Page last updated: 2024-11-13

tildipirosin

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

Description

20,23-dipiperidinyl-mycaminosyl-tylonolide: a veterinary antibiotic [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID24860548
CHEMBL ID3039509
SCHEMBL ID20204354
MeSH IDM0578946

Synonyms (39)

Synonym
CHEMBL3039509
s795at66jb ,
tildipirosin
tildipirosin [usan:inn]
(4r,5s,6s,7r,9r,11e,13e,15r,16r-6-((3,6-dideoxy-3-(dimethylamino)-beta-d-glucopyranosyl)oxy)-16-ethyl-4-hydroxy-5,9,13-trimethyl-7-(2-(piperidin-1-yl)ethyl)-15-((piperidin-1-yl)methyl)oxacyclohexadeca-11,13-diene-2,10-dione
328898-40-4
zuprevo
unii-s795at66jb
D10492
zuprevo [veterinary] (tn)
tildipirosin (usan/inn)
tildipirosin [ema epar veterinary]
tildipirosin [usan]
tildipirosin [inn]
zuprevo component tildipirosin
tylonolide, 20-deoxo-23-deoxy-5-o-(3,6-dideoxy-3-(dimethylamino)-.beta.-d- glucopyranosyl)-20,23-di-1-piperidinyl-
tildipirosin component of zuprevo
tildipirosin [mi]
tildipirosin [green book]
S6423
HY-A0071
CS-3296
AC-32492
(4r,5s,6s,7r,9r,11e,13e,15r,16r)-6-[(2r,3r,4s,5s,6r)-4-(dimethylamino)-3,5-dihydroxy-6-methyloxan-2-yl]oxy-16-ethyl-4-hydroxy-5,9,13-trimethyl-7-(2-piperidin-1-ylethyl)-15-(piperidin-1-ylmethyl)-1-oxacyclohexadeca-11,13-diene-2,10-dione
AKOS027338675
mfcd13194925
J-018917
SCHEMBL20204354
DB11470
AS-35167
Q16069783
DTXSID70954546
tildipirosine
tildipirosina
tildipirosin (ema epar veterinary)
tildipirosinum
zuprevo (veterinary)
tylonolide, 20-deoxo-23-deoxy-5-o-(3,6-dideoxy-3-(dimethylamino)-beta-d-glucopyranosyl)-20,23-di-1-piperidinyl-
20,23-dipiperidinyl-mycaminosyl-tylonolide

Research Excerpts

Overview

Tildipirosin (TIP) is a novel 16-membered-ring macrolide authorized for the treatment of bovine and swine respiratory disease. It is a derivative of the naturally occurring compound tylosin.

ExcerptReferenceRelevance
"Tildipirosin (TIP) is a novel 16-membered-ring macrolide authorized for the treatment of bovine and swine respiratory disease. "( A microbiological assay to estimate the antimicrobial activity of parenteral tildipirosin against foodborne pathogens and commensals in the colon of beef cattle and pigs.
Kilp, S; Menge, M; Nürnberger, M; Pridmore, A; Röpke, R; Rose, M; Shaw, A; Wilhelm, C, 2016
)
2.11
"Tildipirosin is a derivative of the naturally occurring compound tylosin."( Visualizing the 16-membered ring macrolides tildipirosin and tilmicosin bound to their ribosomal site.
Andersen, NM; Douthwaite, S; Poehlsgaard, J; Warrass, R, 2012
)
1.36
"Tildipirosin is a 16-membered-ring macrolide developed to treat bacterial pathogens, including Mannheimia haemolytica and Pasteurella multocida, that cause respiratory tract infections in cattle and swine. "( Inhibition of protein synthesis on the ribosome by tildipirosin compared with other veterinary macrolides.
Andersen, NM; Douthwaite, S; Poehlsgaard, J; Warrass, R, 2012
)
2.07

Treatment

ExcerptReferenceRelevance
"Tildipirosin-treated heifers had lower (P < 0.05) lung lesion scores when compared with DRX- and SAL-treated heifers."( Pulmonary lesions and clinical disease response to Mannheimia haemolytica challenge 10 days following administration of tildipirosin or tulathromycin.
Amrine, DE; Larson, RL; Mosier, DA; White, BJ, 2014
)
1.33

