16 abstracts, including two oral presentations, feature new clinical data from Astellas’ oncology portfolio

包括两次口头报告在内的16篇摘要展示了安斯泰来肿瘤学组合中的新临床数据

TOKYO, May 19, 2025

东京，2025年5月19日

– Astellas Pharma Inc. (TSE: 4503, President and CEO: Naoki Okamura, “Astellas”) will present 16 abstracts featuring new data across its approved cancer therapies at the 2025 American Society of Clinical Oncology (ASCO) Annual Meeting (May 30 - June 3). The research underscores Astellas’ dedication as a pioneer in oncology and focus on clinical outcomes that matter to patients..

– 安斯泰来制药公司（东京证券交易所代码：4503，总裁兼首席执行官：冈村直树，“安斯泰来”）将在2025年美国临床肿瘤学会（ASCO）年会（5月30日至6月3日）上展示16份摘要，呈现其获批癌症疗法的全新数据。这些研究凸显了安斯泰来作为肿瘤学领域先驱的承诺，以及对患者重要的临床结果的关注。

The abstracts include new post hoc analyses of long-term overall survival (OS) data for XTANDI (enzalutamide) and two analyses for PADCEV (enfortumab vedotin), which demonstrate how these standard-of-care medicines can continue to treat patients in metastatic, non-metastatic, castration-resistant, or hormone-sensitive prostate cancer patients and unresectable, locally advanced or metastatic urothelial cancer patients, respectively..

摘要包括对XTANDI（恩杂鲁胺）的长期总生存期（OS）数据的新事后分析，以及对PADCEV（恩福妥单抗vedotin）的两项分析，这些分析分别展示了这些标准治疗药物如何继续治疗转移性、非转移性、去势抵抗性或激素敏感性前列腺癌患者，以及不可切除、局部晚期或转移性尿路上皮癌患者。

Moitreyee Chatterjee-Kishore, Ph.D., M.B.A., Head of Oncology Development, Astellas

Moitreyee Chatterjee-Kishore，博士，工商管理硕士，安斯泰来肿瘤开发部门负责人

“At Astellas, we are dedicated to transforming cancer care through innovative treatment approaches. The data we will present at ASCO this year, including new long-term follow-up data for advanced prostate and bladder cancers, reflect the pioneering role we continue to play in delivering outcomes that matter to patients.

“在安斯泰来，我们致力于通过创新的治疗方法来改变癌症护理。我们今年将在ASCO上展示的数据，包括针对晚期前列腺癌和膀胱癌的全新长期随访数据，体现了我们在为患者提供有意义的结果方面持续发挥的先锋作用。"

We continue to push the boundaries of cancer treatment with our growing pipeline, using novel modalities and precision medicine approaches, to benefit all eligible patients now and in the future.” .

我们通过不断扩展的管线，利用创新模式和精准医疗方法，继续推动癌症治疗的边界，以造福现在和未来的所有符合条件的患者。

Highlights from Astellas at the 2025 ASCO Annual Meeting will include a strong focus on Overall Survival (OS) data updates, confirming the value that these therapies bring to patients:

2025年ASCO年会上，安斯泰来（Astellas）的重点将包括对总生存期（OS）数据更新的强烈关注，确认这些疗法为患者带来的价值：

Enzalutamide:

恩杂鲁胺：

The ARCHES five-year follow-up OS analysis of enzalutamide plus androgen-deprivation therapy (ADT) in patients with metastatic hormone-sensitive prostate cancer (mHSPC) will be featured in an oral presentation

ARCHES 五年随访OS分析，关于恩杂鲁胺联合雄激素剥夺疗法 (ADT) 在转移性激素敏感性前列腺癌 (mHSPC) 患者中的应用，将在口头报告中展示。

In addition to the ARCHES five-year follow-up presentation, Astellas is supporting investigator-sponsored studies. Eight-year data assessing outcomes of enzalutamide vs non-steroidal anti-androgen (NSAA) in mHSPC will be presented from an independent, investigator-sponsored trial (ENZAMET) led by the Australian and New Zealand Urogenital and Prostate Cancer Trials Group (ANZUP)..

除ARCHES五年随访结果展示外，安斯泰来还支持研究者发起的研究。评估恩扎鲁胺与非甾体抗雄激素（NSAA）在mHSPC中疗效的八年数据将由澳大利亚和新西兰泌尿生殖及前列腺癌试验组（ANZUP）主导的一项独立研究者发起的试验（ENZAMET）呈现。

Enfortumab vedotin

恩福单抗 vedotin

Urothelial carcinoma

尿路上皮癌

Two analyses of the phase 3 EV-302 study of enfortumab vedotin in combination with pembrolizumab vs chemotherapy in previously untreated locally advanced or metastatic urothelial carcinoma (la/mUC)

两项关于 enfortumab vedotin 联合 pembrolizumab 对比化疗在既往未治疗的局部晚期或转移性尿路上皮癌（la/mUC）中的 3 期 EV-302 研究分析

Exploratory analysis of responders will be presented in an oral presentation

应答者的探索性分析将在口头报告中呈现。

Poster presentation featuring long-term subgroup analysis

海报展示，包含长期亚组分析

Bladder cancer

膀胱癌

A systematic review and meta-analysis of surrogate endpoints in muscle-invasive bladder cancer trials will be featured in a poster presentation.

一项关于肌层浸润性膀胱癌试验中替代终点的系统评价和荟萃分析将在海报展示中呈现。

Shontelle Dodson, Executive Vice President, Head of Medical Affairs, Astellas

Shontelle Dodson，执行副总裁，医学事务主管，安斯泰来

“Long-term overall survival is the gold standard endpoint in cancer research. New post hoc analysis data from the ARCHES enzalutamide trial demonstrates our mission to help patients live longer, healthier lives. We are committed to maximizing the impact of our therapies as we continue to pioneer the oncology medicines of tomorrow.”.

“长期总生存率是癌症研究的金标准终点。ARCHES恩杂鲁胺试验的新事后分析数据展示了我们帮助患者活得更长、更健康的使命。我们致力于最大化我们疗法的影响，因为我们继续开创明日的肿瘤药物。”

Astellas Presentations at 2025 ASCO Annual Meeting

安斯泰来在2025年ASCO年会上的演讲

Enzalutamide

恩杂鲁胺

Presentation Title

演示标题

Lead Author

主要作者

Presentation Details

演示详情

ARCHES 5-year follow-up overall survival analysis of enzalutamide plus androgen deprivation therapy in patients with metastatic hormone-sensitive prostate cancer

ARCHES 5年随访：恩扎鲁胺联合雄激素剥夺疗法在转移性激素敏感性前列腺癌患者中的总生存分析

A. Armstrong

阿姆斯特朗

Type:

类型：

Oral Presentation

口头报告

Abstract Number:

摘要编号：

5005

5005

Date:

日期：

June 3, 2025, 9:45am – 12:45pm CDT

2025年6月3日，上午9点45分 – 下午12点45分（中部夏令时间）

Cardiovascular event risk in patients with metastatic castration-resistant prostate cancer treated with enzalutamide or abiraterone acetate in the United States

美国转移性去势抵抗性前列腺癌患者使用恩杂鲁胺或醋酸阿比特龙治疗的心血管事件风险

A. Bryce

A. 布莱斯

Type:

类型：

Poster Presentation

海报展示

Abstract Number:

摘要编号：

5041

5041

Date:

日期：

June 2, 2025, 9:00am – 12:00pm CDT

2025年6月2日，上午9:00 – 下午12:00（中部夏令时间）

Secondary outcomes by prior definitive treatment in patients with high-risk biochemically recurrent prostate cancer treated with enzalutamide monotherapy: EMBARK post hoc analysis

高危生化复发前列腺癌患者接受恩杂鲁胺单药治疗的次要结局：按之前的确定性治疗分层的EMBARK事后分析

S. Freedland

S. 弗里德兰

Type:

类型：

Poster Presentation

海报展示

Abstract Number:

摘要编号：

5103

5103

Date:

日期：

June 2, 2025, 9:00am – 12:00pm CDT

2025年6月2日，上午9:00 – 中午12:00（中部夏令时间）

How low do you need to go? Association between various prostate-specific antigen response measures and clinical outcomes in metastatic castration‑sensitive prostate cancer in the Veteran Health Administration data

您需要降到多低？在退伍军人健康管理局数据中，各种前列腺特异性抗原反应指标与转移性去势敏感性前列腺癌临床结果之间的关联

S. Freedland

S. 弗里德兰

Type:

类型：

Poster Presentation

海报展示

Abstract Number:

摘要编号：

5092

5092

Date:

日期：

June 2, 2025, 9:00am – 12:00pm CDT

2025年6月2日，上午9:00 – 下午12:00（中部夏令时间）

Abiraterone acetate is associated with shorter overall survival than enzalutamide in patients with chemotherapy naïve metastatic castration-resistant prostate cancer: Real world data from the Flatiron electronic health records database

醋酸阿比特龙在化疗初治的转移性去势抵抗性前列腺癌患者中的总体生存期比恩杂鲁胺短：来自Flatiron电子健康记录数据库的真实世界数据

D. George

乔治

Type:

类型：

E-Publication Only

仅电子出版

Abstract Number for Publication:

发表编号：

e17033

e17033

Secondary outcomes by prior definitive treatment in patients with high-risk biochemically recurrent prostate cancer (treated with enzalutamide plus leuprolide (combo): EMBARK post hoc analysis

高危生化复发性前列腺癌患者按先前确定性治疗的次要结局（使用恩杂鲁胺联合亮丙瑞林治疗）：EMBARK事后分析

N. Shore

北岸

Type:

类型：

E-Publication Only

仅电子出版物

Abstract Number for Publication:

发表编号：

e17127

e17127

Corticosteroid Use and Risk of Adverse Events in Patients Treated for Metastatic Hormone-Sensitive Prostate Cancer

糖皮质激素使用与转移性激素敏感型前列腺癌患者治疗中不良事件风险的关系

U. Swami

乌.斯瓦米

Type:

类型：

E-Publication Only

仅电子出版物

Abstract Number for Publication:

出版物的摘要编号：

e17097

e17097

Enfortumab vedotin

维博妥珠单抗

Presentation Title

演讲标题

Lead Author

主要作者

Presentation Details

演示详情

EV-302: Long-term subgroup analysis from the phase 3 global study of enfortumab vedotin in combination with pembrolizumab vs chemotherapy in previously untreated locally advanced or metastatic urothelial carcinoma

EV-302：来自第三阶段全球研究的长期亚组分析，该研究针对之前未接受治疗的局部晚期或转移性尿路上皮癌，评估了恩福妥单抗维多汀联合彭布罗利珠单抗与化疗的疗效

J. Bedke

J. 贝德克

Type:

类型：

Poster Presentation

海报展示

Abstract Number:

摘要编号：

4571

4571

Date:

日期：

June 2, 2025, 9:00am – 12:00pm CDT

2025年6月2日，上午9:00 – 中午12:00（中部夏令时间）

Exploratory analysis of responders from the phase 3 EV-302 trial of enfortumab vedotin plus pembrolizumab vs chemotherapy (chemo) in previously untreated locally advanced or metastatic urothelial carcinoma

对来自三期EV-302试验的应答者进行探索性分析，该试验比较了Enfortumab Vedotin联合Pembrolizumab与化疗（chemo）在既往未治疗的局部晚期或转移性尿路上皮癌中的效果

S. Gupta

S. 古普塔

Type:

类型：

Oral Presentation

口头报告

Abstract Number:

摘要编号：

4502

4502

Date:

