复宏汉霖潜在BIC口服KAT6A/B抑制剂HLX97完成I期首例受试者给药，破局乳腺癌内分泌治疗耐药

2026年5月13日，复宏汉霖（2696.HK）宣布，公司自主研发的创新型口服赖氨酸乙酰转移酶6A/B（KAT6A/B）小分子抑制剂HLX97在晚期/转移性实体瘤患者中的I期临床研究于中国完成首例受试者给药。

乳腺癌是全球发病率位居第二且在女性群体中最为高发的恶性肿瘤，亦是导致女性癌症相关死亡的主要原因。其中，雌激素受体阳性（ER+）乳腺癌是最常见的分子亚型，约占所有乳腺癌病例的70%¹。尽管抑制雌激素生成、直接靶向ER的干预措施等内分泌治疗已成为其基石疗法，显著降低了ER+乳腺癌的复发率和死亡率，但新生耐药和获得性耐药仍然是一项重大挑战。

KAT6A（Lysine Acetyltransferase 6A）及其旁系同源物KAT6B（Lysine Acetyltransferase 6B）是MYST 家族的组蛋白赖氨酸乙酰转移酶(HAT)，在多种肿瘤的发生发展和耐药机制中发挥着关键作用。据多项临床前及临床研究显示，在既往接受过多种治疗的ER+/HER2-转移性乳腺癌患者中，KAT6A基因的扩增/过表达与内分泌治疗耐药性的产生密切相关。此外，KAT6A/B基因的异常表达在卵巢癌、子宫颈癌、结直肠癌、前列腺癌、肺癌和脑胶质瘤中等多种实体瘤中广泛存在^2-4，提示KAT6A/B抑制剂在多类肿瘤的治疗中具有广阔的应用潜力。鉴于乳腺癌中KAT6A基因的扩增/过表达已被证实与内分泌治疗耐药性的产生密切相关，抑制KAT6A/B活性有望成为一种克服乳腺癌内分泌治疗耐药的有效策略^5-6。

HLX97是一款具有同类最优（Best-in-class，BIC）潜力的创新型口服KAT6A/B抑制剂，通过精准抑制KAT6A/B的活性，HLX97能够控制肿瘤细胞的增殖，诱导肿瘤细胞凋亡。HLX97具有“快速起效、快速清除”药代动力学特性和高选择性，旨在最大化药物抗肿瘤活性的同时减轻产品的血液毒性。非临床研究显示，HLX97能够显著抑制KAT6A/B活性，并具备良好的抗肿瘤效果及安全性特征。在临床前动物药效模型中，HLX97在ER阳性乳腺癌模型，以及对氟维司群和爱博新（CDK4/6抑制剂）双重耐药的人源乳腺癌皮下移植瘤模型中均表现出显著疗效，且整体耐受性良好。

通过自主研发与战略引进，复宏汉霖已在乳腺癌领域建立了“全域全程全球”的完整治疗生态，产品管线包括中美欧等全球50多个国家和地区获批上市曲妥珠单抗生物类似药汉曲优^®(美国商品名：HERCESSI^™，欧洲商品名：Zercepac^®)，首个美国获批的帕妥珠单抗生物类似药POHERDY^®，早期强化辅助治疗药物汉奈佳^®（奈拉替尼），创新CDK4/6抑制剂复妥宁^®（伏维西利）等上市产品，以及新表位抗HER2单抗HLX22、新型内分泌疗法拉索昔芬片HLX78、LIV-1靶点ADC HLX41、HER2双表位ADC HLX49、HER2 ADC HLX87等高潜创新分子。通过持续推进覆盖乳腺癌各分型与分期的单药及联合疗法的临床探索，复宏汉霖不断强化管线协同效应，全面提升覆盖与治疗价值，致力于”不让一个乳腺癌患者落下“。

未来，复宏汉霖还将持续立足于未满足的临床需求，充分发挥公司在抗体药物领域的一体化平台优势，不断拓展疾病领域和新分子类型，为全球患者带来更多高质量、可负担的创新治疗方案。

