ID Source | ID |
---|---|
PubMed CID | 25185057 |
CHEMBL ID | 3291398 |
SCHEMBL ID | 19766421 |
MeSH ID | M000597233 |
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 |
Excerpt | Reference | Relevance |
---|---|---|
"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 |
Excerpt | Reference | Relevance |
---|---|---|
" 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 |
Excerpt | Relevance | Reference |
---|---|---|
"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 |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1154474 | Antibacterial activity against of methicillin-sensitive Staphylococcus aureus ATCC 19636 infected in iv dosed mouse administered 1 hr after infection measured after 48 hrs | 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. |
AID1666859 | Antibacterial activity against vancomycin-resistant Staphylococcus epidermidis ATCC 700221 assessed as reduction in bacterial growth incubated for 18 hrs by agar dilution method | 2020 | Bioorganic & 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. |
AID1154473 | Antibacterial 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 days | 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. |
AID1154475 | Antibacterial 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 hrs | 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. |
AID1666856 | Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 29213 assessed as reduction in bacterial growth incubated for 18 hrs by agar dilution method | 2020 | Bioorganic & 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. |
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. |
AID1154483 | Inhibition of CYP2D6 in human liver microsomes using dextromethorphan as substrate after 15 mins by LC/MS/MS analysis | 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. |
AID1154472 | Antibacterial activity against clinical isolate of methicillin-sensitive Staphylococcus aureus infected in iv dosed mouse administered 1 hr after infection for 4 days | 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. |
AID1154477 | Antibacterial 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 hrs | 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. |
AID1154469 | Elimination half life in Sprague-Dawley rat at 2 mg/kg, iv administered as cassette dosing | 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. |
AID1154476 | Antibacterial activity against of methicillin-resistant Staphylococcus aureus ATCC 33591 infected in iv dosed neutropenic mouse administered 1 hr after infection measured after 24 hrs | 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. |
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. |
AID1154480 | Inhibition of CYP1A2 in human liver microsomes using phenacetin as substrate after 15 mins by LC/MS/MS analysis | 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. |
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. |
AID1154470 | Clearance in Sprague-Dawley rat at 2 mg/kg, iv administered as cassette dosing | 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. |
AID1666855 | Antibacterial activity against methicillin-resistant Staphylococcus epidermidis 16-5 assessed as reduction in bacterial growth incubated for 18 hrs by agar dilution method | 2020 | Bioorganic & 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. |
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. |
AID1154485 | Inhibition of CYP3A4 in human liver microsomes using testosterone as substrate after 15 mins by LC/MS/MS analysis | 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. |
AID1666857 | Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 33591 assessed as reduction in bacterial growth incubated for 18 hrs by agar dilution method | 2020 | Bioorganic & 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. |
AID1154468 | Mean residence time in Sprague-Dawley rat at 2 mg/kg, iv administered as cassette dosing | 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. |
AID1666854 | Antibacterial activity against methicillin-sensitive Staphylococcus epidermidis ATCC 12228 assessed as reduction in bacterial growth incubated for 18 hrs by agar dilution method | 2020 | Bioorganic & 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. |
AID1154482 | Inhibition of CYP2C19 in human liver microsomes using mephenytoin as substrate after 15 mins by LC/MS/MS analysis | 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. |
AID1154467 | AUC (0 to t) in Sprague-Dawley rat at 2 mg/kg, iv administered as cassette dosing | 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. |
AID1154481 | Inhibition of CYP2C9 in human liver microsomes using tolbutamide as substrate after 15 mins by LC/MS/MS analysis | 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. |
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. |
AID1154484 | Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate after 15 mins by LC/MS/MS analysis | 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. |
AID1666858 | Antibacterial activity against vancomycin-sensitive Staphylococcus epidermidis 16-5 assessed as reduction in bacterial growth incubated for 18 hrs by agar dilution method | 2020 | Bioorganic & 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. |
AID1154471 | Volume of distribution at steady state in Sprague-Dawley rat at 2 mg/kg, iv administered as cassette dosing | 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 | 0 (0.00) | 29.6817 |
2010's | 18 (43.90) | 24.3611 |
2020's | 23 (56.10) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
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.
| This Compound (15.87) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 10 (24.39%) | 5.53% |
Reviews | 13 (31.71%) | 6.00% |
Case Studies | 0 (0.00%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 18 (43.90%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |