Prexasertib Mesylate Hydrate

AP3 Generative AI KaiSR model globally assesses drug effects on the entire intracellular protein signaling network for optimal drug design and precision medicine development Favorable ACR-2316 preclinical data, demonstrating its differentiated and superior pathway effects versus benchmark WEE1 and PKMYT1 inhibitors consistent with prior observations Company to report initial clinical data for ACR-2316 in AP3-predicted tumor types later this year; clinical activity and confirmed partial response observed during dose escalation WATERTOWN, Mass., Oct. 22, 2025 (GLOBE NEWSWIRE) -- Acrivon Therapeutics, Inc. (“Acrivon” or “Acrivon Therapeutics”) (Nasdaq: ACRV), a clinical stage biotechnology company discovering and developing precision medicines utilizing its proprietary Generative Phosphoproteomics AP3 (Acrivon Predictive Precision Proteomics) platform designed to interpret and quantify compound specific, drug-regulated pathway activity levels inside the intact cell in an unbiased and actionable manner, today announced three presentations at the AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics taking place from October 22-26, 2025 in Boston, MA. “At this year’s AACR-NCI-EORTC meeting, we are excited to present a powerful set of posters that illustrate our unique and data-driven approach to precision medicine development and generative AI drug discovery,” said Kristina Masson, Ph.D., M.B.A., co-founder and executive vice president of business operations at Acrivon and president and CEO of the company´s research subsidiary Acrivon AB in Lund, Sweden. “Our presentations feature our innovative AP3 KaiSR ensemble model, which expands our ability to rationally design drugs optimized for desirable activity on biologically relevant pathways in the intact cell, as well as robust mechanistic data for ACR-2316 including pathway analyses that underpin the superior preclinical activity of the asset. We look forward to sharing initial clinical data from our Phase 1 study of ACR-2316 later this year, building upon the disclosed clinical activity already observed across AP3-predicted solid tumor types during the dose-escalation phase." Details for Presentations Poster Title:Global pharmacodynamic effects uncovered with AP3 phosphoproteomic profiling of novel WEE1/PKMYT1 inhibitor ACR-2316 reveals the critical importance of PLK1 for ACR-2316’s superior preclinical activity and differentiated mechanism of actionSession:Poster Session ADate and Time:Thursday, October 23 | 12:30-4:00 p.m. ET Poster Title:Acrivon Therapeutics’ generative AI ensemble model (KaiSR) accurately predicts and expands proprietary, actionable kinase-substrate relationships globally for the human kinomeSession:Poster Session CDate and Time:Saturday, October 25 | 12:30-4:00 p.m. ET Poster Title:ACR-2316 is a novel, differentiated, clinical-stage WEE1/PKMYT1 inhibitor designed by Acrivon’s Generative Phosphoproteomics AP3 Platform for optimal pro-apoptotic pathway effects in tumor cells resulting in superior preclinical activitySession:Poster Session CDate and Time:Saturday, October 25 | 12:30-4:00 p.m. ET The posters will be available on Acrivon’s website in the “Science and Publications” section upon or shortly after presentation at the AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics. About Acrivon Therapeutics Acrivon is a clinical stage