retapamulin profile

retapamulin: a synthetic pleuromutilin [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ID Source	ID
PubMed CID	6918462
CHEMBL ID	1658
CHEBI ID	166679
SCHEMBL ID	365459
SCHEMBL ID	23977320
MeSH ID	M0496256

Synonym
HY-17010
CHEBI:166679
[(1s,2r,3s,4s,6r,7r,8r,14r)-4-ethenyl-3-hydroxy-2,4,7,14-tetramethyl-9-oxo-6-tricyclo[5.4.3.01,8]tetradecanyl] 2-[[(1r,5s)-8-methyl-8-azabicyclo[3.2.1]octan-3-yl]sulanyl]acetate
retapamulin
altabax
altargo
sb-275833
(3as,4r,5s,6s,8r,9r,9ar,10r)-5-hydroxy-4,6,9,10-tetramethyl-1-oxo-6-vinyldecahydro-3a,9-propanocyclopenta[8]annulen-8-yl {[(3-exo)-8-methyl-8-azabicyclo[3.2.1]oct-3-yl]thio}acetate
224452-66-8
DB01256
(3as,4r,5s,6s,8r,9r,9ar,10r)-6-ethenyl-5-hydroxy-4,6,9,10-tetramethyl-1-oxodecahydro-3a,9-propano-3ah-cyclopenta(8)annulen-8-yl (((1r,3s,5s)-8-methyl-8-azabicyclo(3.2.1)oct-3-yl)sulfanyl)acetate
acetic acid, (((3-exo)-8-methyl-8-azabicyclo(3.2.1)oct-3-yl)thio)-, (3as,4r,5s,6s,8r,9r,9ar,10r)-6-ethenyldecahydro-5-hydroxy-4,6,9,10-tetramethyl-1-oxo-3a,9-propano-3ah-cyclopentacycloocten-8-yl ester
sb275833
sb 275833
CHEMBL1658
nsc-759885
nsc 759885
4mg6o8991r ,
retapamulin [usan:inn:ban]
unii-4mg6o8991r
S4056
AKOS016008865
CS-0618
retapamulin [ema epar]
(3as,4r,5s,6s,8r,9r,9ar,10r)-6-ethenyl-5-hydroxy-4,6,9,10-tetramethyl-1-oxodecahydro-3a,9-propano-3ah-cyclopenta[8]annulen-8-yl [[(1r,3s,5s)-8-methyl-8-azabicyclo[3.2.1]oct-3-yl]sulfanyl]acetate
retapamulin [orange book]
retapamulin [mart.]
retapamulin [who-dd]
retapamulin [mi]
retapamulin [vandf]
retapamulin [inn]
retapamulin [usan]
SCHEMBL365459
AC-26826
(3as,4r,5s,6s,8r,9r,9ar,10r)-2-(exo-8-methyl-8-azabicyclo[3.2.1]octan-3-ylsulfanyl)acetic acid 5-hydroxy-4,6,9,10-tetramethyl-1-oxo-6-vinylperhydro-3a,9-propanocyclopentacycloocten-8-yl ester
rebapamulin
AB01566905_01
(1s,2r,3s,4s,6r,7r,8r,14r)-4-ethenyl-3-hydroxy-2,4,7,14-tetramethyl-9-oxotricyclo[5.4.3.0^{1,8}]tetradecan-6-yl 2-{[(1r,5s)-8-methyl-8-azabicyclo[3.2.1]octan-3-yl]sulfanyl}acetate
mfcd11045316
AKOS030485971
NCGC00386248-01
A851322
(3as,4r,5s,6s,8r,9r,9ar,10r)-6-ethenyl-5-hydroxy-4,6,9,10-tetramethyl-1-oxodecahydro-3a,9-propanocyclopenta[8]annulen-8-yl {[(3-exo)-8-methyl-8-azabicyclo[3.2.1]oct-3-yl]sulfanyl}acetate
[(1s,2r,3s,4s,6r,7r,8r,14r)-4-ethenyl-3-hydroxy-2,4,7,14-tetramethyl-9-oxo-6-tricyclo[5.4.3.01,8]tetradecanyl] 2-[[(1r,5s)-8-methyl-8-azabicyclo[3.2.1]octan-3-yl]sulfanyl]acetate
AS-11455
Q7316645
BRD-K33082088-001-03-3
(3ar,4r,5r,7s,8s,9r,9as,12r)-8-hydroxy-4,7,9,12-tetramethyl-5-((3-(((3-exo)-8-methyl-8-azabicyclo[3.2.1]octan-3-yl)thio)prop-1-en-2-yl)oxy)-7-vinyloctahydro-4,9a-propanocyclopenta[8]annulen-3(3ah)-one
CCG-269837
gtpl11035
SCHEMBL23977320
(1s,2r,3s,4s,6r,7r,8r,14r)-4-ethenyl-3-hydroxy-2,4,7,14-tetramethyl-9-oxotricyclo[5.4.3.0,1,8]tetradecan-6-yl 2-{[(1r,3r,5s)-8-methyl-8-azabicyclo[3.2.1]octan-3-yl]sulfanyl}acetate
EN300-7404368

Research Excerpts

Overview

Retapamulin is a newer topical agent of pleuromutilin class approved by the Food and Drug Administration for treatment of impetigo in children. It has been recently made available in the Indian market.

Excerpt	Reference	Relevance
"Retapamulin is a newer topical agent of pleuromutilin class approved by the Food and Drug Administration for treatment of impetigo in children and has been recently made available in the Indian market."	( Retapamulin: a newer topical antibiotic. Dhingra, D; Parakh, A; Ramachandran, S, )	2.3
"Retapamulin is a new topical pleuromutilin antibiotic for the treatment of skin and skin-structure infections, including impetigo. "	( Microbiological profile of a new topical antibacterial: retapamulin ointment 1%. Bouchillon, S; Hoban, D; Scangarella-Oman, NE; Shawar, RM, 2009)	2.04
"Retapamulin is a relatively new pleuromutilin antibiotic designed for topical use."	( Retapamulin: what is the role of this topical antimicrobial in the treatment of bacterial infections in atopic dermatitis? Moody, MN; Morrison, LK; Tyring, SK, 2010)	2.52
"Retapamulin 1% ointment is a unique topical antibiotic formulation that may be a suitable option for the treatment of clinically infected AD."	( Efficacy and tolerability of retapamulin 1% ointment for the treatment of infected atopic dermatitis: a pilot study. Kircik, LH, 2012)	1.39
"Retapamulin is a semisynthetic pleuromutilin derivative being developed as a topical antibiotic for treating bacterial infections of the skin. "	( Biochemical characterization of the interactions of the novel pleuromutilin derivative retapamulin with bacterial ribosomes. Choudhry, AE; Copeland, RA; Gontarek, RR; Madden, L; Voigt, CS; Yan, K, 2006)	2
"Retapamulin is a novel, topical antibacterial of the pleuromutilin class in development for the treatment of secondarily infected traumatic lesions of the skin."	( Retapamulin ointment twice daily for 5 days vs oral cephalexin twice daily for 10 days for empiric treatment of secondarily infected traumatic lesions of the skin. Dalessandro, M; Free, A; Hiram, J; Roth, E; Scangarella, N; Shawar, R; White, S, )	3.02
"Retapamulin is a novel pleuromutilin antibacterial developed for topical use."	( Topical retapamulin ointment, 1%, versus sodium fusidate ointment, 2%, for impetigo: a randomized, observer-blinded, noninferiority study. Chosidow, O; Oranje, AP; Sacchidanand, S; Scangarella, N; Shawar, R; Singh, K; Todd, G; Twynholm, M, 2007)	2.22
"Retapamulin is a highly effective and convenient new treatment option for impetigo, with efficacy against isolates resistant to existing therapies."	( Topical retapamulin ointment, 1%, versus sodium fusidate ointment, 2%, for impetigo: a randomized, observer-blinded, noninferiority study. Chosidow, O; Oranje, AP; Sacchidanand, S; Scangarella, N; Shawar, R; Singh, K; Todd, G; Twynholm, M, 2007)	2.22
"Retapamulin is a semisynthetic pleuromutilin compound with in vitroactivity against Gram-positive bacteria, no cross-resistance to other classes of antimicrobial agents in current use and a low potential for development of resistance. "	( Retapamulin: a semisynthetic pleuromutilin compound for topical treatment of skin infections in adults and children. Jacobs, MR, 2007)	3.23
"Retapamulin acts as a potent inhibitor of bacterial protein synthesis and has a unique mode of antibiotic action."	( Retapamulin: a new topical antibiotic for the treatment of uncomplicated skin infections. Parish, JL; Parish, LC, 2008)	2.51

Effects

Retapamulin has a novel site of action on bacterial ribosomes. It has a low propensity to select resistance and produces an in vitro postantibiotic effect.

Excerpt	Reference	Relevance
"Retapamulin has a novel site of action on bacterial ribosomes."	( Spotlight on retapamulin in impetigo and other uncomplicated superficial skin infections. Keam, SJ; Yang, LP, 2008)	1.44
"Retapamulin has a low potential for resistance selection in S."	( Single- and multistep resistance selection studies on the activity of retapamulin compared to other agents against Staphylococcus aureus and Streptococcus pyogenes. Appelbaum, PC; Bogdanovich, T; Clark, C; Credito, K; Dewasse, B; Kosowska-Shick, K; McGhee, P, 2006)	1.29
"Retapamulin has a low propensity to select resistance and produces an in vitro postantibiotic effect."	( Selection of retapamulin, a novel pleuromutilin for topical use. Biswas, S; Broskey, J; McCloskey, L; Moore, T; Payne, D; Rittenhouse, S; Vasey, S; West, J; Zalacain, M; Zonis, R, 2006)	1.42
"Retapamulin has a novel site of action on bacterial ribosomes."	( Retapamulin: a review of its use in the management of impetigo and other uncomplicated superficial skin infections. Keam, SJ; Yang, LP, 2008)	2.51

Toxicity

The proportion of patients experiencing adverse events, which were typically mild or moderate in severity, was similar between the retapamulin and placebo groups. The most common adverse effect, pruritus at the application site, was reported by 6% and 1% of patients.

Excerpt	Reference	Relevance
" The most common adverse effect, pruritus at the application site, was reported by 6% and 1% of patients in the retapamulin and placebo groups, respectively."	( Efficacy and safety of retapamulin ointment as treatment of impetigo: randomized double-blind multicentre placebo-controlled trial. Chosidow, O; Koning, S; Oranje, AP; Scangarella, N; Singh, KP; Twynholm, M; van der Wouden, JC, 2008)	0.87
"This study shows that topical retapamulin is effective and safe in the treatment of primary impetigo, offering a new treatment option."	( Efficacy and safety of retapamulin ointment as treatment of impetigo: randomized double-blind multicentre placebo-controlled trial. Chosidow, O; Koning, S; Oranje, AP; Scangarella, N; Singh, KP; Twynholm, M; van der Wouden, JC, 2008)	0.95
" The proportion of patients experiencing adverse events, which were typically mild or moderate in severity, was similar between the retapamulin (5."	( The safety and efficacy of topical retapamulin ointment versus placebo ointment in the treatment of secondarily infected traumatic lesions: a randomized, double-blind superiority study. Breton, JJ; Dalessandro, M; Li, G; Martin, M; Scangarella-Oman, N; Tomayko, JF, 2013)	0.87

Bioavailability

Excerpt	Reference	Relevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."	( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019)	0.51

Dosage Studied

The effect of topically applied retapamulin ointment was evaluated using various dosing regimens in the Staphylococcus aureus and Streptococcus pyogenes wound infection model.

