WRN

April 24th, 2025 — Laekna (2105.HK) announced that the company will present two posters at the 2025 Annual Meeting of the American Association for Cancer Research (AACR), showcasing its internally discovered pre-clinical drug candidates for cancer: LAE118, a pan mutant-selective PI3Kα inhibitor, and LAE122, a novel, potent and selective WRN inhibitor. Both drug candidates target prevalent tumor mutations. LAE118 targets against PI3Kα mutations, which are commonly found in patients with breast, colorectal, endometrial, and numerous other cancers. LAE122 is a novel, potent WRN-selective inhibitor for the treatment of MSI-H tumors, including colorectal, gastric, endometrial, and ovarian cancers. Dr. Justin Gu, Chief Scientific Officer of Laekna, said: “Both LAE118 and LAE122 demonstrate robust in vivo anti-tumor efficacy at doses lower than those of competing compounds. Additionally, LAE118 exhibits exceptional in vitro anti-proliferation activities against both kinase and helical domain mutant cells, with IC50 5 to 10-fold lower than those of competing compounds. This positions LAE118 as a promising candidate, offering patients a more precise and effective innovative therapy”. Dr. Justin Gu emphasized that Laekna’s AI-powered structure-based drug design platform enabled the rapid identification of high-potency candidates with optimized drug-like properties by internal discovery team. The AACR Annual Meeting, the most important cancer meeting in the world, will take place from April 25 to 30, 2025, in Chicago, USA. LAE118: A next-generation PI3Kα inhibitor, potentially best-in-class Three hotspot mutations (H1047R, E545K, E542K) on the p110α subunit of PI3Kα are the recognized activating mutations accounting for more than 1/3 of all PI3Kα mutations. Some pan-mutant selective PI3Kαinhibitors demonstrated improved therapeutic window comparing with orthosteric PI3Kα inhibitors and maintained good clinical responses. However, due to relatively weak potency against PIK3CA helical domain mutants, these inhibitors have less favorable clinical responses in these group of patients. Therefore, there is an urgent need to develop novel pan-mutant selective PI3Ka inhibitors with improved activity against helical domain mutants, which would significantly expand the treatable patient population. LAE118 is a novel allosteric pan-mutant selective PI3Kα inhibitor demonstrating excellent in vitro anti-proliferation activities in both kinase and helical domain mutant cells. LAE118 presents strong anti-tumor efficacy and good PK/PD relationship in GP2D (H1047L), HCC1954 (H1047R), MCF7 (E545K) and MDA-MB-361 (E545K) Xenograft models at doses that are significantly lower than other pan-mutant selective PI3Kα inhibitors. Currently, no pan-mutant-selective PI3Kα inhibitor has been commercialized. With its potentially best-in-class features, LAE118 has emerged as a key player for the next generation of PI3Kα inhibitors. It’s currently in IND enabling stage. LAE122: a novel, potent and selective WRN Inhibitor for the treatment of MSI-H tumors DNA mismatch repair (dMMR) deficiency causes Microsatellite instability (MSI-H), which is frequently observed in various tumor types, including colorectal, gastric, endometrial, and ovarian cancers. Although immune checkpoint inhibitors (ICI) have been approved for the treatment of MSI-H tumors, significant unmet medical need remains across several tumor types that fail to respond or relapse with ICI therapies. Werner syndrome ATP-dependent helicase (WRN) is a RecQ family helicase that plays important roles in DNA repair and in the maintenance of genome integrity. Recent studies have identified WRN as a promising synthetic lethal drug target for MSI-H cancers. LAE122 is a novel, potent and selective WRN inhibitor developed by Laekna through structure-based drug design strategy. LAE122 has highly differentiated structure from bench-mark molecules and displayed single digit nanomolar IC50 values in biochemical assay and cell anti-proliferation assay on MSI-H cells but had no effect on Microsatellite stability (MSS) cells up to 10 µM. LAE122 demonstrated favorable drug-like properties, including good in vitro ADMET and in vivo PK with low plasma clearance and high oral bioavailability across animal species. In SW48 and HCT116 CDX models, LAE122 showed robust anti-tumor growth effect at lower doses than bench-mark molecules with strong evidence on biomarker change. LAE122 didn’t have off-target liability in in vitro assays and demonstrated good tolerability in preclinical toxicology studies. Presentation details are as follows: Poster No.1 Abstract Number: 9661 Poster Number: LB437 Title: LAE118, a Pan Mutant-Selective PI3Kα inhibitor with Strong Anti-tumor Growth Effects in both PIK3CA Kinase and Helical Domain Mutant Xenografts Time: Wednesday, April. 