关于HLX97-FIH101

本研究为一项多中心、开放标签的I期临床研究，旨在评估HLX97在晚期或转移性实体瘤患者中的安全性、耐受性、药代动力学（「PK」）特征及初步抗肿瘤疗效。研究分为两个部分：第一部分（Part1）为剂量递增阶段，包括单药剂量递增（Part1A）和联合用药剂量递增（Part1B）；第二部分为剂量扩展阶段（Part2）。Part1A单药递增在晚期/转移性实体瘤患者中开展，设1.0mg至15.0mg共5个剂量水平，HLX97于每个周期第1-28天连续口服给药，每日1次，每4周为1周期；Part1B联合用药将在HR阳性HER2阴性局部晚期或转移性乳腺癌患者中探索2至3个剂量的HLX97联合氟维司群的方案。Part2在HR阳性HER2阴性局部晚期或转移性乳腺癌患者中开展，其中两个组是不同剂量的HLX97联合氟维司群的联合治疗组，一个组为氟维司群单药治疗组。本研究Part1主要终点为评估剂量限制性毒性（DLT）的发生比例、确定HLX97单药及其联合氟维司群治疗的最大耐受剂量（MTD），Part2主要终点为研究者根据RECISTv1.1评估的客观缓解率（ORR）和无进展生存期（PFS），以及HLX97联合氟维司群的2期临床推荐剂量（RP2D）。次要研究终点包括HLX97单药及联合用药的安全性、PK参数、其他疗效指标（如缓解持续时间(DOR)、疾病控制率(DCR)、总生存期(OS)等）以及探索性药效学和预测性生物标志物分析等。

关于复宏汉霖

复宏汉霖（2696.HK）是一家国际化创新生物制药企业，致力于为全球患者提供高品质、可负担的生物药，产品覆盖肿瘤、自身免疫疾病、眼科疾病等领域。自2010年成立以来，公司已构建涵盖全球研发、临床、注册、生产及商业化的全产业链平台，拥有全球员工近4,000人，并在中国、美国和日本等多地设有运营及分支机构。依托生物类似药形成的稳健现金流反哺创新研发，复宏汉霖正稳步迈入“全球化2.0”阶段，持续打造可复制、可持续的全球增长模式。截至2026年初，公司共有10款产品在全球60余个国家和地区获批上市，其中7款已在中国获批。在欧美主流生物药市场，复宏汉霖亦取得多项里程碑式突破，已有4款产品获得美国FDA批准、5款产品获得欧盟EC批准，充分体现了公司在研发体系、质量管理及生产能力方面已全面对标国际最高标准。

在创新驱动方面，复宏汉霖依托上海、美国等多地协同布局的研发体系，构建了多元化、平台化的创新技术矩阵，覆盖免疫检查点抑制剂、免疫细胞衔接器（包括多特异性TCE）、抗体偶联药物（ADC）以及AI驱动的早期研发平台等前沿方向。目前，公司拥有50余项处于早期阶段的创新资产，其中约70%具备同类最佳（Best-in-Class）潜力，并在全球同步推进30余项临床研究。核心产品H药汉斯状^®（斯鲁利单抗，欧洲商品名：Hetronifly^®）作为全球首个获批一线治疗小细胞肺癌的抗PD-1单抗，正加速全球布局，已在全球40余个市场获批上市；同时，多款潜力创新资产，包括PD-L1 ADC HLX43及新表位HER2单抗HLX22正全面推进全球关键性临床研究。依托通过中、欧、美三地GMP认证的生产体系，复宏汉霖已建成总产能达84,000升的生物药生产平台，形成覆盖全球六大洲的稳定供应网络。未来，复宏汉霖将始终坚持以患者为中心，聚焦未满足的临床需求，持续推动创新成果向临床价值与患者可及转化，在全球生物医药创新生态中创造长期而稳健的价值。

Henlius’ potential BIC oral KAT6A/B inhibitor HLX97 completes first patient dosing in Phase 1, aiming to overcome endocrine therapy resistance in breast cancer

Shanghai, China, May 13, 2026 — Shanghai Henlius Biotech, Inc. (2696.HK) announced that the first patient has been dosed in a Phase 1 clinical trial of HLX97, a novel oral lysine acetyltransferase 6A/B (KAT6A/B) small molecule inhibitor, in patients with advanced or metastatic solid tumors in China. Previously, the Investigational New Drug (IND) application for HLX97 in advanced/metastatic solid tumors was approved by the China National Medical Products Administration (NMPA).

Breast cancer is the second most common cancer worldwide and the most common malignant tumor among women, and it is also a leading cause of cancer-related death in women. ER-positive (ER+) breast cancer is the most prevalent subtype, accounting for approximately 70% of all cases.¹ While endocrine therapies—such as estrogen suppression and direct targeting of the estrogen receptor—have become the cornerstone of treatment and significantly reduced recurrence and mortality, both primary and acquired resistance remain major clinical challenges.

