Uses
Tigecycline mesylate (GAR-936 mesylate) 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].
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 (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 in saline, respectively. 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) 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].
| Animal Model: | NOD/SCID mice with OCI-AML2 acute myeloid leukemia (AML) xenograft model[1] |
| Dosage: | 50 mg/kg |
| Administration: | Intraperitoneal injection; twice a day; for 11 days |
| Result: | Reduced tumor volume and weight. |
| Animal Model: | NOD/SCID mice[1] |
| Dosage: | 50 mg/kg |
| Administration: | Intraperitoneal injection; 360 minutes |
| Result: | 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 22.8 μg/mL, 108.9 min, 1912.2 min*μg/mL, 26.1 mL/min/kg, 4109.4 mL/kg, respectively. |
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. DOI:10.1371/journal.pone.0095281
[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. DOI:10.1016/j.ijantimicag.2018.03.009