30, 2025, 09:00 a.m. – 12:00 p.m. CST Location: McCormick Place Convention Center, Chicago, Illinois Poster No.2 Abstract Number: 6302 Poster Number: 4192 Title: Preclinical Characterization of LAE122, a Novel, Potent and Selective WRN Inhibitor for the Treatment of MSI-H Tumors Time: Tuesday, April. 29, 2025, 09:00 a.m. – 12:00 p.m. CST Location: McCormick Place Convention Center, Chicago, Illinois – 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 metabolic diseases, cancer and liver fibrosis around the world. As of December 31, 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. Blocking Activin-ActRII pathway could promote muscle regeneration and decrease fat mass, this positions LAE102 as a promising drug candidate for achieving quality weight control. 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. In November 2024, Laekna entered into a clinical collaboration agreement with Eli Lilly and Company to support and accelerate global clinical development of LAE102 for the treatment of obesity. Laekna team has accumulated tremendous experiences and deep know-how in the specific field of targeting ActRII receptors and is developing more drug candidates (LAE103 and LAE123), in addition to LAE102, to maximize the value of the target. LAE103 is an ActRIIB-selective antibody and LAE123 is a dual inhibitor against ActRIIA/IIB. Both are our internally discovered antibodies for muscle and other disease indications. In the cancer area, Laekna has built a comprehensive portfolio of drug candidates including LAE002(afuresertib), LAE001 and other seven pre-clinical drug candidates. 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 and the study recruitment is on track. 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.

4 IDEAYA/GSK presentations of IDE275 (GSK959) and 4 additional presentations across IDE397/MAT2A, IDE161/PARG, PRMT5, and KAT6/7 programs at AACR 2025 IDE275 (GSK959) has demonstrated a potential best-in-class preclinical profile in the MSI-H setting, with a unique binding mode from previously reported WRN inhibitors Phase 1 dose escalation trial ongoing in MSI-H solid tumors with GSK MSI-H prevalence has been reported at approximately 31%, 20%, and 19% in endometrial, colorectal, and gastric cancers, respectively SOUTH SAN FRANCISCO, Calif., March 26, 2025 /PRNewswire/ -- IDEAYA Biosciences, Inc. (Nasdaq: IDYA), a leading precision medicine oncology company, today announced the publication of abstracts for an oral presentation in the New Drugs on the Horizon series, and three poster presentations on IDE275 (GSK959) at the American Association for Cancer Research (AACR) Annual Meeting, taking place April 25-30, 2025, in Chicago, Illinois. IDE275 (GSK959), a potential best-in-class Werner Helicase (WRN) inhibitor, has demonstrated selective preclinical efficacy in the high microsatellite instability (MSI-H) solid tumor setting, and is advancing in a Phase 1 dose escalation trial in partnership with GSK. "IDE275 (GSK959) has a potential best-in-class profile and the preclinical data to be presented at AACR 2025 with GSK highlights the molecule's selectivity to treat MSI-H solid tumors and potential to be developed clinically as both a monotherapy agent and in combination with PD1," said Yujiro S. Hata, President and Chief Executive Officer, IDEAYA Biosciences. "MSI-H represents a meaningful biomarker-defined population with double-digit percent prevalence observed in multiple solid tumor types, including endometrial, colorectal, and gastric cancers. By binding uniquely to the helicase domain of WRN, IDE275 (GSK959) delivers potent and selective inhibition across MSI-H models," said Michael White, Ph.D., Chief Scientific Officer, IDEAYA Biosciences. IDE275 (GSK959) was discovered through a collaboration between IDEAYA and GSK. Preclinical studies have demonstrated IDE275's (GSK959) potential as a best-in-class WRN inhibitor, inducing single-agent tumor regressions in MSI-H patient-derived xenograft (PDX) and cell line-derived xenograft (CDX) models for endometrial, colorectal, and