SOUTH SAN FRANCISCO, CA -- (MARKET WIRE) -- 12/22/2005 -- Theravance, Inc. (NASDAQ: THRX) today announced the results from recently completed Phase 1 single-dose and multiple-dose studies in healthy volunteers with TD-2749, a novel, selective 5-HT4 agonist and the lead compound in its gastrointestinal (GI) prokinetic program.
In a double-blind, placebo-controlled study of seven ascending, single doses in 41 healthy volunteers, TD-2749 demonstrated a dose-dependent prokinetic effect with rapid onset at the highest doses and was generally well tolerated. In the double-blind, placebo-controlled multiple-dose study of two doses of TD-2749, given once-daily for 14 days to 20 healthy volunteers, the compound demonstrated modest prokinetic activity and was generally well tolerated. Two subjects on TD-2749 and one subject on placebo demonstrated reversible elevations in liver enzymes in the multiple dose study.
Theravance also announced that it has enrolled the first healthy volunteers in a Phase 1 clinical study designed to assess the safety, tolerability and pharmacokinetics of a second, structurally distinct, investigational GI prokinetic, TD-5108.
Both TD-2749 and TD-5108 are selective 5-HT4 agonists discovered by Theravance through the application of multivalent drug design in a drug discovery program dedicated to finding new medicines for GI motility disorders such as chronic constipation, constipation-predominant irritable bowel syndrome (C-IBS), opioid-induced constipation, functional dyspepsia and diabetic gastroparesis.
Dr. Patrick P. A. Humphrey, Executive Vice President of Research at Theravance, said, "We believe that our multivalent approach to drug discovery has the potential to provide a superior next-generation medicine to treat GI motility disorders. TD-5108 is the seventh drug discovered at Theravance to enter into human clinical testing in the last four years and the second compound in this program to enter into human clinical testing in the last twelve months."
"GI disorders potentially amenable to prokinetic treatment are common," said Michael Kitt, MD, Senior Vice President of Development at Theravance. "The goal for our gastrointestinal motility dysfunction program is to develop a once-a-day oral medicine that is more effective than the market leading medicines." Dr. Kitt added, "We completed Phase 1 single dose and multidose studies in healthy volunteers for TD-2749, the first compound in this program. Results from those studies showed that TD-2749 is clearly a GI prokinetic agent in healthy volunteers. In 2006, we plan to further evaluate TD-2749 and complete the initial Phase 1 program for TD-5108. We will make a decision regarding future clinical development of these compounds based on our evaluation of the data."
