This phase I trial evaluates the effects of apalutamide, compared to placebo, on epidermal growth factor receptor (EGFR) protein expression in patients with non-muscle invasive bladder cancer. Apalutamide is in a class of medications called androgen receptor inhibitors. It works by blocking the effects of androgen (a male reproductive hormone) to stop the growth and spread of tumor cells. Previous studies have suggested that expression of a protein called EGFR on tumor cells is related to bladder cancer disease progression. This trial may help doctors evaluate if apalutamide has any effect on EGFR expression in patients with non-muscle invasive bladder cancer.

开始日期2025-04-23

申办/合作机构

National Cancer Institute

NCT06592924

/ Not yet recruiting临床3期IIT

A Randomized Clinical Trial for the Addition of Docetaxel to Androgen Receptor Pathway Inhibitors in Patients With Metastatic Castration Sensitive Prostate Cancer Without Deep PSA Response

This study is being done to answer the following question: can the chance of prostate cancer growing or spreading be lowered by adding a drug to the usual combination of drugs?
This study would like to find out if this approach is better or worse than the usual approach for prostate cancer.
The usual approach for patients who are not in a study is hormone treatment with Androgen Deprivation Therapy (ADT) and Androgen-Receptor Pathway Inhibitor (ARPI).

开始日期2025-01-15

申办/合作机构

Canadian Cancer Trials Group

[+4]

CTR20244619

/ Active, not recruitingN/A

阿帕他胺片人体生物等效性试验

评价中国健康成年男性受试者餐后条件单次单剂量口服阿帕他胺片受试制剂（规格：60mg，杭州中美华东制药有限公司）和参比制剂（商品名：安森珂®，规格：60mg，Janssen-Cilag International NV）后的药代动力学特点和生物等效性。

开始日期2024-12-25

申办/合作机构

杭州中美华东制药有限公司

100 项与阿帕他胺相关的临床结果

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100 项与阿帕他胺相关的转化医学

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100 项与阿帕他胺相关的专利（医药）

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604

项与阿帕他胺相关的文献（医药）

2025-02-01·PROSTATE

Efficacy and Predictive Factors Analysis of Androgen Deprivation Plus Novel Hormone Therapy as Neoadjuvant Treatment for High‐Risk Prostate Cancer

Article

作者: Dong, Liang ; Tao, Hanyang ; Pan, Jiahua ; Du, Xinxing ; Li, Rui ; Wu, Fan ; Xue, Wei ; Dong, Baijun ; Zhu, Yinjie

ABSTRACT:

Background:

This investigation explored the clinical features, pathological outcomes, and biochemical recurrence (BCR) duration among high‐risk prostate cancer (HRPC) patients who have undergone neoadjuvant therapy (NAT) in combination with radical prostatectomy (RP) and pelvic lymph node dissection (PLND). Additionally, we identified prognostic indicators that discern pathological complete response (pCR) or minimal residual disease (MRD) and BCR.

Methods:

In total, we examined 76 HRPC patients, who received NAT with either androgen deprivation therapy (ADT) plus apalutamide or ADT plus abiraterone, with subsequent RP and PLND. We conducted a genetic evaluation of patients receiving neoadjuvant apalutamide. Additionally, patient pathological outcomes, circulating prostate‐specific antigen (PSA) response rates, and BCR duration were analyzed. Lastly, we employed uni‐ and multivariate analyses to screen for prognostic factors that govern pCR or MRD and BCR duration.

Results:

Patient median age and median PSA at presentation were 69 years (IQR: 66–73), and 47.6 ng/mL (IQR: 24.1–105.75), respectively. We observed marked changes in pCR or MRD rates between the two cohorts. In particular, the ADT plus apalutamide cohort (51.5%) exhibited enhanced rates relative to the ADT plus abiraterone cohort (25.6%) (p = 0.03). The median BCR duration was substantially prolonged among neoadjuvant apalutamide cohort relative to the neoadjuvant abiraterone cohort (261 days vs. 76 days, p = 0.04). Using multivariate analysis, we revealed that the postintervention pre‐RP PSA content (≤ 0.1 ng/mL vs. > 0.1 ng/mL) remained a substantial stand‐alone indicator of pCR or MRD (odds ratio: 10.712, 95% CI: 2.725–42.105, p < 0.001). Furthermore, supplemental analyses revealed that the ADT plus apalutamide cohort exhibited an augmented serum response rate, which, in turn, reduced the post‐intervention pre‐RP PSA content. Based on our genetic profiling of the neoadjuvant apalutamide cohort demonstrated high‐frequency deleterious changes in the AR axis (30.3%), followed by TP53 mutations (15.15%). Patients with defective AR axis experienced a remarkably shorter median BCR duration relative to patients with other or no genetic alterations (52.5 days vs. 286 and 336 days, respectively, p < 0.0001). Furthermore, using multivariate analysis, we demonstrated that achieving pCR or MRD (hazard ratio [HR]: 0.170, 95% CI: 0.061–0.477, p < 0.001) and presence of defective AR signaling (HR: 11.193, 95% CI: 3.499–35.806, p < 0.001) were strong stand‐alone indicators of BCR.

Conclusions:

Herein, we demonstrated the superior performance of ADT plus apalutamide in achieving pCR or MRD and in extending BCR duration among HRPC patients. Post‐intervention pre‐RP PSA content as well as genetic shifts, especially in the AR axis, are critical indicators of patient pathological and clinical outcomes. These findings highlight the significance of genetic testing and PSA content monitoring in treating HRPC patients.

2025-02-01·PROSTATE

Comparison of abiraterone, enzalutamide, and apalutamide for metastatic hormone‐sensitive prostate cancer: A multicenter study

Article

作者: Kimura, Takahiro ; Yanagisawa, Takafumi ; Urabe, Fumihiko ; Katsumi, Kouta ; Iwatani, Kosuke ; Tashiro, Kojiro ; Habuchi, Tomonori ; Takahashi, Hidetsugu ; Mori, Keiichiro ; Shimomura, Tatsuya ; Narita, Shintaro ; Hatakeyama, Shingo ; Muramoto, Katsuki ; Fukuokaya, Wataru

Abstract:

Purpose:

We aimed to assess the differential efficacy and safety of androgen receptor pathway inhibitors (ARPI), such as abiraterone, enzalutamide, and apalutamide, in patients with metastatic hormone‐sensitive prostate cancer (mHSPC) in a real‐world practice setting.