gastric cancers. Notably, MSI-H prevalence in these cancers has been reported at approximately 31%, 20%, and 19%, respectively, underscoring the significant patient population that could benefit from this therapeutic approach. As part of the collaboration, GSK is responsible for 80% of global research and development costs for IDE275 (GSK959), and IDEAYA is responsible for 20% of such costs. GSK holds a global, exclusive license to develop and commercialize IDE275 (GSK959). IDEAYA has the potential to earn a $10.0 million milestone payment upon initiation of Phase 1 clinical dose expansion. Additionally, IDEAYA is eligible to receive up to $465 million in future late-stage development and regulatory milestone payments. Upon commercialization, IDEAYA will be eligible to receive up to $475.0 million of commercial milestones, 50% of U.S. net profits and tiered royalties on global non-U.S. net sales of the IDE275 (GSK959) – ranging from high single-digit to sub-teen double-digit percentages, subject to certain customary reductions. At AACR 2025, IDEAYA will have 8 total presentations across 3 clinical and 2 pre-clinical programs. There will be 4 IDEAYA/GSK presentations of IDE275 (GSK959) and 4 additional presentations across the IDE397/MAT2A, IDE161/PARG, PRMT5, and KAT6/7 programs. Details for the oral presentation are as follows: Presenter: Dr. Yanhua Rao, GSK Title: An innovative and reversible WRN helicase inhibitor, GSK4418959 (IDE275), emerges as a promising clinical candidate for MSI-H cancers Session: New Drugs on the Horizon Session, Part 3 (DDT003) Date and Time: Monday, April 28, 2025 at 10:40am CDT Location: Room S406 (Vista Ballroom) - McCormick Place South (Level 4) Poster presentation details are below: Author: Rao, Y. et al. Title: Patient selection, target engagement and pharmacodynamic markers of WRN inhibitor GSK4418959 (IDE275) Poster Number: 6393/30 Session Title: Pharmacokinetics and Pharmacodynamics of Cancer Therapeutics Date and Time: Tuesday, April 29, 2025 at 9:00am – 12:00pm CDT Author: Lee, Y. et al. Title: Preclinical Characterization of GSK4418959 (IDE275): A Potent, Selective, and Highly Efficacious WRN Inhibitor for MSI-H Tumors Across Multiple Cancer Types Poster Number: 2913/20 Session Title: DNA Damage Response and Modulation of DNA Repair 1 Date and Time: Monday, April 28, 2025 at 2:00pm – 5:00pm CDT Author: Taygerly, P. et al. Title: Discovery of GSK4418959 (IDE275): A novel, non-covalent, reversible Werner Helicase inhibitor and a new potential therapeutic for the treatment of MSI-H cancers Poster Number: 5750/50 Session Title: Drug Design, Synthesis, & Disposition Date and Time: Tuesday, April 29, 2025 at 2:00pm CDT Author: Gupta, M. et al. Title: Dual KAT6/7 inhibition disrupts epigenetic programs that promote tumor evolution and adaptive drug resistance Poster Number: 442/3 Session Title: Epigenetic Targets Date and Time: Sunday, April 27, 2025 at 2:00pm – 5:00pm CDT Author: Maskey, R. et al. Title: PARG inhibition provokes a DNA damage-dependent innate immune reaction that enhances ICI-driven anti-tumor immunity Poster Number: 2899/6 Session Title: DNA Damage Response and Modulation of DNA Repair 1 Date and Time: Monday, April 28, 2025 at 2:00pm – 5:00pm CDT Author: Garbett, D. et al. Title: The allosteric MAT2A inhibitor IDE397 uniquely exploits metabolic liabilities associated with MTAP deletion to perturb DNA replication and repair Poster Number: 4268/25 Session Title: New and Emerging Cancer Drug Targets Date and Time: Tuesday, April 29, 2025 at 9:00am – 12:00pm CDT Author: Aubi, O. et al. Title: The impact of metabolite kinetics on dysregulation of essential enzymes in cancers with MTAP deficiencies Poster Number: 4504/15 Session Title: Proteomic Biomarkers and Therapeutics Date and Time: Tuesday, April 29, 2025 at 9:00am – 12:00pm CDT The oral presentation and posters will be available online at following the presentations. About IDEAYA Biosciences IDEAYA is a precision medicine oncology company committed to the discovery and development of targeted therapeutics for patient populations selected using molecular diagnostics. IDEAYA's approach integrates capabilities in identifying and validating translational biomarkers with drug discovery to select patient populations most likely to benefit from its targeted therapies. IDEAYA is applying its research and drug discovery capabilities to synthetic lethality – which represents an emerging class of