艾克苏拜单抗(Alcestobart) - 药物靶点：LAG3_在研适应症：晚期癌症，转移性食管鳞状细胞癌，实体瘤_专利_临床

概要

基本信息

药物类型

单克隆抗体

别名

BGB-LBL-007、LBL 007、LBL-007

+ [1]

靶点

LAG3

作用方式

抑制剂

作用机制

LAG3抑制剂(淋巴细胞活化基因3蛋白抑制剂)

治疗领域

肿瘤消化系统疾病口颌疾病+ [4]

在研适应症

晚期癌症转移性食管鳞状细胞癌实体瘤+ [11]

非在研适应症

晚期淋巴瘤晚期恶性实体瘤微卫星稳定型结直肠癌

原研机构

南京维立志博生物科技股份有限公司

在研机构

BeOne Medicines Ltd.

南京维立志博生物科技股份有限公司广州百济神州生物制药有限公司

+ [2]

非在研机构-

权益机构

南京维立志博生物科技股份有限公司

BeOne Medicines Ltd.

鼎康（武汉）生物医药有限公司

最高研发阶段临床3期

首次获批日期-

最高研发阶段(中国)临床3期

特殊审评-

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结构/序列

Sequence Code 319494283H

来源: *****

Sequence Code 319494284L

来源: *****

关联

13

项与艾克苏拜单抗相关的临床试验

NCT07099430

/ Recruiting临床1/2期

An Open-label, Multicenter Phase Ib/II Clinical Study to Evaluate the Efficacy and Safety of LBL-024 Monotherapy, LBL-024 in Combination With LBL-007 or Toripalimab in Patients With Advanced Melanoma

This study is an open-label, multicenter phase Ib/II study to evaluate the efficacy and safety of LBL-024 monotherapy, LBL-024 in combination with LBL-007 or toripalimab in patients with advanced melanoma,To evaluate the preliminary efficacy and safety of LBL-024 monotherapy and combination therapy in patients with advanced melanoma.

开始日期2025-09-05

申办/合作机构

南京维立志博生物科技股份有限公司

NCT06010303

/ Active, not recruiting临床2期

A Phase 2, Randomized, Active-Controlled, Open-Label Study to Evaluate the Efficacy and Safety of LBL-007 in Combination With Tislelizumab Plus Chemotherapy as First-Line Treatment in Patients With Unresectable Locally Advanced or Metastatic Esophageal Squamous Cell Carcinoma

This is a randomized, open-label study to compare how well LBL-007 works in combination with tislelizumab and chemotherapy versus tislelizumab and chemotherapy when given as the first-line treatment in participants with inoperable locally advanced or metastatic esophageal squamous cell carcinoma (ESCC).

开始日期2023-11-08

申办/合作机构

BeOne Medicines Ltd.

NCT05909904

/ Active, not recruiting临床2期

A Randomized, Phase 2, Open-Label, Multi-Arm Study of Tislelizumab in Combination With Investigational Agents as First-Line Treatment in Patients With Recurrent or Metastatic Head and Neck Squamous Cell Carcinoma

This study is designed to evaluate the efficacy and safety of tislelizumab and tislelizumab in combination with investigational agent(s) in first-line recurrent or metastatic (R/M) head and neck squamous cell carcinoma (HNSCC).

开始日期2023-07-21

申办/合作机构

BeOne Medicines Ltd.

100 项与艾克苏拜单抗相关的临床结果

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100 项与艾克苏拜单抗相关的转化医学

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100 项与艾克苏拜单抗相关的专利（医药）

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3

项与艾克苏拜单抗相关的文献（医药）

2026-02-17·CLINICAL CANCER RESEARCH

Anti–LAG-3 Antibody LBL-007 plus Tislelizumab and Chemotherapy as First-Line Therapy for Advanced Nasopharyngeal Carcinoma: A Multicenter Phase 2 Trial

Article

作者: Wang, Rensheng ; Qu, Song ; Chen, Xiaozhong ; Zhu, Haisheng ; Li, Jingao ; Chen, Gang ; Xiong, Hailin ; Gao, Jin ; Fan, Bin ; Chen, Wu ; Liu, Lei ; Han, Yaqian ; Tang, Wenjun ; Kang, Xiaoqiang ; Zhang, Li ; Huang, Xiaoming ; Yang, Kunyu ; Cai, Shengli ; Hu, Desheng ; Chen, Lisha ; Yang, Yunpeng ; Chen, Yu ; Sun, Dongchen

