TP-2758

TP-2758 is a fully synthetic 7-methoxy-8-pyrrolidinyltetracycline (glycylcycline-class) antibiotic discovered by Tetraphase Pharmaceuticals as part of a program to generate novel tetracycline analogs with enhanced activity against multidrug-resistant Gram-negative bacteria.[1][2][5] It inhibits bacterial protein synthesis via high-affinity binding to the 30S ribosomal subunit, retaining activity against strains expressing common tetracycline resistance mechanisms such as efflux pumps and ribosomal protection proteins.[1][2] In vitro, TP-2758 demonstrates potent activity against extended-spectrum β-lactamase- and carbapenemase-producing Enterobacteriaceae and Acinetobacter species, as well as methicillin-resistant Staphylococcus aureus and vancomycin-resistant Enterococcus, and shows greater potency than tigecycline against many Gram-negative clinical isolates.[1][2] It is orally bioavailable, with significantly improved oral exposure over tigecycline and higher bioavailability in monkeys than tetracycline, and has shown efficacy when administered orally or intravenously in multiple murine infection models, supporting its development as an empiric treatment for serious hospital-acquired infections including hospital-acquired and ventilator-associated pneumonia, complicated urinary tract infections, and complicated intra-abdominal infections.[1][2] TP-2758 advanced to phase 1 clinical trials as an oral formulation in healthy volunteers, but was later removed from Tetraphase’s pipeline.[2][11]

Other names

TP-2758 hydrochlorideTP2758 hydrochlorideTP 2758 hydrochloride