Luye Pharma Group today announced that the first patient has been enrolled for the phase I clinical trial of the company's innovative in-house oncology product, Hydrochloride Irinotecan Floxuridine Compound Liposome Injection (LY01616). This is a multicenter, open, dose-escalation, single and multiple dose phase I/II clinical study designed to evaluate the safety, tolerability, PK profile and preliminary clinical efficacy of LY01616 in patients with advanced gastrointestinal cancers.
LY01616 is China’s first compound liposome formulation to reach the clinical trial stage. It employs a significantly complex preparation method, with a high-tech production process, which wraps irinotecan and floxuridine with a defined synergistic ratio inside a liposome product. Currently, no combination drug product with these active substances is available worldwide. The entry into clinical trial of this drug represents a breakthrough in Luye Pharma’s combinational liposome R&D and manufacturing capability, which was made possible by leveraging the core strengths of its technology platform.
Expected to Increase Weak Synergistic Effects and Reduce Long Infusion Duration of Current Combined Chemotherapy
According to the practice guidelines for colorectal cancer of the National Comprehensive Cancer Network (NCCN) and the Chinese Society of Clinical Oncology (CSCO), irinotecan combined with fluorouracil is one of the first choices in chemotherapy treatment for advanced colorectal cancer. However, there is much room for improvement in the synergistic effects and the infusion duration of this treatment regimen:
To address these problems, LY01616 employs an innovative formulation that wraps hydrochloride irinotecan and floxuridine inside liposome product. Preclinical studies have confirmed that after the administration of LY01616, the synergistic ratio of irinotecan and floxuridine in vivo can be maintained for a long period of time, realizing the synergistic anti-tumor effects and improving efficacy. In addition, the infusion dose of LY01616 is significantly lower, which means less toxicity and fewer adverse effects than existing formulations. The lower dose is expected to make clinical administration more convenient and reduce the duration of intravenous infusion by a considerable margin.
Targeting a Substantial Unmet Need of Patients with Gastrointestinal Cancers
Data from the International Agency for Research on Cancer (IARC) of the World Health Organization show that in 2020 China ranked first in the world in terms of the number of new cancer cases. The relevant figure was 4.57 million, accounting for 23.7% of all new cancer cases worldwide; of the five cancers in China with the highest new incidence rates, three are gastrointestinal: colorectal cancer, gastric cancer and liver cancer – numbering 560,000, 480,000 and 410,000 new cases respectively.
Based on the large unmet patient need indicated above and the positive results demonstrated in preclinical studies with LY01616, this clinical trial is designed to further evaluate the safety, tolerability, PK profile and preliminary clinical efficacy of LY01616 in patients with advanced solid tumors. In vitro cellular assays have demonstrated that when the two drugs are maintained at a specific ratio, the irinotecan and floxuridine combination exhibits synergistic antitumor effects on a variety of tumor cells, including colorectal cancer.
Liposome Technology Platform with Potential to Enhance Clinical Benefits
Liposome is a complicated structure composed of phospholipid bilayers made of cholesterol and other lipid components, surrounding a micro vesicle. Liposomes can be used as drug carriers to change the pharmacokinetic properties of drugs in vivo, which can bring clinical benefits including increased drug stability, prolonged circulation times, and improved passive tumor targeting and efficacy.
Luye Pharma has a long-term focus on the research and development of liposomes and other novel formulations, and has reached an international advanced level in this field. The company researches liposome drugs and prospective lipid nanoparticles (LNP) drug delivery systems, including liposome drug load technology, nucleic acid drugs and drug load technology, LNP phospholipid carrier material technology, and key technologies related to pilot and commercial production, among others. The company has built a highly intelligent liposome production line and a GMP-compliant commercial production workshop to further enhance its commercial production capability. The first innovative product developed on this platform, Paclitaxel Liposome for Injection (Brand Name: Lipusu®), is the only paclitaxel liposome product approved for commercial production in the world. In addition, the company has multiple products in the pipeline such as Ropivacaine Hydrochloride Liposome Suspension Injection.
