A Phase II Randomized Trial of Intermittent Androgen Deprivation Therapy Alone or Combined With [177Lu]Lu-PSMA-617, With or Without Abiraterone and Prednisone, in Patients With Low-Volume Metastatic Hormone-Sensitive Prostate Cancer

This phase II trial tests leuprolide acetate alone versus in combination with 177Lu-PSMA-617, with or without abiraterone acetate and prednisone, for the treatment of hormone-sensitive prostate cancer has spread to a limited number of anatomic sites at the time of initial diagnosis (de novo low volume metastasis) or that has come back after a period of improvement (recurrent). Standard of care treatment for prostate cancer usually includes androgen deprivation therapy, with or without abiraterone acetate and prednisone. Leuprolide acetate is a form of androgen deprivation therapy. It blocks the body from making testosterone (a male hormone) and estradiol (a female hormone). It may stop the growth of prostate cancer cells that need testosterone to grow. 177Lu-PSMA-617 is a type of radioconjugate drug. Upon administration, vipivotide tetraxetan targets and binds to prostate specific membrane antigen (PSMA)-expressing tumor cells. Upon binding, PSMA-expressing tumor cells are destroyed by 177Lu through the specific delivery of radiation. PSMA, a tumor-associated antigen and type II transmembrane protein, is overexpressed on prostate tumor cells. Abiraterone acetate is a type of anti-androgen drug. It blocks tissues from making androgens (male hormones), such as testosterone. This may cause the death of cancer cells that need androgens to grow. Prednisone is in a class of medications called corticosteroids. It is used to reduce inflammation and lower the body's immune response to help lessen the side effects of chemotherapy drugs. Giving 177Lu-PSMA-617 in combination with leuprolide acetate, with or without abiraterone acetate and prednisone, may be more effective at treating patients with recurrent or de novo low volume metastatic hormone-sensitive prostate cancer than giving leuprolide acetate alone.

开始日期2026-07-01

申办/合作机构

Mayo Clinic

NCT07674121

/ Not yet recruitingN/A

Non-Interventional, Observational, Retrospective and Prospective, Single- Arm Study to Assess the Effectiveness of Olaparib and Abiraterone Combination as First Line Therapy in NHA Pre-exposed mCRPC Patients in the GCC Region

The study will generate regionally relevant data to inform clinical practice, support treatment guidelines, and potentially contribute to supportive evidence for health authority discussions or scientific publications. This aligns with AstraZeneca's strategic goal of expanding the real-world evidence (RWE) base for Olaparib in diverse populations and practice settings. The study also complements the strategic priorities and focus areas, as well as strengthening AstraZeneca's leadership position in the management of prostate cancer and establishing the intensification therapy of Poly (ADP-ribose) Polymerase Inhibitor (PARPi) combination in metastatic castration-resistant prostate cancer (mCRPC) with previous exposure to a novel hormonal agent (NHA) for current and future medications (a next-generation PARPi).

开始日期2026-06-30

申办/合作机构

AstraZeneca PLC

NCT07641855

/ Not yet recruiting临床2/3期

A Phase II/III Clinical Study to Evaluate the Efficacy and Safety of BL-B01D1 Combination Therapy in Patients With Metastatic Castration-resistant Prostate Cancer

This study will first conduct a phase II clinical study, and on the basis of the phase II clinical study, subsequent clinical research will be carried out.

开始日期2026-06-01

申办/合作机构

四川百利药业有限责任公司

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100 项与醋酸阿比特龙相关的临床结果

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100 项与醋酸阿比特龙相关的转化医学

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100 项与醋酸阿比特龙相关的专利（医药）

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3,566

项与醋酸阿比特龙相关的文献（医药）

2026-12-31·CANCER BIOLOGY & THERAPY

Targeting the PI3K/AKT pathway in prostate cancer: the role of PTEN deficiency and biomarker-guided therapy

Review

作者: Staton, Allison ; Abel, Melissa ; Figg, William D.