biopharmaceutical company discovering and developing precision medicines utilizing its proprietary Generative Phosphoproteomics AP3 platform. The platform allows the company to interpret and quantify compound specific, drug-regulated pathway activity levels inside the intact cell in an unbiased manner, yielding terabytes of proprietary data and delivering rapid, actionable insights. The Generative Phosphoproteomics AP3 platform is comprised of a growing suite of powerful, internally-developed tools, including the AP3 Data Portal, converting multimodal data into structured data for generative AI analyses, the AP3 KaiSR Kinase Substrate Relationship Predictor, and the AP3 Interactome. These distinctive capabilities enable the company to go beyond the limitations of traditional drug discovery, as well as current AI-based target-centric drug discovery, and rapidly design highly differentiated compounds with desirable pathway effects through intracellular protein network analyses and advance these agents into the clinic for streamlined development. Acrivon is currently advancing its lead program, ACR-368 (also known as prexasertib), a selective small molecule inhibitor targeting CHK1 and CHK2 in a potentially registrational Phase 2b trial for endometrial cancer. The company has received Fast Track designation from the Food and Drug Administration, or FDA, for the investigation of ACR-368 as a monotherapy based on OncoSignature-predicted sensitivity in patients with endometrial cancer. The FDA has granted a Breakthrough Device designation for the ACR-368 OncoSignature assay for the identification of patients with endometrial cancer who may benefit from ACR-368 treatment. In addition, the company has initiated a third arm to the Phase 2b study without the need for a pre-treatment biopsy to evaluate ACR-368 with ultra-low-dose gemcitabine (ULDG) sensitization in all-comer, biomarker-unselected 2nd line patients with endometrial cancer who have all received prior treatment with chemotherapy and anti-PD-1. Acrivon is also leveraging its proprietary Generative Phosphoproteomics AP3 platform for developing its co-crystallography-driven, internally discovered pipeline programs. These include ACR-2316, the company’s second clinical stage asset, a novel, potent, selective WEE1/PKMYT1 inhibitor designed for superior single-agent activity through strong activation of not only CDK1 and CDK2, but also of PLK1 to drive pro-apoptotic cell death, as observed in preclinical studies against benchmark inhibitors. The Phase 1 trial of ACR-2316 is advancing with enrollment in the first three dose-escalation cohorts completed. Drug target engagement was observed at DL1 and 2 using the company’s clinical mass spectrometry-based AP3 profiling, with evidence of approximate dose proportionality based on plasma pharmacokinetic analyses, and initial clinical activity and confirmed partial response. In addition, the company is advancing a preclinical program directed against an undisclosed cell cycle regulatory target. Forward-Looking Statements This press release includes certain disclosures that contain “forward-looking statements” within the meaning of the Private Securities Litigation Reform Act of 1995 about us and our industry that involve substantial risks and uncertainties. All statements other than statements of historical facts contained in this press