August 20, 2008

Whom It May Concern

KYORIN Co., Ltd.
5 Kanda Surugadai, 2-Chome,
Chiyoda-ku, Tokyo(Stock Code#4569
TSE 1st section）

Results of Overseas Clinical Studies for KRP-104, anti-diabetes agent
Kyorin Pharmaceutical Co., Ltd (Tokyo, President: Mr. Itaru Kojo), a subsidiary ofKyorin Co., Ltd. announced that the target goals of major endpoints of overseas Ph1b (inUS) and Ph2a (in US and India) clinical studies for KRP-104 were achieved. KRP-104 isa DPP-4 inhibitor originated by Kyorin Pharmaceutical and jointly filed IND*1 to US FDA
by Kyorin and ActivX Bioscience, Inc. (California, USA, Chairman, President: Dr. John W.
Kozarich), a wholly owned subsidiary of Kyorin Pharmaceutical.
The open labeled, cross-over, Phase 1b trial of KRP-104 in the US enrolled 28 patientswith type 2 diabetes and showed equivalent efficacy on glucose-lowering to a competitivedrug.
The randomized, double-blind, placebo-controlled, Phase 2a trial enrolled 220 patients(baseline of mean hemoglobin A1c (HbA1c) of 7.9%) with type 2 diabetes inadequately
controlled on metformin alone and compared the efficacy, safety and tolerability inplacebo, 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) *2.
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. In addition,
approximately 40% of patients in both groups achieved the American Diabetes
Association (ADA) recommended guideline of HbA1c < 7%.
Similarly, the secondary efficacy endpoint of fasting plasma glucose (FPG) wassignificantly reduced in the 60 mg BID and 120mg QD dose group compared with placebo,and no significant difference was observed between BID and QD dosages. Kyorin
recognizes that these data supports the possibility of the dosing flexibility of KRP-104.
Concerning the safety and tolerability, both KRP-104 administrated groups were notsubstantially different from placebo group and we confirmed highly safety and tolerabilityof KRP-104. Furthermore, since the safety of KRP-104 has observed in long term
toxicological study in non-human primates, the results of this preclinical toxicologicalstudy supports highly safety and tolerability of KRP-104 in Phase 2a.
Based on the Phase 2a, Kyorin recognizes POC*3 was achieved and will shift up its
licensing activity with further detailed analytical results.
(*1) Abbreviation of Investigational New Drug Application; Submitting FDA to initiates
an investigation drug for clinical trials.
(*2) The regimens of 120mg BID provides greater than 95% inhibition of DPP-4 during
24 hours and QD provides greater than 95% inhibition of DPP-4 during daytimehours.
(*3) Abbreviation of Proof of Concept; Confirmation of efficacy and safety in clinical.

Summary of this trial: Ph1b Study
Subject: Type 2 diabetes patient
Study period: Feb 2008 – June 2008
Design: Crossover Open Study
Primary Endpoint: Continuous Glucose
Monitoring, etc

Summary of this trial:Ph2a Study
Subject: Type 2 diabetes patient
Study period: Sept. 2007 – July 2008
Design: Randomized, Double-Blind,multi-center (Placebo-Control)
Primary Endpoint: HbA1C, etc

Reference About DPP4 inhibitor
New class of oral agents for the treatment of type 2 diabetes which block the degradationof GLP-1, Glucagon Like Peptide-1, one of the digestive hormones which involves insulin
release, so called incretin hormones. GLP-1 mediates glucose-dependent insulin
secretion and is inactivated by DPP-4, an enzyme by which GLP-1 decomposed. DPP4
inhibitor block its hydrolytic degradation of GLP-1 and maintain the activity for insulin
secretion. Unlike other anti-diabetic medication, DPP-4 inhibitor is expected with low
incidence of hypoglycemic event though its glucose dependent insulin secretion.

Contact
Management Planning Dept
KYORIN Co., Ltd.
TEL: 03 3293 3424
FAX: 03 3293 3454