Venetoclax

2026 年美国癌症研究协会（AACR）年会，将于当地时间 4 月 17 日至 22 日在圣地亚哥召开。作为全球规模最大的癌症研究会议之一，AACR 历来是国内外药企展示前沿科研成果的重要舞台。 据不完全统计，今年国内有超 100 家药企亮相 AACR，带来了近 400 项研究成果，涉及恒瑞、百济、荣昌、亚盛、先声、齐鲁、映恩生物、复宏汉霖、德琪医药...等多家药企。本文将挑选部分企业进行具体介绍，以供参考。（文末附完整摘要表格下载）    恒瑞 今年 AACR 大会上，恒瑞将要展示 CDK2/4 抑制剂 Cpd-1308 的最新临床前研究数据。结果表明，Cpd-1308 对 CDK4:CDK6 的选择性高于 palbociclib，且展现出明显的克服耐药活性。 1904：双重靶向 CDK4 和 CDK2 克服 HR+ 乳腺癌症对 CDK4/6 抑制剂的耐药性。    百济 今年 AACR 大会上，百济将带来两款 Bcl-2 抑制剂 BGB-21447、Sonrotoclax（BGB-11417），以及 PRMT5 抑制剂 BGB-58067 的最新临床前研究结果。 7899：临床前研究中，下一代 Bcl-2 抑制剂 BGB-21447 显示出在 Bcl-2 过表达的 B 细胞非霍奇金淋巴瘤（NHL）癌症中的高潜力。 4663：下一代 Bcl-2 抑制剂 BGB-21447，在血液系统恶性肿瘤的临床前模型中显示出卓越的效力并克服了 Venetoclax 的耐药性。 3901：BGB-58067 是一种脑渗透性 MTA 协同 PRMT5 抑制剂，在 MTAP 缺失的肿瘤中显示出有前景的抗肿瘤活性和良好的选择性。 2926：Sonrotoclax（BGB-11417）是一种选择性 Bcl-2 抑制剂，在血液学癌症细胞、异种移植物和人类血液中的疗效优于 Venetoclax 和Lisaftoclax。    荣昌 今年 AACR 大会上，荣昌生物将带来多款创新 ADC 和小分子抑制剂的最新临床前研究结果，包括 c-Met ADC RC108、CLDN18.2 ADC RC118、 menin-MLL 抑制剂 RCZY-843、pan-RAS (ON) 抑制剂 RCZY-690等。 2931：RC108 是一种靶向 c-Met 的 ADC，与 Teliso-V 相比，在 cMet 高表达和 HGF 依赖性肿瘤细胞之间表现出不同的细胞毒性，表明其具有潜在的安全优势 5643：RC118 ADC 的临床前特征及其与其他抗 CLDN18.2 抗体的差异结合模式的鉴定。 4503：RCZY-843 是 一种潜在的同类最佳的第二代 menin-MLL 抑制剂，旨在克服临床观察到的 menin 突变介导的耐药性，在急性白血病模型中具有优异的临床前疗效和安全性。 5778：RCZY-690 是一种三重复合物分子胶广谱 RAS (ON) 抑制剂，对 RAS 成瘾的实体瘤具有同类最佳的潜力。 1675：PR-ADCs 是一种旨在降低游离载荷毒性并提升治疗指数的新型 ADC 平台。    亚盛 今年 AACR 大会上，亚盛将带来 BCR-ABL 抑制剂奥雷巴替尼、FAK/ALK/ROS1 三联酪氨酸激酶抑制剂 APG-2449、以及 PRC2/EED 抑制剂 APG-5918 的最新临床前研究结果。 4583：多靶点激酶抑制剂奥雷巴替尼（HQP1351）在子宫内膜癌（EC）临床前模型中具有显著疗效，且与化疗联合时可产生协同增效作用。 5875：多激酶抑制剂奥雷巴替尼（HQP1351）在套细胞淋巴瘤（MCL）临床前模型中具有抗肿瘤疗效，并与 BTK 抑制剂阿可替尼存在协同作用。 1858：在 BRAF V600E 突变肿瘤模型中，APG-2449 通过抑制 FAK 活性增强 MAPK 通路阻断的抗肿瘤作用。 4500：胚胎外胚层发育蛋白（EED）抑制剂 APG-5918 通过表观遗传调控增强化疗敏感性，在小细胞肺癌（SCLC）临床前模型中与拓扑异构酶I抑制剂产生显著协同抗肿瘤效应。 限于篇幅，本文不一一赘述，更多可下载 AACR 2026 会议全部摘要摘要表格。添加小音微信好友，发送「AACR2026」即可获取下载。 封面来源：Insight 制图 免责声明：本文仅作信息分享，不代表 Insight 立场和观点，也不作治疗方案推荐和介绍。如有需求，请咨询和联系正规医疗机构。 编辑：月牙 PR 稿对接：微信 insightxb 投稿：微信 insightxb；邮箱 insight@dxy.cn

SAN DIEGO, March 17, 2026 (GLOBE NEWSWIRE) -- BlossomHill Therapeutics, Inc. , a privately-held, clinical-stage biopharmaceutical company focused on the design and development of next-generation medicines for cancer, today announced it will introduce its next-generation KRAS pipeline at the American Association for Cancer Research (AACR) Annual Meeting 2026. These two non-covalent pan-KRAS inhibitors leverage a differentiated chemical scaffold to address limitations of contemporary molecules - achieving sub-nanomolar potency and a prolonged off-rate, combined with oral bioavailability. In addition, the company will present new preclinical data supporting the continued advancement of its clinical programs BH-30643, a first-in-class, mutant-selective, macrocyclic OMNI-EGFR TM inhibitor, and BH-30236, an oral CLK inhibitor for hematologic malignancies. The AACR Annual Meeting 2026 will be held April 17-22, 2026, in San Diego. “We are excited to share new data from across our pipeline at AACR, including new preclinical data supporting the continued advancement of our lead clinical programs BH-30643 and BH-30236, and the introduction of our novel switch II-targeting KRAS programs, one of which will be highlighted during a minisymposium,” said Jean Cui, Ph.D., Founder and Chief Executive Officer of BlossomHill Therapeutics. “KRAS remains one of the most important and historically difficult targets in oncology. Our next-generation pan-KRAS inhibitors are intentionally designed using a differentiated chemical scaffold to deliver pseudo-irreversible target engagement and improved drug-like properties we believe will translate to clinical impact. We look forward to engaging with the scientific community at the upcoming AACR meeting.” Details of the presentations are as follows: Title: Discovery and characterization of BH-501284: A non-covalent, pan-KRAS inhibitor for treatment of diverse KRAS-mutant tumors (#6736) Date & Time: April 21, 2026; 2:30-4:30 p.m. PT Session Title: Targeted Therapies Session Type: Minisymposium Location: San Diego Convention Center Key