precision medicine targets. Forward-Looking Statements This press release contains forward-looking statements, including, but not limited to, statements related to i) the publication of abstracts and oral and poster presentations on various drug programs; ii) the potential therapeutic benefit of IDE275; iii) the potential patient population that could benefit from IDE275; and iv) the potential for Ideaya to receive development and commercialization milestone payments and subsequent profits and royalties on net sales of IDE275. Such forward-looking statements involve substantial risks and uncertainties that could cause IDEAYA's preclinical and clinical development programs, future results, performance or achievements to differ significantly from those expressed or implied by the forward-looking statements. Such risks and uncertainties include, among others, the uncertainties inherent in the drug development process, including IDEAYA's programs' early stage of development, the process of designing and conducting preclinical and clinical trials, the regulatory approval processes, the timing of regulatory filings, the challenges associated with manufacturing drug products, IDEAYA's ability to successfully establish, protect and defend its intellectual property, and other matters that could affect the sufficiency of existing cash to fund operations. IDEAYA undertakes no obligation to update or revise any forward-looking statements. For a further description of the risks and uncertainties that could cause actual results to differ from those expressed in these forward-looking statements, as well as risks relating to the business of IDEAYA in general, see IDEAYA's Annual Report on Form 10-K dated February 18, 2025 and any current and periodic reports filed with the U.S. Securities and Exchange Commission. Investor and Media Contact IDEAYA Biosciences Andres Ruiz Briseno Chief Accounting Officer [email protected] SOURCE IDEAYA Biosciences, Inc. WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED

Eikon Therapeutics has secured a series of megarounds since its 2021 launch, with the most ambitious being a $517 million series B in 2022.\n Eikon Therapeutics is no stranger to eye-popping funding rounds, and the cancer-focused biotech has continued this trend with a $350.7 million series D to fuel its various clinical trials.California-based Eikon emerged publicly in 2021 with a stated goal to apply live-cell super-resolution microscopy to drug discovery. Headed up by former Merck & Co. EVP Roger Perlmutter, M.D., Ph.D., the biotech has secured a series of megarounds since then, with the most ambitious being a $517 million series B in 2022.Today’s series D, which was led by Eikon’s existing investors, brings the company’s total raised revenue to over $1.1 billion. Some of this money was already deployed a few years ago to buy four clinical-stage assets, although financial terms were never disclosed.One of these programs, a toll-like receptor 7 and 8 agonist immune modulator acquired from Seven and Eight Biopharma, now leads Eikon’s clinical pipeline. The asset, renamed EIK1001, is currently in a phase 3 trial for advanced melanoma.Next in line is EIK1003, a highly selective PARP1 inhibitor acquired from China-based IMPACT Therapeutics that is in a phase 1 trial in patients with breast, ovarian, prostate and pancreatic cancers. Meanwhile, Eikon is about to enter a central nervous system-penetrant PARP1-selective inhibitor licensed from IMPACT into phase 1 studies for brain cancers. Behind those are a pair of androgen receptor antagonists and an internally developed WRN inhibitor that the biotech hopes could be aimed at MSI-high and other DNA repair–deficient cancers.To fund these clinical explorations, Eikon sourced series D funding from the likes of Lux Capital, Alexandria Venture Investments, AME Cloud Ventures, The Column Group, E15 VC, Foresite Capital, General Catalyst and Soros Capital, to name a few.“With clinical studies now operating in 28 countries across five continents, we are accelerating the development of much-needed therapies while continuing to expand our research and development capabilities,” Perlmutter said in the Feb. 26 release.“This financing provides the resources necessary to build a fully integrated, 21st-century biotechnology company that leverages advanced computing, data sciences and decades of experience in bringing innovative medicines to patients,” the CEO added.