和誉医药口服小分子PD-L1抑制剂ABSK043联合艾力斯戈来雷塞治疗非小细胞肺癌完成II期临床首例患者给药

本研究是一项开放性II期临床研究，旨在评估ABSK043联合枸橼酸戈来雷塞治疗携带KRAS G12C突变的局部晚期或转移性NSCLC患者的安全性、耐受性及有效性。该研究已于2025年8月获得中国国家药品监督管理局（NMPA）药品审评中心（CDE）的临床试验申请（IND）批准，首例患者成功给药标志着这一极具潜力的联合疗法临床开发迈出了重要一步。

KRAS是人类癌症中最常见的致癌驱动基因之一，其中KRAS G12C突变在NSCLC患者中的发生率约为14%^1-3。和誉医药口服小分子PD-L1抑制剂ABSK043在先前治疗晚期实体瘤患者的I期临床研究中展现出良好的安全性和抗肿瘤活性，尤其在PD-L1高表达组、EGFR突变组和KRAS突变组中表现出更高的有效率。

关于ABSK043

ABSK043为一款全新的具备优异活性及高度选择性的口服小分子PD-L1抑制剂。癌细胞可以利用PD-1及其配体PD-L1这些免疫检查点来逃避免疫监管和清除，抑制或限制T细胞应答。ABSK043可与PD-L1受体特异性结合并诱导其从细胞表面内吞，有效地抑制PD-1/PD-L1的相互作用，解除PD-L1介导的T细胞活化抑制作用。ABSK043在多个临床前模型中展现出与已获批PD-L1抗体相当的抗肿瘤功效。截至目前，全球已有多款PD-1/PD-L1抗体药物获批上市，但并无PD-1/PD-L1小分子药物获批。ABSK043目前正在澳大利亚和中国开展针对晚期实体肿瘤的I期临床试验。

关于戈来雷塞

枸橼酸戈来雷塞片是一款KRAS G12C抑制剂，目前已在中国、美国及欧洲多国启动多项针对晚期实体瘤患者的临床试验，包括与SHP2抑制剂AST-24082联用治疗非小细胞肺癌，以及单药治疗胰腺癌的注册性临床研究等。其中，胰腺癌适应症在美国获得孤儿药认定，并在中国获得突破性治疗药物认定。2025年5月，戈来雷塞获中国国家药品监督管理局批准上市。

关于艾力斯

上海艾力斯医药科技股份有限公司成立于2004年3月，是一家以全球医药市场需求为导向，专注于肿瘤治疗领域，集新药研发、生产和商业化为一体的创新型制药企业。艾力斯医药以科技关爱生命为发展理念，以开发首创药物和同类最佳药物为首要目标。历经20年坚持不懈的努力，艾力斯已经成功自主研发，获批两款创新药，具备持续创制具有自主产权的疗效确切、市场最优的抗肿瘤新药之综合实力。2020年12月2日，上海艾力斯医药科技股份有限公司正式在上海证券交易所科创板挂牌上市（股票代码：688578）。

参考文献

1. Liu P, Wang Y, Li X. Targeting the untargetable KRAS in cancer therapy. Acta Pharm Sin B. 2019 Sep;9(5):871-879.

2. Pakkala S, Ramalingam SS. Personalized therapy for lung cancer: striking a moving target. JCI Insight. 2018 Aug 9;3(15):e120858.

3. Nassar AH, Adib E, Kwiatkowski DJ. Distribution of KRAS G12C Somatic Mutations across Race, Sex, and Cancer Type. N Engl J Med. 2021 Jan 14;384(2):185-187. 

Abbisko Therapeutics Completes First Patient Dosing in a Phase II Study of ABSK043, an Oral Small-Molecule PD-L1 inhibitor, in Combination with Glecirasib for the Treatment of NSCLC

3 November 2025, Abbisko Therapeutics Co., Ltd. ("Abbisko Therapeutics" hereafter, HKEX code: 02256.HK) today announced that its oral small-molecule PD-L1 inhibitor, ABSK043, combined with KRAS G12C inhibitor, Glecirasib, from Shanghai Allist Pharmaceuticals Co., Ltd. ("Allist" hereafter, SSE code: 688578.SS) has completed first patient dosing in a phase II study for the treatment of patients with Non-Small Cell Lung Cancer (NSCLC) harboring KRAS G12C mutation.

