Currently, the company is developing TRV734 to optimize analgesia while reducing on-target gastrointestinal and central nervous system adverse effects through its new biased ligand mechanism at the mu-opioid receptor.
TRV734 takes advantage of the same receptor specificity mechanism as the company’s Phase II clinical compound TRV130, an intravenous mu-opioid G protein biased ligand under development for acute postoperative pain.
The Phase I trial is designed to evaluate the safety, tolerability, pharmacodynamics (PD) and pharmacokinetics (PK) of TRV734 administered as a single dose and as multiple ascending doses in healthy volunteers.
The company intends to report top line data from the Phase I trial in the first half of 2015, which is aimed at supporting Phase II development.
About 72 healthy volunteers will be enrolled in the two-part Phase I trial. Part A will evaluate the safety, tolerability, PD and PK of single 125mg doses of TRV734 in an open-label, randomized, three-period crossover study in which subjects are fasted, fed a standard meal, or fed a high-fat meal.
Part B will evaluate the safety, tolerability, PD and PK of multiple ascending doses of TRV734 in a double-blind, double-dummy, randomized, active- and placebo-controlled adaptive trial.