Luye Pharma : Patient Enrollment Completed for a Phase 2 Clinical Study of Luye Pharma’s Class 1 Analgesic Drug Candidate LY03014

- Reinforcing the company's CNS portfolio -

Yantai, July 6, 2023 - Luye Pharma Group announced today that patient enrollment has been completed for a Phase 2 clinical study of its investigational drug LY03014 in China. Designated as a "Class 1 Chemical Drug" in China, LY03014 is a small-molecule G protein-biased agonist of the mu-opioid receptor (MOR), intended for treating moderate-to-severe acute postoperative pain and breakthrough cancer pain.

The Phase 2 clinical trial is a multicenter, randomized, double-blind, placebo and positive parallel controlled study. It is designed to evaluate the preliminary efficacy and safety of LY03014 as an analgesic in patients with moderate-to-severe pain after an abdominal surgery. The results of its Phase 1 clinical trial show that a single intravenous infusion of LY03014 could significantly improve the pain threshold and pain tolerance of subjects with a good overall safety profile.

Opioids are commonly used to treat moderate-to-severe acute postoperative pain and breakthrough cancer pain. They can significantly improve the quality of life for 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 is expected to separate analgesia from respiratory depression. It is the only investigational drug that can completely separate the G protein pathway and the β-arrestin-2 pathway, with the latter mainly mediating adverse reactions associated with MOR activation, such as respiratory depression, constipation, and tolerance. In comparison with current G protein-biased MOR agonists, LY03014 is expected to retain high analgesic potency while reducing the risk of OIRD, and thus to meet the huge unmet needs in clinical practice. The results from the study of LY03014 were published in the European Journal of Medicinal Chemistry.¹

Globally, over 300 million patients receive surgeries each year. More than 80% of them suffer from postoperative pain, of which about 75% is acute.² In China, approximately 4.57 million new cancer cases were reported in 2020.³ For patients with malignant tumors, pain is one of the most common symptoms. About 80% of tumor patients will develop cancer pain during their disease treatment and the incidence of breakthrough cancer pain among these patients ranges from 33% to 95%⁴.

The ever-growing demand for analgesics is driven by the huge number of patients. Data from IQVIA shows that the sales of anesthetics and analgesics in China were RMB 37.3 billion in 2022, with a compound annual growth rate (CAGR) of 7.7% from 2018 to 2022. Specifically, the sales of opioids in 2022 were RMB 19 billion, with a CAGR of 10.4% from 2018 to 2022, and the growth rate exceeded the average growth rate in the field of anesthetics and analgesia.

The central nervous system (CNS) therapeutic area, which includes pain management, has long been a strategic focus for Luye Pharma. With frequent breakthroughs in new drug development and a growing portfolio, Luye Pharma is reinforcing its leadership position in the Chinese market for CNS products. This also helps to accelerate the company's global expansion.

The company has built a strong CNS portfolio. In January 2023, Rykindo® (risperidone extended-release microspheres for injection) was approved for marketing in the U.S., making it the first new CNS drug developed by a Chinese pharmaceutical company and approved for use in the U.S. In November 2022, Ruoxinlin® (toludesvenlafaxine hydrochloride extended-release tablets) was approved for marketing in China as the first "Class 1 Chemical Drug" for the treatment of Major Depression Disorder developed by a Chinese company. Other products in the portfolio such as Seroquel® (quetiapine fumarate) and its extended-release tablets, as well as Rivastigmine Transdermal Patches (once daily and multi-day), are sold in China and other major markets. In the company's pipeline, drug candidates such as LY03010 (paliperidone palmitate injection), LY03003 (rotigotine extended-release microspheres for injection), and LY03015, a VMAT2 inhibitor, are being simultaneously developed in China and abroad.

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About Luye Pharma Group

Luye Pharma Group is an international pharmaceutical company dedicated to the R&D, manufacturing and sale of innovative medications. The company has established R&D centers in China, the U.S. and Europe, with a robust pipeline of over 30 drug candidates in China and more than 10 drug candidates in other international markets. Luye Pharma maintains high-level international standards in novel drug delivery technologies including microspheres, liposomes, and transdermal drug delivery systems. The company has achieved multiple innovations in new chemical entities and antibodies, and is also actively making strategic developments in the fields of cell therapies and gene therapies.

Luye Pharma is developing a global supply chain of 8 manufacturing sites built up around the world, with GMP quality management and control systems established in line with international standards. With more than 30 products covering the central nervous system, oncology, cardiovascular, metabolism and other therapeutic areas, business is conducted in over 80 countries and regions around the world, including the largest pharmaceutical markets - China, the U.S., Europe and Japan, as well as in fast growing emerging markets.

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References:

1. Y. Yang, Y. Wang, A. Zuo et al. European Journal of Medicinal Chemistry 228 (2022) 113986.
2. Jeffrey L Apfelbaum1, Connie Chen etal. Postoperative Pain Experience: Results from a National Survey Suggest Postoperative Pain Continues to Be Undermanaged[J]. Anesth Analg, 2003(97):534 - 540.
3. International Agency for Research on Cancer - Cancer Fact Sheets - China. Available at https://gco.iarc.fr/today/data/factsheets/populations/160-china-fact-sheets.pdf Accessed in July 2023.
4. Expert Consensus on Breakthrough Cancer Pain (2018 ed.), Chin J Clin Oncol 2019. Vol. 46. No. 6.