Methods:

We retrospectively reviewed the records of consequent 668 patients with mHSPC treated with ARPI plus androgen deprivation therapy between September 2015 and December 2023. Based on the LATITUDE criteria, the comparison among abiraterone, enzalutamide, and apalutamide was exclusively conducted in high‐risk patients. Prostate‐specific antigen (PSA) responses such as the achievement of 95% and 99% PSA decline, overall survival (OS), cancer‐specific survival (CSS), time to castration‐resistant prostate cancer (CRPC), and the incidence of adverse events (AEs) were compared. All two‐group comparisons relied on propensity score matching (PSM) to minimize the effect on possible confounders.

Results:

In total, 297 patients with high‐risk mHSPC treated with abiraterone, 127 with enzalutamide, and 142 with apalutamide were compared. There were no differences in time to CRPC (p = 0.13), OS (p = 0.7), and CSS (p = 0.5) among the three ARPIs. No differences were observed in the achievement rates for 95% PSA decline at 3 months among the three ARPIs, while abiraterone was significantly better in 99% PSA decline achievement compared to apalutamide (72% vs. 57%, p = 0.003). The aforementioned oncologic outcomes were sustained even when performing PSM analyzes. Although skin rash for APA (34%) was the highest incidence of AEs, there were no differences in the rates of severe AEs across the three ARPIs. Enzalutamide resulted in the lowest treatment discontinuation rates (10%) other than disease progression compared to the other regimens.

Conclusions:

Abiraterone, enzalutamide, and apalutamide have comparable oncologic outcomes in terms of OS, CSS, and time to CRPC in patients with high‐risk mHSPC. Our data on differential treatment discontinuation rates, PSA response, and AE profiles can help guide clinical decision‐making.

2025-02-01·International Journal of Clinical Pharmacy

Disproportionality analysis of flutamide- or bicalutamide-induced liver injury with and without steroids by using the Japanese Adverse Drug Event Report database

Article

作者: Kato, Ryuji ; Tanaka, Saori ; Yamada, Tomoyuki ; Fujimoto, Ayumi ; Kohda, Yuka ; Noda, Takumi ; Urashima, Kazuya

BACKGROUND:

Although the mechanism underlying flutamide- or bicalutamide-induced liver injury may be immune related, the details remain unclear. If this mechanism is immune related, steroid use may be considered as a treatment option.

AIM:

Disproportionality analysis was conducted to evaluate the effect of concomitant steroid use on flutamide- and bicalutamide-induced liver injury.

METHOD:

Male patients aged 20 years or older who were receiving nonsteroidal anti-androgens from April 2004 to October 2023 were screened from the Japanese Adverse Drug Event Report database. Data on liver injury, age, weight, height, steroid use, obesity, hepatic stenosis, alcohol-related hepatic disorders, hepatitis B and C, and common drugs known to cause drug-induced liver injury were analyzed. Liver injury was defined by the Standardized Medical Dictionary for Regulatory Activities query index (code 20000006, version 27.0).

RESULTS:

Among 142,430 patients, 2,316 were administered nonsteroidal anti-androgens. Reports of liver injury were disproportionate depending on the agents used (reporting odds ratio [ROR], 1.29; 95% confidence intervals [CI], 1.13-1.46), especially among flutamide or bicalutamide users (flutamide: ROR, 6.09; 95% CI, 4.51-8.23; bicalutamide: ROR, 1.24; 95% CI, 1.05-1.48). Multivariable logistic regression analysis correlated steroid use with a lower risk of flutamide- or bicalutamide-induced liver injury (flutamide: odds ratio, 0.07; 95% CI, 0.01-0.52; bicalutamide: odds ratio, 0.45; 95% CI, 0.21-0.96).

CONCLUSION:

Our findings suggest that flutamide and bicalutamide may increase the risk of liver injury compared to enzalutamide, apalutamide, and darolutamide. Furthermore, our study indicated that steroid use could aid in the management of liver injury.

