Lefamulin: Uses, Side Effects, Dosage - Drugvu

ℹ️ Compiled from public regulatory records · Last regulator revision: May 27, 2026🚩 Report this page

Lefamulin

Other Antibacterials

Sold as Xenleta

GB MHRAEU EMA

Drug class: Other Antibacterials
Availability: See label
Markets covered: 2
Products on record: 5

Overview

Lefamulin is an active pharmaceutical ingredient in the Other Antibacterials group (J01XX). The information below is compiled per regulator from the product labels on record, with direct links to the original documents.

Regulatory status by market

Market	Regulator	Products	Last revision
GB United Kingdom	MHRA	4	November 21, 2025
EU European Union	EMA	1	May 27, 2026

GBUnited Kingdom· MHRA

4 products

Uses

GBOfficial regulatory label· revised November 21, 2025[1]

1). Consideration should be given to official guidance on the appropriate use of antibacterial agents.

How to take

EUEuropean Union· EMA

1 product

Uses

EUOfficial regulatory label· revised May 27, 2026[2]

1). Consideration should be given to official guidance on the appropriate use of antibacterial agents.

How to take

Drug interactions

Known interactions involving Lefamulin. Select one for details. This list is informational and not a complete interaction checker.

Abarelix Abiraterone Adenosine Alfuzosin Amiodarone Amisulpride Amitriptyline Amoxapine Amprenavir Anagrelide Apalutamide Apomorphine Arsenic Trioxide Asenapine Astemizole Atazanavir Atomoxetine Azithromycin Bedaquiline Bepridil Bicalutamide Boceprevir Bosentan Bosutinib Buprenorphine Cabozantinib Carbamazepine Cenobamate Ceritinib Chloroquine Chlorpromazine Ciprofloxacin Cisapride Citalopram Clarithromycin Clofazimine Clomipramine Clozapine Cobicistat Conivaptan Crizotinib Dabrafenib Dasatinib Daunorubicin Degarelix Delavirdine Desipramine Deutetrabenazine Dexamethasone Diltiazem Disopyramide Dofetilide Dolasetron Doxepin Doxorubicin Dronedarone Droperidol Efavirenz Encorafenib Entrectinib Enzalutamide Epirubicin Eribulin Erythromycin Escitalopram Etravirine Ezogabine Fingolimod Flecainide Fluconazole Fluoxetine Fluphenazine Flutamide Fosamprenavir Foscarnet Fosphenytoin Fostemsavir Gatifloxacin Gemifloxacin Gilteritinib Glasdegib Goserelin Granisetron Grepafloxacin Halofantrine Haloperidol Halothane Histrelin Hydroxychloroquine Hydroxyzine Ibutilide Idarubicin Idelalisib Iloperidone Imipramine Indinavir Inotuzumab Ozogamicin Isoproterenol Itraconazole Ivabradine Ivosidenib Ketoconazole Lapatinib Lenvatinib Leuprolide Levofloxacin Lisdexamfetamine Lithium Carbonate Lofexidine Lomefloxacin Lonafarnib Lorlatinib Lumacaftor Lumefantrine Macimorelin Maprotiline Mefloquine Mesoridazine Metaproterenol Methadone Methotrimeprazine Midostaurin Mifepristone Mirtazapine Mitotane Modafinil Moxifloxacin Nafcillin Nefazodone Nelfinavir Nevirapine Nilotinib Nilutamide Norfloxacin Nortriptyline Ofloxacin Ondansetron Osilodrostat Osimertinib Oxaliplatin Oxytocin Ozanimod Paliperidone Palonosetron Panobinostat Papaverine Pasireotide Pazopanib Pentamidine Perflutren Perphenazine Pexidartinib Phenobarbital Phenytoin Pimavanserin Pimozide Pitolisant Posaconazole Primaquine Primidone Probucol Procainamide Prochlorperazine Promazine Promethazine Propafenone Propoxyphene Protriptyline Quetiapine Quinidine Quinine Ranolazine Relugolix Ribociclib Rifabutin Rifampin Rifapentine Rilpivirine Risperidone Ritodrine Ritonavir Romidepsin Saquinavir Selpercatinib Sertraline Sevoflurane Siponimod Solifenacin Sorafenib Sotalol Sparfloxacin Sunitinib Tacrolimus Tamoxifen Telaprevir Telavancin Telithromycin Terbutaline Terfenadine Tetrabenazine Thioridazine Tizanidine Toremifene Tramadol Trazodone Triclabendazole Trifluoperazine Triflupromazine Trimeprazine Trimipramine Triptorelin Troleandomycin Tucatinib Valbenazine Vandetanib Vardenafil Vemurafenib Venlafaxine Verapamil Voriconazole Ziprasidone Acalabrutinib Albendazole Albuterol Alfentanil Aliskiren Almotriptan Alpelisib Alprazolam Ambrisentan Aminoglutethimide Amlodipine Amobarbital Apixaban Apremilast Aprepitant Arformoterol Aripiprazole Armodafinil Atorvastatin

Showing 240 of 523. Type above to find a specific drug.

Interaction data compiled from DDInter (academic, CC-BY). Severity classification only - this is not a complete interaction checker and not medical advice.

Sources & citations

[1]MHRA (UK) · PLGB536720001 · revised November 21, 2025
[2]European Medicines Agency · EMEA/H/C/005048 · revised May 27, 2026

Information on this page is compiled from public regulatory records. Drugvu is not affiliated with any regulator or pharmaceutical manufacturer. This is not medical advice. Always consult a qualified healthcare professional.

Side effects & warnings

GBOfficial regulatory label· Adverse reactions· revised November 21, 2025[1]

Summary of the safety profile The most frequently reported adverse reactions are administration site reactions (7%), diarrhoea (7%), nausea (4%), vomiting (2%), hepatic enzyme elevation (2%), headache (1%), hypokalaemia (1%), and insomnia (1%).
Administration site reactions apply to intravenous administration and led to treatment discontinuation in <1%. Gastrointestinal disorders were predominantly associated with the oral formulation of lefamulin and led to treatment discontinuation in <1%.
The most frequently reported serious adverse reaction is atrial fibrillation (<1%). Tabulated list of adverse reactions Based on pooled data from Phase 3 trials for both intravenous and oral formulations, the following adverse reactions have been identified with lefamulin.
Adverse reactions are classified according to System Organ Class and frequency. Frequency categories are defined as: very common (≥1/10), common (≥1/100 to <1/10), uncommon (≥1/1,000 to <1/100), rare (≥1/10,000 to <1/1,000), very rare (<1/10,000), and not known (cannot be estimated from the available data).
Table 3:
Frequency of adverse reactions by system organ class from clinical trials System organ class Common Uncommon Infections and infestations Clostridioides difficile colitis Oropharyngeal candidiasis Vulvovaginal mycotic infection Blood and lymphatic system disorders Anaemia Thrombocytopenia Metabolism and nutrition disorders Hypokalaemia Psychiatric disorders Insomnia Anxiety Nervous system disorders Headache Dizziness Somnolence Cardiac disorders Electrocardiogram QT prolonged Atrial fibrillation Palpitations Respiratory, thoracic and mediastinal disorders Oropharyngeal pain Gastrointestinal disorders Diarrhoea Nausea Vomiting Abdominal pain Abdominal pain upper Constipation Dyspepsia Epigastric discomfort Gastritis Gastritis erosive Hepatobiliary disorders Alanine aminotransferase increased* Aspartate aminotransferase increased* Alkaline phosphatase increased Gamma- glutamyltransferase increased Renal and urinary disorders Urinary retention General disorders and administration site conditions Infusion site pain Infusion site phlebitis Infusion site erythema Infusion site bruising Infusion site coldness Investigations Creatinine phosphokinase increased *In Phase 3 trials (pooled data for intravenous and oral formulations), post-baseline alanine aminotransferase values >3x and >5x ULN occurred in 5% and 2% of Xenleta patients compared with 5% and 1% of moxifloxacin patients.
Post-baseline aspartate aminotransferase values >3x and >5x ULN occurred in 4% and 1% of Xenleta patients compared with 2% and 1% of moxifloxacin patients. Those affected were asymptomatic with reversible clinical laboratory findings that typically peaked within the first week of Xenleta dosing.
No Xenleta patient met Hy’s Law criteria. Reporting of suspected adverse reactions Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product.
Healthcare professionals are asked to report any suspected adverse reactions via the national reporting system listed in Appendix V.

GBOfficial regulatory label· Warnings and precautions· revised November 21, 2025[1]

Prolongation of QTc interval and potential QTc-interval prolongation-related clinical conditions Changes in cardiac electrophysiology have been observed in nonclinical and clinical studies with lefamulin. 4 msec. 7% of patients, respectively, and were more frequent following intravenous lefamulin dosing compared to oral dosing.
The magnitude of QT prolongation may increase with increasing concentrations of lefamulin or increasing the rate of infusion of the intravenous formulation. Therefore, the recommended dose and infusion rate should not be exceeded. Lefamulin should be used with caution in patients with renal failure who require dialysis because metabolic disturbances associated with renal failure may lead to QT prolongation.
Lefamulin should be used with caution in patients with mild, moderate, or severe cirrhosis because metabolic disturbances associated with hepatic insufficiency may lead to QT prolongation. Clostridioides (formerly known as Clostridium) difficile- associated diarrhoea C.
difficile associated diarrhoea (CDAD) has been reported with lefamulin and may range in severity from mild diarrhoea to fatal colitis. 8). Careful medical history is necessary since CDAD has been reported to occur over two months after the administration of antibacterial medicinal products.
If CDAD is suspected or confirmed, ongoing antibacterial medicinal product use not directed against C. difficile may need to be discontinued. Appropriate supportive measures together with the administration of specific treatment for Clostridioides difficile should be considered.
Non-susceptible microorganisms Prolonged use may result in the overgrowth of non-susceptible organisms which may require interruption of treatment or other appropriate measures. 8). Hepatic impairment Patients with moderate (Child-Pugh Class B) or severe (Child-Pugh Class C) hepatic impairment have reduced lefamulin protein binding compared to healthy subjects or subjects with mild (Child-Pugh Class A) hepatic impairment.
Treatment should be initiated in patients with moderate or severe hepatic impairment only after a careful benefit/risk evaluation, due to possible adverse reactions related to higher free concentrations of lefamulin, including prolongation of the QTcF interval.

This is not medical advice. Consult a qualified healthcare professional.