Next Generation Antibiotics on the Horizon

Jan 03, 2007: Theravance, Inc. announced today that the first patient was dosed in a Phase 2 clinicalstudy of TD-1792, an investigational heterodimer antibiotic, for the treatment of complicated skin and skin structure infections (cSSSI) caused by Gram-positive bacteria, including resistant strains such as methicillin-resistant Staphylococcus aureus (MRSA).

The goal of this program is to develop a next-generation antibiotic that is more efficacious than vancomycin, the current standard of care for the treatment of serious infections caused by MRSA, and which has an improved resistance profile relative to other available antibiotics.

TD-1792 is a unique heterodimer antibiotic discovered by Theravance that combines the antibacterial activities of a glycopeptide and a beta-lactam in one molecule. Theravance initiated the Phase 2 program based upon favorable data from preclinical studies and Phase 1 studies completed during 2006. In randomized, double-blind, placebo-controlled, single- and multiple-ascending dose Phase 1 studies, which enrolled a total of 51 healthy volunteers, TD-1792 was generally well tolerated and displayed linear pharmacokinetics and exposure profiles consistent with once-daily dosing. In preclinical in-vitro studies, TD-1792 demonstrated marked bactericidal activity and was approximately 30-fold more potent than vancomycin against MRSA and approximately 100-fold more potent than oxacillin against methicillin-sensitive Staphylococcus aureus (MSSA).

The Phase 2 randomized, double-blind, active-controlled study is designed to evaluate the safety and efficacy of TD-1792 in patients with cSSSI due to Gram-positive bacteria such as MRSA. Patients will be randomized to receive either TD-1792 dosed once daily or vancomycin dosed twice daily for up to 14 days. The Phase 2 study will be conducted in the United States with a goal of enrolling approximately 200 patients.

"We are excited about the potential of this compound as a next-generation treatment for serious Gram-positive infections, including those caused by MRSA," said Michael Kitt, MD, Senior Vice President of Development at Theravance. "MRSA is a worldwide health problem. We are striving to provide the best medicines to treat the increasing number of patients who are infected with MRSA."

Theravance is a biopharmaceutical company with a pipeline of internally discovered product candidates. Theravance is focused on the discovery, development and commercialization of small molecule medicines across a number of therapeutic areas including respiratory disease, bacterial infections and gastrointestinal motility dysfunction.