KAT6A (Lysine Acetyltransferase 6A) and its paralog KAT6B (Lysine Acetyltransferase 6B) are members of the MYST family of histone acetyltransferases (HATs) and play key roles in tumorigenesis, disease progression, and the development of drug resistance across multiple cancer types. Preclinical and clinical studies have shown that amplification and/or overexpression of the KAT6A gene is closely associated with endocrine resistance in heavily pretreated patients with ER+/HER2- metastatic breast cancer. In addition, aberrant expression of KAT6A/B has been observed in a range of solid tumors, including ovarian, cervical, colorectal, prostate, lung cancers, and gliomas, suggesting broad therapeutic potential for KAT6A/B inhibitors across tumor types.^2-4 Given that amplification and/or overexpression of the KAT6A gene in breast cancer has been shown to be closely associated with the development of endocrine resistance, targeting KAT6A/B activity may represent a promising strategy to overcome endocrine therapy resistance in breast cancer.^5-6

HLX97 is a novel oral KAT6A/B inhibitor with best-in-class potential. By selectively inhibiting KAT6A/B activity, HLX97 is designed to regulate tumor cell proliferation and induce apoptosis. It demonstrates high selectivity and favorable pharmacokinetic properties characterized by rapid onset and clearance, aiming to maximize antitumor activity while minimizing hematological toxicity. Preclinical studies have shown that HLX97 effectively inhibits KAT6A/B activity and exhibits strong antitumor efficacy with a favorable safety profile. In animal models, HLX97 demonstrated significant efficacy in ER-positive breast cancer as well as in human-derived xenograft models resistant to both fulvestrant and palbociclib (a CDK4/6 inhibitor), with good overall tolerability.

Henlius has built a comprehensive pipeline covering the full continuum of breast cancer care through internal innovation and strategic collaborations. Its marketed products include HANQUYOU (trade name: HERCESSI^™ in the U.S., Zercepac^® in Europe), a trastuzumab biosimilar approved in over 50 countries and regions including China, the U.S., and Europe; POHERDY^®, the first pertuzumab biosimilar approved in the U.S.; HANNAIJIA (neratinib), an extended adjuvant therapy for early-stage breast cancer, and CDK4/6 inhibitor FUTUONING (fovinaciclib). Meanwhile, Henlius is advancing next-generation molecules such as novel epitope anti-HER2 antibody HLX22, oral selective estrogen receptor modulator (SERM) lasofoxifene (HLX78), KAT6A/B inhibitor HLX97, LIV-1-targeting ADC HLX41, HER2×HER2 bispecific epitope ADC HLX49 and HER2 ADC HLX87 through its robust innovation platforms and collaborative R&D. Building on this foundation, Henlius remains committed to advancing monotherapies and combination regimens across all breast cancer subtypes, enhancing therapeutic value through strengthened pipeline synergies.

Moving forward, Henlius will continue to focus on unmet clinical needs by fully leveraging its integrated platform advantages in antibody-based drugs, expanding disease areas, accelerating the development of differentiated molecules, and bringing more high-quality, affordable innovative therapies to patients worldwide.

About HLX97-FIH101

This study is a multicenter, open-label phase 1 clinical trial designed to evaluate the safety, tolerability, pharmacokinetic (“PK”) characteristics, and preliminary antitumor activity of HLX97 in patients with advanced or metastatic solid tumors. The study consists of two parts: Part 1 is the dose‑escalation phase, which includes monotherapy dose escalation (Part 1A) and combination therapy dose escalation (Part 1B); Part 2 is the dose‑expansion phase. Part 1A, the monotherapy dose‑escalation phase, will be conducted in patients with advanced/metastatic solid tumors and will include five dose levels ranging from 1.0 mg to 15.0 mg. HLX97 will be administered orally from Day1 to Day28 of each cycle, once a day, for 4 weeks each cycle. Part 1B, the combination therapy dose‑escalation phase, will explore 2 to 3 dose levels of HLX97 in combination with fulvestrant in patients with HR‑positive, HER2‑negative locally advanced or metastatic breast cancer. Part 2 will be conducted in patients with HR‑positive, HER2‑negative locally advanced or metastatic breast cancer and will include 3 treatment groups: two groups receiving different doses of HLX97 in combination with fulvestrant, and one group receiving fulvestrant monotherapy. The primary endpoints of Part 1 are to evaluate the incidence of dose‑limiting toxicities (DLT) and to determine the maximum tolerated dose (MTD) of HLX97 as monotherapy and in combination with fulvestrant. The primary endpoints of Part 2 are the objective response rate (ORR) and progression‑free survival (PFS) as assessed by the investigator according to RECIST version 1.1, as well as the recommended Phase 2 dose (RP2D) of HLX97 in combination with fulvestrant. Secondary endpoints include the safety of HLX97 as monotherapy and in combination, PK parameters, additional efficacy endpoints (such as duration of response (DOR), disease control rate (DCR), and overall survival (OS)), and exploratory pharmacodynamic and predictive biomarker analyses.

