A partnership of VAST consequence

LONDON—Australian drug development company Alchemia hasannounced a multitarget drug discovery collaboration agreement using itsproprietary chemistry platform to work with biopharmaceutical giant AstraZenecaPLC.

Alchemia will receive an undisclosed upfront payment andwill be eligible for potential additional payments totaling up to $240 millionupon meeting specified preclinical, clinical and commercial-launch milestones.Alchemia will also be entitled to a single-digit royalty on commercial sales ofproducts developed under the auspices of this collaboration.

The collaboration is based around the use of Alchemia'sproprietary Diversity Scanning Array (DSA) library and associated VersatileAssembly on Stable Templates (VAST) chemistry platform to discover and developnovel small molecules against multiple targets selected by AstraZeneca.

The DSA library is a suite of novel compounds that scans 3Dmolecular shapes and peptidomimetic functionality. The array contains more than14,000 compounds related by shape (chemoform) and/or functionality. The DSAforms the basis for Alchemia's VAST discovery platform, which can be screenedin HTS to identify the shape and binding elements required for targetmodulation. Because hits are related by shape and/or functionality, detailedstructure activity relationships are laid bare for rapid optimization.

Under the terms of this agreement, Alchemia will provideAstraZeneca with its VAST chemistry expertise to help to develop severalsmall-molecule clinical candidates. Initially, Alchemia will provideAstraZeneca with assay-ready screening plates of their entire DSA library.AstraZeneca will internally screen up to 10 targets against this library acrossmultiple research areas including oncology, respiratory, cardiovascular, metabolism,infection and neuroscience.

"Identified hit series will be optimized jointly wherebyAlchemia will contribute primarily with its expertise in the build andsynthesis 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 forone or more of the drug targets in AstraZeneca's project portfolio.

"AstraZeneca was and is attracted by Alchemia's VASTdiscovery platform because the compounds of the DSA library cover a specificthree-dimensional shape space that compounds from AstraZeneca's own screeningcollection basically don't," says Kossenjans. "DSA library compounds are …considered by AstraZeneca to be potentially attractive starting points forseveral ongoing but also emerging drug targets."

"This collaboration has the potential to demonstrate theunique capabilities and value of VAST, and is a pivotal step in thecommercialization 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 andproductive alliance with AstraZeneca over the coming years."

"We have been actively seeking access to novel chemicalequity—compounds that differ significantly from our internal compoundlibrary—to screen against important but challenging biological targets," saysKossenjans. "We were aware of Alchemia's publications about their VASTtechnology in MedChem-relevant journals from 2008 to 2010, and have beentalking 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-approveddrug, Fondaparinux—a generic version of GlaxoSmithKline's Arixtra—which is aninjectable anticoagulant approved in the United States for the prevention andtreatment of deep vein thrombosis after knee or hip surgery. Alchemia'spipeline of oncology products is built upon its proprietary platform HyACT,which is used to selectively target cancer drugs to tumors. Alchemia recentlyannounced the final recruitment for its most advanced cancer drug, HA-Irinotecan,which is in Phase III evaluations for the treatment of metastatic colorectalcancer.

AstraZeneca is a global integrated biopharmaceutical companythat focuses on the discovery, development and commercialization ofprescription medicines, primarily for the treatment of cardiovascular,metabolic, respiratory, inflammation, autoimmune, oncology, infection andneuroscience diseases. Its annual revenue for 2012 was nearly $28 billion, andthe company currently employs nearly 52,000 people globally.