Evaluate the susceptibility of VSEfm to lefamulin, showing resistance to lefamulin.
Nat Commun. 2022 Apr 7;13(1):1888
Vancomycin-resistant Enterococcus faecium (VREfm)
0.03 μg/mL
16-18 hours
Evaluate the susceptibility of VREfm to lefamulin, showing a significant increase in sensitivity to lefamulin.
Nat Commun. 2022 Apr 7;13(1):1888
HCCLM3 SR cells
20 ×10^−6 M
48 hours
Evaluate the inhibitory effect of lefamulin alone or combined with sorafenib on cell proliferation, results showed that combined treatment significantly inhibited cell proliferation.
Adv Sci (Weinh). 2024 Aug;11(30):e2401789
HepG2 SR cells
10 ×10^−6 M
48 hours
Evaluate the synergistic effect of lefamulin combined with sorafenib, results showed that combined treatment significantly inhibited cell growth and promoted apoptosis.
Adv Sci (Weinh). 2024 Aug;11(30):e2401789
J774 mouse macrophages
1 or 5 mg/L
5 hours
To evaluate the accumulation of lefamulin in macrophages, results showed rapid accumulation of lefamulin in macrophages, reaching intracellular concentrations of 35.6 mg/L (1 mg/L external concentration) and 218 mg/L (5 mg/L external concentration) after 1 hour, and 54.4 mg/L and 270 mg/L after 5 hours.
S. aureus cell-free transcription-translation system
0.02 μg/ml (IC50)
1 hour
To evaluate the inhibitory effect of lefamulin on protein synthesis in S. aureus. Results showed that lefamulin has a lower IC50 value compared to other pleuromutilin antibiotics, indicating its stronger inhibitory capability.
Sci Rep. 2016 Dec 13;6:39004
Staphylococcus aureus ribosome
44.9 μM (22.8 μg/ml)
6 hours
To study the binding mode of lefamulin to the large ribosomal subunit of S. aureus and its mechanism of protein synthesis inhibition. Results showed that lefamulin binds to the PTC site, forming hydrogen bonds and hydrophobic interactions, thereby inhibiting protein synthesis.
Sci Rep. 2016 Dec 13;6:39004
Vero cells
<0.004–0.063 mg/L
28 days
To evaluate the in vitro antimicrobial activity of lefamulin against Mycoplasma genitalium, results showed high susceptibility of all cultured isolates to lefamulin, with only one strain exhibiting an elevated MIC of 0.063 mg/L.
J Antimicrob Chemother. 2025 Feb 3;80(2):465-471
Lefamulin acetate/醋酸来法莫林 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
Intestinal colonization model and peritonitis-septicemia model
Single dose (intestinal colonization model), every 24 hours (peritonitis-septicemia model)
Evaluate the efficacy of lefamulin against VREfm in vivo, showing effective reduction in colonization and improved survival.
Nat Commun. 2022 Apr 7;13(1):1888
Balb/c nude mice
HCC xenograft model
Intraperitoneal injection
25 or 50 mg/kg
Daily
Evaluate the inhibitory effect of lefamulin alone or combined with sorafenib on tumor growth, results showed that combined treatment significantly inhibited tumor growth and reduced tumor weight.
Adv Sci (Weinh). 2024 Aug;11(30):e2401789
BALB/c mice
Neutropenic pneumonia model
Subcutaneous
1.25–160 mg/kg
Twice daily for 24 hours
To evaluate the pharmacodynamics of lefamulin in a neutropenic pneumonia model, results showed significant reduction in bacterial load correlated with AUC/MIC ratios.
To evaluate the in vivo pharmacodynamics of lefamulin against five Streptococcus pneumoniae and five Staphylococcus aureus strains, finding that efficacy correlated most strongly with the AUC0–24/MIC ratio.
To evaluate the effect of Lefamulin acetate on total cells and neutrophils in LPS-induced inflammation model. Results showed that Lefamulin acetate significantly reduced the number of total cells and neutrophils in BALF.
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