The board of directors of Luye Pharma Group Ltd. announced that the new Class 1 drug LY03014 (LY03014) developed by the Group has completed the patient enrollment for its phase 2 clinical trial in China. LY03014 is a small molecule G protein unbiased at mu-opioid receptor (MOR) agonist, and is indicated for the treatment of moderate to severe acute postoperative pain and breakthrough cancer pain. The phase 2 clinical trial is a multi-center, randomized, double-blind, placebo- and positive-controlled parallel study to preliminarily evaluate the analgesic efficacy and safety of LY03014 in patients with moderate to severe postoperative pain after abdominal surgery.

Opioids are commonly used to treat moderate-to-severe acute post cooperative pain and breakthrough cancer pain. Opioids are used with the aim to improving the quality of life of patients with moderate-to-severe pain. However, opioids for medical use currently available in the marketplace present a common risk of Opioid-induced Respiratory Depression (OIRD), which is a major cause of death in clinical practice.

As a novel analgesic, LY03014 can separate analgesia and respiratory depression, and is expected to meet the unmet clinical needs above. The results of its phase 1 clinical trials show that a single intravenous infusion of LY03014 can significantly improve the pain threshold and pain tolerance of subjects with a good overall safety profile. Non-clinical studies show that LY03014 has good blood-brain barrier permeability and a good pharmacokinetic profile.

A proof-of-concept (POC) study shows that compared to conventional MOR agonists, LY03014 completely separated the G protein pathway and the b-arrestin2 pathway, which mainly alleviates adverse effects associated with MOR activation, such as respiratory depression, constipation, and opioid tolerance. The POC study also shows that at equianalgesic doses, LY03014 was less likely to cause respiratory depression, gastrointestinal dysfunction, or opioid tolerance than morphine.