On December 12, 2024 Laekna (2105.HK) reported that the company will present an internally discovered preclinical candidate at the 2024 San Antonio Breast Cancer Symposium (SABCS) on December 13, 2024 (Press release, Laekna Therapeutics, DEC 12, 2024, View Source [SID1234649090]). The presentation will feature preclinical characterization of LAE118, a novel allosteric pan-mutant selective PI3Kα inhibitor.
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"We appreciate this recognition of our expertise and strength in pre-clinical developments of novel drugs", said Dr. Justin Gu, Chief Scientific Officer of Laekna. "The development of LAE118 was led by Dr. Ming Li, with collaborative contributions from the Med Chem, Biology and AIDD (AI-driven Drug Discovery) teams of Laekna. We have significantly accelerated the development of our preclinical drug candidate with cutting-edge artificial intelligence tools".
"As a novel allosteric inhibitor, LAE118 demonstrates excellent potency and selectivity towards various PI3Kα mutants. With superior efficacy and higher tolerability than its competitors in animal models, LAE118 has great potential to become the best-in-class pan-mutant-selective PI3Kα inhibitor. We look forward to bringing this novel therapy to the patients", said Dr. Justin Gu.
PI3Kα mutations are prevalent in patients with breast, colorectal, lung, endometrial, and numerous other cancers. Targeting PI3Kα in cancer has been validated as a therapeutic strategy, as evidenced by the approved drugs. However, the first-generation drugs inhibit the wild-type PI3Kα with equal potency, which raises concerns of tolerability and therapeutic efficacy. Therefore, there is a pressing need to develop novel PI3Kα-targeted therapies that can minimize on-target toxicities and overcome drug resistance.
While making significant progress in pre-clinical developments of drug candidates in cancer, Laekna has also established a comprehensive Activin-ActRII portfolio in metabolism. Following the clinical collaboration with Eli Lilly on LAE102 (ActRIIA selective antibody), Laekna has progressedLAE103, an ActRIIB selective inhibitor and LAE123, a dual inhibitor against ActRIIA/IIB, into IND-enabling studies, aiming to advance them to the clinical stage swiftly.
The San Antonio Breast Cancer Symposium is an annual event cosponsored by the AACR (Free AACR Whitepaper) and UT Health San Antonio’s Mays Cancer Center. The meeting is the largest and most prestigious scientific gathering on breast cancer research.
Presentation details are as follows:
Abstract Number: SESS-3548
Poster Number: P5-06-16
Title: Preclinical characterization of LAE118, a novel allosteric pan-mutant selective PI3Kα inhibitor
Authors: Ming Li, Ruipeng Zhang, Junyan Chen, Meijuan Hu, Xiaofen Lin, Minhua Zhang, Xiang-Ju Justin Gu
Time: Friday, Dec. 13, 2024, 12:30 p.m. – 14:00 p.m. CST
Location: Halls 2-3, Henry B. Gonzalez Convention Center, San Antonio, Texas
Abstract Highlights:
LAE118 is a novel allosteric pan-mutant selective PI3Kα inhibitor. LAE118 demonstrates excellent in vitro anti-proliferation activities in PI3Kα mutant cell lines and remains active against cells resistant to orthosteric PI3Kα inhibitors. LAE118 shows strong anti-tumor growth effect in Xenograft models at a dose that is much lower than other allosteric inhibitors and has less effect on glucose homeostasis compared to orthosteric PI3Kα inhibitors. In pre-clinical toxicology studies, LAE118 also demonstrated good tolerability. These data indicate that LAE118 offers improved efficacy and larger safety window. LAE118 is currently in IND enabling stage and Laekna aims to submit the IND application at the earliest opportunity.