Peringatan Keamanan

In the case of overdose with lefamulin, the patient should be monitored closely and provided with supportive treatment, according to symptoms and signs. This drug and its active metabolite are not removable by dialysis.L8093

Lefamulin

DB12825

small molecule approved investigational

Deskripsi

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.A183206 Lefamulin is available in intravenous and oral preparations and was granted FDA approval in August 2019.L8093 This drug is the first semi-synthetic pleuromutilin that has been designed for systemic administration. Lefamulin features a novel mechanism of action that shows benefit against resistant bacteria that cause pneumonia.A183161 The chemical structure of lefamulin contains a tricyclic mutilin core that is necessary for some of its antimicrobial activity.A183167

Struktur Molekul 2D

Berat 507.73
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The average elimination half-life of lefamulin is about 8 hours in patients diagnosed with community-acquired bacterial pneumonia.[L8093] One pharmacokinetic study of healthy volunteers revealed a mean half-life of 13.2 hours after an intravenous infusion of lefamulin.[A183227]
Volume Distribusi The average volume of distribution of lefamulin is 86.1 L in patients with community-acquired bacterial pneumonia, but can range from 34.2 to 153 L.[L8093] During clinical studies, lefamulin has been shown to significantly concentrate in the lung tissue, likely increasing its effectiveness in treating pneumonia.[A183167] After lefamulin is administered, penetration into various tissues is observed, and is about 6 times greater in concentration in the fluid of the pulmonary epithelium, when compared with concentrations in the plasma.[A183239] Animal studies demonstrate that lefamulin crosses the placenta.[L8093]
Klirens (Clearance) The total body clearance of lefamulin has been determined to range from 2.94 to 30.0 L/h after an injected dose.[L8093]

Absorpsi

In a pharmacokinetic study of healthy subjects, lefamulin was rapidly absorbed after oral administration. The median Tmax was measured at 1.00 h for the intravenous preparation and 1.76 h for the tablet preparation.A183227At steady-state doses, the Cmax of oral lefamulin is 37.1 mcg/mL.L8093 The AUC at steady-state concentrations of this drug is 49.2 mcg·h/mL. The estimated bioavailability of the oral tablets is 25%. Clinical studies have found that the AUC of lefamulin is decreased by about 10-28% in the fed state.A183167 To optimize absorption, this drug should be administered a minimum of 1 hour before a meal or, at minimum, 2 hours after a meal with water.L8093

Metabolisme

CYP3A4 is the main enzyme responsible for the metabolism of lefamulin.A183167,L8093

Rute Eliminasi

Lefamulin is largely excreted by the gastrointestinal tract and about 14% excreted by the kidneys.A183269 In healthy adult volunteers during clinical trials, a radiolabeled dose of lefamulin was administered. The total radioactivity found to be excreted in the feces was 77.3% on average with 4.2% to 9.1% as unchanged drug when the drug was administered via the intravenous route. A total radioactivity of 88.5% was measured in the feces with 7.8-24.8% as unchanged drug after a dose administered via the oral route. In the urine, it was found to be 15.5% with 9.6-14.1% excretd as unchanged drug after an intravenous dose and 5.3% after an oral dose.L8093

Interaksi Makanan

4 Data
  • 1. Exercise caution with grapefruit products. Grapefruit inhibits CYP3A, which may increase the serum concentration of lefamulin.
  • 2. Exercise caution with St. John's Wort. This herb induces the CYP3A metabolism of lefamulin and may reduce its serum concentration.
  • 3. Take on an empty stomach. This drug should be taken at least 1 hour before or 2 hours after a meal.
  • 4. Take with a full glass of water. The tablet should be swallowed whole with water.

