Targanta Presents First Data Demonstrating In Vitro Activity and In Vivo Efficacy of Prodrugs in Osteomyeli...( Prodrugs Generated from Targant...),Health

Prodrugs Generated from Targanta's Novel Drug Discovery Platform

CHICAGO, Sept. 19 /PRNewswire/ -- Targanta Therapeutics Corporation today released detailed data from two studies highlighting the in vitro activity and in vivo efficacy of its proprietary prodrugs in osteomyelitis models. Results are being presented today at the 47th Annual Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC) taking place in Chicago, IL and represent the first data sets from this proprietary platform.

Osteomyelitis is an acute or chronic bone infection predominantly caused by staphylococci, requiring treatment through prolonged parenteral antibiotic administration and, often, surgical intervention. There are currently no antibiotics approved to treat osteomyelitis, which has been designated by the U.S. Food and Drug Administration (FDA) as a significant unmet medical need. Targanta has developed a novel drug discovery platform through which it tethers bone-targeting bisphosphonates to approved antibiotics to generate molecules that deliver the antibiotics directly to the bone, targeting the site of infection.

In the first study, entitled, "Preparation and In Vitro Evaluation of Fluoroquinolone Prodrugs for the Prevention and Treatment of Osteomyelitis," researchers synthesized a total of 45 bisphosphonated fluoroquinolone prodrugs by tethering ciprofloxacin, gatifloxacin or moxifloxacin to a bisphosphonate via cleavable linkers. The affinity of the prodrugs for bone was determined by exposing individual compounds to a suspension of bovine bone powder. Most were found to bind near quantitatively to bone powder and released the parent fluoroquinolone at various rates. In this in vitro study, the high affinity displayed by the compounds for bone powder and their ability to regenerate active parent compound over time suggests they could be used to concentrate antibacterial fluoroquinolones into the bone via systemic administration.

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