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Enanta Initiates Phase 1 Study on EDP-322, an Oral Antibiotic With Activity Against Hospital- and Community-Acquired MRSA

Tuesday, September 16, 2008 General News
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WATERTOWN, Mass., Sept. 15 Enanta Pharmaceuticals, aleader in the development of small molecule anti-infective drugs, announcedtoday the initiation of a Phase 1 study on investigational oral antibioticEDP-322, a first-in-class MRSA-active Bicyclolide, a novel macrolide-relateddrug class with a distinct resistance profile. The clinical developmentprogram for EDP-322 will include the treatment of hospital- andcommunity-acquired gram-positive infections, including methicillin-resistantStaphylococcus aureus (MRSA). Preclinically, EDP-322 has demonstrated strongin vitro activity against hospital-acquired MRSA strains resistant tovancomycin, Zyvox(R) (linezolid), and CUBICIN(R) (daptomycin).
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"Macrolides have been commonly prescribed to treat community infectionsfor decades due to their convenient oral dosing and favorable safety profile,"said Robert Moellering, M.D., a professor of medicine at Harvard MedicalSchool and Beth Israel Deaconess Medical Center. "Now with the discovery of anew generation of macrolides having high potency against hospital-acquiredpathogens and a distinct resistance profile relative to other hospitalantibiotics, there is a tremendous new opportunity to explore their use withinnot only the community, but the hospital setting as well."
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"In our in vitro studies, EDP-322 demonstrated good potency against bothhospital- and community-acquired MRSA, even against highly drug-resistant MRSAstrains," explained Yat Sun Or, Ph.D., Senior Vice President of Research andDevelopment at Enanta. "The potency of EDP-322 against hospital-acquiredMRSA, community-acquired MRSA, and other gram-positive pathogens, combinedwith the convenience of oral administration, has the potential to uniquelyposition EDP-322 among marketed MRSA drugs in both the hospital and communitysettings."

Phase 1a Study Design

The Phase 1a, double-blind, placebo controlled study for EDP-322 announcedtoday is a single ascending dose trial in healthy volunteers.

About Enanta's Bicyclolide Research Program

Bicyclolides posses a reengineered back-bone structure of traditionalmacrolide antibiotics. The discovery of Bicyclolide effectiveness againstMRSA and VRE infections is part of Enanta's broad antibiotic research program.Enanta has applied several research strategies to develop these new classes ofantibiotics, including innovative medicinal chemistry approaches to createnovel and proprietary chemical structures. Enanta has applied its chemistryapproach to create a promising pipeline of anti-infective drugs and a vastintellectual property estate.

About MRSA

More than 130,000 people each year need hospital care for MRSA infections,according to the Centers for Disease Control and Prevention. Staphylococcusaureus is a bacterium that can live harmlessly on human skin and is found inthe nose of 20 to 40 percent of healthy individuals, but can sometimes causeinfections when exposed to broken skin. MRSA is a particular type of thebacteria that has developed resistance to many antibiotics, includingmethicillin, making it difficult to treat.

About Enanta

Enanta Pharmaceuticals is a research and development company that uses itsnovel chemistry approach and drug discovery capabilities to create best inclass small molecule drugs in the anti-infective field. At the heart ofEnanta is its commitment to innovative chemistry that surpasses traditionalmedicinal chemistry approaches. Enanta is developing novel protease,polymerase, and cyclophilin-based inhibitors targeted against the Hepatitis Cvirus (HCV). Additionally, the Company has created a new class of macrolideantibiotics, called Bicyclolides, which overcomes bacterial resistance.Antibacterial focus areas include superbugs, respiratory tract infections, andintravenous and oral treatments for hospital and community MRSA. Enanta is aprivately held company with offi
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