Excerpt	Relevance	Reference
"The effect of topically applied retapamulin ointment was evaluated using various dosing regimens in the Staphylococcus aureus and Streptococcus pyogenes wound infection model."	( Use of the surgical wound infection model to determine the efficacious dosing regimen of retapamulin, a novel topical antibiotic. Hoover, J; Page, R; Payne, D; Rittenhouse, S; Singley, C, 2006)	0.84
" To treat skin infections such as impetigo, antibacterials with a short dosing schedule and low propensity to develop resistance should be used."	( Retapamulin: an antibacterial with a novel mode of action in an age of emerging resistance to Staphylococcus aureus. Tyring, SK; Weinberg, JM, 2010)	1.8
"A sensitive, stability-indicating reversed-phase high-performance liquid chromatographic method is developed and validated for the quantitative determination of retapamulin in topical dosage form."	( A validated stability-indicating liquid chromatographic method for the determination of retapamulin in topical dosage form. Nalwade, S; Reddy, VR, 2014)	0.82

[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Class	Description
carbotricyclic compound	A carbopolyclic compound comprising of three carbocyclic rings.
carboxylic ester	An ester of a carboxylic acid, R(1)C(=O)OR(2), where R(1) = H or organyl and R(2) = organyl.
cyclic ketone
[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]

Bioassays (133)