Pharmacokinetics

ExcerptReferenceRelevance
" Mean residence time from the time of dosing to the time of last measurable concentration (MRT(last)) and terminal half-life (T(1/2) ) was 6 and 9 days, respectively."( Pharmacokinetics of tildipirosin in bovine plasma, lung tissue, and bronchial fluid (from live, nonanesthetized cattle).
Allan, M; Bohland, C; Kilp, S; Menge, M; Metz, W; Nürnberger, M; Röpke, R; Rose, M; Zschiesche, E, 2012
)
0.7
" Mean residence time from the time of dosing to the time of last measurable concentration (MRTlast) and terminal half-life (T1/2) both were about 4 days."( Pharmacokinetics of tildipirosin in porcine plasma, lung tissue, and bronchial fluid and effects of test conditions on in vitro activity against reference strains and field isolates of Actinobacillus pleuropneumoniae.
Allan, M; Bohland, C; Kilp, S; Menge, M; Metz, W; Nürnberger, M; Röpke, R; Rose, M; Wilhelm, C; Zschiesche, E, 2013
)
0.71

Bioavailability

ExcerptReferenceRelevance
" Absolute bioavailability was 78."( Pharmacokinetics of tildipirosin in bovine plasma, lung tissue, and bronchial fluid (from live, nonanesthetized cattle).
Allan, M; Bohland, C; Kilp, S; Menge, M; Metz, W; Nürnberger, M; Röpke, R; Rose, M; Zschiesche, E, 2012
)
0.7

Dosage Studied

ExcerptRelevanceReference
" Mean residence time from the time of dosing to the time of last measurable concentration (MRT(last)) and terminal half-life (T(1/2) ) was 6 and 9 days, respectively."( Pharmacokinetics of tildipirosin in bovine plasma, lung tissue, and bronchial fluid (from live, nonanesthetized cattle).
Allan, M; Bohland, C; Kilp, S; Menge, M; Metz, W; Nürnberger, M; Röpke, R; Rose, M; Zschiesche, E, 2012
)
0.7
" Mean residence time from the time of dosing to the time of last measurable concentration (MRTlast) and terminal half-life (T1/2) both were about 4 days."( Pharmacokinetics of tildipirosin in porcine plasma, lung tissue, and bronchial fluid and effects of test conditions on in vitro activity against reference strains and field isolates of Actinobacillus pleuropneumoniae.
Allan, M; Bohland, C; Kilp, S; Menge, M; Metz, W; Nürnberger, M; Röpke, R; Rose, M; Wilhelm, C; Zschiesche, E, 2013
)
0.71
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (39)

