Valemetostat Tosilate

SOUTH SAN FRANCISCO, Calif. and SAN DIEGO, April 17, 2026 (GLOBE NEWSWIRE) -- ORIC Pharmaceuticals, Inc. (Nasdaq: ORIC), a clinical stage oncology company focused on developing treatments that address mechanisms of therapeutic resistance, today announced the presentation of multiple poster presentations at the 2026 American Association for Cancer Research (AACR) Annual Meeting highlighting the potential of rinzimetostat (ORIC-944), a potent and selective allosteric inhibitor of PRC2 to treat prostate cancer. The posters can be found in the publication section of ORIC’s website here. “Our research continues to show the therapeutic potential of PRC2 inhibition across the prostate cancer disease spectrum, by reducing tumor adaptability and sustaining the benefit derived from androgen-receptor targeted therapies,” said Lori Friedman, PhD, chief scientific officer. “Additionally, our preclinical studies reveal that targeting PRC2 via EED has potential advantages over targeting EZH2, which, together with the clinical data generated to date, furthers our conviction that rinzimetostat is a potential best-in-class PRC2 inhibitor.” Poster presentations: Rinzimetostat blockade of PRC2 activity, a key mechanism of treatment resistance, improves response of androgen receptor pathway inhibition across a spectrum of prostate cancer models Key findings of the presentation: In a transcriptomics analysis of >1,100 prostate samples spanning normal prostate, primary prostate cancer, and metastatic disease, PRC2 activity was observed early in the development of prostate cancer and was sustained during disease progression and treatment resistance, highlighting it as a critical therapeutic target. More than half of localized primary tumors demonstrated elevated PRC2 activity vs. normal prostate tissue, and an elevated PRC2 activity in locally advanced tumors associates with poor survival, indicative of a key role early in the disease. Elevated PRC2 activity was observed in the vast majority of both metastatic CSPC and metastatic CRPC tumors relative to normal prostate tissue. Rinzimetostat in combination with darolutamide demonstrated antitumor activity across a breadth of in vivo models representing the prostate cancer continuum, including CSPC and CRPC. More than half of localized primary tumors demonstrated elevated PRC2 activity vs. normal prostate tissue, and an elevated PRC2 activity in locally advanced tumors associates with poor survival, indicative of a key role early in the disease. Elevated PRC2 activity was observed in the vast majority of both metastatic CSPC and metastatic CRPC tumors relative to normal prostate tissue. Rinzimetostat, an allosteric EED inhibitor with best-in-class properties for the treatment of prostate cancer, is effective in PRC2 methyltransferase-resistant settings in preclinical studies Key findings of the presentation: PRC2 inhibition induces transcriptional and chromatin effects that restrain tumor plasticity and enhance antitumor activity of androgen receptor inhibitors in prostate cancer models. Differential potency of PRC2 inhibitors on EZH1- vs. EZH2-containing complexes impacts activity in resistance contexts, providing potential advantages for EED targeting. Rinzimetostat retained antitumor activity