Kissei and GlaxoSmithKline Signed License Agreement for KGA, a Novel Diabetic Medicine

Kissei Pharmaceutical Co., Ltd. (President and CEO: Mutsuo Kanzawa) executed a contract with GlaxoSmithKline (GSK; Head office: England) to provide exclusive development and marketing rights for a selective SGLT1 inhibitor (development code: KGA) originally created and developed by Kissei.

Based on this contract, Kissei will provide GSK with exclusive development and marketing rights throughout the world except Japan, South Korea, China and Taiwan, and receive, from GSK, a contract lump-sum payment, milestone payments in line with various development phases, as well as royalty payments associated with product sales.

KGA is a selective inhibitor against sodium-dependent glucose transporter (SGLT1) originally created and developed by Kissei Pharmaceutical. It is a diabetic medicine with a new mechanism of action of suppressing glucose absorption from the digestive tract and improves postprandial hyperglycemia. The drug has been confirmed, via various types of diabetic animal models, to have postprandial hyperglycemia improvement effects, and is expected to become an effective diabetic medicine that uses a new approach.

Regarding the drug's development status, non-clinical studies are currently being carried out by Kissei. In the future, GSK will conduct clinical studies overseas and aim to gain approval and market the drug in countries where the company owns rights.

In Japan, Kissei executed a licensing agreement in 2005 with Dainippon Sumitomo Pharma Co., Ltd. (formerly Dainippon Pharmaceutical Co., Ltd), and the latter company will carry out clinical studies of the drug and sell it in Japan. Regarding commercialization of the drug, Kissei reserves the right to take part in conducting clinical studies that Dainippon Sumitomo Pharma Co., Ltd carries out, as well as the right to conduct parallel sales.

Moreover, in 2002, Kissei provided GSK with the exclusive development and marketing rights throughout the world except Japan, South Korea, China and Taiwan, for a selective SLGT2 inhibitor (development code: KGT) which Kissei had created and manufactured. At present, KGT's clinical studies are being carried out by GSK.

At Kissei, we position diabetes and other metabolic diseases as one of our key sectors, and concentrate our efforts on researching and developing new drugs. To expand the scale of overseas sales, we are promoting international deployment of products we created and developed through licensing-out.


<References>
Overview of GlaxoSmithKline:
Head office: London, England
Established: December 2000
Chief Executive Officer: J. P. Garnier
For details about Elixir Pharmaceuticals, visit the company's website, at http://www.gsk.com/


Sodium-dependent Glucose Transporter 1 (SGLT1):
One of the glucose transporters involved with the transport of glucose in vivo. It is found in large amounts inside the small intestine, and plays a major role in glucose absorption inside the intestinal tract. SGLT1 inhibitors are expected to improve postprandial hyperglycemia by directly inhibiting the actions of SGLT1 and suppressing glucose's absorption into the intestinal tract. Alpha-glucosidase inhibitors inhibit disaccharidase in the small intestine, suppress the breakdown of disaccharides, and delay postprandial glucose absorption.

Sodium-dependent Glucose Transporter 2 (SGLT2):
One of the glucose transporters involved in the transport of glucose in vivo. It exists specifically inside the kidneys and plays a major role in the glucose reabsorption process inside the kidneys. Although blood glucose is filtered by the kidneys and migrates to the urine, SGLT2 returns glucose back to the blood stream. Although this leads to effective use of energy under near-starvation conditions, in the case of diabetes, it would end up taking in even excessive glucose in vivo.