Lefamulin Explained

Iupac Name:(1S,2R,3S,4S,6R,7R,8R,14R)-3-Hydroxy-2,4,7,14-tetramethyl-9-oxo-4-vinyltricyclo[5.4.3.0<sup>1,8</sup>]tetradec-6-yl acetate
Tradename:Xenleta
Dailymedid:Lefamulin
Routes Of Administration:Intravenous, by mouth
Legal Ca:Rx-only
Legal Ca Comment:[1]
Legal Us:Rx-only
Legal Us Comment:[2]
Legal Eu:Rx-only
Legal Eu Comment:[3]
Cas Number:1061337-51-6
Atc Prefix:J01
Atc Suffix:XX12
Pubchem:25185057
Drugbank:DB12825
Chemspiderid:32701544
Chembl:3291398
Unii:21904A5386
Kegg:D11631
Synonyms:BC-3781
C:28
H:45
N:1
O:5
S:1
Smiles: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
Stdinchi: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
Stdinchikey:KPVIXBKIJXZQJX-FCEONZPQSA-N

Lefamulin, sold under the brand name Xenleta, is an antibiotic medication used it to treat adults with community-acquired bacterial pneumonia.[4] It is taken by mouth or by injection into a vein.[5]

Relatively common side effects include diarrhea, nausea, pain at the site of injection, and liver inflammation.[6] It is a pleuromutilin antibiotic that inhibits the large subunit of bacterial ribosomes.[7] [8]

Lefamulin was approved for medical use in the United States in August 2019,[9] and in the European Union in July 2020.[10]

Medical uses

Lefamulin is used to treat adults with community-acquired bacterial pneumonia.[9] It was also investigated for treatment of acute bacterial skin and skin-structure infections (ABSSSI).

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.

History

It was developed by Nabriva Therapeutics and approved in the United States in 2019.[9] 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.[11]

Society and culture

Legal status

Lefamulin was approved for medical use in the United States in August 2019, and in the European Union in July 2020.[12]

Notes and References

  1. Web site: Summary Basis of Decision (SBD) for Xenleta . Health Canada . 23 October 2014 . 29 May 2022.
  2. Web site: Xenleta- lefamulin acetate injection, solution citric buffered normal saline- anhydrous citric acid injection, solution Xenleta- lefamulin acetate tablet, coated . DailyMed . 12 February 2020 . 24 September 2020.
  3. Web site: Xenleta Product information . Union Register of medicinal products . 3 March 2023.
  4. Web site: Drug Trials Snapshots: Xenleta . U.S.Food and Drug Administration (FDA) . 4 September 2019 . https://web.archive.org/web/20191120062236/https://www.fda.gov/drugs/resources-information-approved-drugs/drug-trials-snapshots-xenleta . 20 November 2019 . live . 19 November 2019.
  5. File TM, Goldberg L, Das A, Sweeney C, Saviski J, Gelone SP, Seltzer E, Paukner S, Wicha WW, Talbot GH, Gasink LB . 6 . 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 . November 2019 . 30722059 . 6853694 . 10.1093/cid/ciz090 . free .
  6. Alexander E, Goldberg L, Das AF, Moran GJ, Sandrock C, Gasink LB, Spera P, Sweeney C, Paukner S, Wicha WW, Gelone SP, Schranz J . 6 . 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 . November 2019 . 31560372 . 6865224 . 10.1001/jama.2019.15468 .
  7. Andrei S, Droc G, Stefan G . FDA approved antibacterial drugs: 2018-2019 . Discoveries . 7 . 4 . e102 . December 2019 . 32309620 . 7086080 . 10.15190/d.2019.15 . free .
  8. Eyal Z, Matzov D, Krupkin M, Paukner S, Riedl R, Rozenberg H, Zimmerman E, Bashan A, Yonath A . 6 . A novel pleuromutilin antibacterial compound, its binding mode and selectivity mechanism . Scientific Reports . 6 . 39004 . December 2016 . 27958389 . 5154188 . 10.1038/srep39004 . 2016NatSR...639004E . free .
  9. FDA approves new antibiotic to treat community-acquired bacterial pneumonia . U.S. Food and Drug Administration (FDA) . August 19, 2019 . https://web.archive.org/web/20191120062206/https://www.fda.gov/news-events/press-announcements/fda-approves-new-antibiotic-treat-community-acquired-bacterial-pneumonia . 20 November 2019 . live . 19 November 2019.
  10. Web site: Xenleta EPAR . European Medicines Agency . 26 May 2020 . 24 September 2020.
  11. Veve MP, Wagner JL . Lefamulin: Review of a Promising Novel Pleuromutilin Antibiotic . Pharmacotherapy . 38 . 9 . 935–946 . September 2018 . 30019769 . 10.1002/phar.2166 . 51679073 .
  12. Web site: Drug Approval Package: Xenleta . U.S.Food and Drug Administration (FDA) . 26 September 2019 . 24 September 2020.

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