Drug intelligence / Profile preview

tigecycline

Development stage
Approved
Lead developer
Pfizer
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

Tigecycline is a broad-spectrum, bacteriostatic antibiotic of the glycylcycline class, structurally related to minocycline and derived from tetracyclines. It is administered intravenously and used primarily for complicated skin and skin structure infections, complicated intra-abdominal infections, and community-acquired bacterial pneumonia. Tigecycline acts as a protein synthesis inhibitor by binding reversibly to the 30S ribosomal subunit of bacteria at helix H34, blocking the interaction of aminoacyl-tRNA with the A site of the ribosome. This prevents peptide chain elongation during translation, thereby inhibiting bacterial growth. The drug was developed to overcome common tetracycline resistance mechanisms such as efflux pumps and ribosomal protection proteins through structural modification (addition of an N,N-dimethylglycylamido group at position 9). Tigecycline demonstrates activity against a wide range of Gram-positive and Gram-negative pathogens, including multidrug-resistant organisms[1][2][5][6][7].

Brand names
Tygacil
Other names
tigeciclinatigecyclinum
02

Targets

Bacterial Ribosome

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