Omadacycline (mesylate)

Omadacycline (PTK 0796) mesylate, a first-in-class orally active aminomethylcycline antibacterial, is a member of the tetracycline class of antibiotics. Omadacycline mesylate acts through the inhibition of bacterial protein synthesis by binding to the 30S ribosomal subunit. Omadacycline mesylate possesses broad-spectrum antibacterial activity against aerobic and anaerobic Gram-positive and Gram-negative bacteria, as well as atypical bacteria. Omadacycline mesylate can be used for the research of acute bacterial skin and skin-structure infections, community-acquired pneumonia, and urinary tract infections^[1][2][3][4]. IC50 & Target: bacteria^[1] In Vitro: Omadacycline displays activity against methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant Enterococcus (VRE), beta-hemolytic streptococci, penicillin-resistant Streptococcus pneumonia (PRSP) and Haemophilus influenzae (H. influenzae), with MIC₉₀s of 1.0, 0.25, 0.5, 0.25 and 2.0 μg/mL respectively^[2].
Omadacycline is active against strains expressing tetracycline and other antibiotics resistance by ribosomal protection and active tetracycline efflux^[2]. In Vivo: Omadacycline (0.11-18 mg/kg; a single i.v.) exhibits efficacy against Streptococcus pneumonia, Escherichia coli, and Staphylococcus aureus in mice systemic infection model, with ED₅₀s ranging from 0.30 mg/kg to 3.39 mg/kg^[2].