Interaksi Obat

918 Data
Apalutamide The serum concentration of Lefamulin can be decreased when it is combined with Apalutamide.
Metreleptin The metabolism of Lefamulin can be increased when combined with Metreleptin.
Topiramate The metabolism of Lefamulin can be increased when combined with Topiramate.
Oritavancin The metabolism of Lefamulin can be increased when combined with Oritavancin.
Rufinamide The metabolism of Lefamulin can be increased when combined with Rufinamide.
Armodafinil The metabolism of Lefamulin can be increased when combined with Armodafinil.
Glycerol phenylbutyrate The metabolism of Lefamulin can be increased when combined with Glycerol phenylbutyrate.
Eslicarbazepine acetate The metabolism of Lefamulin can be increased when combined with Eslicarbazepine acetate.
Lesinurad The metabolism of Lefamulin can be increased when combined with Lesinurad.
Sarilumab The metabolism of Lefamulin can be increased when combined with Sarilumab.
Rifabutin The metabolism of Lefamulin can be increased when combined with Rifabutin.
Genistein The metabolism of Lefamulin can be increased when combined with Genistein.
Esketamine The metabolism of Lefamulin can be increased when combined with Esketamine.
Calcitriol The metabolism of Lefamulin can be increased when combined with Calcitriol.
Vitamin E The metabolism of Lefamulin can be increased when combined with Vitamin E.
Flunisolide The metabolism of Lefamulin can be increased when combined with Flunisolide.
Troglitazone The metabolism of Lefamulin can be increased when combined with Troglitazone.
Butalbital The metabolism of Lefamulin can be increased when combined with Butalbital.
Flucloxacillin The metabolism of Lefamulin can be increased when combined with Flucloxacillin.
Clobazam The metabolism of Lefamulin can be increased when combined with Clobazam.
Aminoglutethimide The metabolism of Lefamulin can be increased when combined with Aminoglutethimide.
Griseofulvin The metabolism of Lefamulin can be increased when combined with Griseofulvin.
Secobarbital The metabolism of Lefamulin can be increased when combined with Secobarbital.
Cerivastatin The metabolism of Lefamulin can be increased when combined with Cerivastatin.
Betamethasone The metabolism of Lefamulin can be increased when combined with Betamethasone.
Dicloxacillin The metabolism of Lefamulin can be increased when combined with Dicloxacillin.
Rofecoxib The metabolism of Lefamulin can be increased when combined with Rofecoxib.
Fluocinolone acetonide The metabolism of Lefamulin can be increased when combined with Fluocinolone acetonide.
Triamcinolone The metabolism of Lefamulin can be increased when combined with Triamcinolone.
Clofibrate The metabolism of Lefamulin can be increased when combined with Clofibrate.
Hydrocortamate The metabolism of Lefamulin can be increased when combined with Hydrocortamate.
Phenylbutazone The metabolism of Lefamulin can be increased when combined with Phenylbutazone.
Methylphenobarbital The metabolism of Lefamulin can be increased when combined with Methylphenobarbital.
Terbinafine The metabolism of Lefamulin can be increased when combined with Terbinafine.
Prednisolone The metabolism of Lefamulin can be increased when combined with Prednisolone.
Ethanol The metabolism of Lefamulin can be increased when combined with Ethanol.
Methylprednisolone The metabolism of Lefamulin can be increased when combined with Methylprednisolone.
Metyrapone The metabolism of Lefamulin can be increased when combined with Metyrapone.
Probenecid The metabolism of Lefamulin can be increased when combined with Probenecid.
Sulfinpyrazone The metabolism of Lefamulin can be increased when combined with Sulfinpyrazone.
Thiamylal The metabolism of Lefamulin can be increased when combined with Thiamylal.
Budesonide The metabolism of Lefamulin can be increased when combined with Budesonide.
Corticotropin The metabolism of Lefamulin can be increased when combined with Corticotropin.
Cefradine The metabolism of Lefamulin can be increased when combined with Cefradine.
Amobarbital The metabolism of Lefamulin can be increased when combined with Amobarbital.
Aprobarbital The metabolism of Lefamulin can be increased when combined with Aprobarbital.
Cortisone acetate The metabolism of Lefamulin can be increased when combined with Cortisone acetate.
Paramethasone The metabolism of Lefamulin can be increased when combined with Paramethasone.
Barbital The metabolism of Lefamulin can be increased when combined with Barbital.
Deferasirox The metabolism of Lefamulin can be increased when combined with Deferasirox.
Clevidipine The metabolism of Lefamulin can be increased when combined with Clevidipine.
Fosaprepitant The metabolism of Lefamulin can be increased when combined with Fosaprepitant.
