Page last updated: 2024-11-13

bc-3781

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

Cross-References

ID SourceID
PubMed CID25185057
CHEMBL ID3291398
SCHEMBL ID19766421
MeSH IDM000597233

Synonyms (23)

Synonym
chembl3291398 ,
bdbm50019649
lefamulin ,
1061337-51-6
lefamulin(bc-3781)
62B ,
acetic acid, 2-[[(1r,2r,4r)-4-amino-2-hydroxycyclohexyl]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
(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 {[(1r,2r,4r)-4-amino-2-hydroxycyclohexyl]sulfanyl}acetate
SCHEMBL19766421
1061337-51-6 (free base)
(3ar,4r,5r,7s,8s,9r,9as,12r)-8-hydroxy-4,7,9,12-tetramethyl-3-oxo-7-vinyldecahydro-4,9a-propanocyclopenta[8]annulen-5-yl 2-(((1r,2r,4r)-4-amino-2-hydroxycyclohexyl)thio)acetate
D11631
lefamulin (usan/inn)
bc3781
gtpl10824
compound 7 [pmid: 24874438]
Q27253537
EX-A3600
[(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,2r,4r)-4-amino-2-hydroxycyclohexyl]sulfanylacetate
DTXSID101027896
CS-0012945
HY-16908
AKOS040759180

Research Excerpts

Toxicity

ExcerptReferenceRelevance
"Lefamulin was noninferior to moxifloxacin for the primary efficacy endpoints and was generally safe and well tolerated."( Efficacy and Safety of Intravenous-to-oral Lefamulin, a Pleuromutilin Antibiotic, for the Treatment of Community-acquired Bacterial Pneumonia: The Phase III Lefamulin Evaluation Against Pneumonia (LEAP 1) Trial.
Das, A; File, TM; Gasink, LB; Gelone, SP; Goldberg, L; Paukner, S; Saviski, J; Seltzer, E; Sweeney, C; Talbot, GH; Wicha, WW, 2019
)
0.51
" Two, three, and three subjects reported drug-related treatment-emergent adverse events (TEAE) in Normal, Severe, and Hemodialysis groups, respectively."( Pharmacokinetics and safety of lefamulin after single intravenous dose administration in subjects with impaired renal function and those requiring hemodialysis.
Crandon, JL; Dowell, JA; Ermer, J; Gelone, SP; Leister, C; Marbury, TC; Wicha, WW, 2021
)
0.62

Pharmacokinetics

ExcerptReferenceRelevance
" Data from a phase 2 study of patients with ABSSSI were used to refine a previous population pharmacokinetic (PK) model and explore potential predictors of PK variability."( Population pharmacokinetic analyses for BC-3781 using phase 2 data from patients with acute bacterial skin and skin structure infections.
Ambrose, PG; Bhavnani, SM; Ivezic-Schoenfeld, Z; Prince, WT; Rubino, CM; Wicha, WW; Xue, B, 2015
)
0.68
"Plasma pharmacokinetic (PK) data from a crossover, bioavailability, food-effect study and plasma and ELF PK data from a tissue penetration study in normal healthy volunteers were used to construct a PPK model for lefamulin."( Prediction of lefamulin epithelial lining fluid penetration after intravenous and oral administration using Phase 1 data and population pharmacokinetics methods.
Bhavnani, SM; Rubino, CM; Wicha, WW; Zhang, L, 2019
)
0.51
" This Supplement, entitled 'Pharmacokinetic and pharmacodynamic analyses and dose rationale for lefamulin, a novel pleuromutilin antibiotic, for the treatment of community-acquired bacterial pneumonia', is intended to be a valuable resource for both clinicians and researchers."( Introduction: lefamulin and pharmacokinetic/pharmacodynamic rationale to support the dose selection of lefamulin.
Rodvold, KA, 2019
)
0.51
"Open-label, Phase-1 pharmacokinetic study."( Pharmacokinetics and safety of lefamulin after single intravenous dose administration in subjects with impaired renal function and those requiring hemodialysis.
Crandon, JL; Dowell, JA; Ermer, J; Gelone, SP; Leister, C; Marbury, TC; Wicha, WW, 2021
)
0.62
"Open-label, Phase-1 clinical pharmacokinetic study."( Pharmacokinetics and safety of lefamulin after single intravenous dose administration in subjects with impaired-hepatic function.
Crandon, JL; Dowell, JA; Ermer, J; Gelone, SP; Leister, C; Marbury, TC; Wicha, WW, 2021
)
0.62

