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A partnership of VAST consequence
June 2013
by Jim Cirigliano  |  Email the author
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LONDON—Australian drug development company Alchemia has announced a multitarget drug discovery collaboration agreement using its proprietary chemistry platform to work with biopharmaceutical giant AstraZeneca PLC.  
 
Alchemia will receive an undisclosed upfront payment and will be eligible for potential additional payments totaling up to $240 million upon meeting specified preclinical, clinical and commercial-launch milestones. Alchemia will also be entitled to a single-digit royalty on commercial sales of products developed under the auspices of this collaboration.  
 
The collaboration is based around the use of Alchemia's proprietary Diversity Scanning Array (DSA) library and associated Versatile Assembly on Stable Templates (VAST) chemistry platform to discover and develop novel small molecules against multiple targets selected by AstraZeneca.  
 
The DSA library is a suite of novel compounds that scans 3D molecular shapes and peptidomimetic functionality. The array contains more than 14,000 compounds related by shape (chemoform) and/or functionality. The DSA forms the basis for Alchemia's VAST discovery platform, which can be screened in HTS to identify the shape and binding elements required for target modulation. Because hits are related by shape and/or functionality, detailed structure activity relationships are laid bare for rapid optimization.  
 
Under the terms of this agreement, Alchemia will provide AstraZeneca with its VAST chemistry expertise to help to develop several small-molecule clinical candidates. Initially, Alchemia will provide AstraZeneca with assay-ready screening plates of their entire DSA library. AstraZeneca will internally screen up to 10 targets against this library across multiple research areas including oncology, respiratory, cardiovascular, metabolism, infection and neuroscience.  
 
"Identified hit series will be optimized jointly whereby Alchemia will contribute primarily with its expertise in the build and synthesis of carbohydrate-based peptidomimetics," says Michael Kossenjans, R&D team leader at AstraZeneca.  
 
The aim of the partnership is the identification, optimization and ultimately development of a novel small-molecule modulator for one or more of the drug targets in AstraZeneca's project portfolio.
 
"AstraZeneca was and is attracted by Alchemia's VAST discovery platform because the compounds of the DSA library cover a specific three-dimensional shape space that compounds from AstraZeneca's own screening collection basically don't," says Kossenjans. "DSA library compounds are … considered by AstraZeneca to be potentially attractive starting points for several ongoing but also emerging drug targets."  
 
"This collaboration has the potential to demonstrate the unique capabilities and value of VAST, and is a pivotal step in the commercialization of both the DSA and the VAST platform," Dr. Wim Meutermans, vice president of discovery at Alchemia and co-inventor of the VAST platform, said in a media statement. "I look forward to developing a strong and productive alliance with AstraZeneca over the coming years."  
"We have been actively seeking access to novel chemical equity—compounds that differ significantly from our internal compound library—to screen against important but challenging biological targets," says Kossenjans. "We were aware of Alchemia's publications about their VAST technology in MedChem-relevant journals from 2008 to 2010, and have been talking to them about a potential collaboration for some time."  
Alchemia is a drug development company based in Brisbane, Australia, with a late-stage oncology product pipeline, and one FDA-approved drug, Fondaparinux—a generic version of GlaxoSmithKline's Arixtra—which is an injectable anticoagulant approved in the United States for the prevention and treatment of deep vein thrombosis after knee or hip surgery. Alchemia's pipeline of oncology products is built upon its proprietary platform HyACT, which is used to selectively target cancer drugs to tumors. Alchemia recently announced the final recruitment for its most advanced cancer drug, HA-Irinotecan, which is in Phase III evaluations for the treatment of metastatic colorectal cancer.  
 
AstraZeneca is a global integrated biopharmaceutical company that focuses on the discovery, development and commercialization of prescription medicines, primarily for the treatment of cardiovascular, metabolic, respiratory, inflammation, autoimmune, oncology, infection and neuroscience diseases. Its annual revenue for 2012 was nearly $28 billion, and the company currently employs nearly 52,000 people globally.
 
Code: E061309

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