Seratrodast The metabolism of Lefamulin can be increased when combined with Seratrodast.
Perampanel The metabolism of Lefamulin can be increased when combined with Perampanel.
Formestane The metabolism of Lefamulin can be increased when combined with Formestane.
Fluprednidene The metabolism of Lefamulin can be increased when combined with Fluprednidene.
Barbexaclone The metabolism of Lefamulin can be increased when combined with Barbexaclone.
Meprednisone The metabolism of Lefamulin can be increased when combined with Meprednisone.
Dexamethasone isonicotinate The metabolism of Lefamulin can be increased when combined with Dexamethasone isonicotinate.
Deflazacort The metabolism of Lefamulin can be increased when combined with Deflazacort.
Cortivazol The metabolism of Lefamulin can be increased when combined with Cortivazol.
Prednylidene The metabolism of Lefamulin can be increased when combined with Prednylidene.
Cloprednol The metabolism of Lefamulin can be increased when combined with Cloprednol.
Fluticasone The metabolism of Lefamulin can be increased when combined with Fluticasone.
Estradiol acetate The metabolism of Lefamulin can be increased when combined with Estradiol acetate.
Estradiol benzoate The metabolism of Lefamulin can be increased when combined with Estradiol benzoate.
Estradiol cypionate The metabolism of Lefamulin can be increased when combined with Estradiol cypionate.
Estradiol dienanthate The metabolism of Lefamulin can be increased when combined with Estradiol dienanthate.
Estradiol valerate The metabolism of Lefamulin can be increased when combined with Estradiol valerate.
Mometasone furoate The metabolism of Lefamulin can be increased when combined with Mometasone furoate.
Hydrocortisone acetate The metabolism of Lefamulin can be increased when combined with Hydrocortisone acetate.
Hydrocortisone succinate The metabolism of Lefamulin can be increased when combined with Hydrocortisone succinate.
Eslicarbazepine The metabolism of Lefamulin can be increased when combined with Eslicarbazepine.
Prednisolone hemisuccinate The metabolism of Lefamulin can be increased when combined with Prednisolone hemisuccinate.
Prednisone acetate The metabolism of Lefamulin can be increased when combined with Prednisone acetate.
Clocortolone acetate The metabolism of Lefamulin can be increased when combined with Clocortolone acetate.
Melengestrol acetate The metabolism of Lefamulin can be increased when combined with Melengestrol acetate.
Betamethasone phosphate The metabolism of Lefamulin can be increased when combined with Betamethasone phosphate.
Cortisone The metabolism of Lefamulin can be increased when combined with Cortisone.
Acetaminophen The metabolism of Lefamulin can be increased when combined with Acetaminophen.
Beclomethasone dipropionate The metabolism of Lefamulin can be increased when combined with Beclomethasone dipropionate.
Medroxyprogesterone acetate The metabolism of Lefamulin can be increased when combined with Medroxyprogesterone acetate.
Testosterone The metabolism of Lefamulin can be increased when combined with Testosterone.
Hydrocortisone The metabolism of Lefamulin can be increased when combined with Hydrocortisone.
Oxcarbazepine The metabolism of Lefamulin can be increased when combined with Oxcarbazepine.
Clobetasol propionate The metabolism of Lefamulin can be increased when combined with Clobetasol propionate.
Fluocinonide The metabolism of Lefamulin can be increased when combined with Fluocinonide.
Hydrocortisone butyrate The metabolism of Lefamulin can be increased when combined with Hydrocortisone butyrate.
Mometasone The metabolism of Lefamulin can be increased when combined with Mometasone.
Fluocortolone The metabolism of Lefamulin can be increased when combined with Fluocortolone.
Prednisolone acetate The metabolism of Lefamulin can be increased when combined with Prednisolone acetate.
Difluocortolone The metabolism of Lefamulin can be increased when combined with Difluocortolone.
Quinupristin The metabolism of Lefamulin can be decreased when combined with Quinupristin.
Dalfopristin The metabolism of Lefamulin can be decreased when combined with Dalfopristin.
Cyproterone acetate The metabolism of Lefamulin can be decreased when combined with Cyproterone acetate.
Dapoxetine The metabolism of Lefamulin can be decreased when combined with Dapoxetine.
Vapreotide The metabolism of Lefamulin can be decreased when combined with Vapreotide.
Lanreotide The metabolism of Lefamulin can be decreased when combined with Lanreotide.
Somatostatin The metabolism of Lefamulin can be decreased when combined with Somatostatin.
Manidipine The metabolism of Lefamulin can be decreased when combined with Manidipine.