Assay IDTitleYearJournalArticle
AID1873889Antibacterial activity against Staphylococcus aureus ATCC 29213 incubated for 16 to 20 hrs using 10^6 CFU/ml bacterial inoculum by broth microdilution method2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID1873880Antibacterial activity against Staphylococcus aureus ATCC 25923 infected in kunming mouse assessed as reduction in viable pathogens at 32.5 mg/kg, iv measured after 1 hr2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID1873909Antibacterial activity against Klebsiella pneumoniae ATCC 13883 incubated for 16 to 20 hrs by broth microdilution method2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID1873914Antibacterial activity against Pseudomonas aeruginosa LTP-3 incubated for 16 to 20 hrs by broth microdilution method2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID1873891Antibacterial activity against Staphylococcus aureus ATCC 29213 incubated for 16 to 20 hrs using 10^4 CFU/ml bacterial inoculum by broth microdilution method2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID1873895Antibacterial activity against Escherichia coli ATCC 25922 incubated for 16 to 20 hrs using 10^4 CFU/ml bacterial inoculum by broth microdilution method2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID1873911Antibacterial activity against Streptococcus dysgalactiae incubated for 16 to 20 hrs by broth microdilution method2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID1873916Ratio of MBC to MIC for Escherichia coli ATCC 259222022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID1873944Antibacterial activity against Staphylococcus aureus ATCC 29213 at pH 8.6 incubated for 16 to 20 hrs in absence of foetal bovine serum by broth microdilution method2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID1873888Antibacterial activity against Staphylococcus aureus ATCC 29213 incubated for 16 to 20 hrs using 10^7 CFU/ml bacterial inoculum by broth microdilution method2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID1873904Antibacterial activity against Escherichia coli ATCC 25922 incubated for 16 to 20 hrs in absence of foetal bovine serum by broth microdilution method2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID1873893Antibacterial activity against Escherichia coli ATCC 25922 incubated for 16 to 20 hrs using 10^6 CFU/ml bacterial inoculum by broth microdilution method2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID1873913Antibacterial activity against Escherichia coli incubated for 16 to 20 hrs by broth microdilution method2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID1873917Bactericidal activity against Staphylococcus aureus ATCC 29213 incubated for 20 to 24 hrs by CLSI based analysis2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID1873912Antibacterial activity against Staphylococcus chromogenes incubated for 16 to 20 hrs by broth microdilution method2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID1873943Antibacterial activity against Escherichia coli ATCC 25922 incubated for 16 to 20 hrs in presence of 50% foetal bovine serum by broth microdilution method2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID1873892Antibacterial activity against Staphylococcus aureus ATCC 29213 incubated for 16 to 20 hrs using 10^3 CFU/ml bacterial inoculum by broth microdilution method2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID1873946Antibacterial activity against Staphylococcus aureus ATCC 29213 at pH 8.6 incubated for 16 to 20 hrs in presence of 10% foetal bovine serum by broth microdilution method2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID1873947Antibacterial activity against Staphylococcus aureus ATCC 29213 at pH 8.6 incubated for 16 to 20 hrs in presence of 25% foetal bovine serum by broth microdilution method2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID1873915Bactericidal activity against Escherichia coli ATCC 25922 incubated for 20 to 24 hrs by CLSI based analysis2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID1873910Antibacterial activity against Enterococcus faecium incubated for 16 to 20 hrs by broth microdilution method2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID1873921Bactericidal activity against Escherichia coli ATCC 25922 assessed as reduction in number of viable bacteria at 4 times MIC measured after 6 hrs by time kill assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID1873896Antibacterial activity against Escherichia coli ATCC 25922 incubated for 16 to 20 hrs using 10^5 CFU/ml bacterial inoculum by broth microdilution method2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID1873894Antibacterial activity against Escherichia coli ATCC 25922 incubated for 16 to 20 hrs using 10^7 CFU/ml bacterial inoculum by broth microdilution method2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID1873885Inhibition of protein synthesis in Escherichia coli ATCC 25922 assessed as reduction in protein content at 4 mg/ml measured upto 12 hrs by microporous enzyme labeling method relative to control2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID1873886Inhibition of DNA synthesis in Escherichia coli ATCC 25922 at 4 mg/ml measured upto 12 hrs by DAPI staining based fluorescence microscopic analysis2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID1873940Antibacterial activity against Escherichia coli ATCC 25922 incubated for 16 to 20 hrs in presence of 5% foetal bovine serum by broth microdilution method2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID1873890Antibacterial activity against Staphylococcus aureus ATCC 29213 incubated for 16 to 20 hrs using 10^5 CFU/ml bacterial inoculum by broth microdilution method2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID1873945Antibacterial activity against Staphylococcus aureus ATCC 29213 at pH 8.6 incubated for 16 to 20 hrs in presence of 5% foetal bovine serum by broth microdilution method2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID1873901Antibacterial activity against Staphylococcus aureus ATCC 29213 at pH 8.6 incubated for 16 to 20 hrs in presence of 50% foetal bovine serum by broth microdilution method2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID1873906Antibacterial activity against Staphylococcus aureus ATCC 25923 incubated for 16 to 20 hrs by broth microdilution method2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID1873918Antibacterial activity against Staphylococcus aureus ATCC 29213 incubated for 16 to 20 hrs by broth microdilution method2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID1873919Ratio of MBC to MIC for Staphylococcus aureus ATCC 292132022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID1873905Antibacterial activity against Staphylococcus aureus incubated for 16 to 20 hrs by broth microdilution method2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID1873897Antibacterial activity against Escherichia coli ATCC 25922 incubated for 16 to 20 hrs using 10^3 CFU/ml bacterial inoculum by broth microdilution method2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID1873942Antibacterial activity against Escherichia coli ATCC 25922 incubated for 16 to 20 hrs in presence of 25% foetal bovine serum by broth microdilution method2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID1873941Antibacterial activity against Escherichia coli ATCC 25922 incubated for 16 to 20 hrs in presence of 10% foetal bovine serum by broth microdilution method2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID1873908Antibacterial activity against Cronobacter sakazakii ATCC 29544 incubated for 16 to 20 hrs by broth microdilution method2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
AID1873907Antibacterial activity against Escherichia coli ATCC 25922 incubated for 16 to 20 hrs by broth microdilution method2022European journal of medicinal chemistry, Aug-05, Volume: 238Design, synthesis and activity against drug-resistant bacteria evaluation of C-20, C-23 modified 5-O-mycaminosyltylonolide derivatives.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (20)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's13 (65.00)24.3611
2020's7 (35.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 41.31

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

MetricThis Compound (vs All)
Research Demand Index41.31 (24.57)
Research Supply Index3.40 (2.92)
Research Growth Index4.68 (4.65)
Search Engine Demand Index57.00 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (41.31)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials9 (45.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other11 (55.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]