- |||||||||| Review, Journal: Fighting against Clostridioides difficile infection: Current medications. (Pubmed Central) - Jun 17, 2024
Currently, researchers are investigating therapeutic antibacterial drugs (e.g., teicoplanin, ridinilazole, ibezapolstat, surotomycin, cadazolid, and LFF571), preventive medications against recurrence (e.g., Rebyota, Vowst, VP20621, VE303, RBX7455, and MET-2), primary prevention strategies (e.g., vaccine, ribaxamase, and DAV132) and other anti-CDI medications in the preclinical stage (e.g., Raja 42, Myxopyronin B, and bacteriophage). This narrative review summarizes current medications, including newly marketed drugs and products in development against CDI, to help clinicians treat CDI appropriately and to call for more research on innovation.
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Semi-synthesis of FK506 and GE2270 A analogues and their therapeutic applications (W183b (McCormick Place Convention Center)) - Aug 9, 2022 - Abstract #ACSFall2022ACS_Fall_13828;
Through late-stage functionalization and co-crystal structure-guided design, we identified a novel calcineurin-sparing analogue to improve the safety margin over FK506 and preserves renal function in animal models of acute kidney injury.Using co-crystal structure guided medicinal chemistry, semi-synthetic analogs of the natural product, GE2270 A, were designed, synthesized, and evaluated in animal models of infection. Chemistry efforts led to the clinical candidate, LFF571, evaluated for the treatment of C. difficile infections in humans.
- |||||||||| Review, Journal: Investigational Treatment Agents for Recurrent Clostridioides difficile Infection (rCDI). (Pubmed Central) - Nov 1, 2020
Various emerging potential therapies with narrow spectrum of activity and little systemic absorption that are in development include 1) Ibezapolstat (formerly ACX-362E), MGB-BP-3, and DS-2969b-targeting bacterial DNA replication, 2) CRS3213 (REP3123)-inhibiting toxin production and spore formation, 3) ramizol and ramoplanin-affecting bacterial cell wall, 4) LFF-571-blocking protein synthesis, 5) Alanyl-L-Glutamine (alanylglutamine)-inhibiting damage caused by C. difficile by protecting intestinal mucosa, and 6) DNV3837 (MCB3681)-prodrug consisting of an oxazolidinone-quinolone combination that converts to the active form DNV3681 that has activity in vitro against C. difficile. This review article provides an overview of these developing drugs that can have potential role in the treatment of rCDI and in lowering recurrence rates.
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