Target Protein

50S ribosomal protein L22 rplV

Referensi & Sumber

Artikel (PubMed)
  • PMID: 30513017
    Dillon C, Guarascio AJ, Covvey JR: Lefamulin: a promising new pleuromutilin antibiotic in the pipeline. Expert Rev Anti Infect Ther. 2019 Jan;17(1):5-15. doi: 10.1080/14787210.2019.1554431. Epub 2018 Dec 7.
  • PMID: 30949709
    Rodvold KA: Introduction: lefamulin and pharmacokinetic/pharmacodynamic rationale to support the dose selection of lefamulin. J Antimicrob Chemother. 2019 Apr 1;74(Supplement_3):iii2-iii4. doi: 10.1093/jac/dkz084.
  • PMID: 30019769
    Veve MP, Wagner JL: Lefamulin: Review of a Promising Novel Pleuromutilin Antibiotic. Pharmacotherapy. 2018 Sep;38(9):935-946. doi: 10.1002/phar.2166. Epub 2018 Aug 20.
  • PMID: 30949705
    Bhavnani SM, Zhang L, Hammel JP, Rubino CM, Bader JC, Sader HS, Gelone SP, Wicha WW, Ambrose PG: Pharmacokinetic/pharmacodynamic target attainment analyses to support intravenous and oral lefamulin dose selection for the treatment of patients with community-acquired bacterial pneumonia. J Antimicrob Chemother. 2019 Apr 1;74(Supplement_3):iii35-iii41. doi: 10.1093/jac/dkz089.
  • PMID: 26396535
    Crowther GS, Wilcox MH: Antibiotic therapy and Clostridium difficile infection - primum non nocere - first do no harm. Infect Drug Resist. 2015 Sep 15;8:333-7. doi: 10.2147/IDR.S87224. eCollection 2015.
  • PMID: 27742734
    Paukner S, Riedl R: Pleuromutilins: Potent Drugs for Resistant Bugs-Mode of Action and Resistance. Cold Spring Harb Perspect Med. 2017 Jan 3;7(1). pii: cshperspect.a027110. doi: 10.1101/cshperspect.a027110.
  • PMID: 30949704
    Wicha WW, Prince WT, Lell C, Heilmayer W, Gelone SP: Pharmacokinetics and tolerability of lefamulin following intravenous and oral dosing. J Antimicrob Chemother. 2019 Apr 1;74(Supplement_3):iii19-iii26. doi: 10.1093/jac/dkz087.
  • PMID: 30722059
    File TM Jr, Goldberg L, Das A, Sweeney C, Saviski J, Gelone SP, Seltzer E, Paukner S, Wicha WW, Talbot GH, Gasink LB: Efficacy and Safety of IV-to-Oral Lefamulin, a Pleuromutilin Antibiotic, for Treatment of Community-Acquired Bacterial Pneumonia: The Phase 3 LEAP 1 Trial. Clin Infect Dis. 2019 Feb 4. pii: 5306243. doi: 10.1093/cid/ciz090.
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Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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