Abstract:

Purpose::

Prior studies reported synergistic antitumor activity by dual inhibition of lymphocyte activation gene-3 (LAG-3) and PD-1. This study investigated the activity, safety, and biomarker of LAG-3/PD-1 co-blockade plus chemotherapy as first-line treatment for recurrent or metastatic nasopharyngeal carcinoma (RM-NPC).

Patients and Methods::

Previously untreated patients with RM-NPC received LBL-007 (anti–LAG-3), tislelizumab (anti–PD-1), and gemcitabine-cisplatin for four to six cycles, followed by maintenance therapy with LBL-007 and tislelizumab. The primary endpoint was objective response rate (ORR). Secondary endpoints were progression-free survival (PFS), duration of response (DoR), time to response, disease control rate (DCR), overall survival (OS), and safety. Biomarker analysis included LAG-3 and PD-L1 expression.

Results::

Forty-two patients were enrolled from 15 centers in China. With a median follow-up of 19.0 months, the ORR was 83.3% [95% confidence interval (CI), 68.6%–93.0%], and the DCR was 97.6% (95% CI, 87.4%–99.9%). The median PFS reached 15.8 months (95% CI, 9.9–not estimable); the 12-month PFS rate was 55.1% (95% CI, 41.7%–72.9%). The median DoR was 14.6 months (95% CI, 10.3–not estimable); the median OS was not reached. Grade 3 or higher treatment-related adverse events occurred in 37 patients (98.1%). No new safety signals were identified. In biomarker analysis, patients with dual-positive LAG-3/PD-L1 expression demonstrated more favorable outcomes than those lacking either biomarker, including a 12-month PFS rate of 65.0% versus 40.2% and median PFS of 16.0 versus 10.3 months.

Conclusions::

LBL-007 plus tislelizumab and chemotherapy shows promising clinical benefits and manageable toxicity as first-line therapy for RM-NPC. Dual-positive LAG-3/PD-L1 expression was associated with improved outcomes, supporting further exploration of this biomarker-defined subpopulation in randomized trials.

2025-05-01·Xi bao yu fen zi mian yi xue za zhi = Chinese journal of cellular and molecular immunology

[A novel fully human LAG-3 monoclonal antibody LBL-007 combined with PD-1 antibody inhibits proliferation, migration and invasion of tumor cells via blocking NF-κB pathway].

Article

作者: Zhou, Lijun ; Wu, Chenglin ; Zhou, Huinan ; Qin, Kewei ; Liu, Jianfei

Objective To investigate the effects of LBL-007, a novel fully human lymphocyte activation gene 3 (LAG-3) monoclonal antibody, in combination with programmed cell death protein 1 (PD-1) antibody, on the invasion, migration and proliferation of tumor cells, and to elucidate the underlying mechanisms. Methods Human lymphocyte cells Jurkat were co-cultured with A549 and MGC803 tumor cell lines and treated with the isotype control antibody human IgG, LBL-007, anti-PD-1 antibody BE0188, or tumor necrosis factor-alpha (TNF-α, the NF-κB signaling pathway agonist). Tumor cell proliferation was assessed using a colony formation assay; invasion was measured by Transwell^TM assay; migration was evaluated using a wound healing assay. Western blotting was employed to determine the expression levels of NF-κB pathway-related proteins: IκB inhibitor kinase alpha (Ikkα), phosphorylated Ikkα (p-IKKα), NF-κB subunit p65, phosphorylated p65 (p-p65), NF-κB Inhibitor Alpha (IκBα), phosphorylated IκBα (p-IκBα), matrix metalloproteinase 9 (MMP9), and MMP2. Results Compared with the control and IgG isotype groups, LBL-007 and BE0188 significantly reduced tumor cell proliferation, invasion, and migration. They also decreased the phosphorylation of p-IKKα, p-p65 and p-IκBα, and the expression of MMP9 and MMP2 of tumor cells in the co-culture system. The combined treatment of LBL-007 and BE0188 enhanced inhibitory effects. Treatment with the NF-κB signaling pathway agonist TNF-α reversed the suppressive effects of LBL-007 and BE0188 on tumor cell proliferation, invasion, migration, and NF-κB signaling. Conclusion LBL-007 and anti-PD-1 antibody synergistically inhibit the invasion, migration, and proliferation of A549 and MGC803 tumor cells by blocking the NF-κB signaling pathway.

