Tigecycline: A Novel Broad-Spectrum Antimicrobial

Christine M. Slover, PharmD; Keith A. Rodvold, PharmD; Larry H. Danziger, PharmD

Disclosures

The Annals of Pharmacotherapy. 2007;41(6):965-972. 

In This Article

Pharmacology and Mechanism of Action

Tigecycline is the first drug to be approved from the glycylcyclines, a new class of semisynthetic agents.[4] The agents in this class are being developed to overcome bacterial mechanisms of tetracycline resistance such as ribosomal protection and efflux pumps. Tigecycline has a primary backbone of minocycline with an N-alkyl-glycylamido group substituted at the 9 position, which gives this drug its broad spectrum of activity and protection from resistance mechanisms. Tigecycline is generally considered a bacteriostatic antimicrobial, but some in vitro studies have reported bactericidal activity against Streptococcus pneumoniae, Haemophilus influenzae, and Neisseria gonorrhoeae.[4,5] This drug binds to the 30S ribosomal subunit of bacteria and blocks entry of amino-acyl transfer RNA into the A site of the ribosome.[4] Tigecycline binds 5 times more efficiently to this ribosomal site compared with the tetracyclines.[6]

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