse Events module." (NCT00711802)
Timeframe: Baseline through 14 days after last dose of study drug

,,,,,,,
Interventionpercentage of participants (Number)
At least 1 TEAEAt least 1 drug-related TEAEDiscontinued treatment due to a TEAE
Age Group 1: Daptomycin36.113.92.8
Age Group 1: Standard of Care (SOC)36.810.50
Age Group 2: Daptomycin23.35.51.4
Age Group 2: SOC18.410.50
Age Group 3: Daptomycin50.622.23.7
Age Group 3: SOC38.121.414.3
Age Group 4: Daptomycin46.710.03.3
Age Group 4: SOC73.333.36.7

[back to top]

Number of Participants With Treatment-emergent Creatine Phosphokinase (CPK) Elevations Through End of Therapy/Early Termination (EOT/ET)

The number of participants with CPK elevations of >500 units per liter (U/L) above baseline at any time from Day 1 through the EOT/ET visit are presented. (NCT01104662)
Timeframe: Baseline through EOT/ET

Interventionparticipants (Number)
Daptomycin, Bacteremia, Severe Renal Impairment0
Vancomycin or SSP, Bacteremia, Severe Renal Impairment1
Daptomycin, Bacteremia, Moderate Renal Impairment0
Vancomycin or SSP, Bacteremia, Moderate Renal Impairment0
Daptomycin, cSSSI, Severe Renal Impairment1
Vancomycin or SSP, cSSSI, Severe Renal Impairment0
Daptomycin, cSSSI, Moderate Renal Impairment0
Vancomycin or SSP, cSSSI, Moderate Renal Impairment0

[back to top]

Overall Therapeutic Outcome at Test of Cure (TOC)/Safety Visit

"Participants were assigned a Sponsor-assessed clinical outcome based on the following definitions at the TOC/Safety visit:~Failure: Assessed as a failure at any time by the Investigator or received non-study antimicrobial therapy for lack of efficacy or had the primary site of infection removed completely by surgery or underwent surgery to treat the infection >4 days after starting study medication.~Success: Were not assessed as a failure at any time and were assessed as a cure or improvement by the Investigator at the TOC visit.~Non-evaluable: Received potentially effective antimicrobial therapy during the study period for reasons other than lack of efficacy or received <4 days of study medication or were not assessed by the Investigator." (NCT01104662)
Timeframe: Baseline through TOC/Safety Visit

,,,,,,,
Interventionparticipants (Number)
SuccessFailureNon-evaluable
Daptomycin, Bacteremia, Moderate Renal Impairment121
Daptomycin, Bacteremia, Severe Renal Impairment924
Daptomycin, cSSSI, Moderate Renal Impairment500
Daptomycin, cSSSI, Severe Renal Impairment1032
Vancomycin or SSP, Bacteremia, Moderate Renal Impairment301
Vancomycin or SSP, Bacteremia, Severe Renal Impairment916
Vancomycin or SSP, cSSSI, Moderate Renal Impairment420
Vancomycin or SSP, cSSSI, Severe Renal Impairment924

[back to top]

Cure Rate

To compare the cure rate at Test of Cure evaluation, between the proposed treatment algorithm and the standard of care therapy. (NCT01191840)
Timeframe: Test of cure 2 (up to approximately 42 days)

InterventionParticipants (Count of Participants)
Standard of Care207
Algorithm-determined Therapy209

[back to top]

Number of Participants That Changed From Vancomycin to Another Study Antibiotic Due to an Adverse Event

Patient changes from vancomycin or a protocol-approved study antibiotic to another protocol-approved study antibiotic due to AE associated with study drug (NCT01191840)
Timeframe: Test of cure 2 (up to approximately 42 days)

InterventionParticipants (Count of Participants)
Standard of Care2
Algorithm-determined Therapy5

[back to top]

Number of Participants With Adverse Events Leading to Study Drug Withdrawal

Number of Participants with an Adverse Event leading to study drug withdrawal (NCT01191840)
Timeframe: Test of cure 2 (up to approximately 42 days)

InterventionParticipants (Count of Participants)
Standard of Care1
Algorithm-determined Therapy4

[back to top]

Number of Participants With Serious Adverse Events

Number of Participants that reported a Serious Adverse Event (NCT01191840)
Timeframe: Test of cure 2 (up to approximately 42 days)

InterventionParticipants (Count of Participants)
Standard of Care72
Algorithm-determined Therapy83