Journal of Hematology & Oncology

Anti-LAG-3 antibody LBL-007 plus anti-PD-1 antibody toripalimab in advanced nasopharyngeal carcinoma and other solid tumors: an open-label, multicenter, phase Ib/II trial

Article

作者: Zhao, Yuan-Yuan ; Huang, Yan ; Kang, Xiao-Qiang ; Li, Gui-Ling ; Hu, De-Sheng ; Chen, Gang ; Wang, Hui-Li ; Cai, Sheng-Li ; Ba, Yi ; Fang, Wen-Feng ; Zhou, Ting ; Zhang, Ya-Xiong ; Lin, Jin-Guan ; Wang, Wei ; Sun, Dong-Chen ; Yang, Yun-Peng ; Zhu, Hai-Sheng ; Zhang, Li ; Deng, Chao ; Fu, Zhi-Chao ; Wang, Zhen ; Zhao, Hong-Yun ; Luo, Su-Xia

PURPOSE:

Open-label phase Ib/II study to investigate the safety and efficacy of LBL-007, an anti-LAG-3 antibody, plus toripalimab, an anti-PD-1 antibody, in patients with previously treated advanced nasopharyngeal carcinoma (NPC) and other solid tumors.

METHODS:

Patients with advanced tumors refractory to prior standard therapies were enrolled. In phase Ib, patients received LBL-007 200 mg or 400 mg and toripalimab 240 mg intravenously once every 3 weeks. In phase II, all patients received LBL-007 at the recommended phase II dose (RP2D) and toripalimab 240 mg intravenously once every 3 weeks. The primary end points were safety in phase Ib and objective response rate (ORR) in phase II. The exploratory end point was the predictive capability of LAG-3 and PD-L1 expression for efficacy.

RESULTS:

Between November 30, 2021, and December 1, 2023, 80 patients were enrolled, including 30 (37.5%) with NPC and 50 (62.5%) with other tumors. Median follow-up was 26.0 months. In Phase Ib, LBL-007 was administered at 200 mg to four patients and 400 mg to six patients, with no dose-limiting toxicities observed. Therefore, the 400 mg dose of LBL-007 was established as the RP2D and administered to 70 patients in phase II. Nine (11.3%) of 80 patients had grade 3 or 4 treatment-related adverse events, the most common of which included anemia (2.5%), hyponatremia (2.5%), increased alanine aminotransferase (2.5%), increased aspartate aminotransferase (1.3%), and fatigue (1.3%). Eight patients (10.0%) had treatment-related serious adverse events. No treatment-related deaths were reported. In immunotherapy-naive NPC patients (n = 12), ORR was 33.3%, disease control rate (DCR) was 75%, and median progression-free survival (PFS) was 10.8 months (95% CI, 1.3 to not estimated). In IO-treated NPC patients (n = 17), ORR was 11.8%, DCR was 64.7%, and median PFS was 2.7 months (95% CI, 1.4 to 4.9). For other tumors, ORRs were 15.8% in immunotherapy-naive patients and 3.7% in immunotherapy-treated patients. Patients with ≥ 2 + LAG-3 expression had a higher ORR of 28.0%, compared to 7.7% in those with < 2 + LAG-3 expression.

CONCLUSION:

LBL-007 plus toripalimab exhibited a manageable safety profile in patients with advanced solid tumors and demonstrated promising antitumor activity in NPC, especially in immunotherapy-naive patients. These findings warrant further validation in future studies.