Loss of the PTEN tumor suppressor gene is a common molecular feature in advanced prostate cancer and is associated with activation of the PI3K/AKT signaling pathway, which controls cell growth and survival. Despite major advances in the treatment of metastatic castration-sensitive prostate cancer (mCSPC), patients with PTEN-deficient tumors represent an aggressive subgroup with poorer clinical outcomes and limited targeted therapeutic options. Capivasertib is a selective oral AKT inhibitor designed to suppress downstream signaling from PI3K pathway activation. We highlight the recent results from the Phase III CAPItello-281 trial (NCT04493853) demonstrating that the addition of capivasertib to abiraterone acetate and androgen deprivation therapy (ADT) significantly improved radiographic progression-free survival in patients with PTEN-deficient mCSPC, leading to the FDA-approval of this regimen. Notable adverse events in the cabavisertib arm included hyperglycemia, diarrhea, and rash. CAPItello-281 addresses a significant unmet need for PTEN-deficient mCSPC, suggesting AKT inhibition as a potential new targeted treatment strategy for a sub-population with poor prognosis.

2026-09-26·ENDOCRINE-RELATED CANCER

Body composition in recurrent prostate cancer and the role of steroidogenic genotype

Article

作者: Pilie, Patrick G ; Mukhida, Sagar S ; Corn, Paul G ; Koutroumpakis, Efstratios ; McQuade, Jennifer L ; Tidwell, Rebecca S ; Gregg, Justin R ; Zurita, Amado J ; Hahn, Andrew W ; Aparicio, Ana ; Frigo, Daniel E ; Huff, Chad ; Logothetis, Christopher J ; Subudhi, Sumit K ; Siddiqui, Bilal A ; Venkatesh, Neha ; Yu, Yao

Hormone therapy (HT) to treat prostate cancer is reported to cause adverse changes in body composition. Clinically, interpatient body composition changes are heterogeneous, but the biological and clinical determinants of body composition toxicity are unknown. Herein, we test the hypothesis that inherited polymorphisms in steroidogenic genes are associated with differential changes in body composition after HT. Men with biochemically recurrent prostate cancer (BCR) who received 8 months of LHRH analog (LHRHa) +/− abiraterone acetate (AAP) were eligible if they had: i) CT imaging of L3 prior to and after treatment; and ii) nucleated cells collected. Cardiometabolic co-morbidities were retrospectively extracted. Body composition was measured using an AI-based segmentation tool. Germline DNA whole exome or genome sequencing was performed. In 162 men treated with 8 months of HT, median skeletal muscle mass (SMMi) loss was 6.6% and subcutaneous adipose gain was 12.3%. Men with type 2 diabetes had higher losses of SMMi after treatment (−11.1% vs −6.3%, P = 0.003). For the 150 men with germline NGS, SRD5A2 rs523349 genotype was associated with differential loss in skeletal muscle density after HT, (−1.3% vs −7.1%, P = 0.04). In addition, the HSD3B1 rs104703 genotype was associated with decreased baseline visceral adipose tissue (63.0 cm2/m2 vs 77.9, P = 0.05). In men with BCR, HT induced notable loss of skeletal muscle and increased subcutaneous adipose tissue. An inherited polymorphism in SRD5A2 and T2DM was associated with differential skeletal muscle toxicity. These findings suggest that inherited polymorphisms may contribute to the body composition toxicity observed with HT.

2026-09-01·STEROIDS

Synthesis and cytotoxicity evaluation of steroidal 17β-hydroxy-17α-methylisoxazoles

Article

作者: Chernysheva, Anastasia ; Zavialova, Maria ; Khripach, Vladimir ; Zhabinskii, Vladimir ; Scherbakov, Alexander ; Grabovec, Irina ; Tsybruk, Tatsiana ; Sorokin, Danila ; Aleksandrova, Anna ; Kugaevskaya, Elena ; Mekhtiev, Arif ; Krech, Anastasia ; Timoshenko, Olga ; Scherbakov, Kirill

The aim of this study was to develop an approach to the synthesis of 17β-hydroxy-17α-methylisoxazoles and to evaluate their cytotoxic effects against prostate cancer cell lines. The key reaction in their synthesis was the addition of a dianion generated from ethyl acetoacetate and butyllithium to androstenolone. Subsequent stages included the reaction of the intermediate β-hydroxyketone with hydroxylamine to form an isoxazole heterocycle, as well as manipulations with protecting groups. The cytotoxicity of the obtained compounds was studied using hormone-sensitive and hormone-independent prostate and breast carcinoma cell lines. It was found that 17β-hydroxy-17α-methylisoxazoles exerted a more pronounced inhibitory effect on LNCaP cells in comparison with abiraterone, while only minor cytotoxicity was observed toward PC3, MCF-7, and MDA-MB-231 cells. Analysis of the effects of the compounds on cell cycle progression in LNCaP cells demonstrated that they induced cell cycle arrest in the G0/G1 phase. Compound 4 (17α-(Isoxazol-3-ylmethyl)-androst-5-en-3β,17β-diol) suppressed the activity of key signaling pathways (AKT, S6K, ERKs) in LNCaP cells. Binding analysis of the studied compounds to human CYP17A1 revealed a weak spectral response, suggesting that effective binding does not occur in the active site and their mechanism of action is likely unrelated to CYP17A1 inhibition. The steroidal 17β-hydroxy-17α-methylisoxazoles are the basis for the development of new drugs that regulate the activity of kinase signaling pathways in tumor cells.

