Navigation Links
Targanta Presents First Data Demonstrating In Vitro Activity and In Vivo Efficacy of Prodrugs in Osteomyelitis Models

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.

In the second study, entitled "In Vivo Efficacy of a New Osteotropic Prodrug in a Rabbit Model of Chronic Osteomyelitis," researchers reported on the pharmacokinetics of a rifabutin-bisphosphonate prodrug (TT99000647) and its in vivo efficacy versus both gatifloxacin and rifabutin alone. In the study, osteomyelitis was created in rabbits by injecting Staphylococcus aureus into the medullar cavity of the tibia. Tibiae were harvested 14 days after the end of 28 days of therapy, ground and their bacterial loads determined by plating bone homogenates. The pharmacokinetic study of TT99000647 revealed a Cmax at 303 mcg/g of bone and a terminal half-life of 131 hours in bone. In the efficacy study, treatments resulted in the following proportion of sterilized tibia: 14% (untreated controls); 86% (gatifloxacin, 56 doses of 40 mg/kg); 43% (rifabutin, 10 doses of 30 mg/kg); 43%, 57% and 100% (TT99000647, 4, 7 and 10 doses of 30 mg/kg rifabutin equivalent, respectively). The efficacy demonstrated by rifabutin-bisphosphonate in the rabbit osteomyelitis model in this study suggests further development as a possible therapy for osteomyelitis.

About Targanta Therapeutics

Targanta Therapeutics Corporation is a privately held biopharmaceutical company focused on developing and commercializing innovative antibiotics to treat serious infections in the hospital and other institutional settings. The Company's pipeline includes oritavancin, a semi-synthetic lipoglycopeptide antibiotic, for which Targanta intends to seek U.S. regulatory approval in early 2008, as well as a number of antibacterial agents in pre-clinical development. The company has operations in Cambridge, MA, Indianapolis, IN, Montreal, Quebec, Canada and Toronto, Ontario, Canada. For further information about Targanta, visit the company's website at


All forward-looking statements and other information included in this press release are based on information available to Targanta as of the date hereof, and Targanta assumes no obligation to update any such forward-looking statements or information. Targanta's actual results could differ materially from those described in Targanta's forward-looking statements.

For more information, visit our website at

SOURCE Targanta Therapeutics Corporation
Copyright©2007 PR Newswire.
All rights reserved

Related medicine technology :

1. Targanta Study Shows Oritavancin Treatment Effective in a Mouse Model of Anthrax
2. Targanta Reports Improved Ability of Oritavancin to Stop Bacteria Growth In Vitro Compared With Other Glycopeptide Antibiotics
3. Inspiration Biopharmaceuticals Presents Data From Hemophilia Program at International Society On Thrombosis and Haemostasis (ISTH) Annual Meeting
4. European Society for Medical Oncology (ESMO) Presents Data from the Clinical Trial of MediGenes Cancer-Killing Virus in Press Conference
5. Cytogen Presents Phase 1 Data Showing Promising Antitumor Activity and Safety Profile of Quadramet at International Myeloma Workshop
6. SemBioSys Presents Positive Insulin Data at the American Diabetes Association Conference
7. Tranzyme Pharma Presents Initial Phase IIa Data for its Novel Ghrelin Agonist, TZP-101, in Patients with Diabetic Gastroparesis
8. Novagali Pharma Presents at AACO the Results of its Pivotal Phase III Clinical Trial of Vekacia in Children Suffering From Vernal Keratoconjunctivitis
9. BioLife Solutions Presents Data on CryoStor at International Society for Cellular Therapy Annual Meeting
10. Genaera Presents Preclinical Data on Trodusquemine (MSI-1436) for the Treatment of Obesity at the American Diabetes Association 67th Scientific Session
11. Elixir Pharmaceuticals Presents Preclinical Data Highlighting Its Ghrelin Antagonist Program at the American Diabetes Associations Annual Meeting
Post Your Comments:
(Date:6/24/2016)... CHAPEL HILL, N.C. , June 24, 2016 ... in healthcare decisions and regulators/payers have placed more ... this new environment, patient support programs in the ... support for patients, medications. Consequently, pharmaceutical companies are ... to ensure they are providing products and services ...
(Date:6/24/2016)... DUBLIN , June 24, 2016 ... and Markets has announced the addition of the ... their offering. ... products and provides an updated review, including its applications ... covering the total market, which includes three main industries: ...
(Date:6/24/2016)... ANDOVER, Mass. and SAN CLEMENTE, Calif. ... California -based mobile pulmonary function testing company, is now ... portable PFT devices developed by ndd Medical Technologies , Inc. ... PFT testing done in hospital-based labs.  Thanks to ndd,s EasyOne PRO ... CA , can get any needed testing done in the ...
Breaking Medicine Technology:
(Date:6/26/2016)... ... June 26, 2016 , ... Brent Kasmer, a legally blind and certified personal trainer is helping ... fitness app. The fitness app plans to fix the two major problems leading the fitness ... size fits all type program , They don’t eliminate all the reasons people ...
(Date:6/25/2016)... ... 25, 2016 , ... Austin residents seeking Mohs surgery services, can now turn ... to Dr. Russell Peckham for medical and surgical dermatology. , Dr. Dorsey brings specialization ... selective fellowship in Mohs Micrographic Surgery completed by Dr. Dorsey was under the direction ...
(Date:6/25/2016)... , ... June 25, 2016 , ... First Choice ... States, named Dr. Sesan Ogunleye, as the Medical Director of its new Mesquite-Samuell Farm ... Medical Director of our new Mesquite location,” said Dr. James M. Muzzarelli, Executive Medical ...
(Date:6/25/2016)... ... June 25, 2016 , ... On Friday, June 10, Van Mitchell, Secretary of ... award to iHire in recognition of their exemplary accomplishments in worksite health promotion. , ... Workplace Health & Wellness Symposium at the BWI Marriott in Linthicum Heights. iHire was ...
(Date:6/24/2016)... ... ... Those who have experienced traumatic events may suffer from a complex set ... drug or alcohol abuse, as a coping mechanism. To avoid this pain and suffering, ... traumatic event. , Trauma sufferers tend to feel a range of emotions, from depression, ...
Breaking Medicine News(10 mins):