90

项与艾克苏拜单抗相关的新闻（医药）

2026-05-15

·BioDialectics

维立志博: 下一代肿瘤免疫疗法的领跑者

维立志博专注于下一代肿瘤免疫治疗创新，依托**X-Body®、LeadsBody®、TOPiKinectics®**三大自主技术平台，聚焦IO2.0、TCE、下一代ADC三大核心赛道，核心产品差异化优势显著：LBL-024（PD-L1/4-1BB双抗）作为全球首个进入注册阶段的4-1BB靶向药物，在肺外神经内分泌癌、小细胞肺癌、非小细胞肺癌等实体瘤中展现出高效、安全的泛癌种疗效，计划2026年第三季度提交上市申请；LBL-034（GPRC5D/CD3双抗）凭借条件性激活设计，在复发难治性多发性骨髓瘤中疗效优于同类产品，获FDA孤儿药与快速通道资格，临床进度位居全球前列。公司同步推进LBL-047、LBL-007等管线布局，覆盖肿瘤与自身免疫疾病领域，通过海外授权合作实现研发价值变现，财务状况稳健、现金储备可支撑长期研发投入；未来将持续加速临床开发与适应症拓展，计划2026-2030年实现多款产品商业化，致力于通过精准免疫疗法将肿瘤转化为慢性病，打造全球领先的创新生物药企业。

2026-05-14

·BioSpace

BeOne wins mantle cell lymphoma approval, opening new therapy class

iStock, AdrianHillman Beqalzi is the first BCL2 inhibitor approved for relapsed or refractory mantle cell lymphoma. The FDA has cleared BeOne Medicines’ BCL2 blocker sonrotoclax for the treatment of certain patients with mantle cell lymphoma, an approval that opens a new approach to treating this malignancy. The drug will carry the brand name Beqalzi. Beqalzi is specifically indicated for patients with relapsed or refractory mantle cell lymphoma (R/R MCL) who have undergone at least two prior lines of systemic therapy, including a BTK inhibitor, according to a Thursday news release . Beqalzi was approved under the FDA’s accelerated pathway and will need a confirmatory study to verify its clinical benefits to sustain the approval. Beqalzi is the first BCL2 inhibitor indicated for this indication, BeOne said. The drug is also the company’s third commercial product, coming after the BTK inhibitor Brukinsa, which was cleared in November 2019 for MCL , and the PD-1 inhibitor Tevimbra, which the FDA first approved in March 2024 for esophageal cancer. Despite these distinctions, however, analysts at Truist Securities called Beqalzi’s approval “incremental,” pointing to the “relatively small” market for R/R MCL. The firm forecasts around $300 to $400 million in sales for Beqalzi in this indication. Phase 1/2 data supported the FDA’s decision on Thursday. The trial, a single-arm open-label study , enrolled 125 patients with R/R MCL. Results demonstrated a 52% overall response rate, including a 16% complete response rate, BeOne said. Median duration of response was 15.8 months. BeOne is currently running the Phase 3 CELESTIAL-RRMCL study , which will serve as Beqalzi’s confirmatory trial. The study has a primary completion date of August 2028. Beqalzi is a next-generation BCL2 inhibitor that works by triggering cancer cell death. BeOne is studying Beqalzi as part of a fixed-duration regimen with Beqvez for chronic lymphocytic leukemia. Truist has higher hopes for this market than MCL, with peak sales of over $3.4 billion projected, according to the firm’s Thursday note. While incremental on a market-level, Beqalzi’s approval is nevertheless good news for BeOne, which at the 2026 American Association for Cancer Research annual meeting in April presented underwhelming data . A Phase 2 readout at the conference showed that several combination regimens based on Tevimbra—including with the TIM-3 blocker surzebiclimab and the anti-LAG-3 therapy alcestobart—elicited no significant efficacy improvement over monotherapy in recurrent and/or metastatic head and neck squamous cell carcinoma. Cancer AACR 2026: Moderna, Revolution, Zymeworks and BeOne showcase new data Moderna, Revolution Medicines and Zymeworks record wins in melanoma, lung and breast cancers, while BeOne swings and misses at head and neck cancer. April 21, 2026 · 4 min read · Tristan Manalac Read more

