Project hopes to lead to safer GPCR therapeutic candidates and research tools.

Trevena has been awarded a $7.65 million Grand Opportunity grant from the NIH, to fund a project focused on the identification and characterization of functionally selective biased ligands against GPCRs. Biased GPCR ligands are highly selective binders that either activate or block selective GPCR-mediated signaling pathways.
The project will initially encompass six GPCRs, selected by Trevena using proprietary biological hypotheses. The company will then design and use appropriate assays to identify biased ligands against each receptor. In the second phase of the project, the biased ligands will be optimized for selectivity and potency. The resulting GPCR ligands will be available for study and development both as research tools and as potential therapeutic candidates.

“This grant supports not only Trevena’s work in identifying and characterizing biased ligands for important GPCRs but enables us to share these findings with leading researchers in the field to advance the understanding of GPCR biology,” comments Maxine Gowen, Ph.D., president and CEO.

Trevena is leveraging a fully integrated platform, Advanced Biased Ligand Explorer, for the development of GPCR therapeutics that specifically target the signal cascade responsible for optimal therapeutic effect, without triggering those that may be involved in concomitant side-effects. The company’s lead in-house project is a beta-arrestin-biased candidate, currently in late preclinical development as a potential treatment for acute heart failure.

In February Trevena signed a GPCR therapeutics research collaboration with Ligand Pharmaceuticals, through which Trevena’s platform will be used to screen targets against Ligand’s combinatorial library of compounds.

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