Assay ID	Title	Year	Journal	Article
AID1296008	Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening	2020	SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1	Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346986	P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347159	Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347160	Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346987	P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID368447	Increase in small RNA level in wild type Staphylococcus aureus RN1786 at 10 ng/mL by agilent bioanalyzer analysis	2007	Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9	Retapamulin inhibition of translation and 50S ribosomal subunit formation in Staphylococcus aureus cells.
AID534119	Antibacterial activity against beta-hemolytic Streptococcus group G	2008	Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11	Proposed MIC and disk diffusion microbiological cutoffs and spectrum of activity of retapamulin, a novel topical antimicrobial agent.
AID534118	Antibacterial activity against beta-hemolytic Streptococcus group C	2008	Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11	Proposed MIC and disk diffusion microbiological cutoffs and spectrum of activity of retapamulin, a novel topical antimicrobial agent.
AID449617	Antibacterial activity against methicillin-susceptible Staphylococcus epidermidis by agar dilution method	2009	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 19, Issue:18	Water-soluble phosphate prodrugs of pleuromutilin analogues with potent in vivo antibacterial activity against Gram-positive pathogens.
AID533663	Antimicrobial activity against Staphylococcus aureus RN1024	2008	Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12	Genetic characterization of Vga ABC proteins conferring reduced susceptibility to pleuromutilins in Staphylococcus aureus.
AID534127	Antibacterial activity against gram-negative Bacilli species	2008	Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11	Proposed MIC and disk diffusion microbiological cutoffs and spectrum of activity of retapamulin, a novel topical antimicrobial agent.
AID534122	Antibacterial activity against Streptococcus viridans	2008	Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11	Proposed MIC and disk diffusion microbiological cutoffs and spectrum of activity of retapamulin, a novel topical antimicrobial agent.
AID368445	Effect on 16S rRNA level in methicillin-resistant Staphylococcus aureus A1024 at 10 ng/mL by agilent bioanalyzer analysis	2007	Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9	Retapamulin inhibition of translation and 50S ribosomal subunit formation in Staphylococcus aureus cells.
AID534114	Antibacterial activity against methicillin sensitive coagulase-negative Staphylococcus	2008	Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11	Proposed MIC and disk diffusion microbiological cutoffs and spectrum of activity of retapamulin, a novel topical antimicrobial agent.
AID533654	Antimicrobial activity against Staphylococcus aureus IV20205004 harboring vgaAv positive Tn5406 transposon	2008	Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12	Genetic characterization of Vga ABC proteins conferring reduced susceptibility to pleuromutilins in Staphylococcus aureus.
AID323904	Antibacterial activity against Staphylococcus aureus RN4220 with rplC D159Y mutation	2007	Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6	Stepwise exposure of Staphylococcus aureus to pleuromutilins is associated with stepwise acquisition of mutations in rplC and minimally affects susceptibility to retapamulin.
AID534128	Antibacterial activity against Enterococcus species	2008	Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11	Proposed MIC and disk diffusion microbiological cutoffs and spectrum of activity of retapamulin, a novel topical antimicrobial agent.
AID640892	Antibacterial activity against methicillin-susceptible Staphylococcus epidermidis by agar microdilution method	2012	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2	Design, synthesis, and structure-activity relationship studies of conformationally restricted mutilin 14-carbamates.
AID1154455	Antibacterial activity against penicillin-resistant Streptococcus pneumoniae after 16 hrs by agar dilution method	2014	Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11	Design, synthesis, and structure-activity relationship studies of novel thioether pleuromutilin derivatives as potent antibacterial agents.
AID1701635	Antibacterial activity against methicilin-resistant Staphylococcus aureus 55508 incubated for 20 to 24 hrs by microbroth dilution assay	2020	Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24	Discovery of a Potent Adenine-Benzyltriazolo-Pleuromutilin Conjugate with Pronounced Antibacterial Activity against MRSA.
AID534121	Antibacterial activity against Streptococcus pyogenes	2008	Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11	Proposed MIC and disk diffusion microbiological cutoffs and spectrum of activity of retapamulin, a novel topical antimicrobial agent.
AID1867955	Antibacterial activity against Staphylococcus aureus ATCC 25923 assessed as bacterial growth inhibition incubated for 18 to 24 hrs by microtiter dilution method	2022	European journal of medicinal chemistry, Jul-05, Volume: 237	Discovery of novel pleuromutilin derivatives as potent antibacterial agents.
AID684266	Antibacterial activity against Streptococcus pyogenes	2012	Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19	Novel pleuromutilin derivatives as antibacterial agents: synthesis, biological evaluation and molecular docking studies.
AID534113	Antibacterial activity against methicillin resistant coagulase-negative Staphylococcus	2008	Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11	Proposed MIC and disk diffusion microbiological cutoffs and spectrum of activity of retapamulin, a novel topical antimicrobial agent.
AID368450	Increase in small RNA level in methicillin-resistant Staphylococcus aureus A1024 at 20 ng/mL by agilent bioanalyzer analysis	2007	Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9	Retapamulin inhibition of translation and 50S ribosomal subunit formation in Staphylococcus aureus cells.
AID1701650	Cytotoxicity against human Caco2 cells assessed as cell viability at 33 ug/ml incubated for 3 hrs by MTT assay	2020	Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24	Discovery of a Potent Adenine-Benzyltriazolo-Pleuromutilin Conjugate with Pronounced Antibacterial Activity against MRSA.
AID1867960	Antibacterial activity against Staphylococcus aureus ATCC 25923 assessed as reduction on bacterial count at 1X MIC incubated for 24 hrs by time killing assay	2022	European journal of medicinal chemistry, Jul-05, Volume: 237	Discovery of novel pleuromutilin derivatives as potent antibacterial agents.
AID323920	Antibacterial activity against Staphylococcus aureus 2A1-7 fast2 with rplC D159Y and unmapped mutation	2007	Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6	Stepwise exposure of Staphylococcus aureus to pleuromutilins is associated with stepwise acquisition of mutations in rplC and minimally affects susceptibility to retapamulin.
AID368446	Effect on 16S rRNA level in methicillin-resistant Staphylococcus aureus A1024 at 20 ng/mL by agilent bioanalyzer analysis	2007	Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9	Retapamulin inhibition of translation and 50S ribosomal subunit formation in Staphylococcus aureus cells.
AID1638645	Intrinsic clearance in mouse liver S9 fraction	2019	Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5	Boron-Pleuromutilins as Anti- Wolbachia Agents with Potential for Treatment of Onchocerciasis and Lymphatic Filariasis.
AID368448	Increase in small RNA level in wild type Staphylococcus aureus RN1786 at 20 ng/mL by agilent bioanalyzer analysis	2007	Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9	Retapamulin inhibition of translation and 50S ribosomal subunit formation in Staphylococcus aureus cells.
AID368432	Inhibition of ribosomal 30S subunit formation in wild type Staphylococcus aureus RN1786	2007	Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9	Retapamulin inhibition of translation and 50S ribosomal subunit formation in Staphylococcus aureus cells.
AID368440	Reduction of 23S rRNA level in wild type Staphylococcus aureus RN1786 at 20 ng/mL by agilent bioanalyzer analysis	2007	Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9	Retapamulin inhibition of translation and 50S ribosomal subunit formation in Staphylococcus aureus cells.
AID533653	Antimicrobial activity against Staphylococcus aureus IV20204009 harboring vgaAv positive Tn5406 transposon	2008	Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12	Genetic characterization of Vga ABC proteins conferring reduced susceptibility to pleuromutilins in Staphylococcus aureus.
AID1638646	Fraction unbound in mouse plasma at 2 uM	2019	Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5	Boron-Pleuromutilins as Anti- Wolbachia Agents with Potential for Treatment of Onchocerciasis and Lymphatic Filariasis.
AID534116	Antibacterial activity against methicillin sensitive Staphylococcus aureus	2008	Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11	Proposed MIC and disk diffusion microbiological cutoffs and spectrum of activity of retapamulin, a novel topical antimicrobial agent.
AID1638648	Apparent permeability of the compound in MDCK-MDR1 cells	2019	Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5	Boron-Pleuromutilins as Anti- Wolbachia Agents with Potential for Treatment of Onchocerciasis and Lymphatic Filariasis.
AID534129	Antibacterial activity against coagulase-negative Staphylococcus	2008	Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11	Proposed MIC and disk diffusion microbiological cutoffs and spectrum of activity of retapamulin, a novel topical antimicrobial agent.
AID534115	Antibacterial activity against methicillin resistant Staphylococcus aureus	2008	Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11	Proposed MIC and disk diffusion microbiological cutoffs and spectrum of activity of retapamulin, a novel topical antimicrobial agent.
AID323903	Antibacterial activity against wild type Staphylococcus aureus RN4220	2007	Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6	Stepwise exposure of Staphylococcus aureus to pleuromutilins is associated with stepwise acquisition of mutations in rplC and minimally affects susceptibility to retapamulin.
AID323912	Antibacterial activity against Staphylococcus aureus RN4220 with rplC G152D, D159Y, G155R and H134N mutation	2007	Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6	Stepwise exposure of Staphylococcus aureus to pleuromutilins is associated with stepwise acquisition of mutations in rplC and minimally affects susceptibility to retapamulin.
AID534125	Ratio of MBC90 to MIC90 for coagulase-negative Staphylococcus	2008	Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11	Proposed MIC and disk diffusion microbiological cutoffs and spectrum of activity of retapamulin, a novel topical antimicrobial agent.
AID1154453	Antibacterial activity against methicillin-resistant Staphylococcus aureus after 16 hrs by agar dilution method	2014	Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11	Design, synthesis, and structure-activity relationship studies of novel thioether pleuromutilin derivatives as potent antibacterial agents.
AID323916	Antibacterial activity against Staphylococcus aureus 2A1-8 with rplC G152D, D159Y and unmapped mutation	2007	Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6	Stepwise exposure of Staphylococcus aureus to pleuromutilins is associated with stepwise acquisition of mutations in rplC and minimally affects susceptibility to retapamulin.
AID534126	Ratio of MBC90 to MIC90 for Staphylococcus aureus	2008	Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11	Proposed MIC and disk diffusion microbiological cutoffs and spectrum of activity of retapamulin, a novel topical antimicrobial agent.
AID368441	Reduction of 23S rRNA level in methicillin-resistant Staphylococcus aureus A1024 at 10 ng/mL by agilent bioanalyzer analysis	2007	Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9	Retapamulin inhibition of translation and 50S ribosomal subunit formation in Staphylococcus aureus cells.
AID534117	Antibacterial activity against vancomycin intermediate Staphylococcus aureus	2008	Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11	Proposed MIC and disk diffusion microbiological cutoffs and spectrum of activity of retapamulin, a novel topical antimicrobial agent.
AID1867956	Antibacterial activity against Bacillus subtilis assessed as bacterial growth inhibition incubated for 18 to 24 hrs by microtiter dilution method	2022	European journal of medicinal chemistry, Jul-05, Volume: 237	Discovery of novel pleuromutilin derivatives as potent antibacterial agents.
AID1867936	Antibacterial activity against Escherichia coli assessed as inhibition of bacterial growth incubated for 24 hrs by microbroth two-fold dilution method	2022	European journal of medicinal chemistry, Jul-05, Volume: 237	Design, synthesis and antibacterial activity of novel pleuromutilin derivatives with thieno[2,3-d]pyrimidine substitution.
AID533655	Antimicrobial activity against Staphylococcus aureus IV20217008 harboring vgaAv positive Tn5406 transposon	2008	Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12	Genetic characterization of Vga ABC proteins conferring reduced susceptibility to pleuromutilins in Staphylococcus aureus.
AID449616	Antibacterial activity against methicillin-resistant Staphylococcus aureus by agar dilution method	2009	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 19, Issue:18	Water-soluble phosphate prodrugs of pleuromutilin analogues with potent in vivo antibacterial activity against Gram-positive pathogens.
AID533664	Antimicrobial activity against Staphylococcus aureus RN1024-tms	2008	Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12	Genetic characterization of Vga ABC proteins conferring reduced susceptibility to pleuromutilins in Staphylococcus aureus.
AID449619	Antibacterial activity against Streptococcus pneumoniae by agar dilution method	2009	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 19, Issue:18	Water-soluble phosphate prodrugs of pleuromutilin analogues with potent in vivo antibacterial activity against Gram-positive pathogens.
AID1701637	Antibacterial activity against methicilin-resistant Staphylococcus aureus 4828 incubated for 20 to 24 hrs by microbroth dilution assay	2020	Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24	Discovery of a Potent Adenine-Benzyltriazolo-Pleuromutilin Conjugate with Pronounced Antibacterial Activity against MRSA.
AID323918	Antibacterial activity against Staphylococcus aureus 2A1-1 fast2 with rplC D159Y and unmapped mutation	2007	Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6	Stepwise exposure of Staphylococcus aureus to pleuromutilins is associated with stepwise acquisition of mutations in rplC and minimally affects susceptibility to retapamulin.
AID534120	Antibacterial activity against Streptococcus agalactiae	2008	Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11	Proposed MIC and disk diffusion microbiological cutoffs and spectrum of activity of retapamulin, a novel topical antimicrobial agent.
AID1867953	Antibacterial activity against methicillin-resistant Staphylococcus aureus BNCC 337371 assessed as bacterial growth inhibition incubated for 18 to 24 hrs by microtiter dilution method	2022	European journal of medicinal chemistry, Jul-05, Volume: 237	Discovery of novel pleuromutilin derivatives as potent antibacterial agents.
AID1867935	Antibacterial activity against Streptococcus agalactiae assessed as inhibition of bacterial growth incubated for 24 hrs by microbroth two-fold dilution method	2022	European journal of medicinal chemistry, Jul-05, Volume: 237	Design, synthesis and antibacterial activity of novel pleuromutilin derivatives with thieno[2,3-d]pyrimidine substitution.
AID640891	Antibacterial activity against methicillin-resistant Staphylococcus aureus by agar microdilution method	2012	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2	Design, synthesis, and structure-activity relationship studies of conformationally restricted mutilin 14-carbamates.
AID368431	Inhibition of ribosomal 50S subunit synthesis in methicillin-resistant Staphylococcus aureus A1024	2007	Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9	Retapamulin inhibition of translation and 50S ribosomal subunit formation in Staphylococcus aureus cells.
AID368444	Effect on 16S rRNA level in wild type Staphylococcus aureus RN1786 at 20 ng/mL by agilent bioanalyzer analysis	2007	Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9	Retapamulin inhibition of translation and 50S ribosomal subunit formation in Staphylococcus aureus cells.
AID1701638	Antibacterial activity against methicilin-resistant Staphylococcus epidermis 933010 incubated for 20 to 24 hrs by microbroth dilution assay	2020	Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24	Discovery of a Potent Adenine-Benzyltriazolo-Pleuromutilin Conjugate with Pronounced Antibacterial Activity against MRSA.
AID368430	Inhibition of ribosomal 50S subunit synthesis in wild type Staphylococcus aureus RN1786	2007	Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9	Retapamulin inhibition of translation and 50S ribosomal subunit formation in Staphylococcus aureus cells.
AID323910	Antibacterial activity against Staphylococcus aureus RN4220 with rplC G152D, D159Y and G144R mutation	2007	Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6	Stepwise exposure of Staphylococcus aureus to pleuromutilins is associated with stepwise acquisition of mutations in rplC and minimally affects susceptibility to retapamulin.
AID1428684	Antibacterial activity against Staphylococcus aureus ATCC 29213 after overnight incubation by broth dilution method	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	Design, synthesis and antibacterial evaluation of novel pleuromutilin derivatives possessing piperazine linker.
AID323913	Antibacterial activity against Staphylococcus aureus RN4220 with rplC G152D, D159Y, G155R and A150T mutation	2007	Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6	Stepwise exposure of Staphylococcus aureus to pleuromutilins is associated with stepwise acquisition of mutations in rplC and minimally affects susceptibility to retapamulin.
AID1867961	Antibacterial activity against methicillin-resistant Staphylococcus aureus BNCC 337371 assessed as reduction on bacterial count at 6X MIC incubated for 24 hrs by time killing assay	2022	European journal of medicinal chemistry, Jul-05, Volume: 237	Discovery of novel pleuromutilin derivatives as potent antibacterial agents.
AID1867954	Antibacterial activity against methicillin-resistant Staphylococcus epidermidis ATCC 51625 assessed as bacterial growth inhibition incubated for 18 to 24 hrs by microtiter dilution method	2022	European journal of medicinal chemistry, Jul-05, Volume: 237	Discovery of novel pleuromutilin derivatives as potent antibacterial agents.
AID640893	Antibacterial activity against methicillin-resistant Staphylococcus epidermidis by agar microdilution method	2012	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2	Design, synthesis, and structure-activity relationship studies of conformationally restricted mutilin 14-carbamates.
AID323908	Antibacterial activity against Staphylococcus aureus RN4220 with rplC G152D and D159Y mutation	2007	Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6	Stepwise exposure of Staphylococcus aureus to pleuromutilins is associated with stepwise acquisition of mutations in rplC and minimally affects susceptibility to retapamulin.
