Eravacycline (dihydrochloride)

1334714-66-7

C27H33Cl2FN4O8

H2O : 50 mg/mL (79.18 mM; Need ultrasonic)

Anti-infection

Eravacycline dihydrochloride (TP-434 dihydrochloride) is a potent and broad-spectrum antibacterial agent. In Vitro: Eravacycline is potent antibiotic against A. baumannii, including isolates that are resistant to sulbactam, imipenem/meropenem, levofloxacin, and amikacin/tobramycin. Eravacycline shows greater activity than the comparators of the tetracycline class, levofloxacin, amikacin, tobramycin, and colistin. The eravacycline MIC₅₀/₉₀ values are 0.5/1 mg/L^[1]. Eravacycline shows inhibitory effects on six E. coli with MICs ranging from 0.125 to 0.25 mg/L^[2]. Eravacycline dihydrochloride is a synthetic antibiotic, with inhibits bacterial protein synthesis through binding to the 30S ribosomal subunit. Eravacycline displays broad spectrum activity against gram-negative bacteria in the panel except P. aeruginosa, as well as excellent activity against major gram-positive pathogens, including methicillin-resistant S. aureus. Eravacycline also displays potent ribosomal inhibition^[3]. Eravacycline shows potent broad-spectrum activity against 90% of the isolates (MIC₉₀) in each panel at concentrations ranging from <=0.008 to 2 ug/mL for all species panels except those of Pseudomonas aeruginosa and Burkholderia cenocepacia ((MIC₉₀) values of 32 ug/mL for both organisms). Eravacycline is active against multidrug-resistant bacteria, including those expressing extended-spectrum beta-lactamases and mechanisms conferring resistance to other classes of antibiotics, including carbapenem resistance^[4]. In Vivo: Mice are treated with two-fold increasing doses (range 3.125 to 50 mg/kg) of eravacycline every 12 hours. The mean fAUC/MIC magnitude associated with net stasis and 1-log kill endpoint are 27.97 +/- 8.29 and 32.60 +/- 10.85, respectively^[2]. Eravacycline is active in multiple murine models of infection against clinically important Gram-positive and Gram-negative pathogens. Eravacycline is efficacious in mouse septicemia models, demonstrating 50% protective dose values of <=1 mg/kg of body weight once a day (q.d.) against Staphylococcus aureus, including tetracycline-resistant isolates of methicillin-resistant S. aureus (MRSA), and Streptococcus pyogenes. The PD₅₀ values against Escherichia coli isolates are 1.2 to 4.4 mg/kg q.d^[5].