临床结果上市批准临床3期临床2期AACR会议

2026-05-11

·精准药物

百济神州终止多款创新药开发，包括降解剂

近日，百济神州（BeOne Medicines）更新2026年Q1最新产品线，放弃了五个肿瘤一期项目，并停止了一项IRAK4降解剂BGB-45035在二期关节炎临床试验（这一决定是基于“新出现的数据”做出的），正在分析数据以决定BGB-45035的下一步行动。除了关节炎，BGB-45035目前也被列入针对皮肤病的1期临床开发。百济神州5项肿瘤资产中的4项已完全终止。这些是EGFR CDAC抑制剂BG-60366（肺癌），策略上可能更看重生物药；泛KRAS抑制剂BGB-53038（胃肠道肿瘤和肺癌）、MAT2A抑制剂BG-89894（肺癌和实体瘤）；CDK2抑制剂BG-68501（乳腺癌和实体瘤）。 CDK2抑制剂来自2023年与Ensem Therapeutics（昂胜医药）达成的13.3亿美元的协议，而MAT2A抑制剂来自2024年底与石药集团达成的协议。此外，百济还在开发CDK2降解剂BG-75098处于1期临床，与CDK4抑制剂BGB-43395、Fulvestrant进行联合治疗。 2023年11月，百济神州引进昂胜医药一款在研、即将提交新药临床试验（IND）申请的口服细胞周期蛋白依赖性激酶 2（CDK2）抑制剂的全球独家许可权利。昂胜获得一笔首付款，并基于取得的特定研发、注册和商业化里程碑，有权获得至多13.3亿美元的总交易额款项，以及分级销售特许使用费。 2024年12月，百济神州引进石药集团MAT2A抑制剂（SYH2039）在全球的开发、制造及商业化权益，石药集团收取总计1.5亿美元的预付款，并有权收取最高1.35亿美元的潜在开发里程碑付款及最高15.5亿美元的潜在销售里程碑付款，以及根据该产品的年度销售净额计算的分层销售提成。百济神州表示一项关于实体瘤中CCR8抗体BGB-A3055的研究也已终止，但该资产尚未完全停止。在根据开发标准进行全面审查后，百济神州决定终止几项早期研究资产。终止特定资产并不意味着正在放弃这些靶点领域的创新。将继续通过多药物形式方法追求这些靶点，其中几个靶点的有前景的管线资产已经在研究中。稍早之前，百济神州还终止了IL-15 prodrug BGB-R046、HPK1抑制剂BGB-15025（但是另一款HPK1抑制剂BGB-26808处于1期临床治疗胃肠道肿瘤）、B7-H3 ADC BGB-C354（B7-H3 x ITGB6 bsADC预计2026年进入1期临床阶段）、OX40单抗BGB-A445、LAG-3单抗BGB-LBL-007（估值31.3亿元！维立志博提交港股IPO，百济神州已退回LAG-3抗体）、TIGIT单抗Ociperlimab等项目开发。 2021年维立志博与百济神州订立LAG-3抗体LBL-007的授权及合作协议，维立志博有资格获得高达7.72亿美元的首付款（3000万美元）及里程碑付款，另加双位数百分比的分级特许权使用费。根据百济神州提供的终止通知所指，百济神州已于2025年5月18日终止。百济神州并无披露亦无计划披露终止百济神州协议的原因。该终止后，维立志博已重新获得开发、生产及商业化LBL-007的全部全球权利。声明：发表/转载本文仅仅是出于传播信息的需要，并不意味着代表本公众号观点或证实其内容的真实性。据此内容作出的任何判断，后果自负。若有侵权，告知必删！长按关注本公众号粉丝群/投稿/授权/广告等请联系公众号助手觉得本文好看，请点这里↓

100 项与艾克苏拜单抗相关的药物交易

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研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
晚期癌症	临床3期	美国	BeOne Medicines Ltd.	2019-12-19
晚期癌症	临床3期	中国	BeOne Medicines Ltd.	2019-12-19
晚期癌症	临床3期	日本	BeOne Medicines Ltd.	2019-12-19
晚期癌症	临床3期	澳大利亚	BeOne Medicines Ltd.	2019-12-19
晚期癌症	临床3期	法国	BeOne Medicines Ltd.	2019-12-19
晚期癌症	临床3期	意大利	BeOne Medicines Ltd.	2019-12-19
晚期癌症	临床3期	马来西亚	BeOne Medicines Ltd.	2019-12-19
晚期癌症	临床3期	新西兰	BeOne Medicines Ltd.	2019-12-19
晚期癌症	临床3期	波兰	BeOne Medicines Ltd.	2019-12-19
晚期癌症	临床3期	韩国	BeOne Medicines Ltd.	2019-12-19