日期：

June 1, 2025, 9:45am – 12:45pm CDT

2025年6月1日，上午9点45分至中午12点45分（中部夏令时间）

Evaluation of surrogate endpoints in muscle-invasive bladder cancer: A systematic review and meta-analysis

肌肉浸润性膀胱癌中替代终点的评估：系统综述与荟萃分析

M. Galsky

M. 加尔斯基

Type:

类型：

Poster Presentation

海报展示

Abstract Number:

摘要编号：

4580

4580

Date:

日期：

June 2, 2025, 9:00am – 12:00pm CDT

2025年6月2日，上午9:00 – 中午12:00（北美中部夏令时间）

Study EV-103 Cohort H: Neoadjuvant treatment with enfortumab vedotin monotherapy in cisplatin-ineligible patients with muscle-invasive bladder cancer: 3-year efficacy results

研究EV-103队列H：在顺铂不耐受的肌层浸润性膀胱癌患者中使用Enfortumab Vedotin单药新辅助治疗：3年疗效结果

N. Mar

N. 马尔

Type:

类型：

Poster Presentation

海报展示

Abstract Number:

摘要编号：

4583

4583

Date:

日期：

June 2, 2025, 9:00am – 12:00pm CDT

2025年6月2日，上午9:00 – 中午12:00（北美中部夏令时间）

Recent trends in US real-world first-line treatment patterns for patients with locally advanced or metastatic urothelial carcinoma

美国近期局部晚期或转移性尿路上皮癌患者真实世界一线治疗模式的趋势

G. Sonpavde

G. 桑帕韦德

Type:

类型：

E-Publication Only

仅电子出版物

Abstract Number for Publication:

用于发布的摘要编号：

e16556

e16556

Patient and clinician expert perspectives on the impactful symptoms of head and neck squamous cell carcinoma and its treatment

头颈部鳞状细胞癌及其治疗有影响的症状的患者和临床专家视角

E. Theodorou

E. 塞奥多鲁

Type:

类型：

E-Publication Only

仅电子出版物

Abstract Number for Publication:

出版物的摘要编号：

e18001

e18001

Zolbetuximab

佐妥昔单抗

Presentation Title

演示标题

Lead Author

首席作者

Presentation Details

演示详情

A real-world study on epidemiology, biomarker test results, clinical characteristics, and treatment patterns of unresectable locally advanced or metastatic gastric and gastroesophageal junction adenocarcinoma in China

中国不可切除的局部晚期或转移性胃和胃食管结合部腺癌的流行病学、生物标志物检测结果、临床特征及治疗模式的真实世界研究

Y. Chen

陈 Y.

Type:

类型：

E-Publication Only

仅电子出版物

Abstract Number for Publication:

用于出版的摘要编号：

e16013

e16013

Gilteritinib

吉列替尼

Presentation Title

演示标题

Lead Author

主要作者

Presentation Details

演示详情

Real-world adherence and tolerability of FLT3 inhibitors s post-allogeneic transplant maintenance therapy in older adults with AML: A Medicare claims cohort study

FLT3抑制剂在老年AML患者异基因移植后维持治疗中的实际依从性与耐受性：一项Medicare索赔队列研究

V. Kennedy

V. 肯尼迪

Type:

类型：

E-Publication Only

仅电子出版物

Pipeline

管道

Presentation Title

演示标题

Lead Author

主要作者

Presentation Details

演示详情

Trial in progress: Phase 1 study of the selective protein degrader ASP4396 in patients with locally advanced or metastatic solid tumors with KRAS G12D mutation

正在进行的试验：选择性蛋白降解剂 ASP4396 在携带 KRAS G12D 突变的局部晚期或转移性实体瘤患者中的 1 期研究

Shiraj Sen

希拉杰·森

Type:

类型：

Poster Presentation

海报展示

Abstract Number:

摘要编号：

TPS3178

TPS3178

Date:

日期：

June 2, 2025, 1:30 – 4:30pm CDT

2025年6月2日，下午1:30 – 4:30（中部夏令时间）

About Astellas

关于安斯泰来

Astellas is a global life sciences company committed to turning innovative science into VALUE for patients. We provide transformative therapies in disease areas that include oncology, ophthalmology, urology, immunology and women's health. Through our research and development programs, we are pioneering new healthcare solutions for diseases with high unmet medical need.

安斯泰来是一家全球生命科学公司，致力于将创新科学转化为对患者的 VALUE。我们在肿瘤学、眼科学、泌尿学、免疫学和女性健康等疾病领域提供变革性疗法。通过我们的研发项目，我们正在为那些存在高度未满足医疗需求的疾病开拓新的医疗解决方案。

Learn more at .

了解更多，请访问。

www.astellas.com

www.astellas.com

.

。

About PADCEV and the Astellas, Pfizer and Merck Collaboration

关于PADCEV以及安斯泰来、辉瑞和默克的合作关系

Astellas and Pfizer have a clinical collaboration agreement with Merck to evaluate the combination of Astellas' and Pfizer's PADCEV (enfortumab vedotin) and Merck's KEYTRUDA (pembrolizumab) in patients with previously untreated metastatic urothelial cancer. KEYTRUDA is a registered trademark of Merck Sharp & Dohme Corp., a subsidiary of Merck & Co., Inc., Rahway, NJ, USA (known as MSD outside of the United States and Canada)..

安斯泰来和辉瑞与默克公司达成了一项临床合作协议，评估安斯泰来和辉瑞的 PADCEV（enfortumab vedotin）与默克公司的 KEYTRUDA（pembrolizumab）联合用于既往未接受治疗的转移性尿路上皮癌患者的效果。KEYTRUDA 是默克公司子公司默克夏普与多姆公司（Merck Sharp & Dohme Corp.，美国新泽西州拉威）的注册商标（在美国和加拿大以外地区称为 MSD）。

About XTANDI and the Pfizer/Astellas Collaboration

关于XTANDI和辉瑞/安斯泰来合作

In October 2009, Medivation, Inc., which is now part of Pfizer (NYSE:PFE), and Astellas (TSE: 4503) entered into a commercial agreement to jointly develop and commercialize XTANDI

2009年10月，当时隶属于辉瑞公司（纽约证券交易所代码：PFE）的Medivation公司和安斯泰来（东京证券交易所代码：4503）达成商业协议，共同开发和商业化XTANDI。

®

®

(enzalutamide) in the United States, while Astellas has responsibility for manufacturing and all additional regulatory filings globally, as well as commercializing the product outside the United States. Pfizer receives alliance revenues as a share of U.S. profits and receives royalties on sales outside the U.S..

在美国，恩杂鲁胺由辉瑞负责，而安斯泰来则负责全球的生产、所有额外的监管申报，以及在美国以外地区的商业化。辉瑞作为美国利润的一部分获得联盟收入，并在美囝以外的销售额中收取特许权使用费。

XTANDI Important Safety Information

XTANDI重要安全信息

Warnings and Precautions

警告和注意事项

Seizure

癫痫发作

occurred in 0.6% of patients receiving XTANDI in eight randomized clinical trials. In a study of patients with predisposing factors for seizure, 2.2% of XTANDI-treated patients experienced a seizure. It is unknown whether anti-epileptic medications will prevent seizures with XTANDI. Patients in the study had one or more of the following predisposing factors: use of medications that may lower the seizure threshold, history of traumatic brain or head injury, history of cerebrovascular accident or transient ischemic attack, and Alzheimer’s disease, meningioma, or leptomeningeal disease from prostate cancer, unexplained loss of consciousness within the last 12 months, history of seizure, presence of a space occupying lesion of the brain, history of arteriovenous malformation, or history of brain infection.

在八项随机临床试验中，接受XTANDI治疗的患者中有0.6%发生了癫痫发作。在一项针对具有癫痫发作诱因的患者的研究中，2.2%接受XTANDI治疗的患者经历了癫痫发作。目前尚不清楚抗癫痫药物是否能够预防XTANDI引发的癫痫发作。研究中的患者具有以下一种或多种诱发因素：使用可能降低癫痫发作阈值的药物、有脑外伤或头部损伤史、有脑血管意外或短暂性脑缺血发作史、阿尔茨海默病、脑膜瘤或由前列腺癌引起的软脑膜疾病、过去12个月内无法解释的意识丧失、有癫痫发作史、存在脑部占位性病变、有动静脉畸形史或脑部感染史。

Advise patients of the risk of developing a seizure while taking XTANDI and of engaging in any activity where sudden loss of consciousness could cause serious harm to themselves or others. Permanently discontinue XTANDI in patients who develop a seizure during treatment..

告知患者在服用XTANDI时存在癫痫发作的风险，并在从事任何因突然失去意识可能对自己或他人造成严重伤害的活动时予以注意。对于在治疗期间出现癫痫发作的患者，应永久停用XTANDI。

Posterior Reversible Encephalopathy Syndrome (PRES)

后部可逆性脑病综合征 (PRES)

There have been reports of PRES in patients receiving XTANDI. PRES is a neurological disorder that can present with rapidly evolving symptoms including seizure, headache, lethargy, confusion, blindness, and other visual and neurological disturbances, with or without associated hypertension. A diagnosis of PRES requires confirmation by brain imaging, preferably MRI.

有报道称接受XTANDI治疗的患者出现了PRES。PRES是一种神经系统疾病，可能伴有迅速发展的症状，包括癫痫发作、头痛、嗜睡、意识模糊、失明以及其他视觉和神经系统紊乱，伴或不伴高血压。确诊PRES需要通过脑部影像学检查确认，最好进行MRI检查。

Discontinue XTANDI in patients who develop PRES..

在出现PRES的患者中停用XTANDI。

Hypersensitivity

超敏反应

reactions, including edema of the face (0.5%), tongue (0.1%), or lip (0.1%) have been observed with XTANDI in eight randomized clinical trials. Pharyngeal edema has been reported in post-marketing cases. Advise patients who experience any symptoms of hypersensitivity to temporarily discontinue XTANDI and promptly seek medical care.

在八项随机临床试验中，观察到XTANDI引起的一些反应，包括面部（0.5%）、舌头（0.1%）或嘴唇（0.1%）水肿。上市后病例中也有咽部水肿的报告。建议出现任何过敏症状的患者暂时停用XTANDI，并立即寻求医疗帮助。

Permanently discontinue XTANDI for serious hypersensitivity reactions..

因严重过敏反应，永久停止使用XTANDI。

Ischemic Heart Disease

缺血性心脏病

In the combined data of five randomized, placebo-controlled clinical studies, ischemic heart disease occurred more commonly in patients on the XTANDI arm compared to patients on the placebo arm (3.5% vs 2%). Grade 3-4 ischemic events occurred in 1.8% of patients on XTANDI versus 1.1% on placebo. Ischemic events led to death in 0.4% of patients on XTANDI compared to 0.1% on placebo.

在五项随机、安慰剂对照临床研究的综合数据中，与安慰剂组相比，XTANDI组患者发生缺血性心脏病的比例更高（3.5% vs 2%）。XTANDI组中有1.8%的患者发生了3-4级缺血事件，而安慰剂组为1.1%。XTANDI组中有0.4%的患者因缺血事件导致死亡，而安慰剂组为0.1%。

Monitor for signs and symptoms of ischemic heart disease. Optimize management of cardiovascular risk factors, such as hypertension, diabetes, or dyslipidemia. Discontinue XTANDI for Grade 3-4 ischemic heart disease..

监测缺血性心脏病的体征和症状。优化心血管风险因素的管理，如高血压、糖尿病或血脂异常。对于3-4级缺血性心脏病，应停止使用XTANDI。

Falls and Fractures

跌倒和骨折

occurred in patients receiving XTANDI. Evaluate patients for fracture and fall risk. Monitor and manage patients at risk for fractures according to established treatment guidelines and consider use of bone-targeted agents. In the combined data of five randomized, placebo-controlled clinical studies, falls occurred in 12% of patients treated with XTANDI compared to 6% of patients treated with placebo.

接受XTANDI治疗的患者中出现了相关事件。评估患者的骨折和跌倒风险。根据既定的治疗指南监测和管理有骨折风险的患者，并考虑使用针对骨骼的药物。在五项随机、安慰剂对照临床研究的综合数据中，接受XTANDI治疗的患者中有12%发生跌倒，而接受安慰剂治疗的患者中有6%发生跌倒。

Fractures occurred in 13% of patients treated with XTANDI and in 6% of patients treated with placebo..

接受XTANDI治疗的患者中有13%发生骨折，而接受安慰剂治疗的患者中有6%发生骨折。

Embryo-Fetal Toxicity

胚胎-胎儿毒性

The safety and efficacy of XTANDI have not been established in females.

XTANDI 在女性中的安全性和有效性尚未确定。

XTANDI can cause fetal harm and loss of pregnancy when administered to a pregnant female. Advise males with female partners of reproductive potential to use effective contraception during treatment with XTANDI and for 3 months after the last dose of XTANDI.

XTANDI在给怀孕女性使用时可能导致胎儿伤害和妊娠丢失。建议有生育潜力的女性伴侣的男性在使用XTANDI治疗期间以及最后一次服用XTANDI后3个月内使用有效避孕措施。

Dysphagia or Choking

吞咽困难或窒息

Severe dysphagia or choking, including events that could be life-threatening requiring medical intervention or fatal, can occur due to XTANDI product size. Advise patients to take each capsule or tablet whole with a sufficient amount of water to ensure that all medication is successfully swallowed.

由于XTANDI产品的尺寸，可能会发生严重的吞咽困难或窒息，包括可能危及生命需要医疗干预或致命的事件。建议患者用足量的水整粒吞服每粒胶囊或药片，以确保所有药物都被成功吞下。

Consider use of a smaller tablet size of XTANDI in patients who have difficulty swallowing. Discontinue XTANDI for patients who cannot swallow capsules or tablets..

考虑给吞咽困难的患者使用较小片剂规格的XTANDI。对于无法吞咽胶囊或片剂的患者，请停止使用XTANDI。

Adverse Reactions (ARs)

不良反应 (ARs)

In the data from the five randomized placebo-controlled trials, the most common ARs (≥ 10%) that occurred more frequently (≥ 2% over placebo) in XTANDI-treated patients were musculoskeletal pain, fatigue, hot flush, constipation, decreased appetite, diarrhea, hypertension, hemorrhage, fall, fracture, and headache.

在五项随机安慰剂对照试验的数据中，XTANDI治疗患者中发生率较高（比安慰剂高≥2%）的最常见不良反应（≥10%）为肌肉骨骼疼痛、疲劳、潮热、便秘、食欲减退、腹泻、高血压、出血、跌倒、骨折和头痛。

In the bicalutamide-controlled study, the most common ARs (≥ 10%) reported in XTANDI-treated patients were asthenia/fatigue, back pain, musculoskeletal pain, hot flush, hypertension, nausea, constipation, diarrhea, upper respiratory tract infection, and weight loss..

在比卡鲁胺对照研究中，接受XTANDI治疗的患者报告的最常见的不良反应（≥10%）为乏力/疲劳、背部疼痛、肌肉骨骼疼痛、潮热、高血压、恶心、便秘、腹泻、上呼吸道感染和体重减轻。

In AFFIRM, the placebo-controlled study of metastatic CRPC (mCRPC) patients who previously received docetaxel, Grade 3 and higher ARs were reported among 47% of XTANDI-treated patients.

在AFFIRM研究中，既往接受多西他赛治疗的转移性去势抵抗性前列腺癌（mCRPC）患者的安慰剂对照研究显示，47%的XTANDI治疗患者报告了3级及更高级别的不良反应（ARs）。

Discontinuations due to ARs were reported for 16% of XTANDI-treated patients. In PREVAIL, the placebo-controlled study of chemotherapy-naive mCRPC patients, Grade 3-4 ARs were reported in 44% of XTANDI patients and 37% of placebo patients. Discontinuations due to ARs were reported for 6% of XTANDI-treated patients.

因不良反应（AR）而停药的情况在16%的XTANDI治疗患者中被报告。在PREVAIL研究中，一项针对未接受化疗的mCRPC患者的安慰剂对照研究，44%的XTANDI患者和37%的安慰剂患者报告了3-4级不良反应（AR）。因不良反应（AR）而停药的情况在6%的XTANDI治疗患者中被报告。

In TERRAIN, the bicalutamide-controlled study of chemotherapy-naive mCRPC patients, Grade 3-4 ARs were reported in 39% of XTANDI patients and 38% of bicalutamide patients. Discontinuations with an AR as the primary reason were reported for 8% of XTANDI patients and 6% of bicalutamide patients..

在TERRAIN研究中，对未接受化疗的mCRPC患者进行的比卡鲁胺对照研究显示，39%的XTANDI患者和38%的比卡鲁胺患者报告了3-4级不良反应（ARs）。因不良反应为主要原因而停药的情况在8%的XTANDI患者和6%的比卡鲁胺患者中被报告。

In PROSPER, the placebo-controlled study of nonmetastatic CRPC (nmCRPC) patients, Grade 3 or higher ARs were reported in 31% of XTANDI patients and 23% of placebo patients.

在PROSPER研究中，针对非转移性去势抵抗性前列腺癌（nmCRPC）患者的安慰剂对照试验显示，31%的XTANDI患者和23%的安慰剂患者报告了3级或更高级别的不良反应（ARs）。

Discontinuations with an AR as the primary reason were reported for 9% of XTANDI patients and 6% of placebo patients.

因AR作为主要原因而停药的情况在XTANDI患者中占9%，在安慰剂患者中占6%。

In ARCHES, the placebo-controlled study of metastatic CSPC (mCSPC) patients, Grade 3 or higher ARs were reported in 24% of XTANDI-treated patients. Permanent discontinuation due to ARs as the primary reason was reported in 5% of XTANDI patients and 4% of placebo patients.

在ARCHES研究中，针对转移性CSPC（mCSPC）患者的安慰剂对照研究显示，24%的接受XTANDI治疗的患者报告了3级或更高级别的不良反应（ARs）。因不良反应（ARs）作为主要原因导致永久停药的比例为：XTANDI组5%，安慰剂组4%。

In EMBARK, the placebo-controlled study of nonmetastatic CSPC (nmCSPC) with high-risk biochemical recurrence (BCR) patients, Grade 3 or higher adverse reactions during the total duration of treatment were reported in 46% of patients treated with XTANDI plus leuprolide, 50% of patients receiving XTANDI as a single agent, and 43% of patients receiving placebo plus leuprolide.

在EMBARK研究中，针对具有高风险生化复发（BCR）的非转移性CSPC（nmCSPC）患者的安慰剂对照研究显示，在整个治疗期间，接受XTANDI联合亮丙瑞林治疗的患者中有46%报告了3级或更高级别的不良反应，单独使用XTANDI治疗的患者中有50%，而接受安慰剂联合亮丙瑞林治疗的患者中有43%。

Permanent treatment discontinuation due to adverse reactions during the total duration of treatment as the primary reason was reported in 21% of patients treated with XTANDI plus leuprolide, 18% of patients receiving XTANDI as a single agent, and 10% of patients receiving placebo plus leuprolide..

在整个治疗期间，因不良反应而永久停止治疗的主要原因报告为：接受XTANDI联合亮丙瑞林治疗的患者中有21%，接受XTANDI单药治疗的患者中有18%，而接受安慰剂联合亮丙瑞林治疗的患者中有10%。

Lab Abnormalities:

实验室异常：

Lab abnormalities that occurred in ≥ 5% of patients, and more frequently (> 2%) in the XTANDI arm compared to placebo in the pooled, randomized, placebo-controlled studies are hemoglobin decrease, neutrophil count decreased, white blood cell decreased, hyperglycemia, hypermagnesemia, hyponatremia, hypophosphatemia, and hypercalcemia..

在汇总的随机、安慰剂对照研究中，发生在≥5%的患者中，并且在XTANDI组比安慰剂组更频繁（>2%）的实验室异常包括：血红蛋白减少、中性粒细胞计数减少、白细胞减少、高血糖、高镁血症、低钠血症、低磷血症和高钙血症。

Hypertension:

高血压：

In the combined data from five randomized placebo-controlled clinical trials, hypertension was reported in 14% of XTANDI patients and 7% of placebo patients. Hypertension led to study discontinuation in < 1% of patients in each arm.

在五项随机安慰剂对照临床试验的综合数据中，14% 的 XTANDI 患者和 7% 的安慰剂患者报告出现高血压。在每组中，不到 1% 的患者因高血压导致研究中断。

Drug Interactions

药物相互作用

Effect of Other Drugs on XTANDI

其他药物对XTANDI的影响

Avoid coadministration with strong CYP2C8 inhibitors. If coadministration cannot be avoided, reduce the dosage of XTANDI.

避免与强效CYP2C8抑制剂联合使用。如果无法避免联合使用，减少XTANDI的剂量。

Avoid coadministration with strong CYP3A4 inducers. If coadministration cannot be avoided, increase the dosage of XTANDI.

避免与强效CYP3A4诱导剂联合使用。如果无法避免联合使用，增加XTANDI的剂量。

Effect of XTANDI on Other Drugs

XTANDI对其他药物的影响

Avoid coadministration with certain CYP3A4, CYP2C9, and CYP2C19 substrates for which minimal decrease in concentration may lead to therapeutic failure of the substrate. If coadministration cannot be avoided, increase the dosage of these substrates in accordance with their Prescribing Information. In cases where active metabolites are formed, there may be increased exposure to the active metabolites..

避免与某些CYP3A4、CYP2C9和CYP2C19底物联合使用，因为浓度的微小降低可能导致这些底物的治疗失败。如果无法避免联合使用，应根据其处方信息增加这些底物的剂量。在形成活性代谢物的情况下，可能会增加对活性代谢物的暴露。

Full Prescribing Information

完整处方信息

PADCEV Important Safety Information

PADCEV重要安全信息

Warnings and Precautions

警告和注意事项

Skin reactions

皮肤反应

Severe cutaneous adverse reactions, including fatal cases of SJS or TEN occurred in patients treated with PADCEV. SJS and TEN occurred predominantly during the first cycle of treatment but may occur later. Skin reactions occurred in 70% (all grades) of the 564 patients treated with PADCEV in combination with pembrolizumab in clinical trials.

接受PADCEV治疗的患者中，发生了严重的皮肤不良反应，包括致命的SJS或TEN病例。SJS和TEN主要发生在第一个治疗周期，但也可能在之后发生。在临床试验中，564名接受PADCEV联合派姆单抗治疗的患者中，70%（所有等级）出现了皮肤反应。

When PADCEV was given in combination with pembrolizumab, the incidence of skin reactions, including severe events, occurred at a higher rate compared to PADCEV as a single agent. The majority of the skin reactions that occurred with combination therapy included maculo-papular rash, macular rash and papular rash.

当PADCEV与pembrolizumab联合使用时，皮肤反应（包括严重事件）的发生率相较于PADCEV单药治疗更高。联合治疗中多数皮肤反应包括斑丘疹、斑疹和丘疹。

Grade 3-4 skin reactions occurred in 17% of patients (Grade 3: 16%, Grade 4: 1%), including maculo-papular rash, bullous dermatitis, dermatitis, exfoliative dermatitis, pemphigoid, rash, erythematous rash, macular rash, and papular rash. A fatal reaction of bullous dermatitis occurred in one patient (0.2%).

