Daptomycin antibacterial activity

Woodworth JR, Nyhart EH, Brier GL, Wolny JD, Black HR. (1992) Single-dose pharmacokinetics and antibacterial activity of daptomycin, a new hpopeptide antibiotic, in healthy volunteers. Antimicrob Agents Chemother 36 318-325. 

Having developed an enzymatic route to remove the fatty acid side chains of the natural A21978C factors, Lilly scientists were able to reacylate the core peptide with different fatty acids to optimise antibacterial activity while minimising toxicity. This led to the discovery of daptomycin, which has a decanoic acid side chain.8... 

The activity of daptomycin against both vancomycin-sensitive and vancomycin-resistant Enterococcus faecalis was greater than that of quinupristin + dalfopristin (5). Daptomycin was as active as quinupristin + dalfopristin but more active than linezolid. At concentrations four times the MIC, daptomycin and vancomycin achieved 99.9% killing of methicillin-resistant Staphylococcus aureus after 8 hours, which was greater than the killing seen with linezolid and quinupristin + dalfopristin. However, the antibacterial activity of daptomycin strongly depended on the calcium concentration of the medium. 

It may also have ANTIPSYCHOTIC activity, dapiprazole hydrochloride dapiprazole. dapitant [inn] (RPR 100893) is a substituted isoindole, a TACHYKININ RECEPTOR ANTAGONIST, selective for the NK,-receptor subtype. It has potential as an ANTIMIGRAINE AGENT, dapsone [ban, inn, usan] is a sulphone with actions similar to SULPHONAMIDES and with ANTIBACTERIAL activity. It can be used as an antileprotic and for infective dermatitis herpetiformis. and is being investigated for the treatment and prevention of Pneumocystis carinii pneumonia (e.g. in AIDS), daptomycin [ban, inn, usan] is an (aminoglycoside) antibiotic. It has antibacterial properties. 

Table 3 In Vitro Antibacterial Activity Daptomycin gainst Grani Positive Bacteria...

Table 4 M Vitro Antibacterial Activity of Daptomycin Against AncibiotiC Resiscant Pathogens...

Lee BL, Sachdeva M, Chambers HR Effect of protein binding of daptomycin on MIC and antibacterial activity. Antimicrob Agent Chemother 1991 35 2505-2508. 

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