US-based clinical-stage pharmaceutical firm Trevena has started its first phase 1 study for TRV734, a novel drug candidate being developed as an orally administered treatment of patients with moderate to severe acute and chronic pain.
TRV734 is being developed to optimise analgesia while minimising on-target gastrointestinal and respiratory effects through its new biased ligand mechanism at the mu-opioid receptor.
It targets the mu-opioid receptors, a class of opioid receptors that are found primarily in the brainstem and medial thalamus and play a role in analgesia.
The company said that TRV734 takes advantage of the same receptor specificity mechanism as does its phase 2 clinical candidate, TRV130, an intravenous mu-opioid G protein biased ligand being developed for the treatment of acute postoperative pain.
Trevena senior vice-president of clinical development David Soergel said: "With a targeted mechanism of action giving the potential to mitigate a number of dose-limiting side effects associated with current opioid treatments, we believe TRV734 holds great promise as a novel analgesic.
"In preclinical studies, TRV734 demonstrated an encouraging therapeutic profile, with a potent analgesic effect and a reduced impact on gastrointestinal motility at equianalgesic doses compared to oxycodone."
The main objective of the study is to assess the safety, tolerability, pharmacokinetics and pharmacodynamics of single ascending doses of TRV734 in healthy patients.
In the trial, the potentially efficacious dose range of TRV734 will also be assessed using pupilometry, a validated biomarker for mu-opioid receptor engagement.
Trevena president and CEO Maxine Gowen said: "The initiation of this trial represents another step in our continued progress towards translating our groundbreaking biased ligand technology into the next generation of G protein coupled receptor targeted medicines.
"With TRV734, we now have three clinical-stage drug candidates that we are developing to address significant unmet medical needs, and are focused on driving their development while continuing to pursue additional candidates identified with our ABLE™ platform."