247

项与阿帕他胺相关的新闻（医药）

10 小时之前

·医药魔方

强生2024年财报出炉！达雷妥尤单抗116亿美元，传奇CAR-T同比增长92.7%

1月22日，强生公布了2024年业绩，全年总营收888.21亿美元，同比增长4.3%。强生旗下两大核心业务板块——创新制药和医疗科技，分别实现了569.64亿美元（+4.0%）以及318.57亿美元（+4.8%）的收入。强生的创新制药业务主要聚焦肿瘤、自身免疫、神经科学、感染、肺动脉高压、心血管及代谢这几大关键领域。其中，肿瘤和自免对业绩的贡献最为突出，前者在2024全年取得了207.81亿美元的收入，同比增长17.7%；后者收入178.28亿美元，同比下降1.2%。此外，肺动脉高压产品收入42.82亿美元，同比增长12.3%，同样成为了整体业务不断发展的强劲推动力。 2024年强生肿瘤业务的增长主要归功于Darzalex（达雷妥尤单抗）、Erleada（阿帕他胺）、Carvykti（西达基奥仑赛）、Tecvayli（特立妥单抗）等产品强劲驱动。其中，靶向CD38的多发性骨髓瘤治疗药物Darzalex在全球所有地区的市场份额持续增长，全年收入达116.70亿美元，同比增长19.8%。这是该药自2015年上市以来，销售额首次突破100亿美元大关。多发性骨髓瘤是强生重点布局的疾病领域，CD38单抗Darzalex之外，BCMA CAR-T细胞疗法Carvykti（与传奇生物合作开发）、CD3/BCMA双抗Tecvayli、CD3/GPRC5D双抗Talvey（talquetamab，皮下注射制剂）均取得不俗表现。 Carvykti凭借着92.7%的增长速度一马当先，成为了强生2024年创新制药业务中增长最为迅猛的产品，其全年销售额达9.63亿美元，比去年翻了近1倍。2024年4月，FDA基于CARTUDE-4研究结果，批准该药用于多发性骨髓瘤的二线治疗，这是Carvykti获批的第二个适应症。随着适应症的扩大及产能提升，该药未来还具有很大增长空间。此外，强生的双抗TCE Tecvayli销售额达5.49亿美元，同比增长38.8%。另一款双抗TCE Talvey上市一年，尽管未披露具体销售额，但也将持续扩大强生在多发性骨髓瘤领域的竞争优势。强生血液瘤另一重磅产品Imbruvica（伊布替尼）因面临激烈的竞争压力，2024年的销售额同比下降6.9%，为30.38亿美元。前列腺癌重磅产品Zytiga（阿比特龙）因专利到期，销售额同样严重下滑，为6.31亿美元（-28.8%）。不过雄激素受体抑制剂Erleada（阿帕他胺）已接棒Zytiga，成为强生在该领域的核心产品。该药自2018年上市以来，以每年两位数或更高的增长率，迅速占领市场份额，2024年全年收入达29.99亿美元（+25.6%）。为保持在该领域的领先优势，强生还在2023年推出了阿比特龙+尼拉帕利复方制剂Akeega。 2024年，强生在非小细胞肺癌（NSCLC）领域也迎来了重大突破，其EGFR/c-Met双抗Rybrevant（埃万妥单抗）和EGFR T790M抑制剂Lazcluze（兰泽替尼）重磅产品组合获FDA批准，成为了EGFR 19号外显子缺失（ex19del）或L858R突变NSCLC患者的一线无化疗治疗方案。Rybrevant与化疗联用方案还被FDA批准用于EGFR 20号外显子插入突变NSCLC一线治疗、EGFR ex19del或L858R突变NSCLC二线治疗。这将推动强生肿瘤业务的进一步扩张。强生预测Rybrevant/Lazcluze产品组合销售峰值将突破50亿美元。在自身免疫领域，强生的销售业绩有所下滑，这主要是因为大单品Stelara（乌司奴单抗）受到生物类似药的冲击，收入同比下降了4.6%，为103.61亿美元，其欧洲市场已持续被侵蚀，预计2025年美国市场也将迎来生物类似药带来的巨大挑战。Remicade（英夫利西单抗）也因专利到期导致销售额连续下跌，2024年其全年收入为16.05亿美元，同比下降12.8%。Simponi（戈利木单抗）销售额为也略微下滑（-0.3%），为21.90亿美元。 Tremfya（古塞奇尤单抗）则继续保持着两位数的增长，2024年的销售额达到了36.70亿美元（+16.6%）。为了应对自免领域的危机，强生一方面挖掘已上市产品Tremfya的更多潜力，开展了多项该药治疗克罗恩病、溃疡性结肠炎、银屑病关节炎等疾病的III期临床研究，以拓展其适应症范围。另一方面，强生正在加速FcRn单抗nipocalimab、口服IL-23R拮抗剂JNJ-2113、组合抗体疗法JNJ-4804等候选药物的研发进程。2024年11月，JNJ-2113治疗斑块状银屑病的两项III期研究告捷，成为首款成功完成III期研究的口服IL-23R靶向药物。可以预见，强生将积极推动这些新产品上市，以弥补Stelara、Remicade、Simponi等产品业绩下降带来的影响。神经科学领域，Spravato（艾司氯胺酮鼻喷雾剂）表现亮眼，销售额达10.77亿美元，同比增长56.4%，成为强生又一个“十亿美元分子”。近期FDA还批准了Spravato单药治疗难治性抑郁症的新适应症，这将成为该药又一个极具潜力的增长点。值得注意的是，强生近期还斥资146亿美元收购了Intra-Cellular，进一步加强神经科学领域布局。强生预测这次收购获得的口服抗精神病产品Caplyta（lumateperone）销售峰值有望突破50亿美元。 2024年，强生在肺动脉高压领域收入增长主要得益于Opsumit（马昔腾坦）和Uptravi（司来帕格），这两款药物销售额分别为21.84亿美元（+10.7%）、18.17亿美元（+14.9%）。这一年里，强生在生物制药并购交易方面也相对活跃，3月份，以20亿美元完成了对ADC公司Ambrx的收购，加强了肿瘤产品管线；6月份，以8.5亿美元完成了对双抗公司Proteologix的收购，获得多个针对特应性皮炎和哮喘的抗体项目；7月份，以12.5亿美元完成了对Yellow Jersey的收购，获得了一款靶向IL-4Rα和IL-31的first-in-class双抗NM26的全球权益，用于治疗特应性皮炎。 2024年，强生的创新制药产品管线在注册监管和重要临床研究数据读出方面也达成了多个关键的里程碑事件（详见下图）。展望2025年，强生预计会有2.5%-3.5%的增幅，总收入有望达到909-917亿美元。推荐阅读全球首个治疗“慢性排异”ROCK2抑制剂正式纳入医保报销 Copyright © 2025 PHARMCUBE. All Rights Reserved. 欢迎转发分享及合理引用，引用时请在显要位置标明文章来源；如需转载，请给微信公众号后台留言或发送消息，并注明公众号名称及ID。免责申明：本微信文章中的信息仅供一般参考之用，不可直接作为决策内容，医药魔方不对任何主体因使用本文内容而导致的任何损失承担责任。