1,434

项与醋酸阿比特龙相关的新闻（医药）

2026-07-14

·investors.oricpharma.com

ORIC® Pharmaceuticals Announces Initiation of Himalayas-1 Phase 3 Trial in mCRPC Evaluating Rinzimetostat in Combination with NUBEQA® (Darolutamide), Supported by Clinical Collaboration with Bayer

Initiated Himalayas-1 global Phase 3 trial in patients with mCRPC previously treated with abiraterone Entered into a clinical trial collaboration and supply agreement with Bayer to provide darolutamide for Himalayas-1 SOUTH SAN FRANCISCO, Calif. and SAN DIEGO, July 14, 2026 (GLOBE NEWSWIRE) -- ORIC Pharmaceuticals, Inc. (Nasdaq: ORIC), a clinical stage oncology company focused on developing treatments that address mechanisms of therapeutic resistance, today announced the initiation of the Himalayas-1 global Phase 3 registrational trial in patients with metastatic castration-resistant prostate cancer (mCRPC) previously treated with abiraterone and announced a clinical trial collaboration and supply agreement with Bayer AG (“Bayer”). Himalayas-1 Global Phase 3 Registrational Trial Initiation ORIC previously presented dose optimization data for rinzimetostat in combination with darolutamide and selected 400 mg once daily rinzimetostat as the recommended Phase 3 dose (RP3D). Following End-of-Phase 1 interactions with the FDA and other global health authorities, ORIC finalized the trial protocol and has initiated the Himalayas-1 global Phase 3 registrational trial. The Himalayas-1 trial is expected to enroll approximately 600 patients from over 250 sites in 25 countries, randomized 1:1 to receive the RP3D of 400 mg once daily rinzimetostat (with or without food) in combination with darolutamide versus physician’s choice of an androgen receptor (AR) inhibitor or docetaxel. The primary endpoint is radiographic progression-free survival, the key secondary endpoint is overall survival, and additional secondary endpoints include PSA response rate, objective response rate and patient reported outcomes. Clinical Trial Collaboration and Supply Agreement with Bayer Under the terms of the agreement, ORIC will conduct and sponsor the Himalayas-1 trial and Bayer will provide their AR inhibitor, NUBEQA® (darolutamide), at no cost for use in the trial in combination with rinzimetostat. This agreement does not grant Bayer any license, option, or other rights to rinzimetostat and ORIC retains full global development and commercial rights to rinzimetostat. “Given the significant unmet need in prostate cancer and the potential best-in-disease clinical profile that rinzimetostat has continued to demonstrate, the initiation of our Himalayas-1 Phase 3 trial represents an important milestone toward establishing rinzimetostat as a potentially practice-changing therapy for patients,” said Jacob M. Chacko, M.D., president and chief executive officer. “This collaboration with Bayer strengthens our global operational readiness by securing access to darolutamide for Himalayas-1 and underscores our shared interest in evaluating this regimen for patients with prostate cancer.” About ORIC Pharmaceuticals, Inc. ORIC Pharmaceuticals is a clinical stage biopharmaceutical company dedicated to improving patients’ lives by Overcoming Resistance In Cancer. ORIC’s clinical stage product candidates include (1) rinzimetostat, an allosteric inhibitor of the polycomb repressive complex 2 (PRC2) via the EED subunit, being developed for prostate cancer, and (2) enozertinib, a brain-penetrant inhibitor targeting EGFR exon 20 insertion and EGFR atypical mutations, being developed for NSCLC. ORIC has offices in South San Francisco and San Diego, California. For more information, please go to www.oricpharma.com, and follow us on X or LinkedIn. Cautionary Note Regarding Forward-Looking Statements This press release contains forward-looking statements as that term is defined in Section 27A of the Securities Act of 1933 and Section 21E of the Securities Exchange Act of 1934. Statements in this press release that are not purely historical are forward-looking statements. Such forward-looking statements include, among other things, expectations and plans regarding the Himalayas-1 global Phase 3 registrational trial in mCRPC evaluating rinzimetostat in combination with NUBEQA® (darolutamide); the continued clinical development of rinzimetostat; the potential advantages of rinzimetostat; clinical outcomes, which may materially change as patient enrollment continues or more patient data become available; statements regarding the potential best-in-disease profile of rinzimetostat; and statements by the company’s chief executive officer. Words such as “believes,” “anticipates,” “plans,” “expects,” “intends,” “will,” “goal,” “potential” and similar expressions are intended to identify forward-looking statements. The forward-looking statements contained herein are based upon ORIC’s current expectations and involve assumptions that may never materialize or may prove to be incorrect. Actual results could differ materially from those projected in any forward-looking statements due to numerous risks and uncertainties, including but not limited to: risks associated with the process of discovering, developing and commercializing drugs that are safe and effective for use as human therapeutics and ORIC’s limited operating history; ORIC’s ability to complete clinical trials for, obtain approvals for and commercialize rinzimetostat; delays or difficulties in the enrollment and/or maintenance of patients in the Himalayas-1 clinical trial; changes in ORIC’s plans to develop and commercialize rinzimetostat; the potential for clinical trials of rinzimetostat to differ from preclinical, initial, interim, preliminary, expected or prior clinical trial results; negative impacts of health emergencies, economic instability or international conflicts on ORIC’s operations, including clinical trials; the risk of the occurrence of any event, change or other circumstance that could give rise to the termination of ORIC’s license and collaboration agreements or its clinical trial collaboration and supply agreements, including its agreement with Bayer; the potential market for ORIC’s product candidates, and the progress and success of competing therapeutics currently available or in development; ORIC’s ability to raise any additional funding it will need to continue to pursue its business and product development plans; regulatory developments in the United States and foreign countries; ORIC’s reliance on third parties, including contract manufacturers and contract research organizations; ORIC’s ability to obtain and maintain intellectual property protection for its product candidates; the loss of key scientific or management personnel; competition in the industry in which ORIC operates; general economic and market conditions; and other risks. Information regarding the foregoing and additional risks may be found in the section entitled “Risk Factors” in ORIC’s Quarterly Report on Form 10-Q filed with the Securities and Exchange Commission (the SEC) on May 4, 2026, and ORIC’s future reports to be filed with the SEC. These forward-looking statements are made as of the date of this press release, and ORIC assumes no obligation to update the forward-looking statements, or to update the reasons why actual results could differ from those projected in the forward-looking statements, except as required by law. Contact: Dominic Piscitelli, Chief Financial Officer dominic.piscitelli@oricpharma.com info@oricpharma.com