3-4级皮肤反应发生在17%的患者中（3级：16%，4级：1%），包括斑丘疹、大疱性皮炎、皮炎、剥脱性皮炎、类天疱疮、皮疹、红斑性皮疹、斑疹和丘疹。其中一名患者（0.2%）发生了致命的大疱性皮炎反应。

The median time to onset of severe skin reactions was 1.7 months (range: 0.1 to 17.2 months). Skin reactions led to discontinuation of PADCEV in 6% of patients..

严重皮肤反应的中位发病时间为1.7个月（范围：0.1至17.2个月）。皮肤反应导致6%的患者停止使用PADCEV。

Skin reactions occurred in 58% (all grades) of the 720 patients treated with PADCEV as a single agent in clinical trials. Twenty-three percent (23%) of patients had maculo-papular rash and 34% had pruritus. Grade 3-4 skin reactions occurred in 14% of patients, including maculo-papular rash, erythematous rash, rash or drug eruption, symmetrical drug-related intertriginous and flexural exanthema (SDRIFE), bullous dermatitis, exfoliative dermatitis, and palmar-plantar erythrodysesthesia.

在临床试验中，720名接受PADCEV单药治疗的患者中有58%（所有等级）出现皮肤反应。23%的患者出现斑丘疹，34%的患者出现瘙痒。14%的患者出现3-4级皮肤反应，包括斑丘疹、红斑疹、皮疹或药物性皮疹、对称性药物相关的皱褶和屈侧红斑（SDRIFE）、大疱性皮炎、剥脱性皮炎以及掌跖红斑感觉异常。

The median time to onset of severe skin reactions was 0.6 months (range: 0.1 to 8 months). Among patients experiencing a skin reaction leading to dose interruption who then restarted PADCEV (n=75), 24% of patients restarting at the same dose and 24% of patients restarting at a reduced dose experienced recurrent severe skin reactions.

严重皮肤反应发作的中位时间为0.6个月（范围：0.1至8个月）。在因皮肤反应导致剂量中断后重新开始使用PADCEV的患者（n=75）中，重新使用相同剂量的患者中有24%以及重新使用减量剂量的患者中有24%经历了再次发生的严重皮肤反应。

Skin reactions led to discontinuation of PADCEV in 3.1% of patients..

皮肤反应导致3.1%的患者停止使用PADCEV。

Monitor patients closely throughout treatment for skin reactions. Consider topical corticosteroids and antihistamines, as clinically indicated. For persistent or recurrent Grade 2 skin reactions, consider withholding PADCEV until Grade ≤1. Withhold PADCEV and refer for specialized care for suspected SJS, TEN or for Grade 3 skin reactions.

在治疗过程中密切监测患者的皮肤反应。根据临床需要，考虑使用局部皮质类固醇和抗组胺药。对于持续或复发的2级皮肤反应，考虑暂停PADCEV直至反应降至1级或以下。若怀疑SJS、TEN或出现3级皮肤反应，应暂停PADCEV并转诊进行专业治疗。

Permanently discontinue PADCEV in patients with confirmed SJS or TEN; or Grade 4 or recurrent Grade 3 skin reactions..

确认患者出现SJS或TEN；或4级或复发性3级皮肤反应时，永久停止使用PADCEV。

Hyperglycemia and diabetic ketoacidosis (DKA),

高血糖和糖尿病酮症酸中毒 (DKA)，

including fatal events, occurred in patients with and without pre-existing diabetes mellitus, treated with PADCEV. Patients with baseline hemoglobin A1C ≥8% were excluded from clinical trials. In clinical trials of PADCEV as a single agent, 17% of the 720 patients treated with PADCEV developed hyperglycemia of any grade; 7% of patients developed Grade 3-4 hyperglycemia (Grade 3: 6.5%, Grade 4: 0.6%).

包括致命事件在内，接受PADCEV治疗的患者中，无论是否预先存在糖尿病，均有相关事件发生。基线血红蛋白A1C ≥8% 的患者被排除在临床试验之外。在PADCEV单药临床试验中，720名接受PADCEV治疗的患者中有17%发生了任意级别的高血糖；7%的患者出现了3-4级高血糖（3级：6.5%，4级：0.6%）。

Fatal events of hyperglycemia and DKA occurred in one patient each (0.1%). The incidence of Grade 3-4 hyperglycemia increased consistently in patients with higher body mass index and in patients with higher baseline A1C. The median time to onset of hyperglycemia was 0.5 months (range: 0 to 20 months).

高血糖和DKA的致命事件各发生一例（0.1%）。3-4级高血糖的发生率在体重指数较高和基线A1C较高的患者中持续增加。高血糖发作的中位时间为0.5个月（范围：0至20个月）。

Hyperglycemia led to discontinuation of PADCEV in 0.7% of patients. Five percent (5%) of patients required initiation of insulin therapy for treatment of hyperglycemia. Of the patients who initiated insulin therapy for treatment of hyperglycemia, 66% (23/35) discontinued insulin at the time of last evaluation.

高血糖导致0.7%的患者停止使用PADCEV。5%的患者需要开始胰岛素治疗以应对高血糖。在那些开始胰岛素治疗的患者中，66%（23/35）在最后一次评估时停止了胰岛素治疗。

Closely monitor blood glucose levels in patients with, or at risk for, diabetes mellitus or hyperglycemia. If blood glucose is elevated (>250 mg/dL), withhold PADCEV..

密切监测糖尿病或高血糖患者，或有风险的患者的血糖水平。如果血糖升高（> 250 mg/dL），则暂停使用PADCEV。

Pneumonitis/Interstitial Lung Disease (ILD)

肺炎/间质性肺病 (ILD)

Severe, life-threatening or fatal pneumonitis/ILD occurred in patients treated with PADCEV. When PADCEV was given in combination with pembrolizumab, 10% of the 564 patients treated with combination therapy had pneumonitis/ILD of any grade and 4% had Grade 3-4. A fatal event of pneumonitis/ILD occurred in two patients (0.4%).

接受PADCEV治疗的患者中出现了严重、威胁生命或致命的肺炎/间质性肺病（ILD）。当PADCEV与派姆单抗联合使用时，在接受联合治疗的564名患者中，有10%发生了任何级别的肺炎/ILD，4%发生了3-4级的肺炎/ILD。两名患者（0.4%）发生了致命的肺炎/ILD事件。

The incidence of pneumonitis/ILD, including severe events, occurred at a higher rate when PADCEV was given in combination with pembrolizumab compared to PADCEV as a single agent. The median time to onset of any grade pneumonitis/ILD was 4 months (range: 0.3 to 26 months)..

当PADCEV与pembrolizumab联合使用时，包括严重事件在内的肺炎/间质性肺病的发生率比单独使用PADCEV更高。任何级别肺炎/间质性肺病的中位发病时间为4个月（范围：0.3至26个月）。

In clinical trials of PADCEV as a single agent, 3% of the 720 patients treated with PADCEV had pneumonitis/ILD of any grade and 0.8% had Grade 3-4. The median time to onset of any grade pneumonitis/ILD was 2.9 months (range: 0.6 to 6 months).

在 PADCEV 单药治疗的临床试验中，720 名接受 PADCEV 治疗的患者中有 3% 出现任何级别的肺炎/间质性肺病（ILD），0.8% 出现 3-4 级。任何级别肺炎/间质性肺病的中位发病时间为 2.9 个月（范围：0.6 至 6 个月）。

Monitor patients for signs and symptoms indicative of pneumonitis/ILD such as hypoxia, cough, dyspnea or interstitial infiltrates on radiologic exams. Evaluate and exclude infectious, neoplastic and other causes for such signs and symptoms through appropriate investigations. Withhold PADCEV for patients who develop Grade 2 pneumonitis/ILD and consider dose reduction.

监测患者是否出现肺炎/间质性肺病（ILD）的体征和症状，例如低氧血症、咳嗽、呼吸困难或影像学检查中显示的间质浸润。通过适当的检查评估并排除这些体征和症状的感染性、肿瘤性及其他原因。对于发生2级肺炎/ILD的患者，暂停使用PADCEV，并考虑减少剂量。

Permanently discontinue PADCEV in all patients with Grade 3 or 4 pneumonitis/ILD..

对所有 3 级或 4 级肺炎/间质性肺病患者永久停用 PADCEV。

Peripheral neuropathy (PN)

周围神经病变 (PN)

When PADCEV was given in combination with pembrolizumab, 67% of the 564 patients treated with combination therapy had PN of any grade, 36% had Grade 2 neuropathy, and 7% had Grade 3 neuropathy. The incidence of PN occurred at a higher rate when PADCEV was given in combination with pembrolizumab compared to PADCEV as a single agent.

当PADCEV与pembrolizumab联合使用时，接受联合治疗的564名患者中有67%发生了任何级别的PN（周围神经病变），36%出现了2级神经病变，7%出现了3级神经病变。与单独使用PADCEV相比，联合使用PADCEV和pembrolizumab时PN的发生率更高。

The median time to onset of Grade ≥2 PN was 6 months (range: 0.3 to 25 months)..

3级或以上周围神经病变（PN）的中位发病时间为6个月（范围：0.3至25个月）。

PN occurred in 53% of the 720 patients treated with PADCEV as a single agent in clinical trials including 38% with sensory neuropathy, 8% with muscular weakness and 7% with motor neuropathy. Thirty percent of patients experienced Grade 2 reactions and 5% experienced Grade 3-4 reactions. PN occurred in patients treated with PADCEV with or without preexisting PN.

在临床试验中，720名接受PADCEV单药治疗的患者中有53%发生了PN（周围神经病变），其中包括38%的感觉神经病变、8%的肌肉无力和7%的运动神经病变。30%的患者出现了2级反应，5%的患者出现了3-4级反应。无论患者是否预先存在PN，接受PADCEV治疗的患者中均发生了PN。

The median time to onset of Grade ≥2 PN was 4.9 months (range: 0.1 to 20 months). Neuropathy led to treatment discontinuation in 6% of patients..

出现2级或以上外周神经病变（PN）的中位时间为4.9个月（范围：0.1至20个月）。神经病导致6%的患者停止治疗。

Monitor patients for symptoms of new or worsening PN and consider dose interruption or dose reduction of PADCEV when PN occurs. Permanently discontinue PADCEV in patients who develop Grade ≥3 PN.

监测患者是否出现新的或恶化的PN症状，当PN发生时，考虑暂停或减少PADCEV的剂量。对于出现3级或以上PN的患者，永久停用PADCEV。

Ocular disorders

眼部疾病

were reported in 40% of the 384 patients treated with PADCEV as a single agent in clinical trials in which ophthalmologic exams were scheduled. The majority of these events involved the cornea and included events associated with dry eye such as keratitis, blurred vision, increased lacrimation, conjunctivitis, limbal stem cell deficiency, and keratopathy.

在384名接受PADCEV单药治疗的患者中，40%的患者报告了眼部检查相关事件，这些临床试验中安排了眼科检查。大多数事件涉及角膜，包括与干眼相关的情况，如角膜炎、视力模糊、泪液增多、结膜炎、边缘干细胞缺乏和角膜病变。

Dry eye symptoms occurred in 30% of patients, and blurred vision occurred in 10% of patients, during treatment with PADCEV. The median time to onset to symptomatic ocular disorder was 1.7 months (range: 0 to 30.6 months). Monitor patients for ocular disorders. Consider artificial tears for prophylaxis of dry eyes and ophthalmologic evaluation if ocular symptoms occur or do not resolve.

