Drug intelligence / Profile preview

daptomycin + gentamicin

Development stage
Preclinical
Lead developer
Merck
Modality
RNA-Targeting Small Molecules → Nucleic Acid-Directed Small Molecules → Small Molecules, Peptides
Administration
Intravenous, Intramuscular
01

Overview

Daptomycin + gentamicin is a combination of two antibiotics used primarily for the treatment of serious Gram-positive bacterial infections, including methicillin-resistant Staphylococcus aureus (MRSA), methicillin-susceptible Staphylococcus aureus (MSSA), and Enterococcus faecalis, particularly in complicated cases such as endocarditis and implant-associated infections. Daptomycin is a cyclic lipopeptide antibiotic that binds to bacterial cell membranes in a calcium-dependent manner, causing rapid depolarization, inhibition of protein, DNA, and RNA synthesis, and ultimately cell death. Gentamicin is an aminoglycoside antibiotic that binds to the 30S ribosomal subunit of bacteria, inhibiting protein synthesis and leading to bactericidal activity. The combination has demonstrated synergistic effects in vitro and animal models by enhancing bactericidal activity against resistant strains while potentially minimizing toxicity when short-course or single high-dose regimens are used[1][2][3][5][6]. This synergy may help prevent resistance emergence during therapy.

02

Targets

Bacterial Ribosome

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