免疫疗法细胞疗法财报专利到期上市批准

15 小时之前

·米内网

【重磅】科伦1类新药来袭！猛攻1400亿市场

精彩内容近段时间，科伦药业研发进展不断：抗PD-L1单抗塔戈利单抗获批新适应症，联合顺铂和吉西他滨一线治疗复发或转移性鼻咽癌；米诺地尔搽剂、利丙双卡因乳膏、阿帕他胺片、他克莫司缓释胶囊4款新品同日获批生产并视同过评；1类新药注射用SKB445首次获批临床，拟用于治疗晚期实体瘤。注射用SKB445是一款由科伦博泰研发的具有自主知识产权的新型ADC药物，在临床前研究中显示出良好的疗效和安全窗。其临床申请于2024年11月获得CDE承办受理，并于近日获批临床，拟用于治疗晚期实体瘤。米内网数据显示，近年来抗肿瘤药（化+生）在中国三大终端六大市场（统计范围详见本文末）销售额均达千亿规模，2023年超过1400亿元，2024上半年以约10%的增速继续增长。从细分终端看，零售药店（城市实体药店+网上药店）虽占比不足2成，但销售规模呈现持续提升态势。近年来中国零售药店终端抗肿瘤药（化+生）销售情况（单位：万元）来源：米内网格局数据库抗肿瘤药是科伦药业重点布局的领域之一。在该治疗领域，公司已有塔戈利单抗注射液（抗PD-L1单抗）、注射用芦康沙妥珠单抗（TROP2 ADC）2款1类新药获批上市，其中注射用芦康沙妥珠单抗为首个国产TROP2 ADC药物。在研新药中，1类新药注射用博度曲妥珠单抗（HER2 ADC）、生物类似药西妥昔单抗注射液已申报NDA，上市可期。此外，注射用SKB315（CLDN18.2 ADC）、注射用SKB410（Nectin-4 ADC）、SKB337注射液（PD-L1/CTLA4双抗）、注射用SKB571（新型双抗ADC）等均已步入I期临床。科伦药业同日获批生产并视同过评的4个新品中，利丙双卡因乳膏为公司首款获批的软膏剂。近年来中国三大终端六大市场化药软膏剂销售额逐年上涨，2023年超过140亿元。阿帕他胺片、克莫司缓释胶囊均属于抗肿瘤和免疫调节剂，其中阿帕他胺片为国产第2家获批，原研产品2023年在三大终端六大市场的销售额超过7亿元；他克莫司缓释胶囊为国产第3家获批，该产品2023年在三大终端六大市场的销售额超过3亿元。米内网数据显示，2024年至今，科伦药业（含联营公司）有50个品种过评或视同过评，其中35个品种以新注册分类报产获批而视同过评，15个品种以补充申请方式过评。资料来源：米内网数据库、公司公告等注：米内网《中国三大终端六大市场药品竞争格局》，统计范围是：城市公立医院和县级公立医院、城市社区中心和乡镇卫生院、城市实体药店和网上药店，不含民营医院、私人诊所、村卫生室，不含县乡村药店；上述销售额以产品在终端的平均零售价计算。数据统计截至2025年1月21日，如有疏漏，欢迎指正！本文为原创稿件，转载请注明来源和作者，否则将追究侵权责任。投稿及报料请发邮件到872470254@qq.com稿件要求详询米内微信首页菜单栏商务及内容合作可联系QQ：412539092 ●温馨提示● 因为微信公众号修改了推送规则，最近很多读者反映没有及时看到推文。把米内网设为“星标”，就能每天与我们不见不散啦，具体操作如下：【分享、点赞、在看】点一点不失联哦

抗体药物偶联物临床1期生物类似药上市批准申请上市

2025-01-19

·药明康德

疾病控制率达90%的创新疗法；靶点作用率达95%的PI3Kα共价抑制剂…… | 一周盘点

▎药明康德内容团队编辑本期看点 1. 多肽偶联药物（PDC）AVA6000在治疗唾液腺癌（SGC）患者的1a期临床试验中获得积极数据，疾病控制率（DCR）达90%。 2. 蛋白降解药物BHV-1400在首个人体临床试验中获得积极结果，在最低剂量下只需一次注射，就可在4小时内将致病抗体水平降低60%。 3. PI3Kα共价抑制剂TOS-358在一项1期临床试验中对PI3Kα的靶点作用率达到95%。药明康德内容团队整理 AVA6000：公布1期临床试验数据 Avacta Therapeutics公司宣布，其在研多肽偶联药物AVA6000在治疗唾液腺癌患者的1a期临床试验中获得积极数据。唾液腺癌是一种在转移性阶段尚无标准治疗方案的疾病。AVA6000是Avacta研发管线中的首个多肽偶联药物，由阿霉素（doxorubicin）与Avacta专有的pre|CISION多肽偶联而成，该多肽可在肿瘤微环境中由成纤维细胞激活蛋白-α（FAP）特异性切割。FAP在大多数实体瘤中，与健康组织相比表达水平显著升高。Avacta的多肽偶联药物利用这一特征在肿瘤微环境中特异性释放活性药物，从而降低系统暴露和毒性，为患者提供最佳治疗效果。此次公布的数据显示，AVA6000在唾液腺癌患者中实现了显著且具有临床意义的肿瘤缩小。在接受250 mg/m²及以上剂量治疗的10名唾液腺癌患者中，DCR达90%，5名患者肿瘤显著缩小，其中包括一例部分缓解（PR，肿瘤缩小45%）和四例轻微缓解（MR，肿瘤缩小10%-19.5%）。安全性方面，在每两周一次和每三周一次两个剂量组中，AVA6000的耐受性良好，与常规剂量阿霉素相比，其血液学和心脏毒性明显降低。目前尚未在任一剂量组中确定最大耐受剂量（MTD）。 BHV-1400：公布1期临床试验的初步数据 Biohaven公司公布了其蛋白降解药物管线中的双特异性分子BHV-1400的最新结果。BHV-1400是一款基于耶鲁大学（Yale University）的MoDE技术的双特异性分子，它的一端与半乳糖缺乏型IgA1（Gd-IgA1）抗体结合，另一端与肝细胞表面的去唾液酸糖蛋白受体（ASGPR）结合。ASGPR介导肝细胞通过内吞过程，将靶点蛋白吞入细胞内进行降解。IgA肾病是由于Gd-IgA1的过度生产造成的，BHV-1400通过降低血液循环和肾脏中的Gd-IgA1水平，有望从根源治疗IgA肾病。此次公布的初步数据显示，BHV-1400在首个人体临床试验中获得积极结果，在最低剂量下只需一次注射，就可在4小时内将致病抗体水平降低60%。在某些患者中，观察到在8小时内将Gd-IgA1水平降低70%。此外，Gd-IgA1水平的降低在单次注射后可维持数天。安全性方面，迄今为止，BHV-1400在1期临床试验中的安全性和耐受性良好，未发现具有临床意义的先天和适应性免疫力的变化，并且未观察到剂量限制性毒性。这项研究将继续提高BHV-1400的剂量，探索降低Gd-IgA1水平的范围。基于该研究的积极结果，该公司还计划直接启动关键性临床试验，评估BHV-1400治疗IgA肾病的疗效和安全性。 ▲BHV-1400快速降低Gd-IgA1水平（图片来源：Biohaven公司官网） TOS-358：公布1期临床试验数据 Totus Medicines公司公布了其在研PI3Kα共价抑制剂TOS-358的1期临床试验数据。TOS-358是一款具高度特异性、强效的PI3Kα抑制剂，可在临床前模型中实现近100%的PI3Kα抑制，诱导带有PI3Kα突变的异种移植实体瘤的细胞死亡，包含结直肠癌、肺癌、乳腺癌、卵巢癌、食管癌、头颈癌，且几乎没有观察到非靶向抑制。此次公布的研究结果表明，TOS-358在低至5 mg每日两次（BID）的剂量下具有泛突变临床活性，对PI3Kα的靶点作用率达到95%，且观察到未经确认的完全缓解（CR）。安全性方面，未报道3/4级毒性。值得注意的是，几名接受给药的患者现在已超过6个月未发生进展。在成功完成1期剂量递增研究后，该公司现在启动了一项扩展研究，针对乳腺癌、子宫内膜癌、尿路上皮癌和头颈癌。 ORIC-944：公布1b期联合治疗试验数据 ORIC Pharmaceuticals公司公布了其选择性PRC2别构抑制剂ORIC-944联用阿帕鲁胺治疗转移性去势抵抗性前列腺癌（mCRPC）的1b期临床试验数据。截至2024年12月10日的数据，6例患者中有3例达到确认的PSA50应答（即PSA水平降低50%），其中2例达到确认的PSA90应答。所有PSA应答均维持≥12周，其中包括一例在38周时仍然持续的、确认的PSA90应答。 Soquelitinib：公布1期临床试验的中期数据 Corvus Pharmaceuticals公司公布了其小分子白细胞介素-2诱导的T细胞激酶（ITK）抑制剂soquelitinib用于治疗中度至重度特应性皮炎的1期临床试验的新中期数据。ITK是一种主要表达于T细胞中的酶，在T细胞和自然杀伤（NK）细胞的免疫功能中起重要作用。通过抑制ITK，soquelitinib有望抑制自身免疫和炎症反应。此次公布的结果显示，与安慰剂相比，soquelitinib治疗组在研究者总体评估（IGA）评分为0/1（皮肤症状清除或几乎清除）和湿疹面积和严重度指数较基线减少75%（EASI 75）这些临床终点方面显示出良好的疗效特征。在soquelitinib组的19例患者中，26%的患者达到IGA 0/1，37%的患者达到EASI 75。在安慰剂组的7例患者中，没有人达到IGA 0/1，也没有人达到EASI 75。安全性方面，未观察到明显的安全问题，也未发现临床上显著的实验室检测异常。 ▲治疗第28天达到终点IGA 0/1、EASI 75的患者占比（图片来源：参考资料[4]） ISM5411：公布两项1期临床试验数据英矽智能（Insilico Medicine）公司宣布，其自主研发的候选药物ISM5411已完成在澳大利亚和中国开展的两项1期研究，并取得了积极的初步结果。ISM5411是一种潜在用于治疗炎症性肠病（IBD）的小分子抑制剂，靶向PHD1/2靶点且具有新颖的分子结构，该候选药物设计和优化得到了英矽智能生成化学平台Chemistry42的支持。此次公布的结果显示，在所有剂量组中ISM5411均表现出良好的安全性和耐受性，并初步验证了肠道限制性药代动力学（PK）特征。基于1期临床试验的积极结果，英矽智能预计将于2025年下半年启动一项评估ISM5411在活动性溃疡性结肠炎患者中的2期临床试验。 MBX 1416：公布1期临床试验数据 MBX Biosciences公司公布了在健康成年受试者中开展的MBX 1416单剂量递增和多剂量递增临床试验的积极结果。MBX 1416是一种长效胰高血糖素样肽1（GLP-1）受体拮抗剂，用于治疗减肥后的低血糖症（PBH）。MBX 1416采用MBX公司新颖、专有的精准内分泌肽（PEP）平台设计，旨在防止PBH患者发生严重低血糖，使他们能够过上更健康、更独立的生活。此次公布的结果显示，MBX 1416通常安全性和耐受性良好，并且具有良好的药代动力学特征，支持每周一次给药。基于这些结果，该公司计划于2025年下半年在PBH患者中启动一项2期研究，以进一步优化剂量。 ▲欲了解更多前沿技术在生物医药产业中的应用，请长按扫描上方二维码，即可访问“药明直播间”，观看相关话题的直播讨论与精彩回放参考资料（可上下滑动查看） [1] Avacta Announces Positive New Data from the AVA6000 Phase 1 trial Demonstrating Clinically Meaningful Tumor Shrinkage in Patients with Salivary Gland Cancers. Retrieved January 16, 2025, from https://www.globenewswire.com/news-release/2025/01/16/3010665/0/en/Avacta-Announces-Positive-New-Data-from-the-AVA6000-Phase-1-trial-Demonstrating-Clinically-Meaningful-Tumor-Shrinkage-in-Patients-with-Salivary-Gland-Cancers.html [2] Biohaven Highlights Portfolio Progress, Innovation, and Anticipated Milestones at the 43rd Annual J.P. Morgan Healthcare Conference; Reports Positive Degrader Data with Rapid, Deep, and Selective Lowering of Galactose-Deficient IgA1 with Next Generation Potential Therapy for IgA Nephropathy. Retrieved January 14, 2025, from https://www.prnewswire.com/news-releases/biohaven-highlights-portfolio-progress-innovation-and-anticipated-milestones-at-the-43rd-annual-jp-morgan-healthcare-conference-reports-positive-degrader-data-with-rapid-deep-and-selective-lowering-of-galactose-deficient-ig-302349336.html [3] Totus Medicines Announces Successful Completion of a Phase 1 Dose-Escalation Study and Initiation of an Expansion Trial Evaluating TOS-358, a Covalent PI3Ka Selective Therapy for the Treatment of Select Solid Tumors and Appoints Zelanna Goldberg as Chief Medical Officer. Retrieved January 17, 2025, from https://www.globenewswire.com/news-release/2025/01/10/3007658/0/en/Totus-Medicines-Announces-Successful-Completion-of-a-Phase-1-Dose-Escalation-Study-and-Initiation-of-an-Expansion-Trial-Evaluating-TOS-358-a-Covalent-PI3Ka-Selective-Therapy-for-th.html [4] Corvus Pharmaceuticals Announces Data from Cohort 2 of Placebo-Controlled Phase 1 Clinical Trial of Soquelitinib for Atopic Dermatitis. Retrieved January 17, 2025, from https://www.globenewswire.com/news-release/2025/01/13/3008374/0/en/Corvus-Pharmaceuticals-Announces-Data-from-Cohort-2-of-Placebo-Controlled-Phase-1-Clinical-Trial-of-Soquelitinib-for-Atopic-Dermatitis.html [5] ORIC® Pharmaceuticals Provides Early Phase 1b Combination Data for ORIC-944, Operational Highlights for 2024, and Anticipated Upcoming Milestones. Retrieved January 17, 2025, from https://www.globenewswire.com/news-release/2025/01/13/3008495/0/en/ORIC-Pharmaceuticals-Provides-Early-Phase-1b-Combination-Data-for-ORIC-944-Operational-Highlights-for-2024-and-Anticipated-Upcoming-Milestones.html [6] 英矽智能公布炎症性肠病药物ISM5411两项I期临床试验的积极结果. Retrieved January 17, 2025, from https://www.prnasia.com/story/474986-1.shtml [7] MBX Biosciences Announces Positive Phase 1 Topline Results for MBX 1416 for the Treatment of Post-bariatric Hypoglycemia. Retrieved January 17, 2025, from https://www.globenewswire.com/news-release/2025/01/07/3005223/0/en/MBX-Biosciences-Announces-Positive-Phase-1-Topline-Results-for-MBX-1416-for-the-Treatment-of-Post-bariatric-Hypoglycemia.html [8] Mersana Therapeutics Announces Positive Initial Clinical Data from Phase 1 Clinical Trial of Emiltatug Ledadotin (XMT-1660); Initiation of Expansion in Triple Negative Breast Cancer. Retrieved January 17, 2025, from https://www.globenewswire.com/news-release/2025/01/10/3007493/0/en/Mersana-Therapeutics-Announces-Positive-Initial-Clinical-Data-from-Phase-1-Clinical-Trial-of-Emiltatug-Ledadotin-XMT-1660-Initiation-of-Expansion-in-Triple-Negative-Breast-Cancer.html [9] Axcynsis Therapeutics Receives FDA Clearance for IND Application of AT03-65, a Differentiated CLDN6-Targeting ADC, Powered by AxcynDOT™ Technology. Retrieved January 17, 2025, from https://www.prnewswire.com/news-releases/axcynsis-therapeutics-receives-fda-clearance-for-ind-application-of-at03-65-a-differentiated-cldn6-targeting-adc-powered-by-axcyndot-technology-302350114.html [10] Ocugen, Inc. Announces Positive 2-Year Data Across Multiple Mutations from Phase 1/2 Clinical Trial of OCU400 —A Novel Modifier Gene Therapy for Retinitis Pigmentosa. Retrieved January 17, 2025, from https://www.globenewswire.com/news-release/2025/01/13/3008252/0/en/Ocugen-Inc-Announces-Positive-2-Year-Data-Across-Multiple-Mutations-from-Phase-1-2-Clinical-Trial-of-OCU400-A-Novel-Modifier-Gene-Therapy-for-Retinitis-Pigmentosa.html [11] Verismo Therapeutics Announces First Patient Infused in Phase 1 CELESTIAL-301 Clinical Trial of SynKIR™-310. Retrieved January 17, 2025, from https://www.prnewswire.com/news-releases/verismo-therapeutics-announces-first-patient-infused-in-phase-1-celestial-301-clinical-trial-of-synkir-310-302347464.html [12] Caribou Biosciences Initiates the CB-010 GALLOP Phase 1 Trial in Lupus and Provides Outlook for Multiple Clinical Datasets in 2025. Retrieved January 17, 2025, from https://www.globenewswire.com/news-release/2025/01/13/3008079/0/en/Caribou-Biosciences-Initiates-the-CB-010-GALLOP-Phase-1-Trial-in-Lupus-and-Provides-Outlook-for-Multiple-Clinical-Datasets-in-2025.html [13] Arcturus Therapeutics Announces Initiation of Phase 1 H5N1 Flu Vaccine Trial. Retrieved January 17, 2025, from https://ir.arcturusrx.com/news-releases/news-release-details/arcturus-therapeutics-announces-initiation-phase-1-h5n1-flu [14] Korro Bio Announces Dosing of First Participants in REWRITE Phase 1/2a Study of KRRO-110 for Alpha-1 Antitrypsin Deficiency and Provides Pipeline Update. Retrieved January 17, 2025, from https://www.globenewswire.com/news-release/2025/01/13/3008445/0/en/Korro-Bio-Announces-Dosing-of-First-Participants-in-REWRITE-Phase-1-2a-Study-of-KRRO-110-for-Alpha-1-Antitrypsin-Deficiency-and-Provides-Pipeline-Update.html [15] NextCure Announces First Patient Dosed in the Phase 1 Study of LNCB74 (B7-H4 ADC) as Therapeutic for Treating Multiple Cancers. Retrieved January 17, 2025, from https://ir.nextcure.com/news-releases/news-release-details/nextcure-announces-first-patient-dosed-phase-1-study-lncb74-b7 [16] LAVA Doses First Patient in Phase 1 LAVA-1266 Study in Hematological Cancers. Retrieved January 17, 2025, from https://www.globenewswire.com/news-release/2025/01/10/3007674/0/en/LAVA-Doses-First-Patient-in-Phase-1-LAVA-1266-Study-in-Hematological-Cancers.html [17] Context Therapeutics Announces First Patient Dosed in the Phase 1 Clinical Trial of CTIM-76. Retrieved January 17, 2025, from https://www.globenewswire.com/de/news-release/2025/01/14/3009673/0/en/Context-Therapeutics-Announces-First-Patient-Dosed-in-the-Phase-1-Clinical-Trial-of-CTIM-76.html [18] Ocugen, Inc. Announces First Patient Dosed in Phase 1 Clinical Trial of OCU200—a Novel Integrin-Targeting Biologic for Diabetic Macular Edema. Retrieved January 17, 2025, from https://ir.ocugen.com/news-releases/news-release-details/ocugen-inc-announces-first-patient-dosed-phase-1-clinical-trial [19] ProMIS Neurosciences Initiates Phase 1b Clinical Trial (PRECISE-AD) in Alzheimer’s Disease. Retrieved January 17, 2025, from https://www.promisneurosciences.com/news-media/press-releases/detail/236/promis-neurosciences-initiates-phase-1b-clinical-trial [20] Aptose Announces First AML Patients Dosed with Tuspetinib Triplet Frontline Therapy in TUSCANY Trial. Retrieved January 17, 2025, from https://www.aptose.com/news-media/press-releases/detail/307/aptose-announces-first-aml-patients-dosed-with-tuspetinib [21] ORYZON announces first patient dosed in NCI-sponsored iadademstat in combination with venetoclax and azacitidine clinical trial in first line acute myeloid leukemia. Retrieved January 17, 2025, from https://www.oryzon.com/en/news-events/news/oryzon-announces-first-patient-dosed-nci-sponsored-iadademstat-combination [22] 한미약품-GC녹십자, ‘파브리병’ 국내 1/2상 IND 승인. Retrieved January 17, 2025, from https://www.biospectator.com/news/view/24043 免责声明：药明康德内容团队专注介绍全球生物医药健康研究进展。本文仅作信息交流之目的，文中观点不代表药明康德立场，亦不代表药明康德支持或反对文中观点。本文也不是治疗方案推荐。如需获得治疗方案指导，请前往正规医院就诊。版权说明：本文来自药明康德内容团队，欢迎个人转发至朋友圈，谢绝媒体或机构未经授权以任何形式转载至其他平台。转载授权请在「药明康德」微信公众号回复“转载”，获取转载须知。分享，点赞，在看，聚焦全球生物医药健康创新