AID1701633	Antibacterial activity against methicilin-resistant Staphylococcus aureus USA300 FPR3757 incubated for 20 to 24 hrs by microbroth dilution assay	2020	Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24	Discovery of a Potent Adenine-Benzyltriazolo-Pleuromutilin Conjugate with Pronounced Antibacterial Activity against MRSA.
AID1154451	Antibacterial activity against Staphylococcus aureus ATCC 292135 after 16 hrs by agar dilution method	2014	Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11	Design, synthesis, and structure-activity relationship studies of novel thioether pleuromutilin derivatives as potent antibacterial agents.
AID533658	Antimicrobial activity against Staphylococcus aureus IHMA127277 harboring vgaAv positive Tn5406 transposon	2008	Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12	Genetic characterization of Vga ABC proteins conferring reduced susceptibility to pleuromutilins in Staphylococcus aureus.
AID684265	Antibacterial activity against Staphylococcus aureus	2012	Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19	Novel pleuromutilin derivatives as antibacterial agents: synthesis, biological evaluation and molecular docking studies.
AID640890	Antibacterial activity against methicillin-susceptible Staphylococcus aureus by agar microdilution method	2012	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2	Design, synthesis, and structure-activity relationship studies of conformationally restricted mutilin 14-carbamates.
AID534124	Ratio of MBC90 to MIC90 for Streptococcus pyogenes	2008	Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11	Proposed MIC and disk diffusion microbiological cutoffs and spectrum of activity of retapamulin, a novel topical antimicrobial agent.
AID1154486	Antibacterial activity against methicillin-resistant Staphylococcus epidermidis after 16 hrs by agar dilution method	2014	Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11	Design, synthesis, and structure-activity relationship studies of novel thioether pleuromutilin derivatives as potent antibacterial agents.
AID533656	Antimicrobial activity against Staphylococcus aureus IV20217033 harboring vgaA positive plasmid VGA	2008	Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12	Genetic characterization of Vga ABC proteins conferring reduced susceptibility to pleuromutilins in Staphylococcus aureus.
AID323914	Antibacterial activity against Staphylococcus aureus 2A1-1 with rplC G152D, D159Y and unmapped mutation	2007	Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6	Stepwise exposure of Staphylococcus aureus to pleuromutilins is associated with stepwise acquisition of mutations in rplC and minimally affects susceptibility to retapamulin.
AID368443	Effect on 16S rRNA level in wild type Staphylococcus aureus RN1786 at 10 ng/mL by agilent bioanalyzer analysis	2007	Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9	Retapamulin inhibition of translation and 50S ribosomal subunit formation in Staphylococcus aureus cells.
AID525143	Antimicrobial activity against linezolid-resistant Staphylococcus aureus isolate 004-737X expressing cfr and ermA gene isolated from paraplegic patient by broth microdilution method	2008	Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6	First report of cfr-mediated resistance to linezolid in human staphylococcal clinical isolates recovered in the United States.
AID368428	Inhibition of protein synthesis in wild type Staphylococcus aureus RN1786	2007	Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9	Retapamulin inhibition of translation and 50S ribosomal subunit formation in Staphylococcus aureus cells.
AID368437	Inhibition of ribosomal 50S subunit synthesis in methicillin-resistant Staphylococcus aureus A1024 at 8 ng/mL by [3H]uridine pulse-chase labeling method	2007	Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9	Retapamulin inhibition of translation and 50S ribosomal subunit formation in Staphylococcus aureus cells.
AID368433	Inhibition of ribosomal 30S subunit formation in methicillin-resistant Staphylococcus aureus A1024	2007	Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9	Retapamulin inhibition of translation and 50S ribosomal subunit formation in Staphylococcus aureus cells.
AID323907	Antibacterial activity against Staphylococcus aureus RN4220 with rplC G152D mutation	2007	Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6	Stepwise exposure of Staphylococcus aureus to pleuromutilins is associated with stepwise acquisition of mutations in rplC and minimally affects susceptibility to retapamulin.
AID1867959	Antibacterial activity against methicillin-resistant Staphylococcus aureus BNCC 337371 assessed as reduction on bacterial count at 1X MIC incubated for 24 hrs by time killing assay	2022	European journal of medicinal chemistry, Jul-05, Volume: 237	Discovery of novel pleuromutilin derivatives as potent antibacterial agents.
AID1428686	Antibacterial activity against Enterococcus faecium ATCC 35667 after overnight incubation by broth dilution method	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	Design, synthesis and antibacterial evaluation of novel pleuromutilin derivatives possessing piperazine linker.
AID1701641	Cytotoxicity against differentiated human Caco2 cells assessed as increase in ATP level at 33 ug/ml incubated for 3 hrs by Cell-titer Glo assay	2020	Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24	Discovery of a Potent Adenine-Benzyltriazolo-Pleuromutilin Conjugate with Pronounced Antibacterial Activity against MRSA.
AID1867933	Antibacterial activity against Staphylococcus aureus assessed as diameter of the inhibition circle at 1 mg/ml incubated for 48 hrs	2022	European journal of medicinal chemistry, Jul-05, Volume: 237	Design, synthesis and antibacterial activity of novel pleuromutilin derivatives with thieno[2,3-d]pyrimidine substitution.
AID323909	Antibacterial activity against Staphylococcus aureus RN4220 with rplC G152D and G155R mutation	2007	Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6	Stepwise exposure of Staphylococcus aureus to pleuromutilins is associated with stepwise acquisition of mutations in rplC and minimally affects susceptibility to retapamulin.
AID368427	Inhibition of total viable cell number in methicillin-resistant Staphylococcus aureus A1024	2007	Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9	Retapamulin inhibition of translation and 50S ribosomal subunit formation in Staphylococcus aureus cells.
AID1867957	Antibacterial activity against Enterococcus faecalis assessed as bacterial growth inhibition incubated for 18 to 24 hrs by microtiter dilution method	2022	European journal of medicinal chemistry, Jul-05, Volume: 237	Discovery of novel pleuromutilin derivatives as potent antibacterial agents.
AID330278	Antimicrobial activity against Staphylococcus aureus	2007	Proceedings of the National Academy of Sciences of the United States of America, Mar-13, Volume: 104, Issue:11	Induced-fit tightens pleuromutilins binding to ribosomes and remote interactions enable their selectivity.
AID1867962	Antibacterial activity against Staphylococcus aureus ATCC 25923 assessed as reduction on bacterial count at 6X MIC incubated for 24 hrs by time killing assay	2022	European journal of medicinal chemistry, Jul-05, Volume: 237	Discovery of novel pleuromutilin derivatives as potent antibacterial agents.
AID323917	Antibacterial activity against Staphylococcus aureus 2A1-1 fast1 with rplC D159Y and unmapped mutation	2007	Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6	Stepwise exposure of Staphylococcus aureus to pleuromutilins is associated with stepwise acquisition of mutations in rplC and minimally affects susceptibility to retapamulin.
AID368426	Inhibition of total viable cell number in wild type Staphylococcus aureus RN1786	2007	Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9	Retapamulin inhibition of translation and 50S ribosomal subunit formation in Staphylococcus aureus cells.
AID1638643	Antimicrobial activity against Wolbachia pipientis infected in Asian tiger mosquito C6/36 cells after 7 days by SYTO11 DNA dye-based confocal imaging analysis	2019	Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5	Boron-Pleuromutilins as Anti- Wolbachia Agents with Potential for Treatment of Onchocerciasis and Lymphatic Filariasis.
AID368429	Inhibition of protein synthesis in methicillin-resistant Staphylococcus aureus A1024	2007	Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9	Retapamulin inhibition of translation and 50S ribosomal subunit formation in Staphylococcus aureus cells.
AID533662	Antimicrobial activity against Staphylococcus aureus RN4220 harboring vgaAv positive plasmid CU1	2008	Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12	Genetic characterization of Vga ABC proteins conferring reduced susceptibility to pleuromutilins in Staphylococcus aureus.
AID330277	Displacement of [3H]SB-2587891 from Escherichia coli ribosomes	2007	Proceedings of the National Academy of Sciences of the United States of America, Mar-13, Volume: 104, Issue:11	Induced-fit tightens pleuromutilins binding to ribosomes and remote interactions enable their selectivity.
AID368442	Reduction of 23S rRNA level in methicillin-resistant Staphylococcus aureus A1024 at 20 ng/mL by agilent bioanalyzer analysis	2007	Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9	Retapamulin inhibition of translation and 50S ribosomal subunit formation in Staphylococcus aureus cells.
AID533665	Antimicrobial activity against Staphylococcus aureus ATCC 29213	2008	Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12	Genetic characterization of Vga ABC proteins conferring reduced susceptibility to pleuromutilins in Staphylococcus aureus.
AID323919	Antibacterial activity against Staphylococcus aureus 2A1-7 fast1 with rplC D159Y and unmapped mutation	2007	Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6	Stepwise exposure of Staphylococcus aureus to pleuromutilins is associated with stepwise acquisition of mutations in rplC and minimally affects susceptibility to retapamulin.
AID323906	Antibacterial activity against Staphylococcus aureus RN4220 with rplC S158L mutation	2007	Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6	Stepwise exposure of Staphylococcus aureus to pleuromutilins is associated with stepwise acquisition of mutations in rplC and minimally affects susceptibility to retapamulin.
AID449618	Antibacterial activity against methicillin-resistant Staphylococcus epidermidis by agar dilution method	2009	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 19, Issue:18	Water-soluble phosphate prodrugs of pleuromutilin analogues with potent in vivo antibacterial activity against Gram-positive pathogens.
AID330279	Antimicrobial activity against Streptococcus pyogenes	2007	Proceedings of the National Academy of Sciences of the United States of America, Mar-13, Volume: 104, Issue:11	Induced-fit tightens pleuromutilins binding to ribosomes and remote interactions enable their selectivity.
AID368434	Antibacterial activity against wild type Staphylococcus aureus RN1786	2007	Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9	Retapamulin inhibition of translation and 50S ribosomal subunit formation in Staphylococcus aureus cells.
AID368449	Increase in small RNA level in methicillin-resistant Staphylococcus aureus A1024 at 10 ng/mL by agilent bioanalyzer analysis	2007	Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9	Retapamulin inhibition of translation and 50S ribosomal subunit formation in Staphylococcus aureus cells.
AID1701636	Antibacterial activity against methicilin-resistant Staphylococcus aureus 52518 incubated for 20 to 24 hrs by microbroth dilution assay	2020	Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24	Discovery of a Potent Adenine-Benzyltriazolo-Pleuromutilin Conjugate with Pronounced Antibacterial Activity against MRSA.
AID533657	Antimicrobial activity against Staphylococcus aureus IV20222009 harboring vgaAv positive Tn5406 transposon	2008	Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12	Genetic characterization of Vga ABC proteins conferring reduced susceptibility to pleuromutilins in Staphylococcus aureus.
AID533660	Antimicrobial activity against Staphylococcus aureus RN4220 harboring plasmid VGA	2008	Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12	Genetic characterization of Vga ABC proteins conferring reduced susceptibility to pleuromutilins in Staphylococcus aureus.
AID641049	Antibacterial activity against Streptococcus pneumoniae by agar microdilution method	2012	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2	Design, synthesis, and structure-activity relationship studies of conformationally restricted mutilin 14-carbamates.
AID1867934	Antibacterial activity against Staphylococcus aureus assessed as inhibition of bacterial growth incubated for 24 hrs by microbroth two-fold dilution method	2022	European journal of medicinal chemistry, Jul-05, Volume: 237	Design, synthesis and antibacterial activity of novel pleuromutilin derivatives with thieno[2,3-d]pyrimidine substitution.
AID368439	Reduction of 23S rRNA level in wild type Staphylococcus aureus RN1786 at 10 ng/mL by agilent bioanalyzer analysis	2007	Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9	Retapamulin inhibition of translation and 50S ribosomal subunit formation in Staphylococcus aureus cells.
AID1701644	Cytotoxicity against differentiated human Caco2 cells assessed as ATP level at 33 ug/ml incubated for 3 hrs by Cell-titer Glo assay	2020	Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24	Discovery of a Potent Adenine-Benzyltriazolo-Pleuromutilin Conjugate with Pronounced Antibacterial Activity against MRSA.
AID449615	Antibacterial activity against methicillin-susceptible Staphylococcus aureus by agar dilution method	2009	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 19, Issue:18	Water-soluble phosphate prodrugs of pleuromutilin analogues with potent in vivo antibacterial activity against Gram-positive pathogens.
AID1638644	Antimicrobial activity against Wolbachia wMel infected in Drosophila melanogaster LDW1 cells after 6 days by DAPI-based fluorescence in-situ hybridization assay	2019	Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5	Boron-Pleuromutilins as Anti- Wolbachia Agents with Potential for Treatment of Onchocerciasis and Lymphatic Filariasis.
AID1867937	Antibacterial activity against Methicillin-resistant Staphylococcus aureus BNCC 337371 assessed as inhibition of bacterial growth incubated for 24 hrs by microbroth two-fold dilution method	2022	European journal of medicinal chemistry, Jul-05, Volume: 237	Design, synthesis and antibacterial activity of novel pleuromutilin derivatives with thieno[2,3-d]pyrimidine substitution.
AID1867958	Antibacterial activity against Escherichia coli CICC 10389 assessed as bacterial growth inhibition incubated for 18 to 24 hrs by microtiter dilution method	2022	European journal of medicinal chemistry, Jul-05, Volume: 237	Discovery of novel pleuromutilin derivatives as potent antibacterial agents.
AID1154452	Antibacterial activity against methicillin-sensitive Staphylococcus aureus after 16 hrs by agar dilution method	2014	Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11	Design, synthesis, and structure-activity relationship studies of novel thioether pleuromutilin derivatives as potent antibacterial agents.
AID1701634	Antibacterial activity against methicilin-resistant Staphylococcus aureus USA300 FPR3757 incubated for 20 hrs by microbroth dilution assay	2020	Journal of medicinal chemistry, 12-24, Volume: 63, Issue:24	Discovery of a Potent Adenine-Benzyltriazolo-Pleuromutilin Conjugate with Pronounced Antibacterial Activity against MRSA.
AID533659	Antimicrobial activity against Staphylococcus aureus RN4220	2008	Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12	Genetic characterization of Vga ABC proteins conferring reduced susceptibility to pleuromutilins in Staphylococcus aureus.
AID323911	Antibacterial activity against Staphylococcus aureus RN4220 with rplC G152D, D159Y and G155R mutation	2007	Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6	Stepwise exposure of Staphylococcus aureus to pleuromutilins is associated with stepwise acquisition of mutations in rplC and minimally affects susceptibility to retapamulin.
AID368436	Inhibition of ribosomal 30S subunit synthesis in methicillin-resistant Staphylococcus aureus A1024 at 8 ng/mL by [3H]uridine pulse-chase labeling method	2007	Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9	Retapamulin inhibition of translation and 50S ribosomal subunit formation in Staphylococcus aureus cells.
AID1428683	Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 after overnight incubation by broth dilution method	2017	European journal of medicinal chemistry, Feb-15, Volume: 127	Design, synthesis and antibacterial evaluation of novel pleuromutilin derivatives possessing piperazine linker.
AID525144	Antimicrobial activity against Staphylococcus epidermidis isolate 426-3147L expressing cfr gene by broth microdilution CLSI method	2008	Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6	First report of cfr-mediated resistance to linezolid in human staphylococcal clinical isolates recovered in the United States.
AID368438	Inhibition of ribosomal 50S subunit synthesis in wild type Staphylococcus aureus RN1786 at 8 ng/mL by [3H]uridine pulse-chase labeling method	2007	Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9	Retapamulin inhibition of translation and 50S ribosomal subunit formation in Staphylococcus aureus cells.
AID533661	Antimicrobial activity against Staphylococcus aureus RN4220 harboring plasmid CU1	2008	Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12	Genetic characterization of Vga ABC proteins conferring reduced susceptibility to pleuromutilins in Staphylococcus aureus.
AID323915	Antibacterial activity against Staphylococcus aureus 2A1-7 with rplC G152D, D159Y and unmapped mutation	2007	Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6	Stepwise exposure of Staphylococcus aureus to pleuromutilins is associated with stepwise acquisition of mutations in rplC and minimally affects susceptibility to retapamulin.
AID534123	Antibacterial activity against Staphylococcus aureus	2008	Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11	Proposed MIC and disk diffusion microbiological cutoffs and spectrum of activity of retapamulin, a novel topical antimicrobial agent.
AID368435	Antibacterial activity against methicillin-resistant Staphylococcus aureus A1024	2007	Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9	Retapamulin inhibition of translation and 50S ribosomal subunit formation in Staphylococcus aureus cells.
AID323905	Antibacterial activity against Staphylococcus aureus RN4220 with rplC G155R mutation	2007	Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6	Stepwise exposure of Staphylococcus aureus to pleuromutilins is associated with stepwise acquisition of mutations in rplC and minimally affects susceptibility to retapamulin.
AID1154454	Antibacterial activity against methicillin-sensitive Staphylococcus epidermidis after 16 hrs by agar dilution method	2014	Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11	Design, synthesis, and structure-activity relationship studies of novel thioether pleuromutilin derivatives as potent antibacterial agents.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	31 (38.27)	29.6817
2010's	37 (45.68)	24.3611
2020's	13 (16.05)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	9 (10.11%)	5.53%
Reviews	12 (13.48%)	6.00%
Case Studies	3 (3.37%)	4.05%
Observational	0 (0.00%)	0.25%
Other	65 (73.03%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (18)

