Community-Acquired Bacterial Pneumonia (CABP) XENLETA is indicated for the treatment of adults with community-acquired bacterial pneumonia (CABP) caused by the following susceptible microorganisms: Streptococcus pneumoniae, Staphylococcus aureus

1. DRUG CLUB PRESENTATION ON XENLETA
Dr. P. Asma Afreen

2.  Brand name: xenleta
 Generic name: lefamulin
 Dose: tab-600mg/inj-150mg
 Dosage form: tablet/injection
 Class:Pleuromutilin
 Fda approved drug: Aug 19, 2019
 Treatment:Pneumonia

3. Dosage Forms & Strengths
tablet
 600mg
intravenous solution
 150mg/15mL 0.9% NaCl (further dilution required)

4. Description
 Lefamulin is a pleuromutilin antibiotic used for the treatment of bacterial
community-acquired pneumonia. A pleuromotilin is a more recently
developed type of antibiotic that is derived from the fungus, Pleurotus
mutilus. XENLETA is a semi-synthetic antibacterial agent for oral and
intravenous administration

5. CHEMICAL DESCRIPTION
XENLETA, a pleuromutilin
derivative, is available as 14-O-
{[(1R,2R,4R)-4-amino-2-
hydroxycyclohexylsulfanyl]-
acetyl}-mutilin in the form of an
acetic acid salt (acetate).
molecular weight - 567.79 grams
per mole. formula -
C30H49NO7S

6. Dosage form
 XENLETA :tablet:600mg
injection:150mg

7. MECHANISM OF ACTION
XENLETA is a systemic pleuromutilin
antibacterial. It inhibits bacterial protein
synthesis through interactions (hydrogen
bonds, hydrophobic interactions, and Van der
Waals forces) with the A-and P-sites of the
peptidyl transferase center (PTC) in domain
V of the 23s rRNA of the 50S subunit. The
binding pocket of the bacterial ribosome
closes around the mutilin core for an induced
fit that prevents correct positioning of tRNA
XENLETA

8. Pharmacokinetic parameters
Absorption –
The mean oral bioavailability - 25%
peak plasma concentration - 0.88 to 2 hours.
Distribution –
Mean plasma protein binding - 94.8% at 2.35 mcg/mL .
volume of distribution - 86.1 L (34.2 to 153 L)
Metabolism -
primarily metabolized by CYP3A4
Excretion -
total body clearance -11.9 L/h
In healthy adult subjects, the mean % of total radioactivity excreted in feces was
77.3% and 88.5% and in urine was 15.5% and 5.3% following 150 mg IV or 600

9. Indications
Community-Acquired Bacterial Pneumonia (CABP) XENLETA is
indicated for the treatment of adults with community-acquired
bacterial pneumonia (CABP) caused by the following susceptible
microorganisms: Streptococcus pneumoniae, Staphylococcus aureus
, Haemophilus influenzae, Mycoplasma pneumoniae, and
Chlamydophila pneumoniae.
To reduce the development of drug-resistant bacteria and maintain the
effectiveness of XENLETA and other antibacterial drugs,
XENLETA should be used only to treat or prevent infections that are
proven or strongly suspected to be caused by susceptible bacteria.

10. Adverse drug reaction
 Administration site reactions
 Hepatic enzyme elevation
 Nausea
 Hypokalemia
 Insomnia
 Headache
 Diarrhea
 Vomiting

11. Drug interactions
 antiarrhythmics
 antipsychotics
 erythromycin
 moxifloxacin
 tricyclic

12. Storage
 Tablets: Store at room temperature of 20-25ºC (68-77ºF); excursions permitted to 15-30ºC
(59-86ºF)
 IV
 Before dilution
 Vials: Refrigerate at 2-8ºC (36-46ºF); do not freeze
 Diluent bags: Store at 20-25ºC (68-77ºF); excursions permitted to 15-30ºC (59-86ºF)
 After dilution
 Room temperature: Up to 24 hr
 Refrigerated at 2-8ºC (36-46ºF): Up to 48 hr

13. Thank you