
Approximately 40% of modern medicinal products target GPCRs and GPCRs remain the largest class of targets currently under clinical evaluation. Currently marketed GPCR drugs suffer significant problems such as limited efficacy and undesirable adverse effects, which generally limit their overall use. Furthermore, there are many GPCRs linked to disease that cannot be translated into medicines because of specific target-related adverse effects.
Trevena’s novel drug discovery approach deploys a proprietary set of tools to uncover the biological pathways eliciting beneficial and deleterious effects of a target GPCR. Trevena then uses its proprietary platform to discover a ‘biased ligand’ that targets only the pathways associated with the beneficial effects. Employing this ‘biased ligand’ method, Trevena is improving on existing medicinal approaches, tackling difficult targets and uncovering novel GPCR biology. Trevena’s approach represents the latest development in targeted therapies and will provide the next generation of GPCR drugs.
G-protein coupled receptors, or GPCRs, make up a large protein family of transmembrane receptors that sense molecules outside of the cell and activate internal signal pathways and cellular responses. Trevena's 'biased ligand' approach to GPCRs enables the targeting and activation or deactivation of specific signaling pathways, as opposed to the current industry approach of activating or deactivating all signaling pathways. This enhanced functional specificity enables Trevena to create agents with increased efficacy and decreased adverse effects.
Trevena’s ABLE™ Platform
Trevena’s proprietary Advanced Biased Ligand Explorer, or ABLE™, platform is the first ever fully assembled set of integrated tools for identifying and characterizing functionally selective biased ligands for a wide range of GPCRs. The platform includes customized assays, proprietary software, animal models and unique biological signaling information across multiple GPCRs.
Trevena uses ABLE™ to generate proprietary biological information highlighting the specific biological pathways and their role in producing either the beneficial or adverse effects of an agent.