FAZ-053

SHANGHAI and WARREN, N.J., April 7, 2024 /PRNewswire/ -- Laekna (2105.HK) announced that the company has presented two internally-discovered preclinical candidates, in addition to a poster presentation on a clinical trial, at the 2024 Annual Meeting of the American Association for Cancer Research (AACR) in San Diego, California. The presentations featured preclinical data of two novel selective inhibitors, LAE119, a novel PARP1 selective inhibitor and trapper, and LAE120, a novel selective USP1 inhibitor. "After advancing LAE102, our internally discovered antibody against ActRIIA, into IND stage, Laekna continues to strengthen our internal discovery efforts, with new drug candidates emerging", said Dr. Justin Gu, Chief Scientific Officer of Laekna. "The MOA of LAE119 and LAE120 is synthetic lethality, both exhibit strong anti-tumor efficacy and good safety in preclinical models. LAE 119 is a PARP1-selective inhibitor with the strongest DNA-trapping activity among all the PARP inhibitors tested. It shows good activity even in tumor cells with low PARP1 protein level. LAE120 is a novel USP1 inhibitor currently at IND-enabling studies stage. It has a unique chemical scaffold differentiated from all the other disclosed USP1 inhibitors and is expected to induce a different conformational change in USP1. The quick advance of these two projects into PCC stage demonstrates the effectiveness of the close collaboration among Med Chem, Biology and AIDD (AI-driven Drug Discovery) teams. Laekna will continue our internal effort of discovery novel drug candidates to provide more options for patients." Laekna's internal discovery focuses on innovation, scarcity, and differentiation, covering three areas: cancer, metabolic diseases，and liver fibrosis. The company has internally discovered 14 drug candidates, among which seven have been optimized and advanced to PCC (pre-clinical candidate) stage. The company plans to have one drug candidate entering the clinical stage each year. The Annual Meeting of AACR is set for April 05 to 10, 2024 at the San Diego Convention Center, California, USA. It is the focal point of the cancer research community, where scientists, clinicians, other health care professionals, survivors, patients, and advocates gather to share the latest advances in cancer science and medicine. [1] Presentation details are as follows: Title: Preclinical characterization of LAE119, a novel PARP1 selective inhibitor and trapper Authors: Ming Li, Yan Chen, Junyan Chen, Ling Jiang, Xiaofen Lin, Justin Gu Session Category: Experimental and Molecular Therapeutics Session Title: DNA Damage and Repair Session Date and Time: Wednesday, Apr 10, 2024 9:00 AM- 12:30 PM (PT) Location: Poster Section 22 Poster Board Number: 27 Abstract Highlights: LAE119 is a potent and selective PARP1 inhibitor and PARP1-DNA trapper. It demonstrates more than 1000-fold selectivity for PARP1 DNA trapping activity over PARP2. In comparison to most PARP inhibitors including AZD5305, LAE119 exhibits extremely long residence time on PARP1 in both biochemical and cellular assays and shows good activity even in tumor cells with low PARP1 protein level. It demonstrates robust anti-tumor effect in BRCA2-/- DLD-1 and MDA-MB-436 Xenograft models and has minimal effects on hematologic parameters. Full texts of the abstracts are available here. Title: Preclinical candidate LAE120, a novel selective USP1 inhibitor shows effective anticancer and combination activity with PARP inhibitors Authors: Jintao Wang, Yan Chen, Junyan Chen, Ling Jiang, Xiaofen Lin, Chaojun Cai, Minhua Zhang, Ming Li, Justin Gu Session Category: Experimental and Molecular Therapeutics Session Title: Novel Antitumor Agents 2 Session Date and Time: Sunday, Apr 7, 2024 1:30 PM- 5:00 PM (PT) Location: Poster Section 27 Poster Board Number: 16 Abstract Highlights: LAE120 is a novel, allosteric and highly potent USP1 inhibitor, displaying monotherapy potency and combination activity with PARP inhibitor in HRD (homologous recombination deficiency) cancers. It has a unique chemical structure differentiated from all the other disclosed USP1 inhibitors and is expected to induce a different conformational change in USP1. LAE120 shows robust tumor inhibitory activity in MDA-MB-436 and K562 xenograft models as a single agent and exhibits synergistic effect in combination with PARP inhibitors. LAE120 demonstrates good therapeutic window in DRF study and is currently at IND-enabling stage. Full texts of the abstracts are available here. About Laekna Founded in 2016, Laekna is a science-driven, clinical-stage biotechnology company committed to bringing novel therapies to cancer, metabolic diseases and liver fibrosis patients worldwide. As of December 31, 2023, we have initiated six clinical trials for Afuresertib (LAE002), LAE001 and LAE005 for the treatment of breast cancer, prostate cancer, ovarian cancer and PD-1/ PD-L1 drug-resistant solid tumors to address the unmet medical needs. Among the six clinical trials, three are multi-regional clinical trials (MRCTs). 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 or completed the pivotal-stage clinical development for anti-cancer treatment globally. Laekna's internal drug discovery platform has discovered 14 drug candidates. LAE102 is our internally discovered antibody against ActRIIA. We've submitted IND applications to CDE and FDA respectively for LAE102 in relation to obesity in the first quarter of 2024. Blocking Activin-ActRII pathway could promote skeletal muscle regeneration and decrease fat mass. Laekna team has accumulated tremendous experiences and deep knowhow in this specific field and is developing more drug candidates (LAE103 and LAE123) to maximize the value of targeting ActRII receptors. Laekna, Inc. was listed on the Main Board of The Stock Exchange of Hong Kong Limited (the "Hong Kong Stock Exchange") on June 29, 2023, with the stock code 2105.HK. 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

