Tuesday, Jan 22, 1991

Telios Pharmaceuticals and Genentech to Develop Anti-Clotting Drug

San Diego, Calif. -- January 22, 1991 --

Telios Pharmaceuticals Inc. and Genentech Inc. today announced they have entered into a $15 million collaborative research agreement to develop and commercialize an injectable drug to help prevent the formation of blood clots.

Under the agreement , the companies will co-develop a drug based on Telios' proprietary matrix-peptide technology and Genentech's expertise in peptide design and recombinant-receptor assay screening. Genentech will provide Telios with milestone-based payments, and will pay the company royalties on sales. In return, Genentech will have the right to market the drug worldwide, except in Japan and the Far East. Other financial details were not disclosed.

IIb/IIIa Inhibitor

The new drug could be developed as a adjuvant to clot-dissolving agents such as tissue plasminogen activator (t-PA, Activase®) for the treatment of acute myocardial infarction, or heart attack. Known as a IIb/IIIa inhibitor, the drug will be designed to be highly selective in preventing the blood clots that can form due to platelet aggregation, even after thrombolytic therapy.

The IIb/IIIa inhibitor could complement another t-PA adjuvant, argatroban, which Genentech currently has in clinical trials. Argatroban is being tested for its efficacy in inhibiting another part of the clotting process. Other potential applications for the IIb/IIIa inhibitor include preventing re-occlusion of blood vessels after balloon angioplasty, as well as uses in unstable angina, peripheral arterial occlusion and stroke.

"Our agreement is aimed at developing a new class of cardiovascular drugs designed to control blood-clotting with minimal side effects," said Robert J. Erickson, Ph.D., Telios Pharmaceuticals' president and chief operating officer. "By combining our unique technologies and capabilities, we aim to expedite the commercialization of a major therapeutic against cardiovascular disease."

"The collaboration with Telios represents a significant step toward further expanding our cardiovascular markets," said G. Kirk Raab, Genentech's president and chief executive officer. "A IIb/IIIa inhibitor could enhance the efficacy of Activase for a variety of indications , and be and excellent complement to our products on the market and in development."

Matrix Peptide Technology

At the heart of Telios' technology is a protein fragment , or peptide, comprised of a trio of amino acids -- arginine, glycine and aspartic acid -- abbreviated "RGD," and discovered by scientists at the La Jolla Cancer Research Foundation, a nonprofit organization that holds significant equity in Telios. RGD is found in a variety of extracellular-matrix molecules, and mediates key interactions between cells - especially those involved in wound healing, blood clotting and cancer.

Platelets are a type of blood cell that enables the blood to clot. When platelets encounter a damaged or obstructed blood vessel, the IIb/IIIa protein receptor on the surface of each platelet is activated. This caused the platelet to clump or aggregate with each other. Normally a beneficial process to stop bleeding of damaged tissue, platelet aggregation can be a serious problem following cardiovascular treatments such as thrombolytic therapy, angioplasty, or coronary by-pass surgery. RGD peptides could act to block the binding site of the IIb/IIIa receptor, thus preventing it from mediating platelet aggregation.

Telios Pharmaceuticals is a privately held company based in San Diego, Calif. The company is a joint venture established in 1987 by the La Jolla Cancer research Foundation and Hambrecht & Quist Life Science Ventures.

Genentech is a leading biotechnology company focusing on the development , manufacture and marketing of pharmaceuticals produced by recombinant DNA technology.

Activase® is a registered trademark of Genentech, Inc.

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