Glycylcyclines
What are Glycylcyclines?
Presently, tigecycline is the only glycylcycline approved for antibiotic use.
Tigecycline, sold under the brand name Tygacil, is a tetracycline antibiotic medication for a number of bacterial infections. It is a glycylcycline class drug that is administered intravenously.
List of Glycylcyclines
Fig. 1. Effects of various GAR-936 (a), WAY 152,288 (b), and minocycline (c) dosage regimens on the number of S. pneumoniae ATCC 10813 organisms in the neutropenic mouse thigh muscle infection model after 48 h of treatment. The dashed horizontal line represents the number of CFU per thigh at the start of treatment. ●, single dose; ○, once-daily dose; ▾, twice-daily dose; ▿, four-times-daily dose; ——, single dose; ······, once-daily dose; –––, twice-daily dose; —··, four-times-daily dose; —–, log CFU at start of treatment.
Fig. 2. Dose-effect relationship of the glycylcyclines GAR-936 (a) and WAY 152,288 (b) in an experimental thigh muscle infection withS. pneumoniae 1199 in neutropenic mice. Each point represents the results for a single mouse. The sigmoid curve represents the dose-effect curve established according to the Hill equation.
Fig. 3. In vivo PAE of GAR-936 after administration of 3 mg/kg subcutaneously to neutropenic mice infected with S. pneumoniae ATCC 10813 (a) and E. coli ATCC 25922 (b). t>MIC, period when an active concentration of GAR-936 is present; ●, untreated mice; ○, GAR-936-treated mice.
Fig. 4. Relationship between pharmacokinetic-pharmacodynamic parameters and therapeutic efficacy of GAR-936 (free drug) againstS. pneumoniae 1199 in the neutropenic mouse thigh muscle infection model (R2 = 0.82, 0.83, and 0.54 for panels a, b, and c, respectively). (a) time above the 0.5 × MIC versus effect. (b) Log AUC versus effect. (c) LogCmax versus effect.
