New aminoglycoside antibiotics.
BACKGROUND
Nosocomial infections caused by multi-drug resistant (MDR) Gram-negative bacteria are on the increase, often with few or no therapeutic options for treatment. Historically, a successful approach to generate novel antibiotics has been the chemical modification of existing classes, addressing deficiencies such as resistance mechanisms, safety profile or pharmacokinetic parameters. Aminoglycosides (AGs) represent one of the five clinically-used classes (AGs, β-lactams, quinolones, tetracyclines and sulfonamides) with activity against Gram-negative bacteria.


METHODS
A summary of the AG patent literature between the beginning of 2005 and February 2010 with the main focus on novel AG analogs with potential for therapeutic activity against MDR Gram-negative pathogens.


RESULTS
Overview of the patent literature in the aminoglycoside field during the past 5 years including an assessment of the therapeutic potential for the derivatives described.


CONCLUSIONS
A few companies and academic groups have recently reawakened the dormant field of AG antibiotics, successfully applying novel technologies. So far, this has yielded one clinical candidate, ACHN-490, currently undergoing a Phase II evaluation in complicated urinary tract infections.
Dozzo
Paola
P
Achaogen, Inc., 7000 Shoreline Court, South San Francisco, CA 94080, USA.
Moser
Heinz E
HE
D000617:Aminoglycosides / Q000494:pharmacology / Q000627:therapeutic use*; D000900:Anti-Bacterial Agents / Q000494:pharmacology / Q000627:therapeutic use*; D024901:Drug Resistance, Multiple, Bacterial; D006090:Gram-Negative Bacteria / Q000187:drug effects; D016905:Gram-Negative Bacterial Infections / Q000188:drug therapy; D006801:Humans
D000617:Aminoglycosides; D000900:Anti-Bacterial Agents