Peringatan Keamanan

Information on cefiderocol toxicity is not yet available. In case of overdose supportive care is recommended.FDA Label Hemodialysis has proven effective in removing cefiderocol with a 3-4 hour session removing 60% of circulating drug.

Cefiderocol

DB14879

small molecule approved investigational

Deskripsi

Cefiderocol is a cephalosporin antibacterial drug and exerts a mechanism of action similar to other ?-lactam antibiotics.FDA Label Unlike other agents in this category, cefiderocol is a siderophore able to undergo active transport into the bacterial cell through iron channels.A189057 It represents a significant addition to antibacterial treatment option as it has proven to be effective *in vitro* against multidrug resistant strains including extended spectrum ?-lactamase producers and carbapenemase producing bacteria.

Cefiderocol was granted designation as a Qualified Infectious Disease Product and granted priority review status by the FDA on November 14, 2019.L10893 It is indicated for use in complicated urinary tract infections in patients with limited or no alternative treatments available.FDA Label This indication was supported by a positive clinical trial composed of 448 patients with complicated urinary tract infections which demonstrated a 72.6% rate of symptom resolution and bacterial eradication with cefiderocol compared to 54.6% with the comparator, imipenem/cilastatin.A189150 A concern noted in the trial was a 0.3% higher rate of all cause mortality, the cause of which has not been determined.

Struktur Molekul 2D

Berat 752.21
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The terminal elimination half-life of cefiderocol is 2-3 h.[FDA Label]
Volume Distribusi Cefiderocol has a mean volume of distribution of 18 L.[FDA Label]
Klirens (Clearance) Cefiderocol has a mean clearance of 5.18 L/h.[FDA Label]

Absorpsi

A single intravenous dose of 2 g of cefiderocol in healthy patients produces a Cmax of 89.7 mg/L and an AUC of 386 mg\*h/L.FDA Label In patients with complicated urinary tract infections and a creatinine clearance of at least 60 mL/min, doses of 2 g cefiderocol every 8 hours produced an AUC of 394.7 mg*h/L and a Cmax of 138 mg/L. However the infusion rate for this chronic dosing was 3 times the recommended rate. Cmax and AUC are known to increase proportionally with dosage.

Metabolisme

Cefiderocol undergoes a small degree of metabolism to a cefiderocol epimer at the 7 position, cefiderocol catechol-3-methoxy and -4-methoxy, and a pyrrolidine chlorobenzamide product (PCBA).A189033 PCBA undergoes further metabolism to sulfated, methylated, and glucuronidated metabolites. The enzymes involved in these reactions have yet to be identified and cefiderocol has not been shown to interfere in the metabolism of other agents.FDA Label

Rute Eliminasi

98.6% of cefiderocol is eliminated in the urine with 90.6% as the unchanged parent drug.FDA Label The remaining 8% is eliminated as metabolites. 2.8% is eliminated in the feces. Less than 10% of cefiderocol is metabolized.

Interaksi Obat

3 Data
Technetium Tc-99m oxidronate Cefiderocol may decrease effectiveness of Technetium Tc-99m oxidronate as a diagnostic agent.
Betibeglogene autotemcel The risk or severity of adverse effects can be increased when Cefiderocol is combined with Betibeglogene autotemcel.
Exagamglogene autotemcel The risk or severity of myelosuppression can be increased when Exagamglogene autotemcel is combined with Cefiderocol.

Target Protein

Cell division protein pbpB
Penicillin-binding protein 1A mrcA
Penicillin-binding protein 1B ponB
Penicillin-binding protein 2 pbpA
D-alanyl-D-alanine carboxypeptidase DacB dacB

Referensi & Sumber

Artikel (PubMed)
  • PMID: 30730562
    Miyazaki S, Katsube T, Shen H, Tomek C, Narukawa Y: Metabolism, Excretion, and Pharmacokinetics of (14) C-Cefiderocol (S-649266), a Siderophore Cephalosporin, in Healthy Subjects Following Intravenous Administration. J Clin Pharmacol. 2019 Jul;59(7):958-967. doi: 10.1002/jcph.1386. Epub 2019 Feb 7.
  • PMID: 29061741
    Ito A, Sato T, Ota M, Takemura M, Nishikawa T, Toba S, Kohira N, Miyagawa S, Ishibashi N, Matsumoto S, Nakamura R, Tsuji M, Yamano Y: In Vitro Antibacterial Properties of Cefiderocol, a Novel Siderophore Cephalosporin, against Gram-Negative Bacteria. Antimicrob Agents Chemother. 2017 Dec 21;62(1). pii: AAC.01454-17. doi: 10.1128/AAC.01454-17. Print 2018 Jan.
  • PMID: 6295267
    Kobayashi Y, Takahashi I, Nakae T: Diffusion of beta-lactam antibiotics through liposome membranes containing purified porins. Antimicrob Agents Chemother. 1982 Nov;22(5):775-80. doi: 10.1128/aac.22.5.775.
  • PMID: 30509675
    Portsmouth S, van Veenhuyzen D, Echols R, Machida M, Ferreira JCA, Ariyasu M, Tenke P, Nagata TD: Cefiderocol versus imipenem-cilastatin for the treatment of complicated urinary tract infections caused by Gram-negative uropathogens: a phase 2, randomised, double-blind, non-inferiority trial. Lancet Infect Dis. 2018 Dec;18(12):1319-1328. doi: 10.1016/S1473-3099(18)30554-1. Epub 2018 Oct 25.
Textbook
  • ISBN: 978-1-25-958473-2
    Brunton LL, Hilal-Dandan R, Knollmann BC. eds (2018). Goodman & Gilman's: The Pharmacological Basis of Therapeutics (13th ed.). McGraw-Hill Education.

Contoh Produk & Brand

Produk: 2 • International brands: 0
Produk
  • Fetcroja
    Injection, powder, for solution • 1 g • Intravenous • EU • Approved
  • Fetroja
    Injection, powder, for solution • 1 g/10mL • Intravenous • US • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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