在接受PADCEV治疗期间，30%的患者出现干眼症状，10%的患者出现视力模糊。发生症状性眼部疾病的中位时间为1.7个月（范围：0至30.6个月）。应监测患者的眼部疾病。考虑使用人工泪液预防干眼，并在出现眼部症状或症状未缓解时进行眼科评估。

Consider treatment with ophthalmic topical steroids, if indicated after an ophthalmic exam. Consider dose interruption or dose reduction of PADCEV for symptomatic ocular disorders..

如果眼科检查后有指征，考虑使用眼科局部类固醇治疗。对于有症状的眼部疾病，考虑中断或减少PADCEV的剂量。

Infusion site extravasation

输注部位外渗

Skin and soft tissue reactions secondary to extravasation have been observed after administration of PADCEV. Of the 720 patients treated with PADCEV as a single agent in clinical trials, 1% of patients experienced skin and soft tissue reactions, including 0.3% who experienced Grade 3-4 reactions. Reactions may be delayed.

在使用PADCEV治疗后，观察到与外渗相关的皮肤和软组织反应。在临床试验中接受PADCEV单药治疗的720名患者中，有1%的患者出现皮肤和软组织反应，其中0.3%的患者出现3-4级反应。反应可能会延迟发生。

Erythema, swelling, increased temperature, and pain worsened until 2-7 days after extravasation and resolved within 1-4 weeks of peak. Two patients (0.3%) developed extravasation reactions with secondary cellulitis, bullae, or exfoliation. Ensure adequate venous access prior to starting PADCEV and monitor for possible extravasation during administration.

红斑、肿胀、温度升高和疼痛在渗漏后2-7天内加重，并在峰值后1-4周内消退。两名患者（0.3%）出现伴有继发性蜂窝织炎、水疱或脱皮的渗漏反应。在开始使用PADCEV之前确保静脉通路充足，并在给药期间监测可能的渗漏情况。

If extravasation occurs, stop the infusion and monitor for adverse reactions..

如果发生外渗，停止输液并监测不良反应。

Embryo-fetal toxicity

胚胎-胎儿毒性

PADCEV can cause fetal harm when administered to a pregnant woman. Advise patients of the potential risk to the fetus. Advise female patients of reproductive potential to use effective contraception during PADCEV treatment and for 2 months after the last dose. Advise male patients with female partners of reproductive potential to use effective contraception during treatment with PADCEV and for 4 months after the last dose..

PADCEV在给予孕妇时可能对胎儿造成伤害。请告知患者对胎儿的潜在风险。建议有生育潜力的女性患者在PADCEV治疗期间以及最后一剂后两个月内使用有效避孕措施。建议有生育潜力女性伴侣的男性患者在PADCEV治疗期间以及最后一剂后四个月内使用有效避孕措施。

ADVERSE REACTIONS

不良反应

Most common adverse reactions, including laboratory abnormalities (≥20%) (PADCEV in combination with pembrolizumab)

最常见的不良反应，包括实验室异常（≥20％）（PADCEV与pembrolizumab联合使用）

Increased aspartate aminotransferase (AST), increased creatinine, rash, increased glucose, PN, increased lipase, decreased lymphocytes, increased alanine aminotransferase (ALT), decreased hemoglobin, fatigue, decreased sodium, decreased phosphate, decreased albumin, pruritus, diarrhea, alopecia, decreased weight, decreased appetite, increased urate, decreased neutrophils, decreased potassium, dry eye, nausea, constipation, increased potassium, dysgeusia, urinary tract infection and decreased platelets..

天冬氨酸氨基转移酶（AST）升高、肌酐升高、皮疹、血糖升高、周围神经病变（PN）、脂肪酶升高、淋巴细胞减少、丙氨酸氨基转移酶（ALT）升高、血红蛋白减少、疲劳、钠减少、磷减少、白蛋白减少、瘙痒、腹泻、脱发、体重减轻、食欲减退、尿酸升高、中性粒细胞减少、钾减少、干眼症、恶心、便秘、钾升高、味觉障碍、尿路感染和血小板减少。

Most common adverse reactions, including laboratory abnormalities (≥20%) (PADCEV monotherapy)

最常见的不良反应，包括实验室异常（≥20%）（PADCEV单药治疗）

Increased glucose, increased AST, decreased lymphocytes, increased creatinine, rash, fatigue, PN, decreased albumin, decreased hemoglobin, alopecia, decreased appetite, decreased neutrophils, decreased sodium, increased ALT, decreased phosphate, diarrhea, nausea, pruritus, increased urate, dry eye, dysgeusia, constipation, increased lipase, decreased weight, decreased platelets, abdominal pain, dry skin..

血糖升高、AST升高、淋巴细胞减少、肌酐升高、皮疹、疲劳、PN（周围神经病变）、白蛋白降低、血红蛋白降低、脱发、食欲减退、中性粒细胞减少、钠降低、ALT升高、磷酸盐降低、腹泻、恶心、瘙痒、尿酸升高、干眼症、味觉障碍、便秘、脂肪酶升高、体重减轻、血小板减少、腹痛、皮肤干燥。

EV-302 Study: 440 patients with previously untreated la/mUC (PADCEV in combination with pembrolizumab)

EV-302研究：440名既往未治疗的la/mUC患者（PADCEV联合pembrolizumab）

Serious adverse reactions

严重的不良反应

occurred in 50% of patients treated with PADCEV in combination with pembrolizumab. The most common serious adverse reactions (≥2%) were rash (6%), acute kidney injury (5%), pneumonitis/ILD (4.5%), urinary tract infection (3.6%), diarrhea (3.2%), pneumonia (2.3%), pyrexia (2%), and hyperglycemia (2%).

在接受PADCEV联合派姆单抗治疗的患者中，50%发生了严重不良反应。最常见的严重不良反应（≥2%）为皮疹（6%）、急性肾损伤（5%）、肺炎/间质性肺病（4.5%）、尿路感染（3.6%）、腹泻（3.2%）、肺炎（2.3%）、发热（2%）和高血糖（2%）。

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Fatal adverse reactions

致命的不良反应

occurred in 3.9% of patients treated with PADCEV in combination with pembrolizumab including acute respiratory failure (0.7%), pneumonia (0.5%), and pneumonitis/ILD (0.2%).

在接受PADCEV联合pembrolizumab治疗的患者中，3.9%发生了相关事件，包括急性呼吸衰竭（0.7%）、肺炎（0.5%）以及肺炎/间质性肺病（0.2%）。

Adverse reactions leading to discontinuation of PADCEV occurred in 35% of patients.

导致停止使用PADCEV的不良反应发生在35%的患者中。

The most common adverse reactions (≥2%) leading to discontinuation

导致停药的最常见不良反应（≥2%）

of PADCEV were PN (15%), rash (4.1%) and pneumonitis/ILD (2.3%). Adverse reactions leading to dose interruption of PADCEV occurred in 73% of patients.

PADCEV的不良反应包括周围神经病变（15%）、皮疹（4.1%）和肺炎/间质性肺病（2.3%）。导致PADCEV剂量中断的不良反应发生在73%的患者中。

The most common adverse reactions (≥2%) leading to dose interruption

导致剂量中断的最常见的不良反应（≥2%）

of PADCEV were PN (22%), rash (16%), COVID 19 (10%), diarrhea (5%), pneumonitis/ILD (4.8%), fatigue (3.9%), hyperglycemia (3.6%), increased ALT (3%) and pruritus (2.5%). Adverse reactions leading to dose reduction of PADCEV occurred in 42% of patients.

PADCEV的不良反应包括周围神经病变（22%）、皮疹（16%）、新冠肺炎（10%）、腹泻（5%）、肺炎/间质性肺病（4.8%）、疲劳（3.9%）、高血糖（3.6%）、ALT升高（3%）和瘙痒（2.5%）。导致PADCEV剂量减少的不良反应发生在42%的患者中。

The most common adverse reactions (≥2%) leading to dose reduction

导致剂量减少的最常见不良反应（≥2%）

of PADCEV were rash (16%), PN (13%) and fatigue (2.7%).

PADCEV的不良反应包括皮疹（16%）、周围神经病变（13%）和疲劳（2.7%）。

EV-103 Study: 121 patients with previously untreated la/mUC who were not eligible for cisplatin-containing chemotherapy (PADCEV in combination with pembrolizumab)

EV-103研究：121名既往未接受治疗的la/mUC患者，这些患者不符合使用含顺铂化疗的条件（PADCEV联合派姆单抗）。

Serious adverse reactions

严重的不良反应

occurred in 50% of patients treated with PADCEV in combination with pembrolizumab; the most common (≥2%) were acute kidney injury (7%), urinary tract infection (7%), urosepsis (5%), sepsis (3.3%), pneumonia (3.3%), hematuria (3.3%), pneumonitis/ILD (3.3%), urinary retention (2.5%), diarrhea (2.5%), myasthenia gravis (2.5%), myositis (2.5%), anemia (2.5%), and hypotension (2.5%).

在使用PADCEV联合派姆单抗治疗的患者中，发生了50%的不良反应；最常见的（≥2%）是急性肾损伤（7%）、尿路感染（7%）、尿脓毒症（5%）、败血症（3.3%）、肺炎（3.3%）、血尿（3.3%）、肺炎/间质性肺病（3.3%）、尿潴留（2.5%）、腹泻（2.5%）、重症肌无力（2.5%）、肌炎（2.5%）、贫血（2.5%）和低血压（2.5%）。

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Fatal adverse reactions

致命的不良反应

occurred in 5% of patients treated with PADCEV in combination with pembrolizumab, including sepsis (1.6%), bullous dermatitis (0.8%), myasthenia gravis (0.8%), and pneumonitis/ILD (0.8%).

在使用PADCEV联合派姆单抗治疗的患者中，有5%发生了以下情况，包括败血症（1.6%）、大疱性皮炎（0.8%）、重症肌无力（0.8%）以及肺炎/间质性肺病（0.8%）。

Adverse reactions leading to discontinuation

导致停药的不良反应

of PADCEV occurred in 36% of patients; the most common (≥2%) were PN (20%) and rash (6%).

在36%的患者中发生了PADCEV；最常见的（≥2%）是PN（20%）和皮疹（6%）。

Adverse reactions leading to dose

导致剂量的不良反应

interruption of PADCEV occurred in 69% of patients; the most common (≥2%) were PN (18%), rash (12%), increased lipase (6%), pneumonitis/ILD (6%), diarrhea (4.1%), acute kidney injury (3.3%), increased ALT (3.3%), fatigue (3.3%), neutropenia (3.3%), urinary tract infection (3.3%), increased amylase (2.5%), anemia (2.5%), COVID 19 (2.5%), hyperglycemia (2.5%), and hypotension (2.5%).

PADCEV中断发生在69%的患者中；最常见的（≥2%）是周围神经病变（18%）、皮疹（12%）、脂肪酶升高（6%）、肺炎/间质性肺病（6%）、腹泻（4.1%）、急性肾损伤（3.3%）、ALT升高（3.3%）、疲劳（3.3%）、中性粒细胞减少（3.3%）、尿路感染（3.3%）、淀粉酶升高（2.5%）、贫血（2.5%）、COVID-19（2.5%）、高血糖（2.5%）和低血压（2.5%）。

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Adverse reactions leading to dose reduction

导致剂量减少的不良反应

of PADCEV occurred in 45% of patients; the most common (≥2%) were PN (17%), rash (12%), fatigue (5%), neutropenia (5%), and diarrhea (4.1%).