Bioavailability

ExcerptReferenceRelevance
" The absorption rate was slower and bioavailability was decreased after a high-fat/high-calorie meal."( Prediction of lefamulin epithelial lining fluid penetration after intravenous and oral administration using Phase 1 data and population pharmacokinetics methods.
Bhavnani, SM; Rubino, CM; Wicha, WW; Zhang, L, 2019
)
0.51

Dosage Studied

ExcerptRelevanceReference
"Single and repeated dosing of iv and oral lefamulin resulted in comparable exposure."( Pharmacokinetics and tolerability of lefamulin following intravenous and oral dosing.
Gelone, SP; Heilmayer, W; Lell, C; Prince, WT; Wicha, WW, 2019
)
0.51
"
Lefamulin does not require dosage adjustment in renal impairment."
( A Review of Newly Approved Antibiotic Treatment for Community-Acquired Bacterial Pneumonia: Lefamulin.
Charles, CV; Wang, H, 2020
)
0.56
"No dosage adjustment is required for patients with renal impairment, and lefamulin can be administered without regard to hemodialysis timing."( Pharmacokinetics and safety of lefamulin after single intravenous dose administration in subjects with impaired renal function and those requiring hemodialysis.
Crandon, JL; Dowell, JA; Ermer, J; Gelone, SP; Leister, C; Marbury, TC; Wicha, WW, 2021
)
0.62
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (28)

