Compounds > lff571
Page last updated: 2024-11-13

lff571

Description

LFF571: an antibacterial agent; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID42638236
CHEMBL ID2063705
SCHEMBL ID18391833
SCHEMBL ID18392088
MeSH IDM0575065

Synonyms (16)

Synonym
3U2Q
lff-571
CHEMBL2063705
j3.333.591a ,
lff571
unii-w7aul2r95z
lff 571
W7AUL2R95Z ,
1160959-55-6
SCHEMBL18391833
SCHEMBL18392088
DB13013
Q27292430
CS-0016947
HY-19906
AKOS040748742

Research Excerpts

Overview

LFF571 is a novel semisynthetic thiopeptide antibacterial that is undergoing investigation for safety and efficacy in patients with moderate Clostridium difficile infections. L FF571 is an exploratory agent that inhibits EF-Tu.

ExcerptReferenceRelevance
"LFF571 is an experimental agent undergoing evaluation in humans for the treatment of moderate C."( In vitro selection, via serial passage, of Clostridium difficile mutants with reduced susceptibility to fidaxomicin or vancomycin.
Barnes, SW; Leeds, JA; Mullin, S; Ruzin, A; Sachdeva, M, 2014)		1.12
"LFF571 is a novel semisynthetic thiopeptide antibacterial that is undergoing investigation for safety and efficacy in patients with moderate Clostridium difficile infections. "( Subinhibitory concentrations of LFF571 reduce toxin production by Clostridium difficile.
Leeds, JA; Sachdeva, M, 2015)		2.14
"LFF571 is a novel thiopeptide antibacterial that shows in vitro potency against C."( Pharmacokinetics of LFF571 and vancomycin in patients with moderate Clostridium difficile infections.
Bhansali, SG; Dabovic, K; Leeds, JA; Mullane, K; Pertel, P; Praestgaard, J; Ting, LS, 2015)		1.46
"LFF571 is a semisynthetic thiopeptide with potency against C."( Multicenter, randomized clinical trial to compare the safety and efficacy of LFF571 and vancomycin for Clostridium difficile infections.
Blais, J; Bressler, A; Buitrago, M; Dabovic, K; Lee, C; Leeds, JA; Mullane, K; Pertel, P; Praestgaard, J; Weiss, K, 2015)		1.37
"LFF571 is an exploratory agent that inhibits EF-Tu."( Antibacterials Developed to Target a Single Organism: Mechanisms and Frequencies of Reduced Susceptibility to the Novel Anti-Clostridium difficile Compounds Fidaxomicin and LFF571.
Leeds, JA, 2016)		1.35
"LFF571 is a novel semisynthetic thiopeptide antibiotic with potent activity against a variety of Gram-positive pathogens, including Clostridium difficile. "( Efficacy of LFF571 in a hamster model of Clostridium difficile infection.
Lamarche, MJ; Leeds, JA; McKenney, D; Praestgaard, J; Trzasko, A, 2012)		2.2
"LFF571 is a novel semisynthetic thiopeptide and potent inhibitor of Gram-positive bacteria. "( Mechanism of action of and mechanism of reduced susceptibility to the novel anti-Clostridium difficile compound LFF571.
Dzink-Fox, J; Lamarche, MJ; Leeds, JA; Mullin, S; Sachdeva, M, 2012)		2.03
"LFF571 is a novel inhibitor of the prokaryotic translation elongation factor Tu and is active against a range of bacterial species, including C."( A first-in-human, randomized, double-blind, placebo-controlled, single- and multiple-ascending oral dose study to assess the safety and tolerability of LFF571 in healthy volunteers.
Grunenberg, N; Leeds, JA; Pertel, P; Praestgaard, J; Ting, LS; Yang, JC, 2012)		1.3

Toxicity

ExcerptReferenceRelevance
" There were no deaths, no serious adverse events, and no subject withdrawals due to an adverse event."( A first-in-human, randomized, double-blind, placebo-controlled, single- and multiple-ascending oral dose study to assess the safety and tolerability of LFF571 in healthy volunteers.
Grunenberg, N; Leeds, JA; Pertel, P; Praestgaard, J; Ting, LS; Yang, JC, 2012)		0.58
" LFF571 was generally safe and well tolerated."( Multicenter, randomized clinical trial to compare the safety and efficacy of LFF571 and vancomycin for Clostridium difficile infections.
Blais, J; Bressler, A; Buitrago, M; Dabovic, K; Lee, C; Leeds, JA; Mullane, K; Pertel, P; Praestgaard, J; Weiss, K, 2015)		1.56
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (20)