临床结果临床1期多肽偶联药物

100 项与阿帕他胺相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D11040	阿帕他胺	L02BB05	DB11901

研发状态

批准上市

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
转移性前列腺癌	日本	Janssen Pharmaceutical KK	2020-05-29
转移性去势抵抗性前列腺癌	美国	Janssen Biotech, Inc.	2019-09-17
激素依赖性前列腺癌	欧盟	Janssen-Cilag International NV	2019-01-14
激素依赖性前列腺癌	冰岛	Janssen-Cilag International NV	2019-01-14
激素依赖性前列腺癌	列支敦士登	Janssen-Cilag International NV	2019-01-14
激素依赖性前列腺癌	挪威	Janssen-Cilag International NV	2019-01-14
前列腺癌	加拿大	Janssen Research & Development LLC	2018-07-27
去势敏感前列腺癌	澳大利亚	Janssen-Cilag Pty Ltd.	2018-07-05
去势抵抗性前列腺癌	美国	Janssen Biotech, Inc.	2018-02-14

未上市

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
非转移性前列腺癌	临床3期	法国	Janssen Pharmaceutica NV	2020-01-09
阿尔茨海默症	临床3期	美国	Janssen Research & Development LLC	2015-12-07
阿尔茨海默症	临床3期	美国	Aragon Pharmaceuticals, Inc.	2015-12-07
阿尔茨海默症	临床3期	美国	西安杨森制药有限公司	2015-12-07
阿尔茨海默症	临床3期	日本	Janssen Research & Development LLC	2015-12-07
阿尔茨海默症	临床3期	日本	Aragon Pharmaceuticals, Inc.	2015-12-07
阿尔茨海默症	临床3期	日本	西安杨森制药有限公司	2015-12-07
阿尔茨海默症	临床3期	阿根廷	Aragon Pharmaceuticals, Inc.	2015-12-07
阿尔茨海默症	临床3期	阿根廷	Janssen Research & Development LLC	2015-12-07
阿尔茨海默症	临床3期	阿根廷	西安杨森制药有限公司	2015-12-07

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临床结果

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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


