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GEN News Highlights : May 27, 2010

Logical Therapeutics Pockets $16.9M to Advance NSAID Prodrugs

Lead candidate is in Phase IIb/III study comparing the rate of gastric ulcers versus Naprosyn in osteoarthritis patients.

Logical Therapeutics closed on a $16.9 million Series C equity financing. The round was led by existing investor SV Life Sciences and included Burrill & Company, Novo A/S, and Novitas Capital.

Logical Therapeutics is developing a family of NCEs using its patented bio-activated technology, which modifies the chemical structure of nonsteroidal anti-inflammatory drugs (NSAIDs). It aims to develop NSAID prodrugs that reduce gastrointestinal (GI) side effects that are associated with NSAIDs.

The company's lead compound, LT-NS001, is currently being studied in a Phase IIb/III study comparing the cumulative rate of gastric ulcers versus Naprosyn® (naproxen) in osteoarthritis patients after 12 weeks of treatment. Completion of the study is expected in late 2010.

The Series C financing round is expected to provide sufficient capital to advance the firm’s development program through further clinical and nonclinical activities necessary for registration. Logical Therapeutics says that it intends to seek a business partner prior to commercialization.

NSAIDs work by inhibiting the activity of cyclooxygenase (COX) enzymes and thereby blocking the formation of prostaglandins. The induction of NSAID-induced GI ulcers is proposed to follow a two-step process: direct NSAID exposure causing topical irritation followed by exacerbation of the deleterious effect by inhibition of PG synthesis.

LT-NS001 is pharmacologically inactive as a COX inhibitor in the GI tract. Once absorbed into the bloodstream, it is converted rapidly and quantitatively to naproxen. Inside the GI tract, LT-NS001 is lipophilic and neutral as opposed to hydrophilic and acidic as is naproxen. As a result, treatment of patients with LT-NS001 is associated with less GI toxicity including fewer gastric ulcers than treatment with equivalent doses of naproxen. The compound has demonstrated improved GI safety without the need for concomitant alkalinizing agents and their associated risks.

In a Phase I/II double-blind, randomized, active comparator study of LT-NS001 vs. naproxen in volunteers 45 to 70 years of age, subjects receiving LT-NS001 experienced a 79% reduction in the rate of gastric ulcers and fewer gastric and duodenal erosions when compared with those receiving Naprosyn. Overall, subjects in the naproxen arm had 29 total ulcers, while three ulcers were seen in the LT-NS001 arm. Individuals dosed with LT-NS001 or naproxen twice-daily for seven days had the same plasma concentrations of naproxen.