PADCEV的发生率为45%；最常见的（≥2%）是周围神经病变（17%）、皮疹（12%）、疲劳（5%）、中性粒细胞减少（5%）和腹泻（4.1%）。

EV-301 Study: 296 patients previously treated with a PD-1/L1 inhibitor and platinum-based chemotherapy (PADCEV monotherapy)

EV-301研究：296名既往接受过PD-1/L1抑制剂和铂类化疗的患者（PADCEV单药治疗）

Serious adverse reactions

严重的不良反应

occurred in 47% of patients treated with PADCEV; the most common (≥2%) were urinary tract infection, acute kidney injury (7% each), and pneumonia (5%).

接受PADCEV治疗的患者中有47%发生；最常见的（≥2%）是尿路感染、急性肾损伤（各占7%）和肺炎（5%）。

Fatal adverse reactions

致命的不良反应

occurred in 3% of patients, including multiorgan dysfunction (1%), hepatic dysfunction, septic shock, hyperglycemia, pneumonitis/ILD, and pelvic abscess (0.3% each).

发生在3%的患者中，包括多器官功能障碍（1%）、肝功能障碍、感染性休克、高血糖、肺炎/间质性肺病和盆腔脓肿（各0.3%）。

Adverse reactions leading to discontinuation

导致停药的不良反应

occurred in 17% of patients; the most common (≥2%) were PN (5%) and rash (4%).

发生在17%的患者中；最常见的（≥2%）是PN（5%）和皮疹（4%）。

Adverse reactions leading to dose interruption

导致剂量中断的不良反应

occurred in 61% of patients; the most common (≥4%) were PN (23%), rash (11%), and fatigue (9%).

61%的患者出现；最常见的（≥4%）是PN（23%）、皮疹（11%）和疲劳（9%）。

Adverse reactions leading to dose reduction

导致剂量减少的不良反应

occurred in 34% of patients; the most common (≥2%) were PN (10%), rash (8%), decreased appetite, and fatigue (3% each).

34%的患者中发生；最常见的（≥2%）是PN（10%）、皮疹（8%）、食欲减退和疲劳（各3%）。

EV-201, Cohort 2 Study: 89 patients previously treated with a PD-1/L1 inhibitor and not eligible for cisplatin-based chemotherapy (PADCEV monotherapy)

EV-201，队列2研究：89名先前接受过PD-1/L1抑制剂治疗且不符合顺铂化疗条件的患者（PADCEV单药治疗）

Serious adverse reactions

严重的不良反应

occurred in 39% of patients treated with PADCEV; the most common (≥3%) were pneumonia, sepsis, and diarrhea (5% each).

接受 PADCEV 治疗的患者中有 39% 出现了该情况；其中最常见的（≥3%）是肺炎、败血症和腹泻（各占 5%）。

Fatal adverse

致命的不利因素

reactions occurred in 8% of patients, including acute kidney injury (2.2%), metabolic acidosis, sepsis, multiorgan dysfunction, pneumonia, and pneumonitis/ILD (1.1% each).

8%的患者出现了反应，包括急性肾损伤（2.2%）、代谢性酸中毒、败血症、多器官功能障碍、肺炎和肺炎/间质性肺病（各1.1%）。

Adverse reactions leading to discontinuation

导致停药的不良反应

occurred in 20% of patients; the most common (≥2%) was PN (7%).

发生在20%的患者中；最常见的（≥2%）是PN（7%）。

Adverse reactions leading to dose interruption

导致剂量中断的不良反应

occurred in 60% of patients; the most common (≥3%) were PN (19%), rash (9%), fatigue (8%), diarrhea (5%), increased AST, and hyperglycemia (3% each).

发生在60%的患者中；最常见的（≥3%）是PN（19%）、皮疹（9%）、疲劳（8%）、腹泻（5%）、AST升高和高血糖（各3%）。

Adverse reactions leading to dose reduction

导致剂量减少的不良反应

occurred in 49% of patients; the most common (≥3%) were PN (19%), rash (11%), and fatigue (7%).

发生在49%的患者中；最常见的（≥3%）是PN（19%）、皮疹（11%）和疲劳（7%）。

DRUG INTERACTIONS

药物相互作用

Effects of other drugs on PADCEV

其他药物对PADCEV的影响

(

(

Dual P-gp and Strong CYP3A4 Inhibitors

双重P-糖蛋白和强效CYP3A4抑制剂

)

)

Concomitant use with dual P-gp and strong CYP3A4 inhibitors may increase unconjugated monomethyl auristatin E exposure, which may increase the incidence or severity of PADCEV toxicities. Closely monitor patients for signs of toxicity when PADCEV is given concomitantly with dual P-gp and strong CYP3A4 inhibitors..

同时使用双重P-gp和强效CYP3A4抑制剂可能会增加未结合的单甲基澳瑞他汀E的暴露量，这可能会增加PADCEV毒性的发生率或严重程度。当PADCEV与双重P-gp和强效CYP3A4抑制剂同时给药时，应密切监测患者的毒性迹象。

SPECIFIC POPULATIONS

特定人群

Lactation

泌乳

Advise lactating women not to breastfeed during treatment with PADCEV and for 3 weeks after the last dose.

告知哺乳期妇女在使用PADCEV治疗期间以及最后一剂后的3周内不要进行母乳喂养。

Hepatic impairment

肝功能不全

Avoid the use of PADCEV in patients with moderate or severe hepatic impairment.

避免在中度或重度肝功能不全的患者中使用PADCEV。

Full Prescribing Information

完整的处方信息

VYLOY Important Safety Information

VYLOY重要安全信息

Warnings and Precautions

警告和注意事项

Hypersensitivity reactions, including serious anaphylaxis reactions, and serious and fatal infusion-related reactions (IRR)

超敏反应，包括严重的过敏反应，以及严重和致命的输液相关反应 (IRR)

have been reported in clinical studies when VYLOY has been administered.

在临床研究中，当VYLOY被施用时已被报告。

Any grade hypersensitivity reactions,

任何等级的超敏反应，

including anaphylactic reactions, occurring with VYLOY in combination with mFOLFOX6 or CAPOX was 18%.

包括与VYLOY联合mFOLFOX6或CAPOX使用时发生的过敏反应在内，发生率为18%。

Severe (Grade 3 or 4) hypersensitivity reactions,

严重（3级或4级）超敏反应，

including anaphylactic reactions, occurred in 2% of patients. Seven patients (1.3%) permanently discontinued VYLOY for hypersensitivity reactions, including two patients (0.4%) who permanently discontinued VYLOY due to anaphylactic reactions. Seventeen (3.2%) patients required dose interruption, and three patients (0.6%) required infusion rate reduction due to hypersensitivity reactions.

包括过敏反应在内的不良反应发生在2%的患者中。七名患者（1.3%）因超敏反应永久停用VYLOY，其中两名患者（0.4%）因过敏反应永久停用VYLOY。十七名（3.2%）患者需要中断剂量，三名患者（0.6%）因超敏反应需要降低输注速度。

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All grade IRRs

所有等级的IRR

occurred in 3.2% in patients administered VYLOY in combination with mFOLFOX6 or CAPOX. Severe (Grade 3) IRRs occurred in 2 (0.4%) patients who received VYLOY. An IRR led to permanent discontinuation of VYLOY in 2 (0.4%) patients and dose interruption in 7 (1.3%) patients. The infusion rate was reduced for VYLOY for 2 (0.4%) patients due to an IRR.

在接受VYLOY联合mFOLFOX6或CAPOX治疗的患者中，3.2%发生了输注相关反应（IRR）。重度（3级）IRR发生在2名（0.4%）接受VYLOY治疗的患者中。因IRR导致2名（0.4%）患者永久停用VYLOY，7名（1.3%）患者中断用药剂量。因IRR，2名（0.4%）患者的VYLOY输注速率被降低。

Monitor patients during infusion with VYLOY and for 2 hours after completion of infusion or longer if clinically indicated, for hypersensitivity reactions with symptoms and signs that are highly suggestive of anaphylaxis (urticaria, repetitive cough, wheeze and throat tightness/change in voice). Monitor patients for signs and symptoms of IRRs including nausea, vomiting, abdominal pain, salivary hypersecretion, pyrexia, chest discomfort, chills, back pain, cough and hypertension.

在输注VYLOY期间以及输注完成后2小时内（或根据临床需要更长时间）监测患者是否出现过敏反应，特别是高度提示过敏性休克的症状和体征（如荨麻疹、反复咳嗽、喘息和喉咙紧缩/声音改变）。监测患者是否出现包括恶心、呕吐、腹痛、唾液分泌过多、发热、胸部不适、寒战、背痛、咳嗽和高血压在内的输注相关反应的症状和体征。

If a severe or life-threatening hypersensitivity or IRR reaction occurs, discontinue VYLOY permanently, treat symptoms according to standard medical care, and monitor until symptoms resolve. For any Grade 2 hypersensitivity or IRR, interrupt the VYLOY infusion until Grade ≤1, then resume at a reduced infusion rate for the remaining infusion.

如果发生严重或危及生命的超敏反应或IRR反应，应永久停止使用VYLOY，按照标准医疗护理治疗症状，并监测直至症状消退。对于任何2级超敏反应或IRR，中断VYLOY输注直至降至1级或以下，然后以降低的输注速率恢复剩余输注。

Follow Grade 2 management for Grade 3 infusion-related nausea and vomiting. Premedicate the patient with antihistamines for the subsequent infusions, and closely monitor the patient for symptoms and signs of a hypersensitivity reaction. The infusion rate may be gradually increased as tolerated..

对于3级输液相关的恶心和呕吐，按照2级管理进行处理。在后续输液前，使用抗组胺药对患者进行预处理，并密切监测患者是否出现超敏反应的症状和体征。根据患者的耐受情况，可以逐渐提高输液速度。

Severe Nausea and Vomiting.

严重恶心和呕吐。

VYLOY is emetogenic. Nausea and vomiting occurred more often during the first cycle of treatment.

VYLOY具有致吐性。在第一个治疗周期中，恶心和呕吐发生得更为频繁。

All grade nausea and vomiting

所有级别的恶心和呕吐

occurred in 82% and 67% respectively of patients treated with VYLOY in combination with mFOLFOX6 and 69% and 66% in combination with CAPOX, respectively.

分别发生在接受VYLOY联合mFOLFOX6治疗的患者中的82%和67%，以及联合CAPOX治疗的患者中的69%和66%。

Severe (Grade 3) nausea

重度（3级）恶心

occurred in 16% and 9% of patients treated with VYLOY in combination with mFOLFOX6 or CAPOX respectively.

在接受VYLOY联合mFOLFOX6或CAPOX治疗的患者中，分别有16%和9%的患者发生了该情况。

Severe (Grade 3) vomiting

严重（3级）呕吐

occurred in 16% and 12% of patients treated with VYLOY in combination with mFOLFOX6 or CAPOX. Nausea led to permanent discontinuation of VYLOY in combination with mFOLFOX6 or CAPOX in 18 (3.4%) patients and dose interruption in 147 (28%) patients. Vomiting led to permanent discontinuation of VYLOY in combination with mFOLFOX6 or CAPOX in 20 (3.8%) patients and dose interruption in 150 (28%) patients.

在接受VYLOY联合mFOLFOX6或CAPOX治疗的患者中，分别有16%和12%的患者发生了不良反应。恶心导致18名（3.4%）患者永久停用VYLOY联合mFOLFOX6或CAPOX，147名（28%）患者中断用药。呕吐导致20名（3.8%）患者永久停用VYLOY联合mFOLFOX6或CAPOX，150名（28%）患者中断用药。

Pretreat with antiemetics prior to each infusion of VYLOY. Manage patients during and after infusion with antiemetics or fluid replacement. Interrupt the infusion, or permanently discontinue VYLOY based on severity..

