Firm claims biased ligand approach will lead to more effective and safer GPCR-targeting drugs.

Trevena raised $35 million in a Series B round of financing with all its existing investors. The firm says the funds will be used for Phase II trials with its lead heart failure drug TRV120027 and to progress its pipeline of GPCR-biased ligands.

“This financing will allow us to demonstrate clinical proof of concept for TRV120027, the first biased ligand dosed in human clinical trials, and to advance our pain and inflammation programs through discovery and into the clinic,” comments Maxine Gowen, Ph.D., the firm’s president and CEO. “Despite the success of GPCR-targeted drugs to date, there is huge scope to enhance the therapeutic properties of these molecules through more targeted signaling.”

TRV120027 is an angiotensin II type I receptor (AT1R) β-arrestin biased ligand in development for the treatment of acute heart failure.

Trevena is exploiting a drug-discovery platform designed to uncover and differentiate between biological pathways eliciting beneficial and deleterious effects of a target GPCR and then identify a biased ligand that targets only the pathways associated with beneficial effects. The firm claims that in contrast with current GPCR-targeting approaches that tend to activate and deactivate all related signaling pathways, its biased-ligand approach enables the precise targeting and activation/deactivation of specific signaling pathways, resulting in potentially more effective and safer drugs. The approach also provides new insights into novel GPCR biology and could help address targets that would otherwise be difficult to address, the firm adds.

Trevena’s technology hinges on its Advanced Biased Ligand Explorer (ABLE™), platform, which comprises a 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 biological signaling information across multiple GPCRs.

TRV120027 is the firm’s lead compound and the first to start in clinical development. Additional preclinical-stage candidates include lead optimization-stage candidates for the treatment of pain. Targets in the fields of inflammation and oncology supportive care have also been identified.  

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