Thursday August 20, 2008

La Jolla, Calif., — Activx Biosciences, Inc., a wholly owned subsidiary of Tokyo-based Kyorin Pharmaceutical Co., Ltd., announced today topline results from their Phase Ib and Phase IIa clinical trials with KRP-104, a dipeptidyl peptidase-4 (DPP-4) inhibitor, for the treatment of type 2 diabetes. In Phase IIa, KRP-104 was shown to be well tolerated and efficacious in the treatment of hyperglycemia in patients with type 2 diabetes resulting in highly significant improvements in glycemic control compared to placebo.

The open labeled, cross-over, Phase Ib trial of KRP-104 in the US enrolled 28 patients with type 2 diabetes and showed equivalent efficacy on glucose-lowering to a competitive drug.

The randomized, double-blind, placebo-controlled, multi-center Phase IIa trial in the US and India enrolled 220 patients with type 2 diabetes inadequately controlled on metformin alone. The study evaluated the safety, tolerability, and efficacy of a total daily dose of 120 mg of KRP-104, administered either as a once daily (QD) dose or as a split dose of 60 mg (BID) added to stable metformin therapy for 12-weeks of treatment. Both dosing regimens provide greater than 95% inhibition of DPP-4 during daytime hours, but the BID dosing regimen provides this high level of inhibition continuously, whereas the QD dose results in considerably less DPP-4 inhibition overnight.

At baseline, the study population had a mean hemoglobin A1c (HbA1c) of 7.9%. Both KRP-104 dose groups demonstrated comparable, highly significant reductions in HbA1c  of -0.64% (p < 0.0001) and -0.54% (p = 0.0003) in the 60 mg BID and 120 mg QD groups, respectively, compared with placebo over 12 weeks. Approximately 40% of patients in both groups achieved the American Diabetes Association (ADA) recommended guideline of HbA1c < 7%. Similarly, KRP-104 significantly reduced the secondary efficacy endpoint of fasting plasma glucose (FPG) in the 60 mg BID and 120mg QD dose group compared with placebo. No significant difference was observed between BID and QD dosages on reduction of HbA1c and FPG.   The safety and tolerability of KRP-104 were not substantially different from placebo.

“These data demonstrate unequivocal, excellent efficacy mediated by KRP-104 that is comparable to the marketed and late stage DPP-4 compounds and supports the dosing flexibility possible with KRP-104 suggested in the studies,” said Dr. Diane Plotkin, Sr. Director of Clinical Development. “The good tolerability observed in this trial is well supported by our extensive preclinical experience including non-human primates,” she added.

“We continue to be optimistic about the potential of KRP-104,” said Dr. John W. Kozarich, Chairman & President of ActivX and Chief Scientific Advisor for Kyorin.  “This Phase IIa trial clearly demonstrates the efficacy of KRP-104 and we believe that our other studies differentiate KRP-104 from the competition and support our position that KRP-104 has best-in-class potential and is an attractive partnering candidate.”

About Activx Biosciences, Inc.
Activx Biosciences, Inc. (, a wholly owned subsidiary of Tokyo-based Kyorin Pharmaceutical Co., Ltd., in La Jolla, California, has drug discovery, proteomics technology and clinical development capabilities. The company applies proprietary chemical technologies and high-throughput protein analysis to the drug discovery and development process. By focusing on functional proteins, ActivX addresses disease mechanisms directly, in contrast to approaches such as expression profiling, in which the measured analyte is several steps removed from the site of drug action. ActivX and its partners are using ActivX’s proprietary technology to address critical challenges in drug discovery, including selectivity profiling of candidate drug molecules across whole protein families in biological samples to guide their medicinal chemistry optimization; identifying novel drug targets and biomarkers; and characterizing off-target activities of candidate and established drugs to understand the basis for their efficacy and toxicity.

About Kyorin Pharmaceutical
Kyorin Pharmaceutical Co. Ltd. ( is a fully integrated, research-oriented pharmaceutical company headquartered in Tokyo, Japan, with a focus in the areas of infectious diseases, immunology and allergic diseases and metabolic diseases. Some of its key products and development compounds include Norfloxacin (first new quinolone antibiotic licensed to Merck and Co.) and Gatifloxacin (new quinolone antibiotic licensed to Bristol-Myers Squibb). In addition to ActivX, Kyorin has extended its research capabilities through the establishment of Kyorin-Scotland Research Laboratories in conjunction with Scottish Biomedical Foundation Limited and with the formation of an affiliate company, Nisshin Kyorin Pharmaceutical Co., Ltd.

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