Synonyms: CRS-3123 | REP-3123 | REP3123
Compound class:
Synthetic organic
Comment: CRS3123 is an orally bioactive, diaryldiamine compound that inhibits bacterial methionyl-tRNA synthetases in Gram-positive bacteria [1]. It has limited antibacterial activity against normal anaerobic gut flora (e.g. Clostridium ramosum, bifidobacteria, lactobacilli of the Lactobacillus casei-rhamnosus-plantarum group) and Gram-negative anaerobes.
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References |
1. Citron DM, Warren YA, Tyrrell KL, Merriam V, Goldstein EJ. (2009)
Comparative in vitro activity of REP3123 against Clostridium difficile and other anaerobic intestinal bacteria. J Antimicrob Chemother, 63 (5): 972-6. [PMID:19240076] |
2. Lomeli BK, Galbraith H, Schettler J, Saviolakis GA, El-Amin W, Osborn B, Ravel J, Hazleton K, Lozupone CA, Evans RJ et al.. (2019)
Multiple-Ascending-Dose Phase 1 Clinical Study of the Safety, Tolerability, and Pharmacokinetics of CRS3123, a Narrow-Spectrum Agent with Minimal Disruption of Normal Gut Microbiota. Antimicrob Agents Chemother, 64 (1). [PMID:31685472] |
3. Nayak SU, Griffiss JM, Blumer J, O'Riordan MA, Gray W, McKenzie R, Jurao RA, An AT, Le M, Bell SJ et al.. (2017)
Safety, Tolerability, Systemic Exposure, and Metabolism of CRS3123, a Methionyl-tRNA Synthetase Inhibitor Developed for Treatment of Clostridium difficile, in a Phase 1 Study. Antimicrob Agents Chemother, 61 (8). DOI: 10.1128/AAC.02760-16 [PMID:28584140] |