Afuresertib

– A total of 64 healthy subjects with an average BMI of 23.2±2.2 kg/m2 enrolled into the SAD Study, including 5 intravenous cohorts and 3 subcutaneous cohorts – The SAD Study data demonstrated an encouraging safety and tolerability profile, with no reported case of diarrhea or serious adverse events – Obvious target engagements and expected pharmacodynamic biomarker changes have been observed. Single doses of LAE102 resulted in significant and sustained increases in activin A level, indicating robust target engagement – Positive outcomes established a solid foundation for coming MAD Study in China and Phase I study in collaboration with Lilly in the U.S. January 13, 2025 — Laekna, Inc. (2105.HK) (“Laekna”) today announced that the Group has successfully completed the phase I single ascending dose study (the “SAD Study”) of LAE102 for the treatment of obesity. The SAD Study enrolled a total of 64 healthy subjects with an average BMI of 23.2±2.2 kg/m2, including 5 intravenous cohorts and 3 subcutaneous cohorts. The positive outcomes of the SAD Study results have established a solid foundation for the coming phase I multiple ascending dose study (the “MAD Study”) in China as well as the phase I clinical study in collaboration with Eli Lilly & Company (“Lilly”) in the U.S.. The SAD Study data of LAE102 analyzed to date demonstrated an encouraging safety and tolerability profile, with no serious adverse events and no discontinuations due to adverse events. All treatment emergent adverse events reported to date were very well tolerated, with the majority of them being reported as mild (grade 1) lab test abnormality without any clinical symptoms or signs. There is no reported case of diarrhea. Obvious target engagements and expected pharmacodynamic biomarker changes have been observed. Single doses of LAE102 resulted in significant and sustained increasing in activin A level, indicating a robust target engagement. The duration of target engagement correlated to the dose level. The detailed study results will be presented in a scientific conference as soon as possible. The positive SAD Study results support continuing the investigation of LAE102 for the treatment of obesity. The Group plans to initiate the MAD Study in the first quarter of 2025 and to work closely with Lilly to commence the phase I clinical study in U.S. as soon as possible. The MAD Study is a randomized, double-blind, placebo-controlled study to evaluate the safety, tolerability, pharmacokinetics and pharmacodynamics of LAE102, administered subcutaneously, in 60 overweight/obese subjects. The Group aims to bring this precision therapy to overweight and obese patients who are in need of novel treatment options for achieving quality weight control. "We are excited to have new clinical data with LAE102. The SAD result demonstrated the potential of selective Activin A receptor inhibition as an important therapeutic approach," said Dr. Chris Lu, Chairman and Chief Executive Officer of Laekna. "The dedication of all principal investigators and subjects are much appreciated. We are committed to accelerating the global development of LAE102 and making a meaningful impact on the lives of millions of people affected by obesity." LAE102 is an internally discovered monoclonal antibody selectively targeting ActRIIA, a receptor that plays an important role in muscle regeneration and lipid metabolism. In the pre-clinical models, LAE102 has been shown to increase lean mass and decrease fat mass. In combination with GLP1R agonist, LAE102 can further reduce fat mass and significantly regain the lean mass loss induced by GLP1R agonist. This positions LAE102 as a promising drug candidate for achieving quality weight control. Laekna announced, in November, 2024, a clinical collaboration with Lilly to support and accelerate global development of LAE102 for the treatment of obesity. —End— Contact Us IR ir@laekna.com Media communication@laekna.com Corporate and Business Development BD@laekna.com About Laekna Stock Code: 2105.HK Founded in 2016, Laekna is a science-driven, clinical-stage biotechnology company committed to bringing novel therapeutics to patients with cancer, metabolic diseases and liver fibrosis patients around the world. As of June 30, 2024, Laekna has initiated seven clinical trials for LAE102, LAE002(afuresertib), LAE001 and LAE005 to address unmet medical needs in obesity and cancers. LAE102 is our internally discovered antibody against ActRIIA. It has been shown in the pre-clinical studies to increase lean mass and decrease fat mass. We’ve obtained IND approvals from the FDA and the CDE for LAE102 in obesity indication and are advancing the Phase I clinical trial in China. Blocking Activin-ActRII pathway could promote muscle regeneration and decrease fat mass. Laekna team has accumulated tremendous experiences and deep know-how in this specific field and is developing more drug candidates (LAE103 and LAE123), in addition to LAE102, to maximize the value of targeting ActRII receptors. In the cancer area, Laekna has built a comprehensive portfolio of drug candidates, covering the treatment of breast cancer, prostate cancer, ovarian cancer and PD-1/ PD-L1 drug-resistant solid tumors. LAE002 (afuresertib) is a potent AKT inhibitor that inhibits all three AKT isoforms (AKT1, AKT2 and AKT3) as well as one of the only two AKT inhibitors in late-stage development for breast and prostate cancer globally. Laekna has commenced the Phase III clinical trial (AFFIRM-205) for LAE002 in patients with HR+/HER2- breast cancer. Laekna, Inc. (2105.HK) was listed on the Main Board of The Stock Exchange of Hong Kong Limited (the “Hong Kong Stock Exchange”) on June 29, 2023. For more information, please visit: https://www.laekna.com/ or https://www.linkedin.com/company/74110713/ Forward-Looking Statements This press release may contain certain “forward-looking statements” which are not historical facts, but instead are predictions about future events based on Laekna’s current beliefs, assumptions and expectations, commonly identified by words such as "would", "may", "expects", "believes", "plans", "intends", "projects" and other terms with similar meaning. Although we believe that our predictions are reasonable, future events are inherently uncertain and our actual future results or performance may be materially different from what we expect. Accordingly, you are strongly cautioned that reliance on any forward-looking statements is subject to significant known and unknown risks and uncertainties. All forward-looking statements contained herein are qualified by reference to the cautionary statements set forth in this section. All information provided in this press release is as of the date of this press release and are based on assumptions that we believe to be reasonable as of this date, and we do not undertake any obligation to update any forward-looking statement, except as required under applicable law.

LOS ANGELES, Dec. 11, 2024 /PRNewswire/ -- Laekna (2105.HK) today announced that the company will present an internally discovered preclinical candidate at the 2024 San Antonio Breast Cancer Symposium (SABCS) on December 13, 2024. The presentation will feature preclinical characterization of LAE118, a novel allosteric pan-mutant selective PI3Kα inhibitor. "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 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. About Laekna Stock Code: 2105.HK Founded in 2016, Laekna is a science-driven, clinical-stage biotechnology company committed to bringing novel therapeutics to patients with cancer, metabolic diseases and liver fibrosis patients around the world. As of June 30, 2024, Laekna has initiated seven clinical trials for LAE102, LAE002(afuresertib), LAE001 and LAE005 to address unmet medical needs in obesity and cancers. LAE102 is our internally discovered antibody against ActRIIA. It has been shown in the pre-clinical studies to increase lean mass and decrease fat mass. We've obtained IND approvals from the FDA and the CDE for LAE102 in obesity indication and are advancing the Phase I clinical trial in China. Blocking Activin-ActRII pathway could promote muscle regeneration and decrease fat mass. Laekna team has accumulated tremendous experiences and deep know-how in this specific field and is developing more drug candidates (LAE103 and LAE123), in addition to LAE102, to maximize the value of targeting ActRII receptors. In the cancer area, Laekna has built a comprehensive portfolio of drug candidates, covering the treatment of breast cancer, prostate cancer, ovarian cancer and PD-1/ PD-L1 drug-resistant solid tumors. LAE002 (afuresertib) is a potent AKT inhibitor that inhibits all three AKT isoforms (AKT1, AKT2 and AKT3) as well as one of the only two AKT inhibitors in late-stage development for breast and prostate cancer globally. Laekna has commenced the Phase III clinical trial (AFFIRM-205) for LAE002 in patients with HR+/HER2- breast cancer. Laekna, Inc. (2105.HK) was listed on the Main Board of The Stock Exchange of Hong Kong Limited (the "Hong Kong Stock Exchange") on June 29, 2023. For more information, please visit: or Forward-Looking Statements This press release may contain certain "forward-looking statements" which are not historical facts, but instead are predictions about future events based on Laekna's current beliefs, assumptions and expectations, commonly identified by words such as "would", "may", "expects", "believes", "plans", "intends", "projects" and other terms with similar meaning. Although we believe that our predictions are reasonable, future events are inherently uncertain and our actual future results or performance may be materially different from what we expect. Accordingly, you are strongly cautioned that reliance on any forward-looking statements is subject to significant known and unknown risks and uncertainties. All forward-looking statements contained herein are qualified by reference to the cautionary statements set forth in this section. All information provided in this press release is as of the date of this press release and are based on assumptions that we believe to be reasonable as of this date, and we do not undertake any obligation to update any forward-looking statement, except as required under applicable law. SOURCE Laekna，Inc. WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED