LA JOLLA, CA, Aug 21 (MARKET WIRE) --
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:
lorried@activx.com
Contact Person:
Lorrie Daggett
Activx Biosciences, Inc.
Email: Email Contact
Telephone Number: 858-526-2505
Website: www.activx.com
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