in prostate cancer cells with overexpressed EZH1 in vitro, while potency was diminished for mevrometostat or tazemetostat. Preclinical studies show that rinzimetostat overcomes acquired resistance mechanisms observed in the clinic for tazemetostat and valemetostat. Rinzimetostat demonstrates improved solubility, oral bioavailability, CYP profile, and clinical half-life versus comparator compounds. Rinzimetostat retained antitumor activity in prostate cancer cells with overexpressed EZH1 in vitro, while potency was diminished for mevrometostat or tazemetostat. Preclinical studies show that rinzimetostat overcomes acquired resistance mechanisms observed in the clinic for tazemetostat and valemetostat. About ORIC Pharmaceuticals, Inc. ORIC Pharmaceuticals is a clinical stage biopharmaceutical company dedicated to improving patients’ lives by Overcoming Resistance In Cancer. ORIC’s clinical stage product candidates include (1) rinzimetostat, an allosteric inhibitor of the polycomb repressive complex 2 (PRC2) via the EED subunit, being developed for prostate cancer, and (2) enozertinib, a brain-penetrant inhibitor targeting EGFR exon 20 and EGFR PACC mutations, being developed for NSCLC. ORIC has offices in South San Francisco and San Diego, California. For more information, please go to www.oricpharma.com, and follow us on X or LinkedIn. Cautionary Note Regarding Forward-Looking Statements This press release contains forward-looking statements as that term is defined in Section 27A of the Securities Act of 1933 and Section 21E of the Securities Exchange Act of 1934. Statements in this press release that are not purely historical are forward-looking statements. Such forward-looking statements include, among other things, the continued clinical development of rinzimetostat; the potential advantages of rinzimetostat; statements regarding the potential best-in-class properties of rinzimetostat; the development plans and timelines for rinzimetostat and enozertinib; plans underlying ORIC’s clinical trials and development; and statements by the company’s chief scientific officer. Words such as “believes,” “anticipates,” “plans,” “expects,” “intends,” “will,” “goal,” “potential” and similar expressions are intended to identify forward-looking statements. The forward-looking statements contained herein are based upon ORIC’s current expectations and involve assumptions that may never materialize or may prove to be incorrect. Actual results could differ materially from those projected in any forward-looking statements due to numerous risks and uncertainties, including but not limited to: risks associated with the process of discovering, developing and commercializing drugs that are safe and effective for use as human therapeutics and operating as an early clinical stage company; ORIC’s ability to develop, initiate or complete preclinical studies and clinical trials for, obtain approvals for and commercialize any of its product candidates; changes in ORIC’s plans to develop and commercialize its product candidates; the potential for clinical trials of rinzimetostat, enozertinib or any other product candidates to differ from preclinical, initial, interim, preliminary or expected results; negative impacts of health emergencies, economic instability or international