Eravacycline (TP-434) is a potent and broad-spectrum antibacterial agent.

Eravacycline dihydrochloride is a synthetic antibiotic that inhibits bacterial protein synthesis by binding to the 30S ribosomal subunit. It exhibits broad-spectrum activity against gram-negative bacteria, excluding P. aeruginosa, and demonstrates exceptional efficacy against major gram-positive pathogens, including methicillin-resistant S. aureus. Eravacycline also shows potent inhibition of the ribosome. It is effective against 90% of bacterial isolates (MIC90) across various species panels at concentrations from ≤0.008 to 2 μg/mL, except for Pseudomonas aeruginosa and Burkholderia cenocepacia, which have MIC90 values of 32 μg/mL for both. The compound is active against multidrug-resistant organisms, even those exhibiting extended-spectrum β-lactamases and resistance to carbapenems. Notably, eravacycline is a potent agent against A. baumannii, even against strains resistant to sulbactam, imipenem/meropenem, levofloxacin, and amikacin/tobramycin. It outperforms comparative antibiotics from the tetracycline class, levofloxacin, amikacin, tobramycin, and colistin, with MIC50/90 values of 0.5/1 mg/L. Moreover, it inhibits six E. coli strains with MICs ranging from 0.125 to 0.25 mg/L[1].

Mice received eravacycline doses escalating twofold (3.125 to 50 mg/kg) bi-daily. The average fAUC/MIC values indicating net stasis and a 1-log kill were 27.97±8.29 and 32.60±10.85, respectively[2]. Eravacycline showed effectiveness in various murine infection models targeting significant Gram-positive and Gram-negative bacteria. In septicemia models using mice, eravacycline achieved a 50% protective dose at ≤1 mg/kg daily against S. aureus, including methicillin-resistant S. aureus (MRSA) and tetracycline-resistant strains, and S. pyogenes. The PD50 for E. coli ranged from 1.2 to 4.4 mg/kg daily[5].