Drug intelligence / Profile preview

amikacin + tigecycline

Development stage
Preclinical
Lead developer
Pfizer
Modality
Small Molecules
Administration
Intravenous, Inhalation, Intramuscular
01

Overview

Amikacin + tigecycline is a combination of two antibiotics used primarily in research and clinical practice for the treatment of multidrug-resistant bacterial infections, particularly those caused by carbapenem-resistant Enterobacteriaceae (CRE) and nontuberculous mycobacteria such as Mycobacteroides abscessus. Amikacin is an aminoglycoside antibiotic that binds to the 30S ribosomal subunit, causing misreading of mRNA and inhibiting protein synthesis, leading to bactericidal activity. Tigecycline is a glycylcycline antibiotic structurally related to minocycline; it inhibits bacterial protein synthesis by binding to the 30S ribosomal subunit and blocking entry of amino-acyl tRNA into the A site, resulting in bacteriostatic activity[6][8][9]. The combination has demonstrated synergistic effects both in vitro and in vivo against resistant Gram-negative bacteria such as KPC-producing Klebsiella pneumoniae, reducing mutational frequency and suppressing resistance emergence more effectively than either agent alone or other combinations like colistin-based regimens[1][3][4][5]. This synergy makes it a promising option for difficult-to-treat infections where monotherapy may fail due to rapid resistance development.

02

Targets

Bacterial Ribosome

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