Omadacycline (hydrochloride)

1196800-39-1

C29H40N4O7.HCl

H2O : >= 50 mg/mL (84.30 mM)

Anti-infection

Omadacycline hydrochloride is novel, aminomethyl tetracycline antibiotic being developed for the treatment of community-acquired bacterial infections. The ED₅₀ for Escherichia coli is 2.02 mg/kg. IC50 & Target: ED50: 2.02 mg/kg (Escherichia coli), 0.30-1.74 mg/kg (Staphylococcus aureus)^[1] In Vitro: The omadacycline MIC_90s for MRSA, VRE, and beta-hemolytic streptococci are 1.0 ug/mL, 0.25 ug/mL, and 0.5 ug/mL, respectively, and the omadacycline MIC90s for PRSP and H. influenzae are 0.25 ug/ml and 2.0 ug/mL, respectively. Omadacycline is active against organisms demonstrating the two major mechanisms of resistance, ribosomal protection and active tetracycline efflux^[1]. Omadacycline inhibits protein synthesis while having no significant effect on RNA, DNA and peptidoglycan synthesis. Further, omadacycline binds to the tetracycline binding site on the 30S subunit of the bacterial ribosome with enhanced binding similar to tigecycline based on additional molecular interactions^[2]. In Vivo: In vivo efficacy of omadacycline is demonstrated using an intraperitoneal infection model in mice. A single intravenous dose of omadacycline exhibits efficacy against Streptococcus pneumoniae, Escherichia coli, and Staphylococcus aureus, including tet (M) and tet (K) efflux-containing strains and MRSA strains. The 50% effective doses (ED₅₀s) for Streptococcus pneumoniae obtained ranged from 0.45 mg/kg to 3.39 mg/kg, the ED₅₀s for Staphylococcus aureus obtained ranges from 0.30 mg/kg to 1.74 mg/kg, and the ED₅₀ for Escherichia coli is 2.02 mg/kg^[1].