Activx Biosciences, Inc. Announces Positive Phase Ib and IIa Clinical Trial Results for KRP-104, a Flexible Dosing DPP-4 Inhibitor for Type 2 Diabetes

LA JOLLA, CA–(EMWNews – August 21, 2008) – 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. (www.activx.com), 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. (www.kyorin-pharm.co.jp) 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.

For more information or a sample copy, Contact: Lorrie Daggett:

[email protected]