Patented Screening Tools

Allosteric modulators are an exciting new class of drugs whose emergence has been largely unanticipated by the majority of drug companies.  In essence, the industry has been and, by and large, continues looking for traditional “orthosteric” (i.e. non-allosteric) drugs because high-throughput screening tools tailored to find allosteric drugs are not widely available.

A large number of putative therapeutic targets that have avoided drug discovery after attempts using the state of the art screening tools for orthosteric drugs may now be accessible to allosteric drug discovery efforts. In addition, in the case of peptide receptors, traditional small molecule screening tools are simply inappropriate, whereas allosteric drug discovery tools can be effective. In short, using the allosteric approach, Addex already has shown that it is successfully pursuing  many well studied targets, some of which have resisted decades of orthosteric drug discovery efforts.

Unlike traditional drugs, allosteric drugs do not directly activate or block activation of their targets; instead, they act more like dimmer switches and either facilitate receptor activation or make it more difficult. Finding molecules that do not turn receptors on/off requires different kinds of screening tools since most orthosteric screening platforms have been built to detect activation (or the blocking of activation) of targeted receptors.

Addex is the first company that has developed patented high-throughput industrial discovery tools for allosteric modulators. Addex has developed proprietary real time kinetic and proximal detection systems that permit the identification of allosteric modulators which modify the molecular response of their target. The outcome of the GLP-1 receptor screening and development of assays leading to the discovery of TNFR1 NAM and IL-1R1 NAM illustrate the power of the unique and proprietary technologies discovered and used at Addex.

Many aspects of these technologies have been patented in order to protect and document our leadership position in allosteric modulator drug discovery.  The company’s approach to leveraging and maintaining its competitive advantage is to keep certain aspects of its platform technology as trade secrets while patenting others.

Proprietary screening assays developed at Addex include Phoenyx, ProxyLite, APRA, ADX-tags 1, ADX-tags 2. These assays are used for screening GPCR and non-GPCR drug targets and are necessary to facilitate medicinal chemistry for lead optimization.

Our existing deal with Janssen Pharmaceuticals, Inc. has validated the Addex allosteric modulator discovery platform and demonstrated that it can generate near term revenues through a mix of recurring up front payments and milestones. Between inception in 2002 and 2011 Addex had received partnering related revenues of CHF46.5 million.

The Addex platform is unique and proprietary, making Addex the best place in the world for partners to find technology and expertise to facilitate discovery of small molecule allosteric drugs for a wide variety of challenging therapeutic targets. Addex is pursuing an opportunistic partnering strategy for molecules against specific targets and/or target specific discovery programs such that we avoid placing too much emphasis on any single product and the platform can grow rapidly to generate both near- and long-term value for our shareholders.