Peringatan Keamanan

There are no data available regarding overdosage with sulopenem etzadroxil.

Sulopenem etzadroxil

DB16335

small molecule approved investigational

Deskripsi

Sulopenem etzadroxil is a prodrug of the penem antibacterial sulopenem. Like other beta-lactam antibacterials, it is a time-dependent inhibitor of bacterial cell wall synthesis.L51768

Sulopenem etzadroxil was approved by the FDA in October 2024 for the treatment of uncomplicated urinary tract infections.L51858 It is administered in combination with probenecid in order to increase antibiotic exposure.L51768

Struktur Molekul 2D

Berat 477.61
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) In the fasted state, the mean elimination half-life of sulopenem is 1.18 hours.[L51768] When administered with a high-fat meal, the mean elimination half-life is 1.28 hours.[L51768]
Volume Distribusi In the fasted state, the apparent volume of distribution of sulopenem is 134 liters.[L51768] When administered with a high-fat meal, the apparent volume of distribution is 92.09 liters.[L51768]
Klirens (Clearance) In the fasted state, the apparent clearance of sulopenem is 77.6 L/h.[L51768] When administered with a high-fat meal, the apparent clearance is 50.55 L/h.[L51768]

Absorpsi

Following rapid conversion into the active moiety, sulopenem bioavailability is approximately 40% in the fasted state, increasing to 64% when administered with a meal.L51768

Metabolisme

After oral administration, sulopenem etzadroxil is hydrolyzed via esterases to the active sulopenem, which is further metabolized via hydrolysis and then dehydrogenation.L51768 Two inactive metabolites of sulopenem have been identified - M1a and M1b - which accounted for 21.8% and 43.6%, respectively, of circulating radioactivity following the administration of a radiolabeled dose.L51768

Rute Eliminasi

Following a single oral dose of radiolabeled sulopenem etzadroxil in healthy adult subjects, 44.3% of radioactive product was recovered in the feces (26.9% as unchanged sulopenem) and 40.8% was recovered in the urine (3.1% as unchanged sulopenem).L51768

Interaksi Makanan

1 Data
  • 1. Take with food. The absorption of sulopenem is improved when administered with a meal.

Interaksi Obat

89 Data
Aspartame The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Aspartame.
Pravastatin The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Pravastatin.
Pantoprazole The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Pantoprazole.
Cefotiam The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Cefotiam.
Liothyronine The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Liothyronine.
Conjugated estrogens The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Conjugated estrogens.
Valproic acid The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Valproic acid.
Indomethacin The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Indomethacin.
Aminohippuric acid The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Aminohippuric acid.
Lansoprazole The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Lansoprazole.
Cefalotin The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Cefalotin.
Tenoxicam The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Tenoxicam.
Cefotaxime The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Cefotaxime.
Zidovudine The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Zidovudine.
Cimetidine The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Cimetidine.
Guanidine The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Guanidine.
Piroxicam The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Piroxicam.
Methotrexate The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Methotrexate.
Cephalexin The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Cephalexin.
Enalapril The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Enalapril.
Diclofenac The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Diclofenac.
Oxytetracycline The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Oxytetracycline.
Linezolid The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Linezolid.
Leucovorin The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Leucovorin.
Latanoprost The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Latanoprost.
Furosemide The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Furosemide.
Esomeprazole The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Esomeprazole.
Tetracycline The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Tetracycline.
Acyclovir The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Acyclovir.
Phenylbutazone The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Phenylbutazone.
Cefaclor The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Cefaclor.
Bumetanide The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Bumetanide.
Quinidine The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Quinidine.
Dinoprostone The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Dinoprostone.
Famotidine The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Famotidine.
Salicylic acid The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Salicylic acid.
Acetylsalicylic acid The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Acetylsalicylic acid.
Ganciclovir The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Ganciclovir.
Ketoprofen The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Ketoprofen.
Minocycline The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Minocycline.
Probenecid The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Probenecid.
Mercaptopurine The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Mercaptopurine.
Ibuprofen The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Ibuprofen.
Novobiocin The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Novobiocin.
Benzylpenicillin The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Benzylpenicillin.
Melatonin The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Melatonin.
Ouabain The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Ouabain.
Rosuvastatin The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Rosuvastatin.
Cefadroxil The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Cefadroxil.
Ceftriaxone The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Ceftriaxone.
Gemfibrozil The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Gemfibrozil.
Cefamandole The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Cefamandole.
Cefazolin The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Cefazolin.
Cefoperazone The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Cefoperazone.
Ceftizoxime The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Ceftizoxime.
Cefacetrile The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Cefacetrile.
Ceftibuten The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Ceftibuten.
Liotrix The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Liotrix.
Cilastatin The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Cilastatin.
Tazobactam The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Tazobactam.
trans-2-hydroxycinnamic acid The serum concentration of Sulopenem etzadroxil can be increased when it is combined with trans-2-hydroxycinnamic acid.
Topiroxostat The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Topiroxostat.
Cholic Acid The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Cholic Acid.
Glutaric Acid The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Glutaric Acid.
Benzoic acid The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Benzoic acid.
Taurocholic acid The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Taurocholic acid.
Caprylic acid The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Caprylic acid.
Dronedarone The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Dronedarone.
Ataluren The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Ataluren.
Teriflunomide The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Teriflunomide.
Dabrafenib The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Dabrafenib.
Dolutegravir The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Dolutegravir.
Cefaloridine The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Cefaloridine.
Lenvatinib The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Lenvatinib.
Tafamidis The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Tafamidis.
Encorafenib The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Encorafenib.
Cabotegravir The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Cabotegravir.
Apalutamide The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Apalutamide.
Capivasertib The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Capivasertib.
Vadadustat The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Vadadustat.
Fexinidazole The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Fexinidazole.
Favipiravir The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Favipiravir.
Pradigastat The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Pradigastat.
Enasidenib The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Enasidenib.
Testosterone The excretion of Sulopenem etzadroxil can be increased when combined with Testosterone.
Methyltestosterone The excretion of Sulopenem etzadroxil can be increased when combined with Methyltestosterone.
Testosterone cypionate The excretion of Sulopenem etzadroxil can be increased when combined with Testosterone cypionate.
Testosterone enanthate The excretion of Sulopenem etzadroxil can be increased when combined with Testosterone enanthate.
Pretomanid The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Pretomanid.

Target Protein

Penicillin-binding protein 2 mrdA
Penicillin-binding protein 1A mrcA
Penicillin-binding protein 1B mrcB
D-alanyl-D-alanine carboxypeptidase DacB dacB
Peptidoglycan synthase FtsI ftsI
D-alanyl-D-alanine carboxypeptidase DacA dacA
D-alanyl-D-alanine carboxypeptidase DacC dacC

Referensi & Sumber

Artikel (PubMed)
  • PMID: 35294769
    Zhanel GG, Pozdirca M, Golden AR, Lawrence CK, Zelenitsky S, Berry L, Schweizer F, Bay D, Adam H, Zhanel MA, Lagace-Wiens P, Walkty A, Irfan N, Naber K, Lynch JP 3rd, Karlowsky JA: Sulopenem: An Intravenous and Oral Penem for the Treatment of Urinary Tract Infections Due to Multidrug-Resistant Bacteria. Drugs. 2022 Apr;82(5):533-557. doi: 10.1007/s40265-022-01688-1. Epub 2022 Mar 16.

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