[back to top]

Antibiotic Days by Treatment Group

This will be analyzed by evaluating the difference in antibiotic days by treatment group and calculating 95% confidence intervals around the difference in antibiotic days among study patients randomized to algorithm-based treatment vs. among study patients randomized to standard treatment. (NCT01191840)
Timeframe: Test of cure 2 (up to approximately 42 days)

,
InterventionDays (Mean)
PP PopulationPPE Population
Algorithm-determined Therapy7.54.4
Standard of Care7.96.2

[back to top]

Number of Participants With 1 or More Adverse Events (AEs)

An AE is any untoward medical occurrence in a participant administered a pharmaceutical product and which does not necessarily have to have a causal relationship with this treatment. An AE can therefore be any unfavorable and unintended sign, clinically significant laboratory finding, symptom, or disease temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product (NCT01922011)
Timeframe: Administration of first dose up to approximately six and a half months after last dose of study drug

InterventionParticipants (Number)
Daptomycin34
Vancomycin or Nafcillin45

[back to top]

Number of Participants With 1 or More Serious Adverse Events (SAEs)

An SAE is any untoward medical occurrence that at any dose results in death; is life threatening; requires in-patient hospitalization or prolongation of existing hospitalization; results in persistent or significant disability/incapacity; or is a congenital anomaly/birth defect. (NCT01922011)
Timeframe: Administration of first dose through the last follow-up visit; an expected time of up to 6.5 months

InterventionParticipants (Number)
Daptomycin5
Vancomycin or Nafcillin4

[back to top]

Percentage of Participants With Clinical Improvement in the 3 General Categories of Pain, Inflammation, and Limb Function Based on the Investigator's Overall Assessment of Severity of Each of the Symptom Categories.

Clinical improvement was based on the Investigator's overall assessment of severity of each of the 3 general symptom categories of Pain, Inflammation, and Limb Function. Based on this evaluation, a participant was considered to have met criteria for clinical improvement according to the following definition: If 3 general categories are present at baseline: at least a 1-point improvement (i.e. severe to moderate, moderate to mild, mild to absent) in at least 2 of the general categories and no worsening in the other. If 2 general categories are present at baseline: at least a 2-point improvement (i.e. severe to mild, moderate to absent) in at least 1 of the general categories and no worsening or new findings in the others OR at least a 1-point improvement in both and no new findings in the other. If 1 general category is present at baseline: at least a 2-point improvement (i.e., severe to mild, moderate to absent) in that category and no new findings in the others. (NCT01922011)
Timeframe: Up to study Day 5

InterventionPercentage of participants (Number)
Daptomycin77.5
Vancomycin or Nafcillin82.9

[back to top]

Percentage of Participants With Clinical Improvement Measured as a Composite End Point of Pain, Inflammation, Limb Function, Body Temperature, and C-reactive Protein at End-of IV (EOIV) Therapy Visit.

A participant had a favorable outcome in this composite endpoint if all 3 of the following criteria were met: Clinical improvement in the general symptom categories of Pain, Inflammation, and Limb Function on or before Study Day 5; Body temperature ≤ 38°C (100.4°F) over the preceding 24 hours; and C-reactive Protein (CRP) decreased from baseline for participants who had a baseline CRP >ULN (upper limit of normal)) or remain <=ULN for participants who had a baseline <=ULN on or before Study Day 5. The EOIV visit is within 24 hours after the last dose of IV study drug and before switch to optional open label (PO) therapy, if applicable. (NCT01922011)
Timeframe: Up to study Day 5

InterventionPercentage of participants (Number)
Daptomycin71.0
Vancomycin or Nafcillin76.5

[back to top]

Plasma Concentration of Daptomycin at 15 Minutes to 1 Hour After the End of IV Infusion

Blood samples were collected, after infusion of IV study drug between the end of infusion on study day 3, up to Day 42 (NCT01922011)
Timeframe: Day 3 up to Day 42

Interventionµg/mL (Mean)
Daptomycin 12 - < 24 Months Old65.533
Daptomycin 24 Months - < 7 Yrs Old84.564
Daptomycin 7 - < 12 Yrs Old70.342
Daptomycin 12 - < 18 Yrs Old57.370

[back to top]

Plasma Concentration of Daptomycin at 2 to 3 Hours After the End of IV Infusion

Blood samples were collected, after infusion of IV study drug between the end of infusion on study day 3, up to Day 42 (NCT01922011)
Timeframe: Day 3 up to Day 42