Findings: BH-501284 is a potent, selective, orally available non-covalent pan-KRAS inhibitor that demonstrates picomolar binding affinity, broad activity across KRAS mutations, and durable tumor regression in non-small cell lung cancer (NSCLC), colorectal cancer (CRC) and pancreatic ductal adenocarcinoma (PDAC models). By preferentially targeting inactive KRAS and maintaining activity under growth factor-driven resistance conditions, BH-501284 may overcome key limitations of existing KRAS inhibitors. Title: Design and discovery of BH-501242, a novel pan-KRAS on/off inhibitor targeting KRAS switch II pocket (#5120) Date & Time: April 21, 2026; 9:00 a.m.-12:00 p.m. PT Session Title: New Ligands and Inhibitors Location: San Diego Convention Center, Poster Section 38 Key Findings: Preclinical data demonstrate that BH-501242, a novel pan-KRAS inhibitor targeting the switch II pocket, potently inhibits a broad range of KRAS mutations, including G12D, G12V, and G12C, with sub-nanomolar cellular activity and robust tumor regression in multiple xenograft models. Its ability to bind both active and inactive KRAS and achieve strong oral exposure supports further development as a differentiated, mutation-agnostic KRAS therapy. Title: CLK inhibitor BH-30236 synergizes with venetoclax in anti-leukemia activity via splicing modulation in preclinical AML and CLL models (#5872) Date & Time: April 21, 2026; 2:00-5:00 p.m. PT Session Title: Tyrosine Kinase, Phosphatase, and Other Inhibitors Location: San Diego Convention Center, Poster Section 18 Key Findings: BH-30236, a novel oral CLK1/2/4 inhibitor, modulates alternative splicing to induce apoptosis and suppress leukemia stem cell–associated pathways, demonstrating robust anti-leukemia activity in acute myeloid leukemia (AML) and chronic lymphocytic leukemia (CLL) models. In combination with venetoclax, BH-30236 produced synergistic tumor regression, including durable, complete responses in resistant xenograft models. Title: BH-30643, a novel macrocyclic non-covalent, mutant-selective EGFR inhibitor, addresses the resistance and potency limitations of contemporary EGFR TKIs (#5877) Date & Time: April 21, 2026; 2:00-5:00 p.m. PT Session Title: Tyrosine Kinase, Phosphatase, and Other Inhibitors Location: San Diego Convention Center, Poster Section 18 Key Findings: BH-30643 is a macrocyclic, non-covalent, mutant-selective OMNI-EGFR inhibitor that uniquely overcomes T790M and C797S resistance mutations while maintaining potent activity against classical EGFR drivers and sparing wildtype EGFR. In preclinical studies, BH-30643 demonstrated prolonged suppression of tumor cell proliferation compared to osimertinib, including under growth factor-mediated resistance conditions. About BlossomHill Therapeutics BlossomHill Therapeutics, Inc. is a privately held, clinical-stage biopharmaceutical company focused on designing and developing next-generation targeted therapies for cancer. Founded and led by industry veteran J. Jean Cui, Ph.D., with her proven track record in oncology drug design and development – including three FDA-approved drugs – BlossomHill applies cutting-edge science to address key oncogenic drivers and improve patient outcomes in difficult-to-treat cancers. The company’s lead clinical programs include BH-30643, a first-in-class, macrocyclic, non-covalent, mutant-selective OMNI-EGFR TM inhibitor for the treatment of EGFR- or HER2-mutated non-small cell lung cancer (NSCLC), and BH-30236, a macrocyclic CLK inhibitor for the treatment of relapsed or refractory acute myeloid leukemia (R/R AML) or higher-risk myelodysplastic syndrome (HR-MDS), representing a first-in-class opportunity. BlossomHill Therapeutics is headquartered in San Diego, California and has raised a total of $257 million from leading life sciences investors. For more information, visit bhtherapeutics.com and follow us on LinkedIn and X . Contacts: Media: Ashlea Kosikowski 1AB ashlea@1abmedia.com Investors: Alicia Davis 1AB alicia@1abmedia.com