Luye Pharma Group today announced that the first patient has been enrolled for the phase I clinical trial of the company's innovative in-house oncology product, Hydrochloride Irinotecan Floxuridine Compound Liposome Injection (LY01616). This is a multicenter, open, dose-escalation, single and multiple dose phase I/II clinical study designed to evaluate the safety, tolerability, PK profile and preliminary clinical efficacy of LY01616 in patients with advanced gastrointestinal cancers.
LY01616 is China’s first compound liposome formulation to reach the clinical trial stage. It employs a significantly complex preparation method, with a high-tech production process, which wraps irinotecan and floxuridine with a defined synergistic ratio inside a liposome product. Currently, no combination drug product with these active substances is available worldwide. The entry into clinical trial of this drug represents a breakthrough in Luye Pharma’s combinational liposome R&D and manufacturing capability, which was made possible by leveraging the core strengths of its technology platform.
Expected to Increase Weak Synergistic Effects and Reduce Long Infusion Duration of Current Combined Chemotherapy
According to the practice guidelines for colorectal cancer of the National Comprehensive Cancer Network (NCCN) and the Chinese Society of Clinical Oncology (CSCO), irinotecan combined with fluorouracil is one of the first choices in chemotherapy treatment for advanced colorectal cancer. However, there is much room for improvement in the synergistic effects and the infusion duration of this treatment regimen:
To address these problems, LY01616 employs an innovative formulation that wraps hydrochloride irinotecan and floxuridine inside liposome product. Preclinical studies have confirmed that after the administration of LY01616, the synergistic ratio of irinotecan and floxuridine in vivo can be maintained for a long period of time, realizing the synergistic anti-tumor effects and improving efficacy. In addition, the infusion dose of LY01616 is significantly lower, which means less toxicity and fewer adverse effects than existing formulations. The lower dose is expected to make clinical administration more convenient and reduce the duration of intravenous infusion by a considerable margin.
Targeting a Substantial Unmet Need of Patients with Gastrointestinal Cancers
Data from the International Agency for Research on Cancer (IARC) of the World Health Organization show that in 2020 China ranked first in the world in terms of the number of new cancer cases. The relevant figure was 4.57 million, accounting for 23.7% of all new cancer cases worldwide; of the five cancers in China with the highest new incidence rates, three are gastrointestinal: colorectal cancer, gastric cancer and liver cancer – numbering 560,000, 480,000 and 410,000 new cases respectively.
Based on the large unmet patient need indicated above and the positive results demonstrated in preclinical studies with LY01616, this clinical trial is designed to further evaluate the safety, tolerability, PK profile and preliminary clinical efficacy of LY01616 in patients with advanced solid tumors. In vitro cellular assays have demonstrated that when the two drugs are maintained at a specific ratio, the irinotecan and floxuridine combination exhibits synergistic antitumor effects on a variety of tumor cells, including colorectal cancer.
Liposome Technology Platform with Potential to Enhance Clinical Benefits
Liposome is a complicated structure composed of phospholipid bilayers made of cholesterol and other lipid components, surrounding a micro vesicle. Liposomes can be used as drug carriers to change the pharmacokinetic properties of drugs in vivo, which can bring clinical benefits including increased drug stability, prolonged circulation times, and improved passive tumor targeting and efficacy.
Luye Pharma has a long-term focus on the research and development of liposomes and other novel formulations, and has reached an international advanced level in this field. The company researches liposome drugs and prospective lipid nanoparticles (LNP) drug delivery systems, including liposome drug load technology, nucleic acid drugs and drug load technology, LNP phospholipid carrier material technology, and key technologies related to pilot and commercial production, among others. The company has built a highly intelligent liposome production line and a GMP-compliant commercial production workshop to further enhance its commercial production capability. The first innovative product developed on this platform, Paclitaxel Liposome for Injection (Brand Name: Lipusu®), is the only paclitaxel liposome product approved for commercial production in the world. In addition, the company has multiple products in the pipeline such as Ropivacaine Hydrochloride Liposome Suspension Injection.
