Drug intelligence / Profile preview

amikacin + cefepime + fluconazole

Development stage
Unknown
Lead developer
Daiichi Sankyo
Modality
Small Molecules
Administration
Intravenous, Intramuscular, Oral, Inhalation, Intrathecal, Intraventricular
01

Overview

This is a combination of three antimicrobial agents—amikacin, cefepime, and fluconazole—used together for the treatment of severe or mixed infections where both bacterial (including resistant Gram-negative and some Gram-positive organisms) and fungal pathogens are suspected or confirmed. - **Amikacin** is an aminoglycoside antibiotic effective against a broad range of Gram-negative bacteria, including resistant strains such as Pseudomonas aeruginosa and Acinetobacter baumannii. It acts by binding to the 30S ribosomal subunit, inhibiting protein synthesis in bacteria[2]. - **Cefepime** is a fourth-generation cephalosporin beta-lactam antibiotic with activity against both Gram-positive and Gram-negative bacteria, including many that produce beta-lactamases. It inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins[5]. - **Fluconazole** is a triazole antifungal agent that inhibits fungal cytochrome P450 enzyme 14α-demethylase (CYP51), disrupting ergosterol synthesis required for fungal cell membrane integrity[1]. This combination may be used empirically in critically ill patients with healthcare-associated infections when there is concern for multidrug-resistant bacteria as well as invasive fungal infection.

02

Targets

CYP51A1 (Sterol 14α-demethylase)Bacterial RibosomePBP (Penicillin-binding protein family)

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