N-[2-[[(1S)-2'-(3-Methylbutoxy)[1,1'-binaphthalen]-2-yl]oxy]acetyl]-D-lysyl-D-arginyl-L-leucine 3-methylbutyl ester hydrochloride

AVX 13616 shows the potent in vivo antibacterial activity of Avexa’s lead antibacterial candidate; particularly against drug-resistant Staphylococcus pathogens. IC50 value: 2-4 ug/ml (MICs) Target: antibacterial agent AVX13616 was as active as mupirocin in a nasal decolonization model but required only a single application. The compounds are being developed for topical indications and/or wound infection/catheter-related infections. AVX13616 and other compounds showed broad spectrum antibacterial activity against a range of isolates with MICs of 2-4 micrograms per millilitre against S. aureus, coagulase negative staphylococci, enterococci, MRSA, VISA and VRSA. A single application of 5% (w/w) AVX13616 (approximately equimolar to 2% mupirocin) was as effective as 2% mupirocin administered twice a day for five days in nasal decolonisation of MRSA in mice.

[1] Avexa Presents Data from Apricitabine and Antibacterial Programs at two International Conferences