Oliceridine HCl (TRV-130)

Description: Oliceridine is now discontinued since it was recently listed as a controlled substance. Oliceridine, formerly known as TRV130, is a u- opioid receptor agonist, that is currently under evaluation in human clinical trials for the treatment of acute severe pain. It is a functionally selective u-opioid receptor agonist developed by Trevena Inc. TRV130 elicits robust G protein signaling, with potency and efficacy similar to morphine, but with far less beta-arrestin 2 recruitment and receptor internalization, it exhibits less adverse effects than morphine. (//en.wikipedia.org/wiki/TRV130).

References: Soergel DG, Subach RA, Burnham N, Lark MW, James IE, Sadler BM, Skobieranda F, Violin JD, Webster LR. Biased agonism of the u-opioid receptor by TRV130 increases analgesia and reduces on-target adverse effects versus morphine: A randomized, double-blind, placebo-controlled, crossover study in healthy volunteers. Pain. 2014 Sep; 155(9):1829-35.