Contact Information: Contact Person: Lorrie Daggett Activx Biosciences, Inc. Email: Telephone Number: 858-526-2505 Website: www.activx.com
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
| Source: Activx Biosciences, Inc.
LA JOLLA, CA--(Marketwire - 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:
lorried@activx.com