Interventionµg/mL (Mean)
Daptomycin 24 Months - < 7 Yrs Old51.150
Daptomycin 7 - < 12 Yrs Old31.200
Daptomycin 12 - < 18 Yrs Old46.756

[back to top]

Plasma Concentration of Daptomycin at 4 to 5 Hours After the End of IV Infusion

Blood samples were collected, after infusion of IV study drug between the end of infusion on study day 3, up to Day 42 (NCT01922011)
Timeframe: Day 3 up to Day 42

Interventionµg/mL (Mean)
Daptomycin 12 - < 24 Months Old35.933
Daptomycin 24 Months - < 7 Yrs Old53.059
Daptomycin 7 - < 12 Yrs Old50.809
Daptomycin 12 - < 18 Yrs Old41.447

[back to top]

Plasma Concentration of Daptomycin at the End of IV Infusion

Blood samples were collected, after infusion of IV study drug between the end of infusion on study day 3, up to Day 42 (NCT01922011)
Timeframe: Day 3 up to Day 42

Interventionµg/mL (Mean)
Daptomycin 12 - < 24 Months Old36.800
Daptomycin 24 Months - < 7 Yrs Old75.772
Daptomycin 7 - < 12 Yrs Old58.940
Daptomycin 12 - < 18 Yrs Old68.907

[back to top]

Concentration of Serum Creatine Kinase (CK)

Serum was collected at Baseline and at End of Therapy IV, from which the concentration of CK was determined. (NCT01922011)
Timeframe: Baseline and End of Therapy IV (up to Day 42)

,
InterventionU/L (Mean)
Baseline (n = 68,72)End of Therapy IV (n= 35,41)
Daptomycin141.789.4
Vancomycin or Nafcillin99.982.4

[back to top]

Percentage of Participants With a Clinical Cure Categorized by Baseline Pathogen at Test of Cure

At Test Of Cure (TOC) clinical cure is defined as resolution of all acute symptoms of AHO or improvement to such an extent that no further antibacterial therapy is required. Favorable microbiological outcomes are either eradication where the source specimen demonstrated absence of the original baseline pathogen; or presumed eradication where the source specimen was not available to culture, and the subject was assessed as a clinical cure. To have a favorable microbiological response, the outcome for each participant's baseline pathogen must be favorable (eradicated or presumed eradicated). Other pathogens include Arcanobacterium haemolyticum, Gram positive cocci, Staphylococcus epidermidis, Streptococcus dysgalactiae, Streptococcus mitis group and Streptococcus pyogenes. (NCT01922011)
Timeframe: Baseline (within 48 hours prior to first dose of IV study drug) - and Test of Cure (21-35 days after last dose of IV study drug) (up to Day 77)

,
InterventionPercentage of participants (Number)
Overall Baseline Infecting Pathogen (n =45,47)Staphylococcus Aureus (SA) (n= 43,42)Methicillin Susceptible SA (MSSA) (n= 39,37)Methicillin Resistant SA (MRSA) (n= 4,4)Other Pathogens (n= 2,7)
Daptomycin77.876.779.550.0100
Vancomycin or Nafcillin87.288.194.625.085.7

[back to top]

Percentage of Participants With a Favorable Clinical Outcome

Favorable clinical outcomes are clinical recovery and clinical cure. Clinical cure is defined as resolution of all acute symptoms of AHO or improvement to such an extent that no further intravenous antibacterial therapy is required. Clinical recovery is defined as clinical improvement in the composite end point three general categories of Pain, Inflammation, and Limb Function on or before Study Day 5, and no development of new symptoms of AHO; body temperature ≤ 38°C (100.4°F) for 24 hours; no new or additional bone or joint infection (e.g., abscess, spreading to other osseous or articular locations) such that no further antibacterial therapy or surgery are required; no hematogenous metastatic infection (e.g., abscess in liver, spleen, lung; other bones) or bacteremia.. The End of Therapy (EOT) visit is within 48 hours of last dose of PO therapy. (NCT01922011)
Timeframe: Baseline (within 48 hours prior to first dose of IV study drug) - and up to Test of Cure (21-35 days after last dose of IV study drug) (up to Day 77)

,
InterventionPercentage of participants (Number)
At End of IV (EOIV) Therapy (n= 71,69)At End of Therapy (EOT) (n= 71,69)At Test Of Cure (TOC) (n= 71,70)
Daptomycin85.983.181.7
Vancomycin or Nafcillin91.389.987.1

