Establishing the Role of Tigecycline in an era of Antimicrobial Resistance

Jason J. Schafer; Debra A. Goff

Disclosures

Expert Rev Anti Infect Ther. 2008;6(5):557-567. 

In This Article

Chemistry and Mechanism of Action

The chemical name of tigecycline is 9-t-butylglycylamido-minocycline and the molecular formula is C29H39N5O8. The addition of the 9-t-butylglycylamido moiety to the minocycline structure at position nine provides tigecycline with the ability to overcome common tetracycline resistance mechanisms in bacteria - ribosomal modification and efflux pumps (Figure 1). As a result, tigecycline displays a broad spectrum of antibacterial activity.[1,2,3,4,5,6]

Figure 1.

Tigecycline. Reproduced from [2].

Similar to tetracycline antibiotics, tigecycline generally exerts bacteriostatic activity through reversible binding to the 30S ribosomal subunits.[1,4,5,6] This mechanism inhibits bacterial protein translation by interrupting amino-acyl tRNA entrance into the A site of the ribosome, which prevents completion of intracellular peptides. In comparison to tetracycline agents, tigecycline binds with a higher affinity to ribosomal target sites, which may account for its greater in vitro activity.[4] Additional data suggest that the increased affinity of tigecycline for the target site may be the result of differences in binding orientation versus other tetracycline agents.

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