Xenleta LefaMulin Acetate Concentrate for Solution for Injection

1. Indications and Usage
Lefamulin is indicated for the treatment of adult patients with community-acquired bacterial pneumonia (CABP) caused by susceptible strains of Streptococcus pneumoniae (including multiple-drug-resistant strains), including cases with concurrent bacteremia, or Haemophilus influenzae.
2. Dosage and Administration
Recommended Dosage: The recommended dosage is 150 mg administered intravenously once every 12 hours.
Administration: The solution should be infused intravenously over 1 hour.
Duration: The total duration of treatment is typically 5 to 7 days.
Switching to Oral: Patients who have shown clinical improvement may be switched to oral lefamulin to complete the treatment course.
3. Mechanism of Action
Lefamulin is a semi-synthetic fluoro酮 antibiotic that inhibits bacterial protein synthesis by binding to the 50S ribosomal subunit of the prokaryotic ribosome. It specifically targets Streptococcus pneumoniae and Haemophilus influenzae, which are common pathogens in CABP.
4. Safety and Warnings
Hepatotoxicity: Elevations in liver enzymes have been reported. Liver function should be monitored during treatment.
QT Prolongation: Lefamulin may prolong the QT interval. It should be used with caution in patients with risk factors for QT prolongation, such as those taking antiarrhythmics or with a history of QT prolongation.
Hypersensitivity: Severe hypersensitivity reactions, including anaphylaxis, have been reported.
5. Adverse Reactions and Clinical Research
Common Adverse Reactions: The most frequent adverse reactions include nausea, vomiting, and diarrhea.
Clinical Research: Clinical trials have demonstrated that lefamulin is non-inferior to moxifloxacin in clearing the causative pathogens in CABP and achieving clinical cure.
6. Drug Interactions
CYP3A4 Inhibitors and Inducers: Lefamulin is metabolized by CYP3A4. Concomitant use with strong CYP3A4 inhibitors (e.g., ketoconazole) or inducers (e.g., rifampin) may significantly alter lefamulin plasma concentrations.
Drugs that Prolong QT Interval: Concomitant use with drugs that prolong the QT interval (e.g., amiodarone, moxifloxacin) may increase the risk of QT prolongation and arrhythmias.
Digoxin: Lefamulin is a P-gp substrate and inhibitor; concomitant use with digoxin may increase digoxin exposure.
7. Pharmaceutical Information
Composition: The active ingredient is lefamulin.
Appearance: The concentrate for solution for injection is a clear to slightly yellowish solution.
Storage: Store at 2°C to 8°C. Do not freeze. Protect from light.