[back to top]

Percentage of Participants With a Favorable Microbiological Response Categorized by Baseline Pathogen at Test of Cure

Favorable microbiological outcomes are either eradication where the source specimen demonstrated absence of the original baseline pathogen; or presumed eradication where the source specimen was not available to culture, and the subject was assessed as a clinical cure. For a favorable microbiological response, the outcome for each baseline pathogen must be eradicated or presumed eradicated. Other pathogens include Arcanobacterium haemolyticum, Gram positive cocci, Staphylococcus epidermidis, Streptococcus dysgalactiae, Streptococcus mitis group and Streptococcus pyogenes. (NCT01922011)
Timeframe: Baseline (within 48 hours prior to first dose of IV study drug) - and Test of Cure (21-35 days after last dose of IV study drug) (up to Day 77)

,
InterventionPercentage of participants (Number)
Overall Baseline Infecting Pathogen (n =45,47)SA (n= 43,42)MSSA (n= 39,37)MRSA (n= 4,4)Other Pathogens (n= 2,7)
Daptomycin82.281.484.650.0100
Vancomycin or Nafcillin91.592.994.675.085.7

[back to top]

Percentage of Participants With Sustained Clinical Improvement

Sustained clinical improvement was defined as participants with clinical improvement who further met the definition of clinical cure. Clinical improvement was in the three general categories of Pain, Inflammation, and Limb Function on or before Study Day 5. Clinical cure is defined as resolution of all acute symptoms of AHO or improvement to such an extent that no further intravenous antibacterial therapy is required. The EOT visit is within 48 hours of last dose of PO therapy. (NCT01922011)
Timeframe: Baseline (within 48 hours prior to first dose of IV study drug) - up to Test of Cure (21-35 days after last dose of IV study drug) (up to Day 77)

,
InterventionPercentage of participants (Number)
EOT (n= 55,57)TOC (n= 55,58)
Daptomycin89.187.3
Vancomycin or Nafcillin94.791.4

[back to top]

Investigator Clinical Response (Success or Failure) at EOT in the Microbiological All-treated (mAT) Population

This efficacy endpoint was determined to be a clinical failure if the subject switched study antibiotic due to lack of clinical response (NCT02208063)
Timeframe: Up to 8 weeks

,
InterventionParticipants (Count of Participants)
SuccessFailureIndeterminateMissing
Standard of Care361501
Telavancin281351

[back to top]

Number of Participants With a Clinical Outcome of Cure at Test of Cure (TOC)

"The efficacy endpoint of clinical outcome of cure at the test of cure (TOC) was determined by subjects who meet all of the following criteria, as determined by the investigator and adjudicated by the blinded independent efficacy adjudication committee (IEAC).~Alive at TOC~Resolution of all clinical signed and symptoms of the Staphylococcus aureus (S. aureus) infection at TOC~No evidence of microbiological persistence of relapse~No new foci of metastatic S. aureus infection after Day 8" (NCT02208063)
Timeframe: Up to 8 weeks

,
InterventionParticipants (Count of Participants)
CureFailureIndeterminate
Standard of Care27214
Telavancin22196

[back to top]

Number of Participants With an Investigator Clinical Outcome of Cure at TOC in the Microbiological All-treated (mAT) Population

"The efficacy endpoint of Investigator clinical outcome of cure at the test of cure (TOC) was determined by the following criteria:~Subject alive at TOC~Resolution of all clinical signs and symptoms of the S. aureus infection at TOC (unless explained by a more likely alternative diagnosis)~No evidence of microbiological persistence or relapse~No new foci of metastatic S. aureus infection after Day 8" (NCT02208063)
Timeframe: Up to 8 weeks

,
InterventionParticipants (Count of Participants)
CureFailureIndeterminateMissing
Standard of Care311902
Telavancin261533

[back to top]

Number of Participants With the Development of a New Metastatic Foci of S. Aureus Infection at Test of Cure (TOC) in the Microbiological All-treated (mAT) Populations

After Day 8, any sign or symptom leading to a subsequent confirmed diagnosis of a new metastatic foci of S. aureus infection (NCT02208063)
Timeframe: Day 8

,
InterventionParticipants (Count of Participants)
YesNoIndeterminate
Standard of Care3418
Telavancin6329

[back to top]