release, including statements regarding our preclinical and clinical results, business strategy and plans and objectives of management for future operations, are forward-looking statements. In some cases, you can identify forward-looking statements because they contain words such as “anticipate,” “believe,” “contemplate,” “continue,” “could,” “estimate,” “expect,” “intend,” “may,” “plan,” “potential,” “predict,” “project,” “should,” “target,” “will,” or “would” or the negative of these words or other similar terms or expressions. Forward-looking statements are based on Acrivon’s current expectations and are subject to inherent uncertainties, risks and assumptions that are difficult to predict. Factors that could cause actual results to differ include, but are not limited to, risks and uncertainties that are described more fully in the section titled “Risk Factors” in our reports filed with the Securities and Exchange Commission. Forward-looking statements contained in this press release are made as of this date, and Acrivon undertakes no duty to update such information except as required under applicable law. Investor and Media Contacts: Adam D. Levy, Ph.D., M.B.A. alevy@acrivon.com Alexandra Santos asantos@wheelhouselsa.com

恒瑞医药 WO2025176180 HER2-艾日布林衍生物 SHR-4602 8月28日，恒瑞医药公开一篇ADC专利，涉及靶点HER2，抗体为 Pertuzumab，有效载荷为艾日布林衍生物，该 ADC 旨在治疗抗 HER2 ADC 耐药的肿瘤，包括乳腺癌、胃癌、结直肠癌、尿路上皮癌、胆管癌、肺癌等。 SHR-4602 是恒瑞自主研发的一种新型抗 HER2 ADC，抗体采用帕妥珠单抗，利用肽连接子偶联有效载荷 ER300（艾日布林衍生物）。恒瑞在2024年的 AACR 会议摘要中披露该药物的临床前数据。2024年12月，SHR-4602 的新药临床申请获 NMPA 批准，用于晚期实体瘤，目前该药物正在进行临床  2 期研究。 SONY WO2025177173 抗体-聚合物偶联物 8月28日，Sony 集团公开一篇抗体聚合物偶联药物专利，靶点涉及 CD33、CD30、CD7、CD123。聚合物含有侧链的脱氧尿苷基团，有效载荷为 MMAE，通过 VC 连接子裂解释放，同时聚合物含有高亲水性结构 HEG（即磷酸-PEG），通过灵调整长度可以根据需要提高或降低 ADC 药物整体水溶性。 日内瓦大学 WO2025176733 ATR或CHK1抑制剂 ADC 8月28日，日内瓦大学公开一篇 ADC 专利，涉及非细胞毒载荷，专利公开采用 ATR 或 CHK1 抑制剂为 ADC 有效载荷，其中 ATR 抑制剂优选 camonsertib、Elimusertib；CHK1抑制剂优选 Prexasertib。实施例将 ATR 或 CHK1 抑制剂通过肽连接子与抗 HER2 抗体偶联，其中肽连接子包括GPVK、GGFG、GGNN、GNLK、GLVK、GPLK、GGGF、GPVR、VC-PABC 等。 Abdera WO2025179051、WO2025179031 DLL3 RDC ABD-147、5T4 RDC 8月28日，Abdera Therapeutics 公开两篇 RDC 专利，涉及靶点 DLL3 和 5T4，靶向部分为抗体片段 VHH-Fc，与螯合剂 DOTA-linker 通过四氟苯酯（OTFP）接头偶联，螯合剂-抗体比（CAR）值约为4，然后分别 111In、177Lu 或 225Ac 进行放射性标记后得到 RDC 药物。 Abdera Therapeutics 的核心研发项目之一 ABD-147 是一款靶向 DLL3 的 RDC 药物，其基于公司独特的 ROVEr™ 平台（设计和开发具有可调节药代动力学特性的放射性药物）开发，以提高治疗效果并减少副作用。ABD-147 的 IND 申请在2024年04月获得美国 FDA 批准，目前正在进行临床 1 期研究，用于治疗小细胞肺癌和肺大细胞神经内分泌癌。 ABD-147 对应的诊断性核药和治疗性核药分别为 111In-ABD147 和 225Ac-ABD147。 往期分享： 专利动态|XDC的新linekr或新靶点 专利动态|偶联药物新专利（2025.08.14） 专利动态|新一周的ADC专利（2025.08.07） 专利动态|最新偶联药物（XDC）专利（2025.07.31） 专利动态 | 新ADC专利公开：新机制载荷/新靶点/新项目(2025.07.24) 专利分享|糖基偶联新型二糖连接子：齐鲁 vs GlycoT 专利动态 | 最新ADC药物相关专利 专利动态 | 在研ADC最新专利公开 专利分享 | 先声药业FGFR2b ADC药物SIM0686 专利分享 | 亲合力生物的白蛋白偶联药物 QHL-1618，肿瘤微环境释放 专利分享 | 新型ADC载荷靶向破解肿瘤耐药 专利分享 | "孤勇者"的妥协？Heidelberg Pharma获华东医药投资后转向TOP1i ADC 专利分享 | 先声药业ADC偶联"接头"新技术公开 专利分享 | MTG酶定点偶联+点击化学：Hummingbird 双载荷ADC技术公开 上海诗健生物新一代ADC平台专利公开 **说明：本公众号内容基于公开信息的整理和分析，如涉及侵权请联系处理；作者水平有限，对专利或文献的解读可能存在疏漏之处，请以原文为准；欢迎个人转发分享，如需转载至公众号或其他平台，请注明出处并遵守版权规范。** 参考资料：      Tian Y, Sun X, Yang C, Liao C. Abstract 3195: SHR-4602, next generation of HER2-targeting ADC with potent anti-tumor efficacy overcoming the resistance of HER2 ADC with Topo I inhibitor payload in xenograft models. Cancer Research. 2024;84(6_Supplement):3195-3195. doi:10.1158/1538-7445.am2024-3195  药物临床试验登记与信息公示平台官网 clinicaltrials 官网 公司官网 END 欢迎关注，与您分享偶联药物领域最新突破