Drug intelligence / Profile preview

negamycin

Development stage
Preclinical
Lead developer
Appili Therapeutics
Modality
Peptides, Small Molecules
Administration
Intravenous, Intramuscular
01

Overview

Negamycin is a **natural antibacterial agent** originally isolated from *Streptomyces* species. It is classified as a **pseudodipeptide/peptide-like antibiotic** with broad-spectrum activity against Gram-negative and Gram-positive bacteria including resistant strains. Negamycin exerts its antibacterial effects by targeting the **bacterial ribosome**: specifically, it binds in the vicinity of helix 34 of the 16S rRNA in the small ribosomal subunit. Its mechanism hinges on stabilizing near-cognate aminoacyl-tRNAs on the ribosome and thus promotes **translational miscoding and stalling**, interfering with mRNA decoding and translocation during protein synthesis. Although its main use is antibacterial, research has explored its use for promoting readthrough of premature stop codons in genetic disorders. It is highly water soluble, amphoteric, and has low toxicity in animals. Clinically, it is used to manage **severe bacterial infections** such as urinary tract infections, respiratory tract infections (including pneumonia), bone and joint infections, CNS infections like meningitis, septicaemia and intra-abdominal infections. It is also noted for efficacy against bacteria resistant to other antibiotics and sometimes in combination regimens for tuberculosis[1][2][3][4][5][6][7][9].

Other names
2-[[[(3R,5R)-3,6-diamino-5-hydroxyhexanoyl]amino]-methylamino]acetic acid3,6-diamino-5-hydroxyhexanoic acid 2-(carboxymethyl)-2-methylhydrazideL-threo-Hexonic acid, 3,6-diamino-2,3,4,6-tetradeoxy-, 2-(carboxymethyl)-2-methylhydrazide
02

Targets

70S ribosome (Bacterial protein synthesis ribosome complex)

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