Tigecycline

Tigecycline (GAR-936) is a broad-spectrum glycylcycline antibiotic. The mean inhibitory concentration (MIC) of Tigecycline for E. coli (MG1655 strain) is approximately 125 ng/mL^[1]. MIC₅₀ and MIC₉₀ are 1 and 2 mg/L for Acinetobacter baumannii (A. baumannii), respectively^[2]. IC50 & Target: Mean MIC: 125 ng/mL (E. coli)^[1]
MIC50: 1 mg/mL (A. baumannii)^[2]
MIC90: 2 mg/mL (A. baumannii)^[2]
In Vitro: Tigecycline (0.63-30 µM, preincubated for 4 days, treated for 72 h) inhibits AML2 cells and HL-60 cells with IC₅₀s of 4.72±0.54 and 3.06±0.85 μM (freshly prepared). Tigecycline inhibits AML2 cells and HL-60 cells with IC₅₀s of 5.64±0.55 and 4.27±0.45 μM (1 day preincubation). Tigecycline inhibits AML2 cells and HL-60 cells with IC₅₀s of 5.02±0.60 and 4.39±0.44 μM (2 day preincubation). Tigecycline inhibits AML2 cells and HL-60 cells with IC₅₀s of 4.09±0.41 and 3.95±0.39 μM (3 day preincubation). After a 4 day preincubation of Tigecycline in saline, Tigecycline lost its ability to kill TEX human leukemia cells (from IC₅₀~5 µM when freshly prepared to IC₅₀>50 µM after 4 days preincubation) as measured by CellTiter Flour assay^[1]. In Vivo: Tigecycline (50 mg/kg; intraperitoneal injection; twice a day; for 11 days) reduces tumor volume and weight in NOD/SCID mice^[1].
The peak plasma concentration (C_max), the terminal half-life (t_1/2), area under the plasma concentration-time curve (AUC), clearance (CL) and volume of distribution (Vz) are 22.8μg/mL, 108.9 min, 1912.2min*μg/mL, 26.1 mL/min/kg, 4109.4 mL/kg for Tigecycline in saline, respectively. The peak plasma concentration (C_max), the terminal half-life (t_1/2), area under the plasma concentration-time curve (AUC), clearance (CL) and volume of distribution (Vz) are15.7μg/mL, 110.3 min, 2036.5 min*μg/mL, 24.6 mL/min/kg, 3906.2 mL/kg for Tigecycline in formulation (60 mg/mL pyruvate, 3 mg/mL ascorbic acid, pH 7 in saline) , respectively^[1].