TBI-223 is an oxazolidinone with excellent oral bioavailability and activity against Gram-positive bacteria, works as protein synthesis inhibitor, targets an early step involving the binding of N-formylmethionyl-tRNA to the ribosome.
TBI-223 showed reduced human and mouse bone marrow progenitor cell toxicity in vitro and bone marrow toxicity in rat and dog models in vivo, compared to linezolid.
TBI-223 had broader efficacy against other antibiotic-resistant Gram-positive bacteria, including vancomycin-resistant enterococci, penicillin- and ceftriaxone-resistant Streptococcus pneumoniae, and coagulase-negative staphylococci
TBI-223 had activity in vitro and in vivo against other bacteria, such as drug-sensitive and drug-resistant Mycobacterium tuberculosis.
TBI-223 had significant efficacy against MRSA infections, including in bacteremia, nondiabetic and diabetic skin wound infections, and OIAI.
TBI-223 had efficacy comparable to that of linezolid in all of the mouse models of bacteremia, nondiabetic and diabetic skin wound models, and OIAI.