TRV734 is
novel, potent, and selective G protein-biased μ-opioid receptor ligand. TRV734 robustly
engage G protein coupling with efficacy and potency comparable to morphine, but
display dramatically reduced β-arrestin
coupling. In rodents, TRV734 is potently analgesic, but display reduced
gastrointestinal dysfunction (GI) compared to morphine. The improved
therapeutic index TRV734 could allow safer, more effective pain management by removing
key barriers to effective opioid therapy.
Data from
Trevena suggest that oral TRV734 may deliver powerful analgesia with better
tolerability than currently used oral opioids for acute and chronic pain.
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