在每次输注VYLOY前预先使用止吐药。在输注期间及之后，使用止吐药或补液管理患者。根据严重程度，中断输注或永久停止使用VYLOY。

ADVERSE REACTIONS

不良反应

Most common adverse reactions (≥15%):

最常见的不良反应（≥15%）：

Nausea, vomiting, fatigue, decreased appetite, diarrhea, peripheral sensory neuropathy, abdominal pain, constipation, decreased weight, hypersensitivity reactions, and pyrexia.

恶心、呕吐、疲劳、食欲减退、腹泻、外周感觉神经病变、腹痛、便秘、体重减轻、超敏反应和发热。

Most common laboratory abnormalities (≥15%):

最常见的实验室异常（≥15%）：

Decreased neutrophil count, decreased leucocyte count, decreased albumin, increased creatinine, decreased hemoglobin, increased glucose, decreased lymphocyte count, increased aspartate aminotransferase, decreased platelets, increased alkaline phosphatase, increased alanine aminotransferase, decreased glucose, decreased sodium, increased phosphate, decreased potassium, and decreased magnesium..

中性粒细胞计数减少，白细胞计数减少，白蛋白减少，肌酐增加，血红蛋白减少，葡萄糖增加，淋巴细胞计数减少，天冬氨酸氨基转移酶增加，血小板减少，碱性磷酸酶增加，丙氨酸氨基转移酶增加，葡萄糖减少，钠减少，磷增加，钾减少，镁减少。

SPOTLIGHT Study: 279 patients with locally advanced unresectable or metastatic HER2-negative gastric or GEJ adenocarcinoma whose tumors were CLDN18.2 positive who received at least one dose of VYLOY in combination with mFOLFOX6

聚光灯研究：279名局部晚期不可切除或转移性HER2阴性的胃或胃食管结合部腺癌患者，其肿瘤为CLDN18.2阳性，并接受至少一剂VYLOY联合mFOLFOX6治疗。

Serious adverse reactions occurred in 45% of patients treated with VYLOY in combination with mFOLFOX6; the

接受VYLOY联合mFOLFOX6治疗的患者中有45%发生了严重不良反应；

most common serious adverse reactions

最常见的严重不良反应

(≥2%) were vomiting (8%), nausea (7%), neutropenia (2.9%), febrile neutropenia (2.9%), diarrhea (2.9%), intestinal obstruction (3.2%), pyrexia (2.5%), pneumonia (2.5%), respiratory failure (2.2%), pulmonary embolism (2.2%), decreased appetite (2.1%) and sepsis (2.0%).

(≥2%) 的患者出现呕吐 (8%)、恶心 (7%)、中性粒细胞减少 (2.9%)、发热性中性粒细胞减少 (2.9%)、腹泻 (2.9%)、肠梗阻 (3.2%)、发热 (2.5%)、肺炎 (2.5%)、呼吸衰竭 (2.2%)、肺栓塞 (2.2%)、食欲减退 (2.1%) 和败血症 (2.0%)。

Fatal adverse reactions

致命的不良反应

occurred in 5% of patients who received VYLOY in combination with mFOLFOX6 including sepsis (1.4%), pneumonia (1.1%), respiratory failure (1.1%), intestinal obstruction (0.7%), acute hepatic failure (0.4%), acute myocardial infarction (0.4%), death (0.4%), disseminated intravascular coagulation (0.4%), encephalopathy (0.4%), and upper gastrointestinal hemorrhage (0.4%).

在接受VYLOY联合mFOLFOX6治疗的患者中，5%的患者出现了以下情况，包括败血症（1.4%）、肺炎（1.1%）、呼吸衰竭（1.1%）、肠梗阻（0.7%）、急性肝衰竭（0.4%）、急性心肌梗死（0.4%）、死亡（0.4%）、弥散性血管内凝血（0.4%）、脑病（0.4%）以及上消化道出血（0.4%）。

Permanent discontinuation of VYLOY due to an adverse reaction occurred in 20% of patients; the .

由于不良反应而永久停用VYLOY的情况发生在20%的患者中；

most common adverse reactions leading to discontinuation

最常见的导致停药的不良反应

(≥2%) were nausea and vomiting. Dosage interruptions of VYLOY due to an adverse reaction occurred in 75% of patients; the

(≥2%)为恶心和呕吐。由于不良反应导致VYLOY剂量中断的情况发生在75%的患者中；

most common adverse reactions leading to dose interruption

最常见的导致剂量中断的不良反应

(≥5%) were nausea, vomiting, neutropenia, abdominal pain, fatigue, and hypertension.

(≥5%)为恶心、呕吐、中性粒细胞减少、腹痛、疲劳和高血压。

GLOW Study: 254 patients with locally advanced unresectable or metastatic HER2-negative gastric or GEJ adenocarcinoma whose tumors were CLDN18.2 positive who received at least one dose of VYLOY in combination with CAPOX

GLOW研究：254名局部晚期不可切除或转移性HER2阴性的胃或胃食管结合部腺癌患者，其肿瘤为CLDN18.2阳性，并接受了至少一剂VYLOY联合CAPOX治疗。

Serious adverse reactions occurred in 47% of patients treated with VYLOY in combination with CAPOX; the

接受VYLOY联合CAPOX治疗的患者中有47%发生了严重不良反应；

most common serious adverse reactions

最常见的严重不良反应

(≥2%) were vomiting (6%), nausea (4.3%), decreased appetite (3.9%), decreased platelet count (3.1%), upper gastrointestinal hemorrhage (2.8%), diarrhea (2.8%), pneumonia (2.4%), pulmonary embolism (2.3%), and pyrexia (2.0%).

(≥2%) 为呕吐 (6%)、恶心 (4.3%)、食欲减退 (3.9%)、血小板计数减少 (3.1%)、上消化道出血 (2.8%)、腹泻 (2.8%)、肺炎 (2.4%)、肺栓塞 (2.3%) 和发热 (2.0%)。

Fatal adverse reactions

致命的不良反应

occurred in 8% of patients who received VYLOY in combination with CAPOX including sepsis (1.2%), pneumonia (0.4%), death (0.8%), upper gastrointestinal hemorrhage (0.8%), cerebral hemorrhage (0.8%), abdominal infection (0.4%), acute respiratory distress syndrome (0.4%), cardio-respiratory arrest (0.4%), decreased platelet count (0.4%), disseminated intravascular coagulation (0.4%), dyspnea (0.4%), gastric perforation (0.4%), hemorrhagic ascites (0.4%), procedural complication (0.4%), sudden death (0.4%), and syncope (0.4%).

在接受VYLOY联合CAPOX治疗的患者中，有8%发生了以下不良事件，包括败血症（1.2%）、肺炎（0.4%）、死亡（0.8%）、上消化道出血（0.8%）、脑出血（0.8%）、腹部感染（0.4%）、急性呼吸窘迫综合征（0.4%）、心肺骤停（0.4%）、血小板减少（0.4%）、弥散性血管内凝血（0.4%）、呼吸困难（0.4%）、胃穿孔（0.4%）、出血性腹水（0.4%）、手术并发症（0.4%）、猝死（0.4%）和晕厥（0.4%）。

Permanent discontinuation of VYLOY due to an adverse reaction occurred in 19% of patients; the .

由于不良反应，19%的患者永久停用了VYLOY；

most common adverse reaction leading to discontinuation

最常见的导致停药的不良反应

(≥2%) was vomiting. Dosage interruption of VYLOY due to an adverse reaction occurred in 55% of patients; the

(≥2%)为呕吐。因不良反应导致VYLOY剂量中断的情况发生在55%的患者中；

most common adverse reactions leading to dose interruption

最常见的导致剂量中断的不良反应

(≥2%) were nausea, vomiting, neutropenia, thrombocytopenia, anemia, fatigue, infusion-related reaction, and abdominal pain.

(≥2%) 为恶心、呕吐、中性粒细胞减少、血小板减少、贫血、疲劳、输液相关反应和腹痛。

SPECIFIC POPULATIONS

特定人群

Lactation

泌乳

Advise lactating women not to breastfeed during treatment with VYLOY and for 8 months after the last dose.

告知哺乳期妇女在使用VYLOY治疗期间及最后一剂后8个月内不要进行母乳喂养。

Full Prescribing Information

完整处方信息

XOSPATA Important Safety Information

XOSPATA重要安全信息

Contraindications

禁忌症

XOSPATA is contraindicated in patients with hypersensitivity to gilteritinib or any of the excipients. Anaphylactic reactions have been observed in clinical trials.

XOSPATA禁用于对吉列替尼或任何辅料过敏的患者。在临床试验中已观察到过敏反应。

Warnings and Precautions

警告和注意事项

Differentiation Syndrome

分化综合征

(See BOXED WARNING) 3% of 319 patients treated with XOSPATA in the clinical trials experienced differentiation syndrome. Differentiation syndrome is associated with rapid proliferation and differentiation of myeloid cells and may be life-threatening or fatal if not treated. Symptoms and other clinical findings of differentiation syndrome in patients treated with XOSPATA included fever, dyspnea, pleural effusion, pericardial effusion, pulmonary edema, hypotension, rapid weight gain, peripheral edema, rash, and renal dysfunction.

（见方框警告）在临床试验中，319名接受XOSPATA治疗的患者中有3%出现了分化综合征。分化综合征与髓样细胞的快速增殖和分化有关，如果不治疗可能危及生命或致命。接受XOSPATA治疗的患者中分化综合征的症状和其他临床表现包括发热、呼吸困难、胸腔积液、心包积液、肺水肿、低血压、体重迅速增加、外周水肿、皮疹和肾功能障碍。

Some cases had concomitant acute febrile neutrophilic dermatosis. Differentiation syndrome occurred as early as 1 day and up to 82 days after XOSPATA initiation and has been observed with or without concomitant leukocytosis. If differentiation syndrome is suspected, initiate dexamethasone 10 mg IV every 12 hours (or an equivalent dose of an alternative oral or IV corticosteroid) and hemodynamic monitoring until improvement.

一些病例同时出现急性发热性中性粒细胞性皮肤病。分化综合征最早可在使用XOSPATA后1天，最晚在82天内发生，并且无论是否伴随白细胞增多均有观察到。如果怀疑出现分化综合征，应每12小时静脉注射10毫克地塞米松（或等效剂量的其他口服或静脉注射皮质类固醇），并进行血流动力学监测，直至病情改善。

Taper corticosteroids after resolution of symptoms and administer corticosteroids for a minimum of 3 days. Symptoms of differentiation syndrome may recur with premature discontinuation of corticosteroid treatment. If severe signs and/or symptoms persist for more than 48 hours after initiation of corticosteroids, interrupt XOSPATA until signs and symptoms are no longer severe..

在症状消退后逐渐减少皮质类固醇的用量，并至少连续使用皮质类固醇3天。如果过早停止皮质类固醇治疗，分化综合征的症状可能会复发。如果在开始使用皮质类固醇后严重症状和/或体征持续超过48小时，应中断XOSPATA的使用，直至严重症状和体征不再存在。

Posterior Reversible Encephalopathy Syndrome (PRES)

后部可逆性脑病综合征 (PRES)

1% of 319 patients treated with XOSPATA in the clinical trials experienced posterior reversible encephalopathy syndrome (PRES) with symptoms including seizure and altered mental status. Symptoms have resolved after discontinuation of XOSPATA. A diagnosis of PRES requires confirmation by brain imaging, preferably magnetic resonance imaging (MRI).

在临床试验中，接受XOSPATA治疗的319名患者中有1%出现了后部可逆性脑病综合征（PRES），症状包括癫痫发作和意识状态改变。停用XOSPATA后症状已缓解。确诊PRES需要通过脑成像检查，最好采用磁共振成像（MRI）。

Discontinue XOSPATA in patients who develop PRES..