About Henlius

Shanghai Henlius Biotech, Inc. (2696.HK) is a global, innovation-driven biopharmaceutical company committed to delivering high-quality, affordable biologic therapies to patients worldwide. The Company focuses on major disease areas including oncology, autoimmune diseases, and ophthalmic diseases. Founded in 2010, Henlius has established an integrated, end-to-end biopharmaceutical platform encompassing global R&D, clinical operations, regulatory affairs, manufacturing, and commercialisation. The Company employs nearly 4,000 people globally and operates across multiple regions, including China, the United States, and Japan. Leveraging the stable cash flow generated from its biosimilar portfolio to support innovation, Henlius is steadily advancing into its “Globalisation 2.0” phase, building a scalable and sustainable global growth model. As of early 2026, Henlius has achieved regulatory approvals for 10 products across over 60 countries and regions worldwide, including seven approvals in China. The Company has also reached multiple milestones in major biopharmaceutical markets, with five products approved by the U.S. Food and Drug Administration (FDA) and five products approved by the European Commission (EC), reflecting its globally aligned R&D capabilities, quality systems, and manufacturing standards.

Driven by innovation, Henlius has built a diversified, platform-based technology ecosystem through coordinated R&D efforts across Shanghai, the United States, and other regions. Its innovation platforms span immune checkpoint inhibitors, immune cell engager technologies (including multispecific T cell engagers), antibody-drug conjugates (ADCs), and AI-enabled early discovery platforms. The Company currently has more than 50 early-stage innovative assets, approximately 70% of which are expected to be best-in-class, with over 30 clinical trials ongoing globally. Henlius’ core product, serplulimab (trade name: Hetronifly^® in Europe), is the world’s first anti–PD-1 mAb approved for first-line treatment of small cell lung cancer and has been approved in more than 40 markets worldwide with an accelerated globalisation process. In parallel, multiple high-potential innovative assets—including the PD-L1 ADC HLX43 and the novel epitope anti-HER2 mAb HLX22—are advancing through global pivotal clinical development. Supported by a biologics manufacturing network with a total capacity of 84,000L and GMP certifications from regulatory authorities in China, Europe, and the United States, Henlius has established a stable global supply system serving six continents. Guided by a patient-centred mission, Henlius remains focused on addressing unmet medical needs and translating scientific innovation into meaningful clinical value and patient access, contributing sustainably to the global biopharmaceutical ecosystem.

To learn more about Henlius, visit https://www.henlius.com/en/index.html and connect with us on LinkedIn at https://www.linkedin.com/company/henlius/.

参考文献

References

1. Nolan E, et al. Deciphering breast cancer: from biology to the clinic. Cell. 2023;186(8):1708-1728.

2. Chen J, et al. Mutations of Chromatin Structure Regulating Genes in Human Malignancies. Curr Protein Pept. Sci. 2016;17(5):411-437.

3. Partynska A, et al. The Expression of Histone Acetyltransferase KAT6A in Non-small Cell Lung Cancer. Anticancer Res. 2022;42(12):5731-5741.

4. Lv D, et al. Histone Acetyltransferase KAT6A Upregulates PI3K/AKT Signaling through TRIM24 Binding. Cancer Res. 2017;77(22):6190-6201.

5. Sharma S, et al. Discovery of a highly potent, selective, orally bioavailable inhibitor of KAT6A/B histone acetyltransferases with efficacy against KAT6A-high ER+ breast cancer. Cell Chem Biol. 2023;30(10):1191-1210.e20.

6. Yu L, et al. Identification of MYST3 as a novel epigenetic activator of ERα frequently amplified in breast cancer. Oncogene. 2017;36(20):2910-2918.

联系方式

媒体：PR@Henlius.com

投资者：IR@Henlius.com