This open-label phase II study is designed to evaluate the safety, tolerability, and efficacy of ABSK043 in combination with Glecirasib in patients with locally advanced or metastatic NSCLC harboring KRAS G12C mutation. The study obtained Investigational New Drug approval from the Center for Drug Evaluation (CDE) of the China National Medical Products Administration (NMPA) in August 2025. This successful first patient dosing marks a significant step forward in the development of this promising combination regimen.

Approximately 14% of non–small cell lung cancers harbor a KRAS G12C mutation^1-3. In a previous phase I clinical study in patients with advanced solid tumors, ABSK043 demonstrated favorable safety and promising anti-tumor activity as a single agent, with high response rates observed in the subset of patients with high PD-L1 expression, and EGFR or KRAS mutations.

About ABSK043

ABSK043 is a novel, orally bioavailable, highly selective small molecule PD-L1 inhibitor wholly owned by Abbisko Therapeutics. Tumor cells can exploit immune checkpoints such as PD-1 and its ligand PD-L1 to evade immune detection and clearance, thereby suppressing or limiting T-cell responses. ABSK043 selectively binds to the PD-L1 receptor and induces its internalization from the cell surface, effectively inhibiting the PD-1/PD-L1 interaction and alleviating PD-L1-mediated suppression of T-cell activation. In preclinical models, ABSK043 has demonstrated anti-tumor efficacy comparable to approved PD-L1 antibodies. While several PD-1/PD-L1 monoclonal antibodies have been approved worldwide, there are currently no approved orally bioavailable PD-1/PD-L1 small molecule drugs. ABSK043 is currently being explored in an ongoing Phase I clinical trial for advanced solid tumors in Australia and China.

About Glecirasib

Glecirasib is a KRAS G12C inhibitor approved for the treatment of NSCLC by the China NMPA.A number of clinical trials are currently ongoing in China, the United States and Europe for patients with advanced solid tumors harboring KRAS G12C mutation. These include combination therapy trials with SHP2 inhibitor, AST-24082, in NSCLC, and monotherapy trials in pancreatic cancer. Glecirasib received orphan drug designation in the United States and breakthrough therapy designation in China for the treatment of pancreatic cancer.

About Abbisko Therapeutics

Founded in April 2016, Abbisko Therapeutics Co., Ltd. (HKEX: 02256.HK), is an oncology-focused biopharmaceutical company based in Shanghai that is dedicated to the discovery and development of innovative medicines to treat unmet medical needs in China and globally. The Company was established by a group of seasoned drug hunters with rich research & development and managerial expertise from top multinational pharmaceutical companies. Since its founding, Abbisko Therapeutics has built an extensive pipeline of innovative programs focused on precision oncology and immuno-oncology.

Please visit www.abbisko.com for more information.

About Allist

Shanghai Allist Pharmaceuticals Co., Ltd, founded in March, 2004, is an innovative pharmaceutical company with a fully integrated system for research and development, manufacturing, and commercialization of novel oncology drugs with a purpose to meet with medical needs across the globe. On December 2nd, 2020, Shanghai Allist Pharmaceuticals Co., Ltd. was officially listed on the Science and Technology Innovation Board of the Shanghai Stock Exchange (stock number: 688578).

Referencce

1. Liu P, Wang Y, Li X. Targeting the untargetable KRAS in cancer therapy. Acta Pharm Sin B. 2019 Sep;9(5):871-879.

2. Pakkala S, Ramalingam SS. Personalized therapy for lung cancer: striking a moving target. JCI Insight. 2018 Aug 9;3(15):e120858.

3. Nassar AH, Adib E, Kwiatkowski DJ. Distribution of KRAS G12C Somatic Mutations across Race, Sex, and Cancer Type. N Engl J Med. 2021 Jan 14;384(2):185-187. 

关于和誉

和誉医药（香港联交所代码：02256）成立于2016年，是一家立足中国，着眼全球的创新药研发公司。公司的创始人和管理团队拥有多年顶尖跨国药企的研发和管理经验，并参与了多个临床及上市新药的研发。和誉医药专注于肿瘤新药研发，以小分子肿瘤精准治疗和小分子肿瘤免疫治疗药物为核心，着眼病患及医药市场的需求，秉承国际新药开发的理念和标准，致力于开发新颖及高潜力药物靶点的潜在first-in-class或best-in-class创新药物，用于改善中国及全球病人的生活质量。自成立以来，和誉医药已经建立了丰富的创新产品管线，涵盖肿瘤精准治疗领域以及肿瘤免疫治疗领域。

更多信息，欢迎访问 www.abbisko.com。