Oritavancin Program

Oritavancin is a novel semi-synthetic glycopeptide antibiotic with potent bactericidal (killing) activity against a broad spectrum of gram-positive bacteria. In its intravenous (IV) formulation, the product candidate has been tested in over 2,100 individuals and has completed two Phase 3 studies for the treatment of complicated skin and skin structure infection (cSSSI) in which the primary endpoints were met. In addition, IV oritavancin completed two Phase 2 trials for the treatment of bacteremia, also with successful outcomes.

Oritavancin is synthetically modified from a naturally occurring compound, and was originally discovered and developed by Eli Lilly to combat a broad spectrum of gram-positive pathogens in response to the emergence of pathogens resistant to vancomycin, the most commonly prescribed antibiotic for resistant gram-positive infections. Targanta acquired worldwide rights to oritavancin from InterMune, Inc. in late 2005.

As a glycopeptide (a short chain of amino acids with attached sugar molecules), oritavancin shares some properties of other members of the glycopeptide class of antibiotics, which includes vancomycin as well as telavancin, for which a U.S. New Drug Application (NDA) was submitted in 2006.

Targanta believes oritavancin's properties may give it distinct advantages over currently marketed therapies for the treatment of serious skin infections:

• Multiple mechanisms of action may lower the likelihood of resistance development.
• Broadest in vitro spectrum of bactericidal activity against gram-positive bacteria
• Unsurpassed in vitro potency versus published data
• Lower incidence of adverse events in clinical trials to date
• Favorable elimination profile, lowering potential for certain adverse events
• Favorable pharmacokinetics, enabling less frequent dosing and possible pharmacoeconomic benefits

Targanta submitted an NDA to the U.S. Food and Drug Administration (FDA) in February 2008 seeking to commercialize oritavancin for the treatment of cSSSI; the FDA accepted the NDA submission for standard review, establishing an action date of December 8, 2008. Additionally, Targanta's Marketing Authorization Application (MAA) for oritavancin was accepted for review by the European Medicines Agency (EMEA) in June 2008. Targanta is also currently conducting a Phase 2 single/infrequent dosing study of IV oritavancin in the treatment cSSSI, and is considering Phase 2/3 development for the treatment of bacteremia and osteomyelitis.

In April 2008, Targanta announced the launch of a program to develop an oral version of oritavancin for the treatment of Clostridium difficile infection including C. difficile-associated diarrhea, or CDAD. C. difficile are anaerobic, gram-positive, spore-forming bacteria that are a major cause of morbidity in the hospitalized elderly. Nosocomial diarrhea is estimated to cost the U.S. healthcare system over $1.1 billion annually, primarily as a result of increased hospital stays.

Targanta holds worldwide marketing and intellectual property rights (greater than 500 patents and patent applications) to oritavancin that extend through 2015.