Shanghai, December 12, 2024 /PR Newswire/ -- Laikai Pharmaceuticals (2105.HK) today announced that the preclinical research results of its independently developed "A Allosteric Inhibitor Targeting Various PI3Kα Mutants - LAE118" has been selected for the 2024 San Antonio Breast Cancer Symposium (SABCS), where relevant research data will be presented in poster form on December 13 in San Antonio, Texas, USA.

"I am very pleased that Laikai's early research results have been selected for SABCS, which again demonstrates Laikai's strength in the field of new drug development," said Dr. Gu Xiangju, Chief Scientific Officer of Laikai Pharmaceuticals. "LAE118 is led by Laikai's young scientist Dr. Li Ming, in collaboration with the drug chemistry, biology, and AI drug discovery teams. Over more than a year, the team fully utilized the latest AI modeling tools, greatly accelerating the research and development process of the project. As a new type of allosteric inhibitor, LAE118 has good activity and selectivity against various PI3Kα mutants, demonstrating stronger efficacy and higher safety in animal experiments compared to competing products, with great best-in-class potential. We hope to bring this candidate new drug to a wide range of patients as soon as possible."

PI3Kα mutations are common among patients with breast cancer, colorectal cancer, lung cancer, endometrial cancer, and other cancers, and therapies targeting this pathway have been validated as effective. However, currently approved PI3Kα inhibitors can also inhibit the wild type without selectivity for the mutants. Therefore, tolerance is poor, and resistance can easily develop. There is an urgent clinical need for a new generation of PI3Kα drugs to improve safety and overcome drug resistance.

While making progress in autonomous cancer research and innovation, Laikai Pharmaceuticals has also established an "Innovation Pipeline Squad" in the metabolic field. Following a clinical collaboration with Eli Lilly and Co on LAE102 (ActRIIA selective antibody), Laikai Pharmaceuticals has also progressed into IND supportive research stages for two other antibodies targeting the Activin-ActRII pathway: ActRIIB selective inhibitor LAE103 and ActRIIA/IIB dual-target inhibitor LAE123, aiming to advance to clinical trials as soon as possible.

The San Antonio Breast Cancer Symposium (SABCS), co-hosted by the American Association for Cancer Research and the University of Texas Health Science Center at San Antonio, is one of the largest and most influential breast cancer academic conferences in the Global, attracting thousands of researchers and representatives from the Medical field each year.

Abstract number: SESS-3548
Poster number: P5-06-16
Abstract title: Preclinical study of a novel allosteric mutational selective PI3Kα inhibitor—LAE118
Authors: Li Ming, Zhang Ruipeng, Chen Junyan, Hu Meijuan, Lin Xiaofen, Zhang Minhua, Gu Xiangju
Display time:
December 13, 2024 (Friday) 12:30 p.m.– 14:00 p.m. (Central Time, USA)

Exhibition location:
Henry B. Gonzalez Convention Center, San Antonio, Texas, USA.

Abstract Highlights:
LAE118 is a novel allosteric fully mutated selective PI3Kα inhibitor. It demonstrates excellent in vitro anti-proliferative activity in PI3Kα mutated cell lines and remains effective in cells resistant to orthosteric PI3Kα inhibitors. LAE118 shows stronger anti-tumor activity in xenograft models when used at doses far lower than those of other allosteric inhibitors. Compared to orthosteric PI3Kα inhibitors, LAE118 has a lesser impact on blood glucose and insulin. In preclinical toxicology studies, LAE118 also shows good tolerance. These data suggest that LAE118 has higher efficacy and a larger safety window. LAE118 is currently in the IND-enabling stage and will submit the IND application as soon as possible.

About Eli Lilly and Co

Stock code: 2105.HK

Laikai Pharmaceutical was established in 2016 as a science-driven, clinical-stage Biomedical Technology company dedicated to bringing new therapies to Global patients with tumors, metabolic diseases, and liver fibrosis.

As of June 30, 2024, Laikai Pharmaceutical has initiated seven clinical trials around LAE102, LAE002 (afuresertib), LAE001, and LAE005 to address unmet Medical needs in obesity and oncology.

LAE102 is a monoclonal antibody independently developed by Laikai targeting ActRIIA. Preclinical studies have shown that it can increase muscle and reduce fat. LAE102 has received approval for a new drug clinical trial (IND) for obesity indications in China and the USA, and Phase I clinical research is advancing at full speed.

Blocking the Activin-ActRII pathway can promote muscle regeneration and reduce fat. The Eli Lilly and Co team has accumulated rich experience and deep expertise in this specific area and is developing more candidate drugs (LAE103, LAE123, etc.) to maximize the value of targeting the ActRII receptor.

In the field of oncology, Eli Lilly and Co has established a comprehensive combination of candidate drugs covering breast cancer, prostate cancer, ovarian cancer, and PD-1/PD-L1 resistant solid tumors.

LAE002 (afuresertib) is a potent AKT inhibitor that inhibits all three AKT subtypes (AKT1, AKT2, and AKT3), and is also one of two AKT inhibitors globally in late-stage clinical development targeting breast cancer and prostate cancer. Currently, Eli Lilly and Co has fully launched a Phase III pivotal study (AFFIRM-205) targeting HR+/HER2- breast cancer.

On June 29, 2023, Eli Lilly and Co was listed on the Main Board of the HKEX with the stock code: 2105.HK.

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