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Biotech / Medical : OSI Pharmaceuticals (OSIP) - formerly Oncogene -- Ignore unavailable to you. Want to Upgrade?

To: tom pope who wrote (415)	1/11/2007 9:46:07 AM
From: tom pope	Respond to of 447

8-K, dated yesterday On January 4, 2007, Prosidion Limited ("Prosidion"), the U.K. subsidiary of OSI Pharmaceuticals, Inc. ("OSI") focused on diabetes and obesity, entered into an Exclusive License Agreement (the "License Agreement") with Eli Lilly and Company ("Eli Lilly"), which grants Eli Lilly an exclusive license in specified territories to PSN010, an oral, small molecule activator of glucokinase with potential applications for the treatment of diabetes, and its back-up molecules, together with related intellectual property (the "Licensed Intellectual Property"). Eli Lilly's exclusive license includes the right to develop and commercialize products utilizing the Licensed Intellectual Property in specified territories, as well the right to grant sublicenses thereunder. The License Agreement provides for an upfront payment of $25 million, along with up to $360 million in potential development and sales milestones and other payments, plus royalties on sales of any compounds successfully commercialized from the Licensed Intellectual Property. The foregoing description of the License Agreement does not purport to be complete and is qualified in its entirety by reference to the License Agreement, a copy of which will be filed as an exhibit to OSI's next annual report filed with the United States Securities and Exchange Commission. ITEM 8.01. Other Events. On January 5, 2007, OSI announced that it had entered into the License Agreement with Eli Lilly. A copy of OSI's press release, dated January 4, 2007, is attached hereto as Exhibit 99.1 and is incorporated herein by reference. On January 9, 2007, OSI announced that its 2.0% Convertible Senior Notes due 2025 (the "Notes") are now convertible at the option of the holders and will remain convertible through March 30, 2007, the last trading day of the current fiscal quarter, as provided for in the Indenture governing the Notes. A copy of OSI's press release, dated January 9, 2007, is attached hereto as Exhibit 99.2 and is incorporated herein by reference. A notice setting forth the procedures for converting the Notes has been provided to the holders of the Notes in accordance with the terms of the Indenture and is attached hereto as Exhibit 99.3 and is incorporated herein by reference. On January 10, 2007, Genentech, Inc., OSI's partner for the distribution and sale in the United States of its oncology drug, Tarceva® (erlotinib), announced that the U.S. net sales of Tarceva for the quarter and year ended December 31, 2006 were approximately $107 million and $402 million, respectively.

To: tom pope who wrote (415)	7/25/2007 11:51:57 AM
From: tuck	Read Replies (1) \| Respond to of 447

The grapevine has it that Roche's competing program in glucokinase activation has died after several tries in P2. Speculation is that the therapeutic window was too narrow to justify P3: pipeline.corante.com Definitely raises questions about the approach, but of course the flip side is that Prosidion and Lilly may be in the lead and alone there. Dr. Lowe doesn't mention the other companies in the space. Banyu appears to be there, as does Astra Zeneca. An abstract from the latter suggests solubility and/or plasma protein binding may be a problem for the class, as it makes the point of addressing it. >> Bioorg Med Chem Lett. 2006 May 15;16(10):2705-9. Epub 2006 Feb 28. Design of a potent, soluble glucokinase activator with excellent in vivo efficacy. McKerrecher D, Allen JV, Caulkett PW, Donald CS, Fenwick ML, Grange E, Johnson KM, Johnstone C, Jones CD, Pike KG, Rayner JW, Walker RP. Cardiovascular and Gastrointestinal Research Area, AstraZeneca R&D, Mereside, Alderley Park, Macclesfield, Cheshire SK10 4TG, UK. darren.mckerrecher@astrazeneca.com The optimisation of a series of glucokinase activators is described, including attempts to uncouple the relationship between potency and plasma protein binding, and to better understand the key pharmacokinetic properties of the series. The use of unbound clearance as an optimisation parameter facilitated the identification of GKA50, a compound which combines excellent potency and pharmacokinetics with good free drug levels and solubility, and exhibits in vivo efficacy at 1mg/kg po in an acute rat OGTT model.<< Whether or not those issues torpedoed the older Roche compound is anybody's guess at this point. Interestingly, Lilly had its own program prior to licensing Prosidion's . . . >>Endocrinology. 2005 Sep;146(9):3696-701. Epub 2005 May 26. A novel glucokinase activator modulates pancreatic islet and hepatocyte function. Efanov AM, Barrett DG, Brenner MB, Briggs SL, Delaunois A, Durbin JD, Giese U, Guo H, Radloff M, Gil GS, Sewing S, Wang Y, Weichert A, Zaliani A, Gromada J. Lilly Research Laboratories, Eli Lilly & Company, Essener Bogen 7, 22419 Hamburg, Germany. efanov_alexander@lilly.com The glucose-sensing enzyme glucokinase (GK) plays a key role in glucose metabolism. We report here the effects of a novel glucokinase activator, LY2121260. The activator enhanced GK activity via binding to the allosteric site located in the hinge region of the enzyme. LY2121260 stimulated insulin secretion in a glucose-dependent manner in pancreatic beta-cells and increased glucose use in rat hepatocytes. In addition, incubation of beta-cells with the GK activator resulted in increased GK protein levels, suggesting that enhanced insulin secretion on chronic treatment with a GK activator may be due to not only changed enzyme kinetics but also elevated enzyme levels. Animals treated with LY2121260 showed an improved glucose tolerance after oral glucose challenge. These results support the concept that GK activators represent a new class of compounds that increase both insulin secretion and hepatic glucose use and in doing so may prove to be effective agents for the control of blood glucose levels in patients with type 2 diabetes.<< Cheers, Tuck