Assay IDTitleYearJournalArticle
AID675929Antibacterial activity against Enterococcus faecalis NB04025 infected in CD1 mouse assessed as mouse survival up to 5 days2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Discovery of LFF571: an investigational agent for Clostridium difficile infection.
AID675939Plasma concentration in Clostridium difficile infected golden syrian hamster at 20 mg/kg, po qd administered for 5 days measured at 3 hrs post dose2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Discovery of LFF571: an investigational agent for Clostridium difficile infection.
AID675936Drug level in Clostridium difficile infected golden syrian hamster cecum at 20 mg/kg, po qd administered for 5 days measured at 1 hr post dose2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Discovery of LFF571: an investigational agent for Clostridium difficile infection.
AID675935Antibacterial activity against Clostridium difficile ATCC 43255 infected in golden syrian hamster assessed as survival rate at 20 mg/kg, po qd administered days 1 to 5 measured on days 6 to 212012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Discovery of LFF571: an investigational agent for Clostridium difficile infection.
AID675921Antibacterial activity against Enterococcus faecium 7130724 by broth microdilution method2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Discovery of LFF571: an investigational agent for Clostridium difficile infection.
AID675931Oral bioavailability in Sprague-Dawley rat2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Discovery of LFF571: an investigational agent for Clostridium difficile infection.
AID675940Antibacterial activity against Clostridium difficile ATCC 43255 infected in golden syrian hamster assessed as decrease in toxin level in cecum after 21 days by ELISA2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Discovery of LFF571: an investigational agent for Clostridium difficile infection.
AID675922Antibacterial activity against Enterococcus faecalis ATCC 29212 by broth microdilution method2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Discovery of LFF571: an investigational agent for Clostridium difficile infection.
AID675928Antibacterial activity against Staphylococcus aureus ATCC 49951 infected in CD1 mouse assessed as mouse survival up to 5 days2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Discovery of LFF571: an investigational agent for Clostridium difficile infection.
AID675924Antibacterial activity against Streptococcus pyogenes ATCC BAA-595 by broth microdilution method2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Discovery of LFF571: an investigational agent for Clostridium difficile infection.
AID675930Aqueous solubility of the compound at pH 7.4 by RP-HPLC analysis2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Discovery of LFF571: an investigational agent for Clostridium difficile infection.
AID675925Antibacterial activity against Clostridium difficile ATCC 43255 by broth microdilution method2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Discovery of LFF571: an investigational agent for Clostridium difficile infection.
AID675927Binding affinity to Escherichia coli GDPNP-labelled EF-Tu by surface plasmon resonance analysis2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Discovery of LFF571: an investigational agent for Clostridium difficile infection.
AID675938Plasma concentration in Clostridium difficile infected golden syrian hamster at 20 mg/kg, po qd administered for 5 days measured at 1 hr post dose2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Discovery of LFF571: an investigational agent for Clostridium difficile infection.
AID675934Antibacterial activity against Clostridium difficile ATCC 43255 infected in golden syrian hamster assessed as survival rate at 2 mg/kg, po qd administered days 1 to 5 measured on days 6 to 212012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Discovery of LFF571: an investigational agent for Clostridium difficile infection.
AID675933Antibacterial activity against Clostridium difficile ATCC 43255 infected in golden syrian hamster assessed as survival rate at 0.2 mg/kg, po qd administered days 1 to 5 measured on days 6 to 212012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Discovery of LFF571: an investigational agent for Clostridium difficile infection.
AID675926Inhibition of protein synthesis in Escherichia coli S30 extract at 2 uM after 75 mins by luciferase based luminescence assay relative to GE2270A2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Discovery of LFF571: an investigational agent for Clostridium difficile infection.
AID675937Drug level in Clostridium difficile infected golden syrian hamster cecum at 20 mg/kg, po qd administered for 5 days measured at 3 hrs post dose2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Discovery of LFF571: an investigational agent for Clostridium difficile infection.