Laekna has developed a proprietary antibody-based drug discovery platform of activated hepatic stellate cells (aHSC) depletion for liver fibrosis. Derived from the platform, LAE105 is a potentially first-in-class drug candidate that depletes aHSC in the fibrotic liver by harnessing innate immunity. The platform enables Laekna to continually discover better therapeutic antibodies for the treatment of NASH/liver fibrosis SHANGHAI and WARREN, N.J., Jan. 3, 2024 /PRNewswire/ -- Laekna (2105.HK), a clinical-stage biotechnology company, today announced that the company will present a novel therapeutical approach to treat liver fibrosis in the form of a poster at the NASH-TAG conference from January 4-6, 2024, in Park City, Utah. The presentation will showcase a novel antibody-based aHSC depletion discovery platform and introduce preclinical anti-fibrosis data of a bi-functional NK-aHSC engager candidates derived from this platform. "Derived from this unique platform, LAE105 is a potentially first-in-class drug candidate that targets aHSC surface antigen and recruits immune cells to elicit aHSC clearance. It has demonstrated significant anti-fibrosis activity in preclinical model. " said Dr. Minhua Zhang, Senior Director of Discovery Research of Biology, Laekna. Liver fibrosis is one of the main underlying catalysts of liver cancer or liver failure, with the accumulation of aHSC being the main contributors for liver fibrogenesis. Current drug development for NASH and liver fibrosis mainly focuses on lowering lipid accumulation in the liver or reducing liver fibrosis by blocking certain activating signaling proteins of hepatic stellate cells. Laekna has taken a different approach to clear aHSC from the liver by re-engaging innate immunity and established a global-leading and proprietary aHSC depletion discovery platform for liver fibrosis. This platform enables Laekna to continually discover and develop the next generation therapeutics against liver fibrosis and potentially other types of fibrotic diseases. "We are delighted that Laekna's preclinical discovery research team has made new progress," said Dr. Justin Gu, Chief Scientific Officer of Laekna. "Liver fibrosis, metabolic diseases, and cancer are the three major indications that Laekna aims to tackle. Currently, no drugs have been approved for liver fibrosis globally. We are working relentlessly to accelerate drug innovation for liver fibrosis by leveraging our know-how, novel discovery approach, and proprietary platform." The NASH-TAG Conference is designed to bring together clinicians and researchers in academia and the pharmaceutical industry for a focused, interactive, educational update highlighting the most relevant advances and challenges in the diagnosis and therapy of NASH and liver fibrosis. Presentation details are as follows: Abstract Number: 32 Title: Preclinical characterization of bi-functional NK-aHSC engager for liver fibrosis Authors: Minhua Zhang, Chaojun Cai, Jinying Zhou, Justin Gu, Chris Lu Presenter: Dr. Chris Lu, Laekna Location: Renoir Ballroom, The Chateaux Deer Valley Date/Time: Saturday, Jan. 6, 2024 (MST) Abstract Highlights: In vitro, a panel of antibodies and bi-functional engagers targeting various aHSC targets have demonstrated potent and dose-dependent aHSC killing activity in the presence of human NK cells. Additionally, the antibodies also promoted phagocytosis of aHSC cells by human macrophage. In vivo, antibodies with enhanced effector function showed significant anti-fibrotic effects in two different liver fibrosis animal models. About Laekna Founded in 2016, Laekna is a science-driven, clinical-stage biotechnology company committed to bringing novel therapies to cancer and liver fibrosis patients worldwide. As of June 30, 2023, Laekna has initiated six clinical trials for afuresertib (LAE002), LAE001 and LAE005 to address unmet medical needs in cancers, such as ovarian cancer, breast cancer and prostate cancer. Among the six clinical trials, three are multi-regional clinical trials (MRCTs), including one pivotal trial. Laekna's internal drug discovery platform has discovered 12 drug candidates. LAE102 is our first internally discovered antibody which has obtained an IND approval from the FDA. Its potential indications include muscle regeneration, obesity, and cancer. Laekna, Inc. was listed on the Main Board of The Stock Exchange of Hong Kong Limited (the "Hong Kong Stock Exchange") on June 29, 2023. The stock code is 2105.HK. 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