From one of the articles: Membrane Active Antim
Post# of 72437
Membrane Active Antimicrobial Peptides: Translating Mechanistic Insights to Design
Quote:
Brilacidin is a small-molecule arylamide mimic of AMPs that shows potent antimicrobial activity against a wide range of drug-susceptible and multidrug-resistant Gram-negative and Gram-positive bacteria (Tew et al., 2002, 2010b; Liu et al., 2004) Brilacidin has a planar, conformationally restrained scaffold with four positive guanadinyl and pyridinyl substitutions and two trufluoromethane hydrophobic substitutions (Figure 4). Brilacidin was first developed by Polymedix Inc. and purchased by Cellceutix corp. in September 2013 (Butler et al., 2017). Brilacidin has completed phase IIa and phase IIb trials for the treatment of acute S. aureus skin and skin structure infections. Compared to daptomycin, the results show no serious adverse effects and the efficacy is similar to daptomycin across all brilacidin treatment groups in 215 patients Similar to other AMPs, brilacidin is a membrane targeting antimicrobial. It causes membrane disruption and shows efficacy in a MRSA keratitis model when applied topically. At 0.5% solution, brilacidin shows minimal irritation and is equally efficacious as vancomycin (Kowalski et al., 2016) In addition to brilacidin, Cellceutix is also developing CTIX-1278 (structure not revealed), a defensin mimetic-compound, against the drug resistant superbug Klebsiella pneumoniae. CTIX-1278 is efficacious in a thigh burden study using a mouse model. The results are encouraging as CTIX-1278 shows similar efficacy compared to carbapenem.
https://www.frontiersin.org/articles/10.3389/...00073/full
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