AID675923Antibacterial activity against Staphylococcus aureus A4.018 by broth microdilution method2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Discovery of LFF571: an investigational agent for Clostridium difficile infection.
AID977611Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Discovery of LFF571: an investigational agent for Clostridium difficile infection.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (12)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's12 (100.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials3 (25.00%)5.53%
Reviews2 (16.67%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other7 (58.33%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (1)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Multi-center, Randomized, Evaluator-blind, Active-controlled,Parallel-group Design to Determine Safety, Tolerability, and Efficacy of Multiple Daily Administration of LFF571 for 10 Days in Patients With Moderate Clostridium Difficile Infections [NCT01232595]Phase 2109 participants (Actual)Interventional2010-10-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
metronidazole
Metronidazole: A nitroimidazole used to treat AMEBIASIS; VAGINITIS; TRICHOMONAS INFECTIONS; GIARDIASIS; ANAEROBIC BACTERIA; and TREPONEMAL INFECTIONS.. metronidazole : A member of the class of imidazoles substituted at C-1, -2 and -5 with 2-hydroxyethyl, nitro and methyl groups respectively. It has activity against anaerobic bacteria and protozoa, and has a radiosensitising effect on hypoxic tumour cells. It may be given by mouth in tablets, or as the benzoate in an oral suspension. The hydrochloride salt can be used in intravenous infusions. Metronidazole is a prodrug and is selective for anaerobic bacteria due to their ability to intracellularly reduce the nitro group of metronidazole to give nitroso-containing intermediates. These can covalently bind to DNA, disrupting its helical structure, inducing DNA strand breaks and inhibiting bacterial nucleic acid synthesis, ultimately resulting in bacterial cell death.		2.520C-nitro compound;
imidazoles;
primary alcohol		antiamoebic agent;
antibacterial drug;
antimicrobial agent;
antiparasitic agent;
antitrichomonal drug;
environmental contaminant;
prodrug;
radiosensitizing agent;
xenobiotic
thiophenes
Thiophenes: A monocyclic heteroarene furan in which the oxygen atom is replaced by a sulfur.. thiophenes : Compounds containing at least one thiophene ring.		3.2510mancude organic heteromonocyclic parent;
monocyclic heteroarene;
thiophenes;
volatile organic compound		non-polar solvent
thiazoles
[no description available]		9.261231,3-thiazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene
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.		6.8172glycopeptideantibacterial drug;
antimicrobial agent;
bacterial metabolite
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.		3.2510carbamate ester;
oxazolidinone		metabolite
fidaxomicin
Fidaxomicin: A narrow-spectrum macrolide antibacterial agent that is used in the treatment of diarrhea associated with CLOSTRIDIUM DIFFICILE INFECTION.. fidaxomicin : An 18-membered macrolide that is a fermentation product obtained from the Actinomycete Dactylosporangium aurantiacum. A narrow spectrum antibiotic used for treatment of Clostridium difficile-related infections.		9.2950
ge 2270 a
GE 2270 A: from Planobispora rosea; inhibits bacterial protein synthesis in vitro by affecting specifically the GTP-bound form of elongation factor Tu; structure given in first source		2.0710
ridinilazole
ridinilazole: antibiotic		3.2510
rep 3123
REP 3123: structure in first source		3.2510
cadazolid
cadazolid: for treatment of Clostridium difficile infections; structure in first source		3.2510
surotomycin
[no description available]		3.2510
ConditionIndicatedRelationship StrengthStudiesTrials
Antibiotic-Associated Colitis
[description not available]		03.1750
Enterocolitis, Pseudomembranous
An acute inflammation of the INTESTINAL MUCOSA that is characterized by the presence of pseudomembranes or plaques in the SMALL INTESTINE (pseudomembranous enteritis) and the LARGE INTESTINE (pseudomembranous colitis). It is commonly associated with antibiotic therapy and CLOSTRIDIUM DIFFICILE colonization.		03.1750
Clostridioides difficile Infection
[description not available]		07.9352
Health Care Associated Infection
[description not available]		02.0810
Clostridium Infections
Infections with bacteria of the genus CLOSTRIDIUM and closely related CLOSTRIDIOIDES species.		07.9352
Cross Infection
Any infection which a patient contracts in a health-care institution.		02.0810
Recrudescence
[description not available]		02.0710
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