Trial Overview

Trial	Phase	Enrollment	Study Type	Start Date	Status
A Randomized, Double-Blind, Placebo-Controlled Trial of the Efficacy of Retapamulin as a Topical Decolonizing Agent for Mupirocin Resistant Methicillin Resistant Staphylococcus Aureus (MRSA) [NCT03304873]	Phase 3	47 participants (Actual)	Interventional	2017-12-01	Completed
Pharmacovigilence for Retapamulin: Age-stratified Monitoring of Prescribed Use in the United States [NCT01153880]		1 participants (Actual)	Observational	2008-12-31	Completed
Pharmacovigilence for Retapamulin: Age-stratified Monitoring of Prescribed Use in the European Union [NCT01153828]		1 participants (Actual)	Observational	2008-11-30	Completed
Use of Altabax Ointment (Retapamulin 1%) BID for 7 Days in Treatment of Secondary Infection With Staphylococcus Aureus (MRSA and MSSA) and Streptococcus Pyogenes in Atopic Dermatitis Patients - Open Label Pilot Study [NCT01064947]	Phase 4	29 participants (Actual)	Interventional	2010-02-28	Completed
Randomized, Double-blind, Placebo-controlled Study to Evaluate the Safety, Tolerability, Pharmacokinetics (PK) and Efficacy of Retapamulin Ointment, 1% Applied Twice Daily for 3 or 5 Days to the Anterior Nares of Healthy Adult Subjects Nasally Colonized W [NCT00539994]	Phase 2	57 participants (Actual)	Interventional	2007-09-30	Completed
A Randomized, Double-Blind, Multicenter, Placebo-controlled, Phase III Superiority Study to Assess the Safety and Efficacy of Topical Retapamulin Ointment, 1%, Versus Placebo Ointment Applied Twice Daily for 5 Days in the Treatment of Adult and Pediatric [NCT00684177]	Phase 3	508 participants (Actual)	Interventional	2008-05-31	Completed
Prevalence of Methicillin-resistant Staphylococcus Aureus (MRSA) in a Medical Center and Efficacy of Altabax in Clearing MRSA Nasal Colonization [NCT00856089]	Phase 4	0 participants (Actual)	Interventional	2009-05-31	Withdrawn(stopped due to Study is withdrawn and no one enrolled due to changes in personnel)
Randomized, Placebo-Controlled Trial of Treatment of Atopic Dermatitis With Concurrent Altabax® and Topical Low-Potency Corticosteroids vs. Low-Potency Corticosteroid Mono-therapy [NCT00871208]	Phase 4	0 participants (Actual)	Interventional	2009-05-31	Withdrawn(stopped due to Funding withdrawn)
Treatment of Patients Colonized With Methicillin-Resistant Staphylococcus Aureus Prior to Bone and Joint Surgery (TOPS-MRSA) [NCT00903279]	Phase 2	0 participants (Actual)	Interventional	2009-08-31	Withdrawn(stopped due to Funding)
Twice Daily Altabax Application for the Treatment of Uncomplicated Soft Tissue Infection [NCT01126268]	Phase 4	38 participants (Actual)	Interventional	2010-04-30	Completed
A Randomised, Double-blind, Multicentre, Superiority Placebo-controlled, Phase III Study to Assess the Efficacy and Safety of Topical 1% SB-275833 Ointment Versus Placebo Ointment Applied Twice Daily for 5 Days in the Treatment of Adults and Paediatric Su [NCT00133848]	Phase 3	210 participants	Interventional	2005-04-30	Completed
An Observer-blind, Multicenter, Non-inferiority, Comparative Study of the Safety and Efficacy of Topical 1% SB-275833 Ointment, Applied Twice Daily for 5 Days, Versus Topical 2% Fusidic Acid Cream Applied Three Times Daily for 7 Days in the Treatment Adul [NCT00133874]	Phase 3	520 participants (Actual)	Interventional	2005-04-30	Completed
A Study to Evaluate the Feasibility of Microdialysis to Determine Skin Concentrations of Retapamulin in Healthy Volunteers [NCT01812382]	Phase 1	3 participants (Actual)	Interventional	2014-04-02	Completed
Retapamulin for Reducing MRSA Nasal Carriage [NCT01461668]	Phase 4	53 participants (Actual)	Interventional	2012-07-31	Completed
An Open Label, Multi-centre, Non-interventional Post-marketing Surveillance (PMS) to Monitor the Safety and Efficacy of ALTARGO(Retapamulin) Administered in Korean Patients According to the Prescribing Information [NCT01445600]		3,612 participants (Actual)	Observational	2012-11-30	Completed
An Open-Label, Non-Comparative Study to Assess the Pharmacokinetics, Safety and Efficacy of Topical Retapamulin (SB-275833) Ointment, 1%, Twice Daily for Five Days in the Treatment of Uncomplicated Skin and Skin Structure Infections in Pediatric Subjects [NCT00555061]	Phase 4	60 participants (Actual)	Interventional	2007-09-30	Completed
A Phase III 3 Arms, Multicenter, Randomised, Investigator-blind Study to Assess the Efficacy and Safety of Ozenoxacin 1% Cream Applied Twice Daily for 5 Days Versus Placebo in the Treatment of Patients With Impetigo [NCT01397461]	Phase 3	465 participants (Actual)	Interventional	2012-03-31	Completed
An Investigator-Initiated Study: Treatment of Staphylococcus Aureus Colonization in Hand Eczema Decreases Severity of Disease [NCT01591785]		60 participants (Actual)	Interventional	2012-01-31	Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

Trial	Outcome
NCT00539994 (13) [back to overview]	Percentage of Participants With Eradication of S. Aureus Nasal Carriage at Day 12 Who Were Categorized as Persistent Carriers of S. Aureus
NCT00539994 (13) [back to overview]	Percentage of Participants With Eradication of S. Aureus Nasal Carriage at Each Post Treatment Visit Stratified by Pharyngeal Carriage Status
NCT00539994 (13) [back to overview]	Plasma Retapumulin Pharmacokinetic Parameters by Treatment at Day 5
NCT00539994 (13) [back to overview]	Plasma Retapumulin Pharmacokinetic Parameters by Treatment at Day 5 Evaluated by Plasma AUC After Dosing
NCT00539994 (13) [back to overview]	Plasma Retapumulin Pharmacokinetic Parameters by Treatment at Day 5 Evaluated by Plasma Cmax After Dosing
NCT00539994 (13) [back to overview]	Number of Participants With a Nasal Culture Negative for MRSA (Methicillin-resistant S. Aureus)
NCT00539994 (13) [back to overview]	Percentage of Participants With Eradication of S. Aureus Nasal Carriage at Days 7 and 33 Who Were Categorized as Persistent Carriers of S. Aureus
NCT00539994 (13) [back to overview]	Percentage of Participants With Nasal Recolonization With S. Aureus on Study Days 12 and 33 Who Were Persistant Carriers Who Tested Positive in the Pharyngeal Region on Days 12 and 33 But Negative in the Nasal Region on Day 7 or Days 7 and 12
NCT00539994 (13) [back to overview]	Percentage of Participants With Nasal Recolonization With S. Aureus on Study Days 12 and 33 Who Were Persistant Carriers Who Tested Positive in the Pharyngeal Region on Days 12 and 33 But Negative in the Nasal Region on Day 7 or Days 7 and 12
NCT00539994 (13) [back to overview]	Plasma Retapumulin Pharmacokinetic Parameters by Treatment at Days 1 and 3 Evaluated by Plasma AUC After Dosing
NCT00539994 (13) [back to overview]	Plasma Retapumulin Pharmacokinetic Parameters by Treatment at Days 1 and 3 Evaluated by Plasma Cmax After Dosing
NCT00539994 (13) [back to overview]	Plasma Retapumulin Pharmacokinetic Parameters, Tmax, by Treatment at Days 1 and 3
NCT00539994 (13) [back to overview]	Prevalence of S. Aureus Nasal and Pharyngeal Carriage by Visit.
NCT00555061 (4) [back to overview]	Bacteriological Success Rate at Follow-up, by Baseline Pathogen
NCT00555061 (4) [back to overview]	Number of Participants With Clinical Success at Follow-up, by Type of Skin Infection and by Age
NCT00555061 (4) [back to overview]	Number of Participants by Age With Therapeutic Response of Success
NCT00555061 (4) [back to overview]	Number of Participants With Measurable Plasma Concentrations, by Age Group
NCT00684177 (6) [back to overview]	Number of Baseline Pathogens With the Indicated Microbiological Outcome at End of Therapy (2-4 Days Post Therapy)
NCT00684177 (6) [back to overview]	Number of Participants With Clinical Success and Failure at Follow-up (7-9 Days Post Therapy) for the Intent-to-Treat Bacteriology (ITTB) Subset of the Primary Efficacy Population
NCT00684177 (6) [back to overview]	Number of Participants With Clinical Success and Failure at Follow-up (7-9 Days Post Therapy) for the Primary Efficacy Population
NCT00684177 (6) [back to overview]	Number of Participants With Microbiological Success and Failure at Follow-up (7-9 Days Post Therapy)
NCT00684177 (6) [back to overview]	Number of Participants With the Indicated Clinical Outcome at End of Therapy (2-4 Days Post Therapy)
NCT00684177 (6) [back to overview]	Number of Participants With Therapeutic Success and Failure at Follow-up (7-9 Days Post Therapy)
NCT01064947 (4) [back to overview]	Bacteriological Culture
NCT01064947 (4) [back to overview]	Investigator Assessment of Clinical Cure
NCT01064947 (4) [back to overview]	Local Tolerability
NCT01064947 (4) [back to overview]	Skin Infection Rating Scale (SIRS)
NCT01126268 (19) [back to overview]	Number of Participants Whose Wound Cultures Were Positive for MRSA and Who Were Determined to be a Clinical Success at the Follow-up Visit
NCT01126268 (19) [back to overview]	Wound Size at Baseline
NCT01126268 (19) [back to overview]	Wound Size at Follow up
NCT01126268 (19) [back to overview]	Clinical Response at Follow up as Assessed by a Rating Scale
NCT01126268 (19) [back to overview]	Crusting (Sign and Symptom of Infection) at Baseline
NCT01126268 (19) [back to overview]	Crusting (Sign and Symptom of Infection) at Follow up
NCT01126268 (19) [back to overview]	Erythema (Sign and Symptom of Infection) at Baseline
NCT01126268 (19) [back to overview]	Erythema (Sign and Symptom of Infection) at Follow up
NCT01126268 (19) [back to overview]	Microbiologic Response at Follow up as Assessed by a Rating Scale
NCT01126268 (19) [back to overview]	Pain (Sign and Symptom of Infection) at Baseline
NCT01126268 (19) [back to overview]	Pain (Sign and Symptom of Infection) at Follow up
NCT01126268 (19) [back to overview]	Purulence (Sign and Symptom of Infection) at Baseline
NCT01126268 (19) [back to overview]	Purulence (Sign and Symptom of Infection) at Follow up
NCT01126268 (19) [back to overview]	Tissue Edema (Sign and Symptom of Infection) at Baseline
NCT01126268 (19) [back to overview]	Tissue Warmth (Sign and Symptom of Infection) at Baseline
NCT01126268 (19) [back to overview]	Tissue Warmth (Sign and Symptom of Infection) at Follow up
NCT01126268 (19) [back to overview]	Number of Participants Reporting Any Adverse Event (AE)
NCT01126268 (19) [back to overview]	Tissue Edema (Sign and Symptom of Infection) at Follow up
NCT01126268 (19) [back to overview]	Number of Participants Who Were a Therapeutic Success
NCT01397461 (1) [back to overview]	Clinical Success
NCT01461668 (1) [back to overview]	Proportion of Participants With MRSA Clearance
NCT01591785 (4) [back to overview]	Number of Participants With PGA of 0 or 1
NCT01591785 (4) [back to overview]	Number of Participants With PGA of 0 or 1
NCT01591785 (4) [back to overview]	Staph Aureus Culture Results
NCT01591785 (4) [back to overview]	Staph Aureus Culture Results
NCT03304873 (2) [back to overview]	Number of Partcipants With MRSA Carriage at 4 Weeks Post Decolonization With Retapamulin or Placebo
NCT03304873 (2) [back to overview]	Number of Participants With MRSA Carriage at 1 Week Post Decolonization With Retapamulin or Placebo

Percentage of Participants With Eradication of S. Aureus Nasal Carriage at Day 12 Who Were Categorized as Persistent Carriers of S. Aureus

Subjects who tested positive as persistent carriers of S. Aureus who on day 12 are negative and have been eradicated of S. Aureus. (NCT00539994)
Timeframe: Day 12

Intervention	Percentage of participants (Number)
Retapamulin 3 Days	94
Retapamulin 5 Days	92
Placebo	15

Intervention	Percentage of participants (Number)
	Culture positive Day 1, Nasal eradication Day 7	Culture negative Day 1, Nasal eradication Day 7	Culture positive Day 1, Nasal eradication Day 12	Culture negative Day 1, Nasal eradication Day 12	Culture positive Day 1, Nasal eradication Day 33	Culture negative Day 1, Nasal eradication Day 33
Placebo	10	33	10	33	30	33
Retapamulin 3 Days	90	100	90	100	80	67
Retapamulin 5 Days	100	100	86	100	88	83

Intervention	Percentage of participants (Number)
	Day 7	Day 33
Placebo	2	4
Retapamulin 3 Days	94	75
Retapamulin 5 Days	100	86

Intervention	Percentage of participants (Number)
	PC pos. D12, NC neg. D7, Recolonized D12	PC pos. D12, NC neg. D7 and D12, Recolonized D33	PC pos. D33, NC neg. D7, Recolonized D12	PC pos. D33, NC neg. D7 and D12, Recolonized D33
Placebo	50	0	0	0
Retapamulin 3 Days	0	33	17	40
Retapamulin 5 Days	33	0	17	25
Total	18	22	15	30

Intervention	Percentage of participants (Number)
	PC neg. D12, NC neg. D7, Recolonized D12	PC neg. D12, NC neg. D7 and D12, Recolonized D33	PC neg. D33, NC neg. D7, Recolonized D12	PC neg. D33, NC neg. D7 and D12, Recolonized D33
Placebo	0	0	100	0
Retapamulin 3 Days	11	13	0	11
Retapamulin 5 Days	0	20	0	13
Total	5	17	6	12

Intervention	ng.h /mL (Mean)
	Day 1, n=5 and 2	Day 3, n=14 and 10
Retapamulin 3 Days	0.8663	4.2802
Retapamulin 5 Days	0.3816	2.0881