Assay IDTitleYearJournalArticle
AID1154474Antibacterial activity against of methicillin-sensitive Staphylococcus aureus ATCC 19636 infected in iv dosed mouse administered 1 hr after infection measured after 48 hrs2014Journal 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.
AID1666859Antibacterial activity against vancomycin-resistant Staphylococcus epidermidis ATCC 700221 assessed as reduction in bacterial growth incubated for 18 hrs by agar dilution method2020Bioorganic & medicinal chemistry letters, 04-01, Volume: 30, Issue:7
Design, synthesis, and biological activity evaluation of a series of pleuromutilin derivatives with novel C14 side chains.
AID1154473Antibacterial activity against clinical isolate of methicillin-sensitive Staphylococcus aureus infected in iv dosed mouse assessed as host survival administered 1 hr after infection for 4 days2014Journal 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.
AID1154475Antibacterial activity against of methicillin-sensitive Staphylococcus aureus ATCC 19636 infected in iv dosed mouse assessed as host survival administered 1 hr after infection measured after 48 hrs2014Journal 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.
AID1666856Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 29213 assessed as reduction in bacterial growth incubated for 18 hrs by agar dilution method2020Bioorganic & medicinal chemistry letters, 04-01, Volume: 30, Issue:7
Design, synthesis, and biological activity evaluation of a series of pleuromutilin derivatives with novel C14 side chains.
AID1638645Intrinsic clearance in mouse liver S9 fraction2019Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
Boron-Pleuromutilins as Anti- Wolbachia Agents with Potential for Treatment of Onchocerciasis and Lymphatic Filariasis.
AID1154483Inhibition of CYP2D6 in human liver microsomes using dextromethorphan as substrate after 15 mins by LC/MS/MS analysis2014Journal 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.
AID1154472Antibacterial activity against clinical isolate of methicillin-sensitive Staphylococcus aureus infected in iv dosed mouse administered 1 hr after infection for 4 days2014Journal 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.
AID1154477Antibacterial activity against of methicillin-resistant Staphylococcus aureus ATCC 33591 infected in iv dosed neutropenic mouse assessed as host survival administered 1 hr after infection measured after 24 hrs2014Journal 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.
AID1154469Elimination half life in Sprague-Dawley rat at 2 mg/kg, iv administered as cassette dosing2014Journal 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.
AID1154476Antibacterial activity against of methicillin-resistant Staphylococcus aureus ATCC 33591 infected in iv dosed neutropenic mouse administered 1 hr after infection measured after 24 hrs2014Journal 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.
AID1638643Antimicrobial activity against Wolbachia pipientis infected in Asian tiger mosquito C6/36 cells after 7 days by SYTO11 DNA dye-based confocal imaging analysis2019Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
Boron-Pleuromutilins as Anti- Wolbachia Agents with Potential for Treatment of Onchocerciasis and Lymphatic Filariasis.
AID1154480Inhibition of CYP1A2 in human liver microsomes using phenacetin as substrate after 15 mins by LC/MS/MS analysis2014Journal 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.
AID1638648Apparent permeability of the compound in MDCK-MDR1 cells2019Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
Boron-Pleuromutilins as Anti- Wolbachia Agents with Potential for Treatment of Onchocerciasis and Lymphatic Filariasis.
AID1154470Clearance in Sprague-Dawley rat at 2 mg/kg, iv administered as cassette dosing2014Journal 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.
AID1666855Antibacterial activity against methicillin-resistant Staphylococcus epidermidis 16-5 assessed as reduction in bacterial growth incubated for 18 hrs by agar dilution method2020Bioorganic & medicinal chemistry letters, 04-01, Volume: 30, Issue:7
Design, synthesis, and biological activity evaluation of a series of pleuromutilin derivatives with novel C14 side chains.
AID1638646Fraction unbound in mouse plasma at 2 uM2019Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
Boron-Pleuromutilins as Anti- Wolbachia Agents with Potential for Treatment of Onchocerciasis and Lymphatic Filariasis.
AID1154485Inhibition of CYP3A4 in human liver microsomes using testosterone as substrate after 15 mins by LC/MS/MS analysis2014Journal 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.
AID1666857Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 33591 assessed as reduction in bacterial growth incubated for 18 hrs by agar dilution method2020Bioorganic & medicinal chemistry letters, 04-01, Volume: 30, Issue:7
Design, synthesis, and biological activity evaluation of a series of pleuromutilin derivatives with novel C14 side chains.
AID1154468Mean residence time in Sprague-Dawley rat at 2 mg/kg, iv administered as cassette dosing2014Journal 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.
AID1666854Antibacterial activity against methicillin-sensitive Staphylococcus epidermidis ATCC 12228 assessed as reduction in bacterial growth incubated for 18 hrs by agar dilution method2020Bioorganic & medicinal chemistry letters, 04-01, Volume: 30, Issue:7
Design, synthesis, and biological activity evaluation of a series of pleuromutilin derivatives with novel C14 side chains.
AID1154482Inhibition of CYP2C19 in human liver microsomes using mephenytoin as substrate after 15 mins by LC/MS/MS analysis2014Journal 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.
AID1154467AUC (0 to t) in Sprague-Dawley rat at 2 mg/kg, iv administered as cassette dosing2014Journal 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.
AID1154481Inhibition of CYP2C9 in human liver microsomes using tolbutamide as substrate after 15 mins by LC/MS/MS analysis2014Journal 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.
AID1638644Antimicrobial activity against Wolbachia wMel infected in Drosophila melanogaster LDW1 cells after 6 days by DAPI-based fluorescence in-situ hybridization assay2019Journal of medicinal chemistry, 03-14, Volume: 62, Issue:5
Boron-Pleuromutilins as Anti- Wolbachia Agents with Potential for Treatment of Onchocerciasis and Lymphatic Filariasis.
AID1154484Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate after 15 mins by LC/MS/MS analysis2014Journal 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.
AID1666858Antibacterial activity against vancomycin-sensitive Staphylococcus epidermidis 16-5 assessed as reduction in bacterial growth incubated for 18 hrs by agar dilution method2020Bioorganic & medicinal chemistry letters, 04-01, Volume: 30, Issue:7
Design, synthesis, and biological activity evaluation of a series of pleuromutilin derivatives with novel C14 side chains.
AID1154471Volume of distribution at steady state in Sprague-Dawley rat at 2 mg/kg, iv administered as cassette dosing2014Journal 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]

Research

Studies (41)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's18 (43.90)24.3611
2020's23 (56.10)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 15.87

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

MetricThis Compound (vs All)
Research Demand Index15.87 (24.57)
Research Supply Index3.95 (2.92)
Research Growth Index4.64 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (15.87)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials10 (24.39%)5.53%
Reviews13 (31.71%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other18 (43.90%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]