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May 3, 2012

Merck & Co. Partners with Trevena to Identify Biased GPCR Receptor Ligands

  • Merck & Co. is teaming up with Trevena on a research collaboration focused on exploiting the latter’s technologies to screen for biased ligands against a specified receptor. Trevana is focused on the discovery and development of GPCR-targeting drugs that are biased toward activating only beneficial receptor signaling pathways, to develop drugs with increased specificity, enhanced efficacy, and reduced side-effects.

    The firm’s expertise hinges on its Advanced Biased Ligand Explorer (ABLE™) platform, which generates biological information that can distinguish between the beneficial and adverse signaling pathways at specific receptors, and identify ligands that activate only those pathways associated with therapeutic effect. The ABLE platform comprises a suite of integrated tools and techniques including diverse assays of GPCR function and regulation.

    Trevena’s in-house pipeline is headed by two clinical-stage candidates. TRV027 is undergoing Phase II clinical trials as a treatment for acute heart failure. The drug is a β-arrestin-biased ligand of the angiotensin II type 1 receptor (AT1R) that simultaneously blocks angiotensin II-stimulated G-protein signaling and stimulates β-arrestin-coupled signaling.

    TRV130 is a G protein-biased μ-opioid receptor ligand in development as a rapidly acting analgesic for the treatment of post-operative pain. Designed to demonstrate fewer μ-opioid receptor-mediated side effects such as respiratory suppression and constipation, the drug selectively stimulates G-protein coupling linked to analgesia, while avoiding β-arrestin coupling linked to inhibition of respiration and gastrointestinal motility. Phase I trials with TRV130 were initiated February. 



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