Navigation Links
Targanta Presents First Data Demonstrating In Vitro Activity and In Vivo Efficacy of Prodrugs in Osteomyelitis Models
Date:9/19/2007

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 http://www.targanta.com.

Disclaimer

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 http://www.targanta.com


'/>"/>
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:
*Name:
*Comment:
*Email:
(Date:4/19/2017)... , April 19, 2017  New research provides evidence that ... Parkinson,s, according to a study released today that will be ... Meeting in Boston , April 22 ... the treatment of Parkinson,s disease, the oral drug levodopa has ... and longevity. But as the disease progresses, the effects of ...
(Date:4/18/2017)... Ohio , April 18, 2017  Cardinal Health ... Non-GAAP 1 fiscal 2017 earnings per share (EPS) ... and 2019.  This is in conjunction with this morning,s ... Deep Vein Thrombosis and Nutritional Insufficiency businesses. ... from continuing operations will be at the bottom of ...
(Date:4/18/2017)... 2017 Research and Markets has announced the ... to their offering. ... arthroscopy devices market to grow at a CAGR of 6.35% during ... Market 2017-2021, has been prepared based on an in-depth market analysis ... and its growth prospects over the coming years. The report also ...
Breaking Medicine Technology:
(Date:4/21/2017)... PA (PRWEB) , ... April 21, 2017 , ... ... firm in Allegheny County that offers services to communities throughout the greater Pittsburgh ... in a charity drive to provide adaptive bicycles for differently-abled children. , Variety ...
(Date:4/21/2017)... ... ... The Patient Advocacy Community of The Beryl Institute presented Eve DeVaro, Director, ... Advocacy Award in recognition of her extraordinary contributions to the field of patient ... Beryl Institute’s annual Patient Experience Conference on March 20 in Denver, Colorado. ...
(Date:4/21/2017)... ... 21, 2017 , ... Crossover Symmetry , an evidence ... active lifestyle company that provides Human Performance Training and education to tactical athletes. ... responders, military officers and others in service through the development and conditioning of ...
(Date:4/21/2017)... ... 2017 , ... Airway Management, the medical device manufacturer of ... and well renowned Asian distributor, Discovery Sleep. The agreement involves the ... and will stabilize and strengthen Airway’s presence with a dedicated, reputable medical device ...
(Date:4/21/2017)... ... April 21, 2017 , ... ... candidates to serve on its Accreditation and Standards Committees to support the ... is improving image quality and reducing patient radiation dose,” reports Eliot Siegel, ...
Breaking Medicine News(10 mins):