Intervention	ng/mL (Mean)
	Day 1, n=10 and 3	Day 3, n=16 and 10
Retapamulin 3 Days	0.4703	0.7893
Retapamulin 5 Days	0.3538	0.6185

Intervention	participants (Number)
	Screening 1, n=430, 429	Screening 2, n =104, 92	Screening 3, n=92 and 58	Day 1, n=58 and 58
Positive Nasal Culture for S. Aureus	135	89	74	53
Positive Pharyngeal Culture for S. Aureus	150	0	0	37

Intervention	number of pathogens eradicated (Number)
	All pathogens, n=93	Staphylococcus aureus (SA), n=44	Methicillin-resistant SA, n=3	Methicillin-susceptible SA, n=41	Mupirocin-susceptible SA, n=44	Fuscidic acid-resistant SA, n=2	Fuscidic acid-susceptible SA, n=42	Streptococcus pyogenes, n=9	Other Gram (+) pathogens, n=11	Gram (-) pathogens, n=29
Retapamulin Ointment, 1%	79	40	3	37	40	2	38	9	9	21

Intervention	participants (Number)
	Impetigo, ≥2 months to ≤6 months, n=11	Impetigo, >6 months to ≤12 months, n=18	Impetigo, >12 months to ≤24 months, n=18	SID, ≥2 months to ≤6 months, n=17	SID, >6 months to ≤12 months, n=9	SID, >12 months to ≤24 months, n=4	SITL, ≥2 months to ≤6 months, n=1	SITL, >6 months to ≤12 months, n=2	SITL, >12 months to ≤24 months, n=6
Retapamulin Ointment, 1%	10	17	17	11	7	4	1	2	6

Intervention	participants (Number)
	All ages	>2 months to <=6 months, n=21	>6 months to <=12 months, n=20	>12 months to <=24 months, n=20
Retapamulin Ointment, 1%	51	15	17	19

Intervention	baseline pathogens (Number)
	Eradication	Presumed Eradication	Presumed Improvement	Persistence	Presumed Persistence
Placebo	5	49	35	13	8
Retapamulin	4	137	94	3	5

Intervention	participants (Number)
	All ages	≥2 months to ≤6 months	>6 months to ≤12 months	>12 months to ≤24 months
Retapamulin Ointment, 1%	36	17	10	9

Intervention	participants (Number)
	Microbiological Success	Microbiological Failure
Placebo	54	30
Retapamulin	139	43

Intervention	participants (Number)
	Clinical Success	Clinical Improvement	Clinical Failure	Unable to Determine
Placebo	52	45	14	2
Retapamulin	130	102	11	3

Intervention	participants (Number)
	S. aureus (MRSA)	S. aureus (MSSA)	S. pyogenes
All Participants at Day 1	13	16	0
Participants With a Positive Culture at Day 1	3	5	0

Intervention	participants (Number)
	clinical cure total	clinical cure improved	failure - confirmed and default
Participants With a Positive Culture at Day 1	12	15	2

Intervention	units on a scale (Median)
	erythema	crusting	necrosis	inflammation	swelling	infection	peeling	contact dermatitis	iritation	itchiness	burning	tenderness	pain
All Participants	1.00	0.00	0.00	0.00	0.00	0.00	0.00	0.00	0.00	0.00	0.00	0.00	0.00

Intervention	units on a scale (Median)
	SIRS at Day 1	SIRS at Day 7
Participants With Positive Culture at Day 1	10.0	1.0

Intervention	participants (Number)
	1. Clinical success	2. Clinical improvement	3. No change	4. Clinical failure	5. Unable to determine
Retapamulin Ointment 1%	23	11	0	1	0

Intervention	participants (Number)
	1. Microbiological eradication	2. Presumed microbiological eradication	3. Presumed microbiological improvement	4. Microbiological persistence	5. Presumed microbiological persistence	6. Unable to determine	7. New pathogen	8. Colonization
Retapamulin Ointment 1%	1	23	10	1	0	0	0	0

Intervention	percentage of participants (Number)
Ozenoxacin 1% Cream	34.8
Ozenoxacin Placebo	19.2
Retapamulin 1% Ointment	37.7

retapamulin

Description

Cross-References

Synonyms (53)

Research Excerpts

Overview

Effects

Toxicity

Bioavailability

Dosage Studied

Drug Classes (3)

Bioassays (133)

Research

Studies (81)

Market Indicators

Research Demand Index: 49.30

Study Types

Clinical Trials (18)

Trial Overview

Trial Outcomes

Percentage of Participants With Eradication of S. Aureus Nasal Carriage at Day 12 Who Were Categorized as Persistent Carriers of S. Aureus

Percentage of Participants With Eradication of S. Aureus Nasal Carriage at Each Post Treatment Visit Stratified by Pharyngeal Carriage Status

Plasma Retapumulin Pharmacokinetic Parameters by Treatment at Day 5

Plasma Retapumulin Pharmacokinetic Parameters by Treatment at Day 5 Evaluated by Plasma AUC After Dosing

Plasma Retapumulin Pharmacokinetic Parameters by Treatment at Day 5 Evaluated by Plasma Cmax After Dosing

Number of Participants With a Nasal Culture Negative for MRSA (Methicillin-resistant S. Aureus)

Percentage of Participants With Eradication of S. Aureus Nasal Carriage at Days 7 and 33 Who Were Categorized as Persistent Carriers of S. Aureus

Percentage of Participants With Nasal Recolonization With S. Aureus on Study Days 12 and 33 Who Were Persistant Carriers Who Tested Positive in the Pharyngeal Region on Days 12 and 33 But Negative in the Nasal Region on Day 7 or Days 7 and 12

Percentage of Participants With Nasal Recolonization With S. Aureus on Study Days 12 and 33 Who Were Persistant Carriers Who Tested Positive in the Pharyngeal Region on Days 12 and 33 But Negative in the Nasal Region on Day 7 or Days 7 and 12

Plasma Retapumulin Pharmacokinetic Parameters by Treatment at Days 1 and 3 Evaluated by Plasma AUC After Dosing

Plasma Retapumulin Pharmacokinetic Parameters by Treatment at Days 1 and 3 Evaluated by Plasma Cmax After Dosing

Plasma Retapumulin Pharmacokinetic Parameters, Tmax, by Treatment at Days 1 and 3

Prevalence of S. Aureus Nasal and Pharyngeal Carriage by Visit.

Bacteriological Success Rate at Follow-up, by Baseline Pathogen

Number of Participants With Clinical Success at Follow-up, by Type of Skin Infection and by Age

Number of Participants by Age With Therapeutic Response of Success

Number of Participants With Measurable Plasma Concentrations, by Age Group

Number of Baseline Pathogens With the Indicated Microbiological Outcome at End of Therapy (2-4 Days Post Therapy)

Number of Participants With Clinical Success and Failure at Follow-up (7-9 Days Post Therapy) for the Intent-to-Treat Bacteriology (ITTB) Subset of the Primary Efficacy Population

Number of Participants With Clinical Success and Failure at Follow-up (7-9 Days Post Therapy) for the Primary Efficacy Population

Number of Participants With Microbiological Success and Failure at Follow-up (7-9 Days Post Therapy)

Number of Participants With the Indicated Clinical Outcome at End of Therapy (2-4 Days Post Therapy)

Number of Participants With Therapeutic Success and Failure at Follow-up (7-9 Days Post Therapy)

Bacteriological Culture

Investigator Assessment of Clinical Cure

Local Tolerability

Skin Infection Rating Scale (SIRS)

Number of Participants Whose Wound Cultures Were Positive for MRSA and Who Were Determined to be a Clinical Success at the Follow-up Visit

Wound Size at Baseline

Wound Size at Follow up

Clinical Response at Follow up as Assessed by a Rating Scale

Crusting (Sign and Symptom of Infection) at Baseline

Crusting (Sign and Symptom of Infection) at Follow up

Erythema (Sign and Symptom of Infection) at Baseline

Erythema (Sign and Symptom of Infection) at Follow up

Microbiologic Response at Follow up as Assessed by a Rating Scale

Pain (Sign and Symptom of Infection) at Baseline

Pain (Sign and Symptom of Infection) at Follow up

Purulence (Sign and Symptom of Infection) at Baseline

Purulence (Sign and Symptom of Infection) at Follow up

Tissue Edema (Sign and Symptom of Infection) at Baseline

Tissue Warmth (Sign and Symptom of Infection) at Baseline

Tissue Warmth (Sign and Symptom of Infection) at Follow up

Number of Participants Reporting Any Adverse Event (AE)

Tissue Edema (Sign and Symptom of Infection) at Follow up

Number of Participants Who Were a Therapeutic Success

Clinical Success

Proportion of Participants With MRSA Clearance

Number of Participants With PGA of 0 or 1

Number of Participants With PGA of 0 or 1

Staph Aureus Culture Results

Staph Aureus Culture Results

Number of Partcipants With MRSA Carriage at 4 Weeks Post Decolonization With Retapamulin or Placebo

Number of Participants With MRSA Carriage at 1 Week Post Decolonization With Retapamulin or Placebo

Related Drugs (56)

Related Conditions (47)

