Compound

Delpazolid (LCB01-0371)

LegoChem Biosciences, Inc.
Names
delpazolid
Chemical Class:
Oxazolidinone
Name of Target:
Protein Synthesis. Binding to domain V of the 23S rRNA
Description

A novel oxazolidinone with cyclic amidrazone synthesized by LegoChem BioSciences Inc. (Daejeon, Republic of Korea).

July 2018. Comparison of in vitro activity and MIC distributions between the novel oxazolidinone delpazolid and linezolid against multidrug-resistant and extensively drug-resistant Mycobacterium tuberculosis in China.  Zong Z, Jing W, Shi J, Wen S, Zhang T, Huo F, Shang Y, Liang Q, Huang H, Pang Y. Antimicrob Agents Chemother. 2018 May 29. pii: AAC.00165-18. doi: 10.1128/AAC.00165-18.

January 2018. Safety, tolerability and pharmacokinetics of 21 day multiple oral administration of a new oxazolidinone antibiotic, LCB01-0371, in healthy male subjects. Choi Y, Lee SW, Kim A, Jang K, Nam H, Cho YL, Yu KS, Jang IJ, Chung JY. J Antimicrob Chemother. 2018 Jan 1;73(1):183-190. doi: 10.1093/jac/dkx367.

June 2017. Enrolling Phase 2 tuberculosis clinical study in Korea.   https://clinicaltrials.gov/show/NCT02836483

December 2010. In vitro and in vivo activities of LCB01-0371, a new oxazolidinone. Jeong JW, Jung SJ, Lee HH, Kim YZ, Park TK, Cho YL, Chae SE, Baek SY, Woo SH, Lee HS, Kwak JH. Antimicrob Agents Chemother. 2010 Dec;54(12):5359-62. doi: 10.1128/AAC.00723-10. Epub 2010 Sep 20. PMID:  20855730

Abstract:  LCB01-0371 is a new oxazolidinone with cyclic amidrazone. In vitro activity of LCB01-0371 against 624 clinical isolates was evaluated and compared with those of linezolid, vancomycin, and other antibiotics. LCB01-0371 showed good activity against Gram-positive pathogens. In vivo activity of LCB01-0371 against systemic infections in mice was also evaluated. LCB01-0371 was more active than linezolid against these systemic infections. LCB01-0371 showed bacteriostatic activity against Staphylococcus aureus.