MRS-2541

MRS-2541 is a novel, orally bioavailable small-molecule antibiotic that selectively inhibits bacterial methionyl-tRNA synthetase (MetRS), an aminoacyl-tRNA synthetase essential for protein synthesis in Gram-positive bacteria and structurally distinct from the mammalian enzyme.[1][2][10][12] It demonstrates potent in vitro activity against key Gram-positive pathogens including methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant Enterococcus faecium (VRE), Streptococcus pyogenes, and other Enterococcus and Streptococcus species, with MIC values typically ≤0.5 µg/mL and efficacy in murine thigh infection models comparable to linezolid via both oral and subcutaneous dosing.[1][2][7][10][14] Developed by TSRL in collaboration with the University of Washington, MRS-2541 is being advanced as a first-in-class oral agent for acute bacterial skin and skin structure infections (ABSSSI) and broader serious Gram-positive infections, supported by NIH SBIR and related grants for preclinical optimization, ADME/PK profiling, and IND-enabling toxicology.[2][7][10][12][14]

Other names

methionyl-tRNA synthetase inhibitorMetRS inhibitortRNA synthase inhibitor