Substance	Relationship Strength	Studies	Trials	Classes	Roles
phosphorylcholine Phosphorylcholine: Calcium and magnesium salts used therapeutically in hepatobiliary dysfunction.. phosphocholine : The phosphate of choline; and the parent compound of the phosphocholine family.	2.17	1	0	phosphocholines	allergen; epitope; hapten; human metabolite; mouse metabolite
taurine [no description available]	2.07	1	0	amino sulfonic acid; zwitterion	antioxidant; Escherichia coli metabolite; glycine receptor agonist; human metabolite; mouse metabolite; nutrient; radical scavenger; Saccharomyces cerevisiae metabolite
ciprofloxacin Ciprofloxacin: A broad-spectrum antimicrobial carboxyfluoroquinoline.. ciprofloxacin : A quinolone that is quinolin-4(1H)-one bearing cyclopropyl, carboxylic acid, fluoro and piperazin-1-yl substituents at positions 1, 3, 6 and 7, respectively.	2.75	3	0	aminoquinoline; cyclopropanes; fluoroquinolone antibiotic; N-arylpiperazine; quinolinemonocarboxylic acid; quinolone antibiotic; quinolone; zwitterion	antibacterial drug; antiinfective agent; antimicrobial agent; DNA synthesis inhibitor; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor; environmental contaminant; topoisomerase IV inhibitor; xenobiotic
cyproheptadine Cyproheptadine: A serotonin antagonist and a histamine H1 blocker used as antipruritic, appetite stimulant, antiallergic, and for the post-gastrectomy dumping syndrome, etc.. cyproheptadine : The product resulting from the formal oxidative coupling of position 5 of 5H-dibenzo[a,d]cycloheptene with position 4 of 1-methylpiperidine resulting in the formation of a double bond between the two fragments. It is a sedating antihistamine with antimuscarinic and calcium-channel blocking actions. It is used (particularly as the hydrochloride sesquihydrate) for the relief of allergic conditions including rhinitis, conjunctivitis due to inhalant allergens and foods, urticaria and angioedema, and in pruritic skin disorders. Unlike other antihistamines, it is also a seratonin receptor antagonist, making it useful in conditions such as vascular headache and anorexia.	2.17	1	0	piperidines; tertiary amine	anti-allergic agent; antipruritic drug; gastrointestinal drug; H1-receptor antagonist; serotonergic antagonist
gentamicin Gentamicins: A complex of closely related aminoglycosides obtained from MICROMONOSPORA purpurea and related species. They are broad-spectrum antibiotics, but may cause ear and kidney damage. They act to inhibit PROTEIN BIOSYNTHESIS.	3.19	1	0
miltefosine miltefosine: hexadecyl phosphocholine derivative of cisplatin; did not substantially activate HIV long terminal repeat; less toxic than cisplatin. miltefosine : A phospholipid that is the hexadecyl monoester of phosphocholine.	2.17	1	0	phosphocholines; phospholipid	anti-inflammatory agent; anticoronaviral agent; antifungal agent; antineoplastic agent; antiprotozoal drug; apoptosis inducer; immunomodulator; protein kinase inhibitor
ketoconazole 1-acetyl-4-(4-{[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazine : A dioxolane that is 1,3-dioxolane which is substituted at positions 2, 2, and 4 by imidazol-1-ylmethyl, 2,4-dichlorophenyl, and [para-(4-acetylpiperazin-1-yl)phenoxy]methyl groups, respectively.	2.06	1	0	dichlorobenzene; dioxolane; ether; imidazoles; N-acylpiperazine; N-arylpiperazine
trimethoprim Trimethoprim: A pyrimidine inhibitor of dihydrofolate reductase, it is an antibacterial related to PYRIMETHAMINE. It is potentiated by SULFONAMIDES and the TRIMETHOPRIM, SULFAMETHOXAZOLE DRUG COMBINATION is the form most often used. It is sometimes used alone as an antimalarial. TRIMETHOPRIM RESISTANCE has been reported.. trimethoprim : An aminopyrimidine antibiotic whose structure consists of pyrimidine 2,4-diamine and 1,2,3-trimethoxybenzene moieties linked by a methylene bridge.	2.04	1	0	aminopyrimidine; methoxybenzenes	antibacterial drug; diuretic; drug allergen; EC 1.5.1.3 (dihydrofolate reductase) inhibitor; environmental contaminant; xenobiotic
chloramphenicol Amphenicol: Chloramphenicol and its derivatives.	2.73	3	0	C-nitro compound; carboxamide; diol; organochlorine compound	antibacterial drug; antimicrobial agent; Escherichia coli metabolite; geroprotector; Mycoplasma genitalium metabolite; protein synthesis inhibitor
uridine [no description available]	2.03	1	0	uridines	drug metabolite; fundamental metabolite; human metabolite
carbostyril Quinolones: A group of derivatives of naphthyridine carboxylic acid, quinoline carboxylic acid, or NALIDIXIC ACID.. quinolin-2(1H)-one : A quinolone that is 1,2-dihydroquinoline substituted by an oxo group at position 2.	5.34	3	1	monohydroxyquinoline; quinolone	bacterial xenobiotic metabolite
cloxacillin Cloxacillin: A semi-synthetic antibiotic that is a chlorinated derivative of OXACILLIN.. cloxacillin : A semisynthetic penicillin antibiotic carrying a 3-(2-chlorophenyl)-5-methylisoxazole-4-carboxamido group at position 6.	3.19	1	0	penicillin allergen; penicillin; semisynthetic derivative	antibacterial agent; antibacterial drug
oxacillin Oxacillin: An antibiotic similar to FLUCLOXACILLIN used in resistant staphylococci infections.. oxacillin : A penicillin antibiotic carrying a 5-methyl-3-phenylisoxazole-4-carboxamide group at position 6beta.	2.04	1	0	penicillin	antibacterial agent; antibacterial drug
alpha-aminopyridine alpha-aminopyridine: RN given refers to parent cpd; structure in Merck Index, 9th ed, #485. aminopyridine : Compounds containing a pyridine skeleton substituted by one or more amine groups.	5.34	3	1
erythromycin Erythromycin: A bacteriostatic antibiotic macrolide produced by Streptomyces erythreus. Erythromycin A is considered its major active component. In sensitive organisms, it inhibits protein synthesis by binding to 50S ribosomal subunits. This binding process inhibits peptidyl transferase activity and interferes with translocation of amino acids during translation and assembly of proteins.. erythromycin : Any of several wide-spectrum macrolide antibiotics obtained from actinomycete Saccharopolyspora erythraea (formerly known as Streptomyces erythraeus).. erythromycin A : An erythromycin that consists of erythronolide A having 2,6-dideoxy-3-C-methyl-3-O-methyl-alpha-L-ribo-hexopyranosyl and 3,4,6-trideoxy-3-(dimethylamino)-beta-D-xylo-hexopyranosyl residues attahced at positions 4 and 6 respectively.	9.43	6	0	cyclic ketone; erythromycin
vancomycin Vancomycin: Antibacterial obtained from Streptomyces orientalis. It is a glycopeptide related to RISTOCETIN that inhibits bacterial cell wall assembly and is toxic to kidneys and the inner ear.. vancomycin : A complex glycopeptide from Streptomyces orientalis. It inhibits a specific step in the synthesis of the peptidoglycan layer in the Gram-positive bacteria Staphylococcus aureus and Clostridium difficile.	8.16	5	0	glycopeptide	antibacterial drug; antimicrobial agent; bacterial metabolite
dicloxacillin Dicloxacillin: One of the PENICILLINS which is resistant to PENICILLINASE.. dicloxacillin : A penicillin that is 6-aminopenicillanic acid in which one of the amino hydrogens is replaced by a 3-(2,6-dichlorophenyl)-5-methyl-1,2-oxazol-4-yl]formyl group.	3.19	1	0	dichlorobenzene; penicillin	antibacterial drug
cephalexin Cephalexin: A semisynthetic cephalosporin antibiotic with antimicrobial activity similar to that of CEPHALORIDINE or CEPHALOTHIN, but somewhat less potent. It is effective against both gram-positive and gram-negative organisms.. cephalexin : A semisynthetic first-generation cephalosporin antibiotic having methyl and beta-(2R)-2-amino-2-phenylacetamido groups at the 3- and 7- of the cephem skeleton, respectively. It is effective against both Gram-negative and Gram-positive organisms, and is used for treatment of infections of the skin, respiratory tract and urinary tract.	9.94	2	1	beta-lactam antibiotic allergen; cephalosporin; semisynthetic derivative	antibacterial drug
amoxicillin Amoxicillin: A broad-spectrum semisynthetic antibiotic similar to AMPICILLIN except that its resistance to gastric acid permits higher serum levels with oral administration.. amoxicillin : A penicillin in which the substituent at position 6 of the penam ring is a 2-amino-2-(4-hydroxyphenyl)acetamido group.	2.07	1	0	penicillin allergen; penicillin	antibacterial drug
potassium phosphate potassium phosphate: used in dental materials and to treat hypophosphatemia; RN given refers to cpd with unspecified MF. tripotassium phosphate : An inorganic potassium salt that is the tripotassium salt of phosphoric acid.	2.1	1	0	inorganic phosphate salt; inorganic potassium salt
oxazolidin-2-one Oxazolidinones: Derivatives of oxazolidin-2-one. They represent an important class of synthetic antibiotic agents.. oxazolidin-2-one : An oxazolidinone that is 1,3-oxazolidine with an oxo substituent at position 2.. oxazolidinone : An oxazolidine containing one or more oxo groups.	3.01	4	0	carbamate ester; oxazolidinone	metabolite
clarithromycin Clarithromycin: A semisynthetic macrolide antibiotic derived from ERYTHROMYCIN that is active against a variety of microorganisms. It can inhibit PROTEIN SYNTHESIS in BACTERIA by reversibly binding to the 50S ribosomal subunits. This inhibits the translocation of aminoacyl transfer-RNA and prevents peptide chain elongation.. clarithromycin : The 6-O-methyl ether of erythromycin A, clarithromycin is a macrolide antibiotic used in the treatment of respiratory-tract, skin and soft-tissue infections. It is also used to eradicate Helicobacter pylori in the treatment of peptic ulcer disease. It prevents bacteria from growing by interfering with their protein synthesis.	2.17	1	0	macrolide antibiotic	antibacterial drug; environmental contaminant; protein synthesis inhibitor; xenobiotic
abiraterone [no description available]	2.17	1	0	3beta-hydroxy-Delta(5)-steroid; 3beta-sterol; pyridines	antineoplastic agent; EC 1.14.99.9 (steroid 17alpha-monooxygenase) inhibitor
levofloxacin Levofloxacin: The L-isomer of Ofloxacin.. levofloxacin : An optically active form of ofloxacin having (S)-configuration; an inhibitor of bacterial topoisomerase IV and DNA gyrase.	2.44	2	0	9-fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid; fluoroquinolone antibiotic; quinolone antibiotic	antibacterial drug; DNA synthesis inhibitor; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor; topoisomerase IV inhibitor
cilengitide Cilengitide: an alphaVbeta3 integrin antagonist that paralyzes cancer cells	2.15	1	0	oligopeptide
trimethoprim, sulfamethoxazole drug combination Trimethoprim, Sulfamethoxazole Drug Combination: A drug combination with broad-spectrum antibacterial activity against both gram-positive and gram-negative organisms. It is effective in the treatment of many infections, including PNEUMOCYSTIS PNEUMONIA in AIDS.. co-trimoxazole : A two-component mixture comprising trimethoprim and sulfamethoxazole.	2.08	1	0
puromycin [no description available]	2.03	1	0	puromycins	antiinfective agent; antimicrobial agent; antineoplastic agent; EC 3.4.11.14 (cytosol alanyl aminopeptidase) inhibitor; EC 3.4.14.2 (dipeptidyl-peptidase II) inhibitor; nucleoside antibiotic; protein synthesis inhibitor
linezolid [no description available]	6.17	11	1	acetamides; morpholines; organofluorine compound; oxazolidinone	antibacterial drug; protein synthesis inhibitor
valnemulin valnemulin: a pleuromutilin derivative	4.95	4	0	carbotricyclic compound; carboxylic ester; cyclic ketone
mupirocin Mupirocin: A topically used antibiotic from a strain of Pseudomonas fluorescens. It has shown excellent activity against gram-positive staphylococci and streptococci. The antibiotic is used primarily for the treatment of primary and secondary skin disorders, nasal infections, and wound healing.. mupirocin : An alpha,beta-unsaturated ester resulting from the formal condensation of the alcoholic hydroxy group of 9-hydroxynonanoic acid with the carboxy group of (2E)-4-[(2S)-tetrahydro-2H-pyran-2-yl]-3-methylbut-2-enoic acid in which the tetrahydropyranyl ring is substituted at positions 3 and 4 by hydroxy groups and at position 5 by a {(2S,3S)-3-[(2S,3S)-3-hydroxybutan-2-yl]oxiran-2-yl}methyl group. Originally isolated from the Gram-negative bacterium Pseudomonas fluorescens, it is used as a topical antibiotic for the treatment of Gram-positive bacterial infections.	6.17	23	0	alpha,beta-unsaturated carboxylic ester; epoxide; monocarboxylic acid; oxanes; secondary alcohol; triol	antibacterial drug; bacterial metabolite; protein synthesis inhibitor
clindamycin Clindamycin: An antibacterial agent that is a semisynthetic analog of LINCOMYCIN.. clindamycin : A carbohydrate-containing antibiotic that is the semisynthetic derivative of lincomycin, a natural antibiotic.	4.26	5	0
zithromax Azithromycin: A semi-synthetic macrolide antibiotic structurally related to ERYTHROMYCIN. It has been used in the treatment of Mycobacterium avium intracellulare infections, toxoplasmosis, and cryptosporidiosis.. azithromycin : A macrolide antibiotic useful for the treatment of bacterial infections.	2.17	1	0	macrolide antibiotic	antibacterial drug; environmental contaminant; xenobiotic
u 100480 U 100480: structure given in first source	2.17	1	0
s 1033 [no description available]	2.17	1	0	(trifluoromethyl)benzenes; imidazoles; pyridines; pyrimidines; secondary amino compound; secondary carboxamide	anticoronaviral agent; antineoplastic agent; tyrosine kinase inhibitor
tiamulin tiamulin: 81723 HFU and tiamutin are for fumarate salt; prevents senescence in ascomycete; pleuromutilin derivative; RN given refers to ((3aS-(3aalpha,4beta,5alpha,6alpha,8beta,9alpha,9abeta,10S*))-isomer. tiamulin : A carbotricyclic compound that is pleuromutilin in which the hydroxyacetate group is replaced by a 2-{[2-(diethylamino)ethyl]sulfanyl}acetate group. An antibacterial drug, tiamulin is used in veterinary medicine (generally as its hydrogen fumarate salt) for the treatment of swine dysentery caused by Serpulina hyodysenteriae.	5.31	9	0	carbotricyclic compound; carboxylic ester; cyclic ketone; organic sulfide; secondary alcohol; semisynthetic derivative; tertiary amino compound; tetracyclic diterpenoid	antibacterial drug
fusidic acid Fusidic Acid: An antibiotic isolated from the fermentation broth of Fusidium coccineum. (From Merck Index, 11th ed). It acts by inhibiting translocation during protein synthesis.. fusidic acid : A steroid antibiotic that is isolated from the fermentation broth of Fusidium coccineum.	6.7	9	1	11alpha-hydroxy steroid; 3alpha-hydroxy steroid; alpha,beta-unsaturated monocarboxylic acid; steroid acid; steroid antibiotic; sterol ester	EC 2.7.1.33 (pantothenate kinase) inhibitor; Escherichia coli metabolite; protein synthesis inhibitor
lincomycin Lincomycin: An antibiotic produced by Streptomyces lincolnensis var. lincolnensis. It has been used in the treatment of staphylococcal, streptococcal, and Bacteroides fragilis infections.. lincomycin : A carbohydrate-containing antibiotic produced by the actinomyces Streptomyces lincolnensis.	2.04	1	0	carbohydrate-containing antibiotic; L-proline derivative; monocarboxylic acid amide; pyrrolidinecarboxamide; S-glycosyl compound	antimicrobial agent; bacterial metabolite
ganglioside, gd2 [no description available]	2.15	1	0
chlorhexidine Chlorhexidine: A disinfectant and topical anti-infective agent used also as mouthwash to prevent oral plaque.. chlorhexidine : A bisbiguanide compound with a structure consisting of two (p-chlorophenyl)guanide units linked by a hexamethylene bridge.	7.1	1	0	biguanides; monochlorobenzenes	antibacterial agent; antiinfective agent
amoxicillin-potassium clavulanate combination Amoxicillin-Potassium Clavulanate Combination: A fixed-ratio combination of amoxicillin trihydrate and potassium clavulanate.	3.19	1	0
valnemulin [no description available]	3.27	5	0
ozenoxacin ozenoxacin: an antibacterial for treatment of impetigo; structure in first source	10.34	3	1	quinolines
pleuromutilin [no description available]	2.58	2	0
gentamicin sulfate [no description available]	2.04	1	0
nvc-422 NVC-422: structure in first source	2.07	1	0
virginiamycin Virginiamycin: A cyclic polypeptide antibiotic complex from Streptomyces virginiae, S. loidensis, S. mitakaensis, S. pristina-spiralis, S. ostreogriseus, and others. It consists of 2 major components, VIRGINIAMYCIN FACTOR M1 and virginiamycin Factor S1. It is used to treat infections with gram-positive organisms and as a growth promoter in cattle, swine, and poultry.. virginiamycin : A mixture of cyclic polypeptide streptogramin antibiotics produced by Streptomyces virginiae, S. loidensis, S. mitakaensis, S. pristina-spiralis, S. ostreogriseus, and others. The two major components are virginiamycin M1 (also known as pristinamycin IIA) and virginiamycin S1. Virginiamycin has been widely used as a growth promotion agent in livestock and has been to have bacteriostatic activity against Gram-positive organisms such as staphylococci and streptococci.	2.25	1	0
quinupristin quinupristin: component of RP 59500; structure in first source	7.25	1	0	cyclodepsipeptide
quinupristin-dalfopristin quinupristin-dalfopristin: RP 59500 is a combination of RP 57669 & RP 54476, which are water soluble derivatives of pristinamycin IA & pristinamycin IIB, respectively	2.25	1	0	organic molecular entity
n-(4-cyanophenylmethyl)-4-(2-diphenyl)-1-piperazinehexanamide N-(4-cyanophenylmethyl)-4-(2-diphenyl)-1-piperazinehexanamide: a 5-HT(7) receptor agonist	2.15	1	0
bc-3781 [no description available]	3.91	3	0
tetracycline Tetracycline: A naphthacene antibiotic that inhibits AMINO ACYL TRNA binding during protein synthesis.. tetracycline : A broad-spectrum polyketide antibiotic produced by the Streptomyces genus of actinobacteria.	2.96	4	0
minocycline Minocycline: A TETRACYCLINE analog, having a 7-dimethylamino and lacking the 5 methyl and hydroxyl groups, which is effective against tetracycline-resistant STAPHYLOCOCCUS infections.. minocycline : A tetracycline analogue having a dimethylamino group at position 7 and lacking the methyl and hydroxy groups at position 5.	2.21	1	0
daptomycin [no description available]	7.48	2	0
dalfopristin dalfopristin: component of RP-59500; structure in first source. dalfopristin : A macrolide that is pristinamycin IIA in which the double bond between positions 26 and 26a of the pyrroline ring has been reduced and position 26R carries a [2-(diethylamino)ethyl]sulfonyl group. It is a semi-synthetic streptogramin antibiotic and often used as a mixture with quinupristin for the treatment of vancomycin-resistant Enterococcus faecium.	2.25	1	0
mutilin mutilin: structure in first source	3.14	1	0
rifampin Rifampin: A semisynthetic antibiotic produced from Streptomyces mediterranei. It has a broad antibacterial spectrum, including activity against several forms of Mycobacterium. In susceptible organisms it inhibits DNA-dependent RNA polymerase activity by forming a stable complex with the enzyme. It thus suppresses the initiation of RNA synthesis. Rifampin is bactericidal, and acts on both intracellular and extracellular organisms. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1160)	2.04	1	0	cyclic ketal; hydrazone; N-iminopiperazine; N-methylpiperazine; rifamycins; semisynthetic derivative; zwitterion	angiogenesis inhibitor; antiamoebic agent; antineoplastic agent; antitubercular agent; DNA synthesis inhibitor; EC 2.7.7.6 (RNA polymerase) inhibitor; Escherichia coli metabolite; geroprotector; leprostatic drug; neuroprotective agent; pregnane X receptor agonist; protein synthesis inhibitor

