WALTHAM, Mass.--(BUSINESS WIRE)--X-Chem, Inc. (X-Chem), a privately held biotechnology company applying its innovative drug discovery platform to the generation of novel small molecule therapeutics, announced today a drug discovery partnership with Gilead Sciences, Inc. (Gilead). Under the terms of the agreement, X-Chem will screen its proprietary DEXTM libraries, which contain >120 billion individually DNA-encoded small molecules, toward the discovery of novel, high-value therapeutic leads against targets in antiviral and additional therapeutic areas. Gilead has the option to license drug leads discovered under the collaboration, and will be responsible for further development and commercialization of the resulting programs.
“Gilead is a world leader in antiviral therapeutics,” said Rick Wagner, Ph.D., Chief Executive Officer of X-Chem. “We are eager to deploy X-Chem’s industry-leading DEXTM drug discovery platform against life-threatening diseases and identify new chemical entities toward which Gilead can apply its R&D expertise.”
Under the terms of the agreement, X-Chem will receive an upfront payment, potential licensing fees, and additional payments for the achievement of pre-defined research, development, and regulatory milestones.
About X-Chem’s DNA-Encoded (DEX™) Libraries and Platform
Due
to the size and diversity of the DEXTM library, X-Chem can
discover multiple series of novel, potent and selective lead compounds
at an unprecedented rate of success against a wide range of targets,
including some that previously failed using conventional screening
methods. A number of proprietary innovations in library design,
screening methodology and bioinformatics underlie the exceptional
performance of the DEXTM platform. In particular, X-Chem’s
approach to library construction allows for additional chemical
reactions to become useable in DNA-encoded library synthesis. Together,
these developments result in a much greater repertoire of diversity for
small molecules, which cover a range of categories including fragment
molecules, small molecular weight heterocyclic compounds, and
macrocyclic structures. This diverse library, combined with a heightened
ability to detect active molecules, has yielded a robust process that
has been highly successful against targets categorized as difficult or
intractable.
About DNA-Encoding
The X-Chem drug discovery engine is based
on a library, currently in excess of 120 billion compounds and growing,
generated by iterative combinatorial synthesis of small molecules
tethered to DNA tags that record the synthetic history of the small
molecule. Every small molecule in the library has a unique DNA barcode
attached to it. The library is screened as a mixture using
affinity-based binding to a target of interest. Certain rare molecules
in the library that bind to the target can be “fished out,” while the
rest of the molecules are washed away. DNA sequencing methods are then
used to detect molecules that are enriched when bound to the target. The
diverse nature of the library produces multiple families or clusters of
related molecules that bind to the target, forming a basis for emergent
structure-activity relationships. Structure-activity relationships are
typically used by medicinal chemists to guide iterative chemical
maturation of a molecule into a drug. Based on the synthetic history
encoded in the DNA sequence information, molecules are then made without
the DNA tag attached, and tested for activity in conventional assays.
About X-Chem
X-Chem, Inc. is a privately-owned biotechnology
company based in Waltham, Massachusetts. The company’s mission is to
apply its powerful product engine to the discovery of small molecule
compounds against high-value therapeutic targets. X-Chem has established
partnerships with Roche, AstraZeneca, Bayer, Pfizer, Alexion, MD
Anderson Cancer Center, Sanofi, Janssen, and several other leading
pharmaceutical companies, biotechnology organizations, and academic
centers. For further information on X-Chem, please visit: http://www.x-chemrx.com/.
