Lefamulin
Clinical data
Trade namesXenleta
Other namesBC-3781
AHFS/Drugs.comMonograph
License data
Routes of
administration		Intravenous, by mouth
ATC code
Legal status
Legal status
Identifiers
  • (1S,2R,3S,4S,6R,7R,8R,14R)-3-Hydroxy-2,4,7,14-tetramethyl-9-oxo-4-vinyltricyclo[5.4.3.01,8]tetradec-6-yl {[(1R,2R,4R)-4-amino-2-hydroxycyclohexyl]sulfanyl}acetate
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
Chemical and physical data
FormulaC28H45NO5S
Molar mass507.73 g·mol−1
3D model (JSmol)
  • C[C@@H]1CC[C@@]23CCC(=O)[C@H]2[C@@]1([C@@H](C[C@@]([C@H]([C@@H]3C)O)(C)C=C)OC(=O)CS[C@@H]4CC[C@H](C[C@H]4O)N)C
  • InChI=1S/C28H45NO5S/c1-6-26(4)14-22(34-23(32)15-35-21-8-7-18(29)13-20(21)31)27(5)16(2)9-11-28(17(3)25(26)33)12-10-19(30)24(27)28/h6,16-18,20-22,24-25,31,33H,1,7-15,29H2,2-5H3/t16-,17+,18-,20-,21-,22-,24+,25+,26-,27+,28+/m1/s1
  • Key:KPVIXBKIJXZQJX-FCEONZPQSA-N

Lefamulin, sold under the brand name Xenleta, is an antibiotic medication used it to treat adults with community-acquired bacterial pneumonia.[5][6] It is taken by mouth or by injection into a vein.[5][6][7]

Relatively common side effects include diarrhea, nausea, pain at the site of injection, and liver inflammation.[5][8] It is a pleuromutilin antibiotic that inhibits the large subunit of bacterial ribosomes.[9][10]

Lefamulin was approved for medical use in the United States in August 2019,[5][11] and in the European Union in July 2020.[3]

Medical uses

Lefamulin is used to treat adults with community-acquired bacterial pneumonia.[5][6][3] It was also investigated for treatment of acute bacterial skin and skin-structure infections (ABSSSI).[12]

Spectrum of activity

Lefamulin has in vitro activity against Streptococcus pneumoniae, viridans group Streptococci, Moraxella catarrhalis, Enterococcus faecium, methicillin-resistant Staphylococcus aureus (MRSA), among other bacteria.[13][14]

History

It was developed by Nabriva Therapeutics and approved in the United States in 2019.[5] It was granted fast track status by the US Food and Drug Administration (FDA) in 2014. Although pleuromutilin antibiotics were first developed in the 1950s, lefamulin is the first to be used for systemic treatment of bacterial infections in humans.[15]

Society and culture

Lefamulin was approved for medical use in the United States in August 2019, and in the European Union in July 2020.[5][3][11]

References

  1. ↑ "Summary Basis of Decision (SBD) for Xenleta". Health Canada. 23 October 2014. Retrieved 29 May 2022.
  2. ↑ "Xenleta- lefamulin acetate injection, solution citric buffered normal saline- anhydrous citric acid injection, solution Xenleta- lefamulin acetate tablet, coated". DailyMed. 12 February 2020. Retrieved 24 September 2020.
  3. 1 2 3 4 "Xenleta EPAR". European Medicines Agency. 26 May 2020. Retrieved 24 September 2020.
  4. ↑ "Xenleta Product information". Union Register of medicinal products. Retrieved 3 March 2023.
  5. 1 2 3 4 5 6 7 "FDA approves new antibiotic to treat community-acquired bacterial pneumonia". U.S. Food and Drug Administration (FDA) (Press release). 19 August 2019. Archived from the original on 20 November 2019. Retrieved 19 November 2019. Public Domain This article incorporates text from this source, which is in the public domain.
  6. 1 2 3 "Drug Trials Snapshots: Xenleta". U.S.Food and Drug Administration (FDA). 4 September 2019. Archived from the original on 20 November 2019. Retrieved 19 November 2019.
  7. ↑ File TM, Goldberg L, Das A, Sweeney C, Saviski J, Gelone SP, et al. (November 2019). "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". Clinical Infectious Diseases. 69 (11): 1856–1867. doi:10.1093/cid/ciz090. PMC 6853694. PMID 30722059.
  8. ↑ Alexander E, Goldberg L, Das AF, Moran GJ, Sandrock C, Gasink LB, et al. (November 2019). "Oral Lefamulin vs Moxifloxacin for Early Clinical Response Among Adults With Community-Acquired Bacterial Pneumonia: The LEAP 2 Randomized Clinical Trial". JAMA. 322 (17): 1661–1671. doi:10.1001/jama.2019.15468. PMC 6865224. PMID 31560372.
  9. ↑ Andrei S, Droc G, Stefan G (December 2019). "FDA approved antibacterial drugs: 2018-2019". Discoveries. 7 (4): e102. doi:10.15190/d.2019.15. PMC 7086080. PMID 32309620.
  10. ↑ Eyal Z, Matzov D, Krupkin M, Paukner S, Riedl R, Rozenberg H, et al. (December 2016). "A novel pleuromutilin antibacterial compound, its binding mode and selectivity mechanism". Scientific Reports. 6: 39004. Bibcode:2016NatSR...639004E. doi:10.1038/srep39004. PMC 5154188. PMID 27958389.
  11. 1 2 "Drug Approval Package: Xenleta". U.S.Food and Drug Administration (FDA). 26 September 2019. Retrieved 24 September 2020.
  12. ↑ Zeitlinger M, Schwameis R, Burian A, Burian B, Matzneller P, Müller M, et al. (April 2016). "Simultaneous assessment of the pharmacokinetics of a pleuromutilin, lefamulin, in plasma, soft tissues and pulmonary epithelial lining fluid". The Journal of Antimicrobial Chemotherapy. 71 (4): 1022–1026. doi:10.1093/jac/dkv442. PMID 26747098.
  13. ↑ Spreitzer H (23 May 2016). "Neue Wirkstoffe - Lefamulin". Österreichische Apothekerzeitung (in German) (11/2016).
  14. ↑ Mendes RE, Farrell DJ, Flamm RK, Talbot GH, Ivezic-Schoenfeld Z, Paukner S, Sader HS (July 2016). "In Vitro Activity of Lefamulin Tested against Streptococcus pneumoniae with Defined Serotypes, Including Multidrug-Resistant Isolates Causing Lower Respiratory Tract Infections in the United States". Antimicrobial Agents and Chemotherapy. 60 (7): 4407–4411. doi:10.1128/AAC.00627-16. PMC 4914675. PMID 27161634.
  15. ↑ Veve MP, Wagner JL (September 2018). "Lefamulin: Review of a Promising Novel Pleuromutilin Antibiotic". Pharmacotherapy. 38 (9): 935–946. doi:10.1002/phar.2166. PMID 30019769. S2CID 51679073.
  • "Lefamulin". Drug Information Portal. U.S. National Library of Medicine.
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