Condition	Relationship Strength	Studies	Trials
Infections, Staphylococcal [description not available]	3.78	10	0
Staphylococcal Infections Infections with bacteria of the genus STAPHYLOCOCCUS.	3.78	10	0
Bacterial Skin Diseases [description not available]	4.99	6	0
Infections, Staphylococcal Skin [description not available]	9.47	14	5
Staphylococcal Skin Infections Infections to the skin caused by bacteria of the genus STAPHYLOCOCCUS.	9.47	14	5
Skin Diseases, Bacterial Skin diseases caused by bacteria.	4.99	6	0
Bancroftian Elephantiasis [description not available]	2.21	1	0
Elephantiasis, Filarial Parasitic infestation of the human lymphatic system by WUCHERERIA BANCROFTI or BRUGIA MALAYI. It is also called lymphatic filariasis.	2.21	1	0
Onchocerciasis Infection with nematodes of the genus ONCHOCERCA. Characteristics include the presence of firm subcutaneous nodules filled with adult worms, PRURITUS, and ocular lesions.	2.21	1	0
Congenital Zika Syndrome [description not available]	2.25	1	0
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	3.23	5	0
Zika Virus Infection A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.	2.25	1	0
Bacterial Infections, Gram-Positive [description not available]	3.68	3	0
Gram-Positive Bacterial Infections Infections caused by bacteria that retain the crystal violet stain (positive) when treated by the gram-staining method.	3.68	3	0
Impetigo Contagiosa [description not available]	9.54	15	5
Impetigo A common superficial bacterial infection caused by STAPHYLOCOCCUS AUREUS or group A beta-hemolytic streptococci. Characteristics include pustular lesions that rupture and discharge a thin, amber-colored fluid that dries and forms a crust. This condition is commonly located on the face, especially about the mouth and nose.	9.54	15	5
Community Acquired Infection [description not available]	3	4	0
Neuroblastoma A common neoplasm of early childhood arising from neural crest cells in the sympathetic nervous system, and characterized by diverse clinical behavior, ranging from spontaneous remission to rapid metastatic progression and death. This tumor is the most common intraabdominal malignancy of childhood, but it may also arise from thorax, neck, or rarely occur in the central nervous system. Histologic features include uniform round cells with hyperchromatic nuclei arranged in nests and separated by fibrovascular septa. Neuroblastomas may be associated with the opsoclonus-myoclonus syndrome. (From DeVita et al., Cancer: Principles and Practice of Oncology, 5th ed, pp2099-2101; Curr Opin Oncol 1998 Jan;10(1):43-51)	2.15	1	0
Pythiosis A granulomatous disease caused by the aquatic organism PYTHIUM insidiosum and occurring primarily in horses, cattle, dogs, cats, fishes, and rarely in humans. It is classified into three forms: ocular, cutaneous, and arterial.	2.17	1	0
Acute Confusional Senile Dementia [description not available]	2.17	1	0
Alzheimer Disease A degenerative disease of the BRAIN characterized by the insidious onset of DEMENTIA. Impairment of MEMORY, judgment, attention span, and problem solving skills are followed by severe APRAXIAS and a global loss of cognitive abilities. The condition primarily occurs after age 60, and is marked pathologically by severe cortical atrophy and the triad of SENILE PLAQUES; NEUROFIBRILLARY TANGLES; and NEUROPIL THREADS. (From Adams et al., Principles of Neurology, 6th ed, pp1049-57)	2.17	1	0
Infection, Wound [description not available]	2.78	3	0
Group A Strep Infection [description not available]	6.79	5	2
Streptococcal Infections Infections with bacteria of the genus STREPTOCOCCUS.	6.79	5	2
Sensitivity and Specificity Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)	2.1	1	0
Infections, Soft Tissue [description not available]	2.49	2	0
Soft Tissue Infections Infections of non-skeletal tissue, i.e., exclusive of bone, ligaments, cartilage, and fibrous tissue. The concept is usually referred to as skin and soft tissue infections and usually subcutaneous and muscle tissue are involved. The predisposing factors in anaerobic infections are trauma, ischemia, and surgery. The organisms often derive from the fecal or oral flora, particularly in wounds associated with intestinal surgery, decubitus ulcer, and human bites. (From Cecil Textbook of Medicine, 19th ed, p1688)	7.49	2	0
Infection, Postoperative Wound [description not available]	2.46	2	0
Injuries Used with anatomic headings, animals, and sports for wounds and injuries. Excludes cell damage, for which pathology is used.	4.4	1	1
Wounds and Injuries Damage inflicted on the body as the direct or indirect result of an external force, with or without disruption of structural continuity.	4.4	1	1
Infectious Skin Diseases [description not available]	6.62	6	2
Skin Diseases, Infectious Skin diseases caused by bacteria, fungi, parasites, or viruses.	6.62	6	2
Allergic Contact Dermatitis [description not available]	2.05	1	0
Facial Dermatoses Skin diseases involving the FACE.	2.05	1	0
Dermatitis, Allergic Contact A contact dermatitis due to allergic sensitization to various substances. These substances subsequently produce inflammatory reactions in the skin of those who have acquired hypersensitivity to them as a result of prior exposure.	2.05	1	0
Eczema, Atopic [description not available]	5.6	3	2
Dermatitis, Atopic A chronic inflammatory genetically determined disease of the skin marked by increased ability to form reagin (IgE), with increased susceptibility to allergic rhinitis and asthma, and hereditary disposition to a lowered threshold for pruritus. It is manifested by lichenification, excoriation, and crusting, mainly on the flexural surfaces of the elbow and knee. In infants it is known as infantile eczema.	5.6	3	2
Dermatitis Any inflammation of the skin.	8.83	2	1
Aspergillus Infection [description not available]	2.06	1	0
Carcinoma, Epidermoid [description not available]	2.06	1	0
Dermatomycoses Superficial infections of the skin or its appendages by any of various fungi.	2.06	1	0
Cancer of Head [description not available]	2.06	1	0
Aspergillosis Infections with fungi of the genus ASPERGILLUS.	2.06	1	0
Carcinoma, Squamous Cell A carcinoma derived from stratified SQUAMOUS EPITHELIAL CELLS. It may also occur in sites where glandular or columnar epithelium is normally present. (From Stedman, 25th ed)	2.06	1	0
Head and Neck Neoplasms Soft tissue tumors or cancer arising from the mucosal surfaces of the LIP; oral cavity; PHARYNX; LARYNX; and cervical esophagus. Other sites included are the NOSE and PARANASAL SINUSES; SALIVARY GLANDS; THYROID GLAND and PARATHYROID GLANDS; and MELANOMA and non-melanoma skin cancers of the head and neck. (from Holland et al., Cancer Medicine, 4th ed, p1651)	2.06	1	0
Diabetes Mellitus, Adult-Onset [description not available]	2.08	1	0
Diabetes Mellitus, Type 2 A subclass of DIABETES MELLITUS that is not INSULIN-responsive or dependent (NIDDM). It is characterized initially by INSULIN RESISTANCE and HYPERINSULINEMIA; and eventually by GLUCOSE INTOLERANCE; HYPERGLYCEMIA; and overt diabetes. Type II diabetes mellitus is no longer considered a disease exclusively found in adults. Patients seldom develop KETOSIS but often exhibit OBESITY.	2.08	1	0