June 16th, 2008
AMPK activator compounds demonstrate significant oral bioavailability
WOBURN, Massachusetts, 16 June 2008 - Mercury Therapeutics, Inc. (MTI), a company that discovers and develops orally active protein kinase targeted drugs, is pleased to announce that it has made significant progress in its drug development program in Type-2 diabetes ("T2DM").
This program is focused on the development of an orally-active drug candidate that directly activates AMP activated protein kinase ("AMPK") to improve glucose and lipid metabolism. Drugs that activate AMPK in animals have been reported to lower blood glucose levels, increase insulin sensitivity, the primary defect in T2DM, and lower circulating triglycerides and free fatty acids.
After previously showing significant blood glucose lowering properties, multiple compounds from one of MTI’s two lead series of direct AMPK activators have now also demonstrated significant oral bioavailability. When compared to the blood levels of compound achieved by injection, MTI’s Series 1 compounds exhibited oral bioavailability of 25-45%. Oral bioavailability is considered an essential feature of new chemical entities in the diabetes space. With drugs that might need to be taken multiple times per day for decades as a means to effectively control blood glucose levels within a safe range, compounds that lack oral bioavailability have little commercial potential and are unattractive from a partnering perspective.
Neal C. Birnberg, Ph.D., Mercury Therapeutics’ President and CEO, said: "We are extremely pleased that compounds from our most robust lead series of direct AMPK activators have been shown to exhibit significant oral bioavailability. This is a key milestone in our development program and is especially significant in light of the fact that a competing program at a large pharmaceutical company was terminated last year due solely to a lack of oral bioavailability in its lead compound."
For further information:
Mercury Therapeutics Inc.
Stan Yakatan, Chairman
Tel: +1 786 229 9795
syakatan@aol.com
For Business Development enquiries:
Marquant Partners LLC
Joy Barton, Ph.D, Partner
Tel: +1 561 271 5311
jbarton@marquantpartners.com
www.marquantpartners.com
About Mercury Therapeutics, Inc. (www.mtipharm.com)
MTI is an early stage drug discovery company focusing on the development of small molecule candidates against selected protein kinase drug targets in metabolic diseases and oncology. MTI’s main focus is on the discovery and development of orally active small molecule activators of AMPK, a well-validated though largely unexploited, protein kinase drug target in metabolic disease. While a number of anti-diabetic drugs currently on the market, including metformin (Glucophage®) and pioglitazone (Actos®), act indirectly to activate AMPK, MTI is seeking to develop the first orally available direct AMPK activator. The potential indications of a successful AMPK targeted drug include Type-2 diabetes, hyperlipidemia, obesity, metabolic syndrome and endocrine cancers.
MTI was launched in 2001, and has an exclusive license to a patent from Dartmouth College and St. Vincent's Institute for Biomedical Research in Melbourne, Australia for AMP activated protein kinase (AMPK). In June 2001, MTI launched its R&D operations following execution of a collaboration agreement with Aventis, AG to develop AMPK activators to treat Type-2 diabetes and obesity. In June 2004, Aventis was acquired by Sanofi, and MTI re-acquired all of its intellectual property rights to AMP kinase as well as the rights to develop compounds identified during the collaboration. In October, 2004: MTI secured external financing from XL TechGroup, Inc. In Q4 2005, MTI demonstrated its first preclinical proof-of-principle of active compounds in a glucose tolerance test in mice.