NCT02489318 (TITAN, Pubmed \| BJU Int)	临床3期	prostate-specific antigen	-	Apalutamide 240 mg/day	糧願壓繭觸壓選網願觸(餘觸夢鹹襯淵壓構築網): HR = 0.24 (95% CI, 0.13 ~ 0.43), P-Value = <0.001 更多	积极	2024-12-01
				Placebo
NCT04523207 (Apa-RP, CTgov)	临床2期	去势抵抗性前列腺癌 \| 非转移性前列腺癌	108	ADT+Apalutamide+Relugolix (Apalutamide Plus ADT (Main Study) + Relugolix Followed by Apalutamide Plus Relugolix (Sub Study))	築積築製鹽糧憲製遞廠(糧憲遞夢窪鏇網積範壓) = 窪範淵壓繭繭積築膚齋膚鑰衊獵憲憲壓願廠衊 (簾衊構淵鹽遞醖艱構衊, 膚膚繭選醖淵膚選鹽鏇 ~ 窪餘膚窪築積觸膚網壓) 更多	-	2024-11-19
				Apalutamide+Relugolix (Sub Study: Relugolix Followed by Apalutamide Plus Relugolix)	構鹹艱簾憲獵鹽壓窪顧(製繭鑰鹽願積積築鏇鏇) = 遞簾憲鑰獵獵積積鏇繭鹽選鹹齋鑰衊築鹽醖鹹 (窪繭選壓憲鑰鏇醖廠鏇, 艱鏇築壓艱積鏇製壓淵 ~ 鑰餘憲膚衊壓積鹽選夢) 更多
NCT01946204 (SPARTAN, Pubmed \| JAMA Netw Open)	临床3期	去势抵抗性前列腺癌一线 prostate-specific antigen doubling time of 10 months or less	1,179	Apalutamide	顧顧膚積醖積觸簾窪蓋(夢願獵窪窪選憲築廠製): HR = 0.22 (95% CI, 0.17 ~ 0.27) 更多	积极	2024-10-15
				Placebo
ECOP2024 人工标引	N/A	去势敏感前列腺癌	3,719	Apalutamide	衊範鏇夢積鏇襯蓋製衊(淵簾襯顧鬱壓範蓋構衊): HR = 0.77 (95% CI, 0.62 ~ 0.96), P-Value = 0.019 更多	积极	2024-10-02
				Enzalutamide
NCT03777982 (CTgov)	临床3期	前列腺癌	12	LHRH Agonist or Antagonist+Apalutamide+Prednisone+Abiraterone Acetate (Prednisone+Apalutamide+Abiraterone Acetate +LHRH Agonist)	築構遞鑰醖鏇鬱築鬱齋(壓衊鹽艱獵積淵鏇壓憲) = 廠淵齋壓積膚構獵廠衊蓋觸廠衊網鹽夢鑰觸遞 (鹹憲襯廠鏇鑰蓋衊範構, 鹽夢遞餘蓋構窪範繭範 ~ 窪築鏇鬱襯願艱窪構衊) 更多	-	2024-09-19
				LHRH Agonist or Antagonist (LHRH Agonist or Antagonist)	築構遞鑰醖鏇鬱築鬱齋(壓衊鹽艱獵積淵鏇壓憲) = 憲獵選簾窪糧餘糧鏇壓蓋觸廠衊網鹽夢鑰觸遞 (鹹憲襯廠鏇鑰蓋衊範構, 襯醖願範淵齋膚簾鏇夢 ~ 膚鬱壓願廠網窪鹹壓簾) 更多
NCT02200614 \| NCT01946204 (SPARTAN \| ARAMIS, ESMO2024)	临床3期	去势抵抗性前列腺癌一线 serum testosterone	-	ADT+apalutamide	壓衊糧壓壓鬱構鹽願壓(製廠衊艱範糧夢顧醖觸): HR = 0.67 (95% CI, 0.44 ~ 0.99)	不佳	2024-09-15
				ADT+darolutamide
NCT04523207 (Apa-RP, Pubmed \| Carcinogenesis \| J Urol) 人工标引	临床2期	局限性前列腺癌辅助 preoperative PSA \| baseline testosterone	108	Apalutamide + ADT	糧選鹹選構窪襯窪鑰鏇(淵壓獵鬱選襯蓋壓齋餘) = 鏇鑰蓋範糧鏇衊廠壓窪簾願築鬱廠艱齋築網蓋 (構憲製鏇鹽鑰遞選窪窪, 93 ~ 100) 更多	积极	2024-08-01
NCT04523207 (Apa-RP, ASCO2024) 人工标引	临床2期	局限性前列腺癌辅助	108	Apa + ADT	積構醖遞衊壓積艱廠衊(簾廠簾衊網製鏇衊簾鏇) = 窪憲鑰鑰繭願醖壓鬱繭淵繭構蓋壓蓋鹽鬱製夢 (繭鏇餘襯網顧糧製遞繭, 93.4 ~ 100.0) 更多	积极	2024-05-24
				Apa + ADT (Black Patients)	積構醖遞衊壓積艱廠衊(簾廠簾衊網製鏇衊簾鏇) = 壓襯鏇觸網獵鹽鹹鹹夢淵繭構蓋壓蓋鹽鬱製夢 (繭鏇餘襯網顧糧製遞繭, 57.9 ~ 100.0) 更多
ASCO2024	N/A	-	-	Apalutamide (APA)	憲鹹鏇鑰憲糧壓糧壓築(鏇蓋構醖觸鹹鹹構遞構) = 遞蓋壓窪艱壓繭鹽簾窪選憲積夢鹽積醖淵淵願 (選構獵齋製夢鬱選鑰遞 )	-	2024-05-24
				Enzalutamide (ENZ)	憲鹹鏇鑰憲糧壓糧壓築(鏇蓋構醖觸鹹鹹構遞構) = 襯鏇憲鏇鹹鏇鏇積鏇願選憲積夢鹽積醖淵淵願 (選構獵齋製夢鬱選鑰遞 )
ASCO2024	N/A	去势敏感前列腺癌 prostate-specific antigen	-	Apalutamide (APA)	齋鬱鹹餘窪鏇鑰鹽繭觸(齋憲願鏇顧壓築鹹艱繭) = 鹹鬱繭構淵鏇夢鏇選鑰繭構窪齋鏇壓襯蓋簾繭 (夢襯膚糧齋淵齋淵壓窪 )	积极	2024-05-24
				Abiraterone acetate (ABI)	齋鬱鹹餘窪鏇鑰鹽繭觸(齋憲願鏇顧壓築鹹艱繭) = 醖製廠艱窪願鬱遞襯餘繭構窪齋鏇壓襯蓋簾繭 (夢襯膚糧齋淵齋淵壓窪 )