Tigecycline (GAR-936) hydrate is a broad-spectrum glycylcycline antibiotic. The mean inhibitory concentration (MIC) of Tigecycline hydrate for E. coli (MG1655 strain) is approximately 125 ng/mL [1]. MIC 50 and MIC 90 are 1 and 2 mg/L for Acinetobacter baumannii ( A. baumannii ), respectively [2].
In Vivo, Tigecycline (50 mg/kg; intraperitoneal injection; twice a day; for 11 days) hydrate reduces tumor volume and weight in NOD/SCID mice[1]. The peak plasma concentration (Cmax), the terminal half-life (t1/2), 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 hydrate in saline, respectively[1].
In Vitro, Tigecycline (0.63-30 µM, preincubated for 4 days, treated for 72 h) hydrate inhibits AML2 cells and HL-60 cells with IC50s of 4.72 and 3.06 μM (freshly prepared)[1].
References:
[1]. Jitkova Y, et al. A novel formulation of tigecycline has enhanced stability and sustained antibacterial and antileukemic activity. PLoS One. 2014 May 28;9(5):e95281.
[2]. Falagas ME, et al. Activity of TP-6076 against carbapenem-resistant Acinetobacter baumannii isolates collected from inpatients in Greek hospitals. Int J Antimicrob Agents. 2018 Aug;52(2):269-271.
In Vivo, Tigecycline (50 mg/kg; intraperitoneal injection; twice a day; for 11 days) hydrate reduces tumor volume and weight in NOD/SCID mice[1]. The peak plasma concentration (Cmax), the terminal half-life (t1/2), 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 hydrate in saline, respectively[1].
In Vitro, Tigecycline (0.63-30 µM, preincubated for 4 days, treated for 72 h) hydrate inhibits AML2 cells and HL-60 cells with IC50s of 4.72 and 3.06 μM (freshly prepared)[1].
References:
[1]. Jitkova Y, et al. A novel formulation of tigecycline has enhanced stability and sustained antibacterial and antileukemic activity. PLoS One. 2014 May 28;9(5):e95281.
[2]. Falagas ME, et al. Activity of TP-6076 against carbapenem-resistant Acinetobacter baumannii isolates collected from inpatients in Greek hospitals. Int J Antimicrob Agents. 2018 Aug;52(2):269-271.