conflicts on ORIC’s operations, including clinical trials; the risk of the occurrence of any event, change or other circumstance that could give rise to the termination of ORIC’s license and collaboration agreements or its clinical trial collaboration and supply agreements; the potential market for ORIC’s product candidates, and the progress and success of competing therapeutics currently available or in development; ORIC’s ability to raise any additional funding it will need to continue to pursue its business and product development plans; regulatory developments in the United States and foreign countries; ORIC’s reliance on third parties, including contract manufacturers and contract research organizations; ORIC’s ability to obtain and maintain intellectual property protection for its product candidates; the loss of key scientific or management personnel; competition in the industry in which ORIC operates; general economic and market conditions; and other risks. Information regarding the foregoing and additional risks may be found in the section entitled “Risk Factors” in ORIC’s Annual Report on Form 10-K filed with the Securities and Exchange Commission (the SEC) on February 23, 2026, and ORIC’s future reports to be filed with the SEC. These forward-looking statements are made as of the date of this press release, and ORIC assumes no obligation to update the forward-looking statements, or to update the reasons why actual results could differ from those projected in the forward-looking statements, except as required by law. Contact: Dominic Piscitelli, Chief Financial Officer dominic.piscitelli@oricpharma.com info@oricpharma.com

2026年4月3日，中国国家药品监督管理局（NMPA）官网公示，上海海和药物研发的1类新药艾普美妥司他片上市申请获受理，并被纳入优先审评审批程序。这款强效、高选择性的EZH1/2双靶小分子抑制剂拟用于治疗不可手术的局部晚期或转移性经治上皮样肉瘤（ES）患者，有望填补国内该领域的治疗空白，为这一罕见且难治的肿瘤患者带来新希望。 一、直击临床痛点：破解罕见肉瘤治疗困局 上皮样肉瘤（Epithelioid Sarcoma, ES）是一种侵袭性软组织肉瘤，发病率不足软组织肉瘤的1%，却以恶性程度高、易转移著称。根据发病部位分为远端型和近端型，前者好发于青壮年，后者多见于中老年人，且男性发病率更高。对于不可手术的局部晚期或转移性患者，传统治疗手段效果有限，靶向治疗选择匮乏，临床需求极为迫切。艾普美妥司他的出现，正是瞄准这一未被满足的医疗“荒漠”。二、双靶机制突破：更彻底的表观遗传调控 艾普美妥司他靶向EZH1和EZH2两个关键蛋白，属于新一代表观遗传调控剂。EZH2作为多梳抑制性复合物2（PRC2）的催化亚基，通过催化H3K27me3修饰调控基因表达，其异常激活与多种肿瘤发生发展密切相关。而EZH1作为EZH2的同源蛋白，可在EZH2被抑制时产生代偿作用。因此，双重抑制EZH1/2能有效阻断代偿机制，更彻底降低细胞内H3K27me3水平，增强抗肿瘤活性。临床前研究显示，艾普美妥司他在EZH2突变淋巴瘤及SWI/SNF复合物突变实体瘤中均展现强大活性，且在同等剂量下，抗肿瘤效果优于已上市的EZH2单靶抑制剂他泽司他。三、临床数据亮眼：为罕见病带来切实希望 2023年美国临床肿瘤学会（ASCO）年会公布的I/II期研究（I期部分）初步结果验证了艾普美妥司他的潜力： 纳入患者：中国4家中心共32名ES患者，中位前线治疗2线，31.3%接受过≥3线治疗，96.9%存在INI1表达缺失（ES典型特征）。 疗效数据： 总体缓解率（ORR）：28.1%，疾病控制率（DCR）：78.1%。 中位至缓解时间仅1.9个月，1例患者实现完全缓解（CR）且持续273天。 400mg BID剂量组表现更优：ORR 36.4%，DCR 81.8%。 这些数据不仅远超传统治疗预期，也印证了EZH1/2双靶策略在ES中的临床价值。四、全球竞速领跑者：国产创新填补空白 在EZH1/2双靶抑制剂赛道，全球目前仅日本第一三共的Valemetostat（伐美妥司他）获批上市。海和药物的艾普美妥司他作为国产首款申报上市的EZH1/2抑制剂，进度领先诺华、和黄医药等国际药企，有望改写中国ES治疗格局。其成功获批将不仅填补临床空白，更代表中国创新药企在表观遗传治疗领域从“跟跑”到“并跑”的突破。五、未来展望：表观遗传治疗新纪元 艾普美妥司他的上市申请获受理，不仅是ES患者的希望曙光，更标志着中国原创新药在罕见病和难治性肿瘤领域的持续突破。随着更多表观遗传调控剂的研发，未来有望通过联合治疗策略进一步延长患者生存、提升生活质量。海和药物的探索，为中国创新药企开辟了新的技术路径，也为全球肿瘤治疗贡献了“中国方案”。 从基础研究到临床突破，从实验室到患者床边，艾普美妥司他走过了一条充满挑战的创新之路。这款药物的潜在获批，不仅将改写ES治疗格局，更彰显中国生物医药产业在攻克罕见病、突破技术壁垒上的坚定决心。期待更多创新成果加速落地，为人类对抗疾病注入更强力量！ 手机耳机党注意！你天天戴的耳机，可能正在把“毒”吸进大脑？ 再添利剑，福元医药重磅口服护肝药获批上市 甘李药业GLR2037片完成首例给药，PROTAC技术开启前列腺癌治疗新纪元 人福医药同日斩获两款重磅仿制药！首仿芬太尼口颊片，切入3.7亿辅助生殖赛道 Ultragenyx基因疗法UX111再获FDA受理！有望成为全球首款MPSⅢA疗法 剑指百亿卵巢癌市场！阿斯利康FRα ADC国内启动III期临床，剑指“药王”索米妥昔单抗