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临床结果

适应症

分期

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT05577702 (BGBLC202, WCLC2025)	临床2期	非小细胞肺癌新辅助	121	Tislelizumab (PD-L1 TC ≥50%, TIS (anti-PD-1))	窪鹽鬱窪網鬱鏇衊遞窪(夢醖窪衊範廠鏇餘鏇網) = 廠膚艱襯鏇顧齋憲廠範製鏇積憲廠簾鹽網鬱壓 (願簾構製鑰鏇壓蓋齋憲 ) 更多	积极	2025-09-08
				Tislelizumab+OciperlimabTislelizumab+Ociperlimabociperlimab (anti-TIGIT) (PD-L1 TC ≥50%, TIS plus ociperlimab (anti-TIGIT))	窪鹽鬱窪網鬱鏇衊遞窪(夢醖窪衊範廠鏇餘鏇網) = 壓廠製願選選鏇積艱鬱製鏇積憲廠簾鹽網鬱壓 (願簾構製鑰鏇壓蓋齋憲 ) 更多
NCT05516914 (LBL-007, ASCO2025)	临床2期	复发性鼻咽癌一线 \| 维持	42	LBL-007 600 mg	觸壓壓築顧壓鹹願淵鏇(製範積遞餘壓構夢餘繭) = 16 patients (38.1%) experienced LBL-007 treatment related SAEs 選願鹹壓壓淵獵廠範簾 (網簾願製蓋憲壓網憲鑰 ) 更多	积极	2025-05-30
NCT05516914 (ASCO2024) 人工标引	临床1/2期	晚期恶性实体瘤 \| 晚期鼻咽癌一线	63	LBL-007 tislelizumab	艱襯夢鬱積醖衊構窪淵(淵鑰顧獵顧壓願構繭醖) = None 餘積簾鏇糧鑰壓鹽齋鹹 (積鑰壓齋鑰壓鬱廠齋簾 ) 更多	积极	2024-05-24
				LBL-007 tislelizumabcisplatin
NCT05102006 (AACR2024) 人工标引	临床1/2期	肿瘤	80	LBL-007 20ToripalimabToripalimab 240 mg	齋憲鹽鹹壓蓋蓋築蓋簾(餘廠選鑰遞鹽鑰窪構膚) = 積簾衊衊鬱衊顧築淵鹹蓋獵壓觸獵顧鬱餘醖繭 (憲壓簾鹹繭醖鹹齋範壓 ) 更多	积极	2024-04-05
NCT04640545 (ASCO 12023 \| ASCO 22023) 人工标引	临床1期	局部晚期黑色素瘤	110	Toripalimab+LBL-007	願鬱鏇襯積窪壓壓範鹽(簾構壓鹽鏇餘製糧鏇壓) = 網鬱艱淵鏇餘繭醖鹽製製製膚膚鑰鏇膚淵構顧 (範築鏇鹹遞鬱鑰憲襯鑰 ) 更多	积极	2023-05-26
				Toripalimab+Axitinib+LBL-007	願鬱鏇襯積窪壓壓範鹽(簾構壓鹽鏇餘製糧鏇壓) = 顧鏇憲壓獵廠鑰齋製簾製製膚膚鑰鏇膚淵構顧 (範築鏇鹹遞鬱鑰憲襯鑰 ) 更多
NCT04640545 (ASCO2022)	临床1期	不可切除的黑色素瘤	37	LBL-007	蓋選窪觸齋積願構艱夢(壓願壓選獵衊鑰醖衊蓋) = 糧廠壓築襯襯簾鏇鬱鑰廠艱齋製衊蓋鏇膚襯構 (襯鏇積積觸遞醖鹹積壓 )	-	2022-06-02
				Toripalimab	蓋選窪觸齋積願構艱夢(壓願壓選獵衊鑰醖衊蓋) = 鬱糧鬱蓋顧願鏇範範製廠艱齋製衊蓋鏇膚襯構 (襯鏇積積觸遞醖鹹積壓 )