在出现PRES的患者中停用XOSPATA。

Prolonged QT Interval

QT间期延长

XOSPATA has been associated with prolonged cardiac ventricular repolarization (QT interval). 1% of the 317 patients with a post-baseline QTc measurement on treatment with XOSPATA in the clinical trial were found to have a QTc interval greater than 500 msec and 7% of patients had an increase from baseline QTc greater than 60 msec.

XOSPATA 与心脏心室复极延长（QT 间期）有关。在临床试验中，317 名接受 XOSPATA 治疗后进行基线后 QTc 测量的患者中，有 1% 的患者 QTc 间期超过 500 毫秒，7% 的患者基线 QTc 增加超过 60 毫秒。

Perform electrocardiogram (ECG) prior to initiation of treatment with XOSPATA, on days 8 and 15 of cycle 1, and prior to the start of the next two subsequent cycles. Interrupt and reduce XOSPATA dosage in patients who have a QTcF >500 msec. Hypokalemia or hypomagnesemia may increase the QT prolongation risk.

在开始使用XOSPATA治疗之前，第1周期的第8天和第15天，以及接下来两个周期开始前进行心电图（ECG）检查。对于QTcF >500毫秒的患者，应中断并减少XOSPATA的剂量。低钾血症或低镁血症可能会增加QT间期延长的风险。

Correct hypokalemia or hypomagnesemia prior to and during XOSPATA administration..

在使用XOSPATA之前和期间，纠正低钾血症或低镁血症。

Pancreatitis

胰腺炎

4% of 319 patients treated with XOSPATA in the clinical trials experienced pancreatitis. Evaluate patients who develop signs and symptoms of pancreatitis. Interrupt and reduce the dose of XOSPATA in patients who develop pancreatitis.

在临床试验中，接受XOSPATA治疗的319名患者中有4%出现胰腺炎。对出现胰腺炎迹象和症状的患者进行评估。对于发生胰腺炎的患者，应中断并减少XOSPATA的剂量。

Embryo-Fetal Toxicity

胚胎-胎儿毒性

XOSPATA can cause embryo-fetal harm when administered to a pregnant woman. Advise females of reproductive potential to use effective contraception during treatment with XOSPATA and for 6 months after the last dose of XOSPATA. Advise males with female partners of reproductive potential to use effective contraception during treatment with XOSPATA and for 4 months after the last dose of XOSPATA.

XOSPATA 在给予孕妇时可能造成胚胎-胎儿伤害。建议具有生殖潜力的女性在使用 XOSPATA 治疗期间以及最后一次服用 XOSPATA 后的 6 个月内使用有效的避孕措施。建议有具生殖潜力女性伴侣的男性在使用 XOSPATA 治疗期间以及最后一次服用 XOSPATA 后的 4 个月内使用有效的避孕措施。

Pregnant women, patients becoming pregnant while receiving XOSPATA or male patients with pregnant female partners should be apprised of the potential risk to the fetus..

接受XOSPATA治疗期间怀孕的孕妇、患者或有怀孕女性伴侣的男性患者应被告知对胎儿的潜在风险。

Adverse Reactions

不良反应

Fatal adverse reactions occurred in 2% of patients receiving XOSPATA. These were cardiac arrest (1%) and one case each of differentiation syndrome and pancreatitis. The most frequent (≥5%) nonhematological serious adverse reactions reported in patients were fever (13%), dyspnea (9%), renal impairment (8%), transaminase increased (6%) and noninfectious diarrhea (5%)..

在接受XOSPATA治疗的患者中，2%的患者发生了致命的不良反应。其中心脏骤停（1%），还有一例分化综合征和一例胰腺炎。患者中最常见（≥5%）的非血液学严重不良反应为发热（13%）、呼吸困难（9%）、肾功能损害（8%）、转氨酶升高（6%）以及非感染性腹泻（5%）。

7% discontinued XOSPATA treatment permanently due to an adverse reaction. The most common (>1%) adverse reactions leading to discontinuation were aspartate aminotransferase increased (2%) and alanine aminotransferase increased (2%).

7%的患者因不良反应永久停止了XOSPATA治疗。导致停药的最常见（>1%）不良反应为天门冬氨酸氨基转移酶升高（2%）和丙氨酸氨基转移酶升高（2%）。

The most frequent (≥5%) grade ≥3 nonhematological adverse reactions reported in patients were transaminase increased (21%), dyspnea (12%), hypotension (7%), mucositis (7%), myalgia/arthralgia (7%), and fatigue/malaise (6%).

患者中报告的最常见的（≥5%）3级或以上非血液学不良反应为转氨酶升高（21%）、呼吸困难（12%）、低血压（7%）、口腔炎（7%）、肌痛/关节痛（7%）以及疲劳/不适（6%）。

Other clinically significant adverse reactions occurring in ≤10% of patients included: electrocardiogram QT prolonged (9%), hypersensitivity (8%), pancreatitis (5%), cardiac failure (4%), pericardial effusion (4%), acute febrile neutrophilic dermatosis (3%), differentiation syndrome (3%), pericarditis/myocarditis (2%), large intestine perforation (1%), and posterior reversible encephalopathy syndrome (1%)..

其他在≤10%的患者中发生的临床显著不良反应包括：心电图QT间期延长（9%）、超敏反应（8%）、胰腺炎（5%）、心力衰竭（4%）、心包积液（4%）、急性发热性中性粒细胞性皮病（3%）、分化综合征（3%）、心包炎/心肌炎（2%）、大肠穿孔（1%）以及后部可逆性脑病综合征（1%）。

Lab Abnormalities Shifts to grades 3-4 nonhematologic laboratory abnormalities in XOSPATA treated patients included phosphate decreased (14%), alanine aminotransferase increased (13%), sodium decreased (12%), aspartate aminotransferase increased (10%), calcium decreased (6%), creatine kinase increased (6%), triglycerides increased (6%), creatinine increased (3%), and alkaline phosphatase increased (2%)..

实验室异常：在使用XOSPATA治疗的患者中，转为3-4级的非血液学实验室异常包括磷酸盐减少（14%）、丙氨酸氨基转移酶升高（13%）、钠减少（12%）、天冬氨酸氨基转移酶升高（10%）、钙减少（6%）、肌酸激酶升高（6%）、甘油三酯升高（6%）、肌酐升高（3%）以及碱性磷酸酶升高（2%）。

Drug Interactions

药物相互作用

Combined P-gp and Strong CYP3A Inducers Concomitant use of XOSPATA with a combined P-gp and strong CYP3A inducer decreases XOSPATA exposure which may decrease XOSPATA efficacy. Avoid concomitant use of XOSPATA with combined P-gp and strong CYP3A inducers.

联合P-gp和强CYP3A诱导剂同时使用XOSPATA与联合P-gp和强CYP3A诱导剂会降低XOSPATA的暴露量，这可能会降低XOSPATA的疗效。避免同时使用XOSPATA与联合P-gp和强CYP3A诱导剂。

Strong CYP3A inhibitors Concomitant use of XOSPATA with a strong CYP3A inhibitor increases XOSPATA exposure. Consider alternative therapies that are not strong CYP3A inhibitors. If the concomitant use of these inhibitors is considered essential for the care of the patient, monitor patient more frequently for XOSPATA adverse reactions.

强效CYP3A抑制剂：XOSPATA与强效CYP3A抑制剂同时使用会增加XOSPATA的暴露量。考虑使用非强效CYP3A抑制剂的替代疗法。如果这些抑制剂的同时使用被认为对患者的治疗至关重要，则应更频繁地监测患者是否出现XOSPATA不良反应。

Interrupt and reduce XOSPATA dosage in patients with serious or life-threatening toxicity..

严重或危及生命的毒性患者应中断并减少XOSPATA剂量。

Drugs that Target 5HT2B Receptor or Sigma Nonspecific Receptor Concomitant use of XOSPATA may reduce the effects of drugs that target the 5HT2B receptor or the sigma nonspecific receptor (e.g., escitalopram, fluoxetine, sertraline). Avoid concomitant use of these drugs with XOSPATA unless their use is considered essential for the care of the patient..

针对5HT2B受体或Sigma非特异性受体的药物：同时使用XOSPATA可能会降低针对5HT2B受体或Sigma非特异性受体的药物（如艾司西酞普兰、氟西汀、舍曲林）的效果。除非认为这些药物对患者的治疗至关重要，否则应避免与XOSPATA同时使用。

P-gp, BCRP, and OCT1 Substrates Based on

基于P-gp、BCRP和OCT1的底物

in vitro

体外

data, gilteritinib is a P-gp, breast cancer resistant protein (BCRP), and organic cation transporter 1 (OCT1) inhibitor. Coadministration of gilteritinib may increase the exposure of P-gp, BCRP, and OCT1 substrates, which may increase the incidence and severity of adverse reactions of these substrates.

数据表明，吉列替尼是一种P-糖蛋白（P-gp）、乳腺癌耐药蛋白（BCRP）和有机阳离子转运体1（OCT1）抑制剂。吉列替尼的共同给药可能会增加P-gp、BCRP和OCT1底物的暴露量，这可能会增加这些底物不良反应的发生率和严重程度。

For P-gp, BCRP, or OCT1 substrates where small concentration changes may lead to serious adverse reactions, decrease the dose or modify the dosing frequency of such substrate and monitor for adverse reactions as recommended in the respective prescribing information..

对于P-gp、BCRP或OCT1底物，若小的浓度变化可能导致严重不良反应，应减少此类底物的剂量或调整给药频率，并按照各自处方信息中的建议监测不良反应。

Specific Populations

特定人群

Lactation Advise women not to breastfeed during treatment with XOSPATA and for 2 months after the last dose.

哺乳建议女性在使用XOSPATA治疗期间以及最后一剂后的2个月内不要进行母乳喂养。

Full Prescribing Information

完整处方信息

Cautionary Notes

注意事项

In this press release, statements made with respect to current plans, estimates, strategies and beliefs and other statements that are not historical facts are forward-looking statements about the future performance of Astellas. These statements are based on management’s current assumptions and beliefs in light of the information currently available to it and involve known and unknown risks and uncertainties.

本新闻稿中，有关当前计划、估算、策略和信念的陈述以及其他非历史事实的陈述是关于安斯泰来未来业绩的前瞻性陈述。这些陈述基于管理层当前的假设和信念，并结合其目前可获得的信息，涉及已知和未知的风险与不确定性。

A number of factors could cause actual results to differ materially from those discussed in the forward-looking statements. Such factors include, but are not limited to: (i) changes in general economic conditions and in laws and regulations, relating to pharmaceutical markets, (ii) currency exchange rate fluctuations, (iii) delays in new product launches, (iv) the inability of Astellas to market existing and new products effectively, (v) the inability of Astellas to continue to effectively research and develop products accepted by customers in highly competitive markets, and (vi) infringements of Astellas’ intellectual property rights by third parties.

可能导致实际结果与前瞻性陈述中讨论的结果存在重大差异的因素包括但不限于：(i) 与医药市场相关的总体经济状况、法律法规的变化，(ii) 汇率波动，(iii) 新产品上市的延迟，(iv) 安斯泰来无法有效营销现有和新产品，(v) 安斯泰来无法在竞争激烈的市场中继续有效研发客户认可的产品，以及 (vi) 第三方侵犯安斯泰来的知识产权。

Information about pharmaceutical products (including products currently in development) which is included in this press release is not intended to constitute an advertisement or medical advice..

本新闻稿中包含的关于药品（包括正在开发中的产品）的信息并非旨在构成广告或医疗建议。

Click below for a copy of the full press release

点击下方获取完整新闻稿的副本