Chemistry:Lefamulin
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| Trade names | Xenleta |
| Other names | BC-3781 |
| AHFS/Drugs.com | Monograph |
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| Routes of administration | Intravenous, by mouth |
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| Formula | C28H45NO5S |
| Molar mass | 507.73 g·mol−1 |
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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
Legal status
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
- ↑ "Summary Basis of Decision (SBD) for Xenleta". 23 October 2014. https://hpr-rps.hres.ca/reg-content/summary-basis-decision-detailTwo.php?linkID=SBD00504&lang=en.
- ↑ "Xenleta- lefamulin acetate injection, solution citric buffered normal saline- anhydrous citric acid injection, solution Xenleta- lefamulin acetate tablet, coated". 12 February 2020. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=101db63d-2fe2-48df-8506-1382d6dcd4a3.
- ↑ 3.0 3.1 3.2 3.3 "Xenleta EPAR". 26 May 2020. https://www.ema.europa.eu/en/medicines/human/EPAR/xenleta.
- ↑ "Xenleta Product information". https://ec.europa.eu/health/documents/community-register/html/h1457.htm.
- ↑ 5.0 5.1 5.2 5.3 5.4 5.5 5.6 "FDA approves new antibiotic to treat community-acquired bacterial pneumonia". U.S. Food and Drug Administration (FDA) (Press release). August 19, 2019. Archived from the original on 20 November 2019. Retrieved 19 November 2019.
This article incorporates text from this source, which is in the public domain.
- ↑ 6.0 6.1 6.2 "Drug Trials Snapshots: Xenleta". 4 September 2019. https://www.fda.gov/drugs/resources-information-approved-drugs/drug-trials-snapshots-xenleta.
- ↑ "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. doi:10.1093/cid/ciz090. PMID 30722059.
- ↑ "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. doi:10.1001/jama.2019.15468. PMID 31560372.
- ↑ "FDA approved antibacterial drugs: 2018-2019". Discoveries 7 (4): e102. December 2019. doi:10.15190/d.2019.15. PMID 32309620.
- ↑ "A novel pleuromutilin antibacterial compound, its binding mode and selectivity mechanism". Scientific Reports 6: 39004. December 2016. doi:10.1038/srep39004. PMID 27958389. Bibcode: 2016NatSR...639004E.
- ↑ 11.0 11.1 "Drug Approval Package: Xenleta". 26 September 2019. https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/211672Orig1s000,%20211673Orig1s000TOC.cfm.
- ↑ "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. April 2016. doi:10.1093/jac/dkv442. PMID 26747098.
- ↑ "Neue Wirkstoffe - Lefamulin" (in de). Österreichische Apothekerzeitung (11/2016). 23 May 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. July 2016. doi:10.1128/AAC.00627-16. PMID 27161634.
- ↑ "Lefamulin: Review of a Promising Novel Pleuromutilin Antibiotic". Pharmacotherapy 38 (9): 935–946. September 2018. doi:10.1002/phar.2166. PMID 30019769.
External links
- "Lefamulin". Drug Information Portal. U.S. National Library of Medicine. https://druginfo.nlm.nih.gov/drugportal/name//lefamulin.
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