临床3期引进/卖出

2026-07-14

·BioSpace

Caris Life Sciences Expands Precision Oncology in Metastatic Prostate Cancer with PTEN IHC Testing

IRVING, Texas , July 14, 2026 /PRNewswire/ -- Caris Life Sciences ® (NASDAQ: CAI), a leading patient-centric next-generation AI TechBio company and precision medicine pioneer, today announced it will offer in-house PTEN immunohistochemistry (IHC) testing following the recent FDA approval of a biomarker-guided therapy and companion diagnostic assay. This testing is designed to help identify patients with PTEN-deficient metastatic androgen pathway modulation-naïve or -sensitive (mAPMN/S) prostate cancer (previously known as metastatic hormone-sensitive prostate cancer) who are eligible for the newly approved biomarker-guided therapy, representing a significant advancement in precision oncology for this disease. Prostate cancer remains one of the most prevalent malignancies in men, with more than 300,000 new cases diagnosed annually in the United States. The FDA approval of capivasertib, in combination with abiraterone and prednisone, for adults with PTEN-deficient mAPMN/S prostate cancer marks a critical turning point for this disease, enabling a more personalized approach to treatment. Historically, therapy selection in mAPMN/S prostate cancer has relied primarily on clinical characteristics rather than changes in protein expression. Caris' PTEN IHC testing expands the company's already extensive menu of IHC assays and will enable oncologists to identify patients whose tumors exhibit PTEN protein loss, a key molecular alteration associated with activation of the PI3K/AKT pathway and potential therapeutic relevance. One in four patients with mAPMN/S prostate cancer have PTEN-deficient tumors, which are associated with faster progression and worse outcomes. "For patients with metastatic hormone-sensitive prostate cancer, treatment decisions have historically been driven largely by clinical factors rather than biomarker-defined molecular alterations," said George W. Sledge , Jr., MD, EVP and Chief Medical Officer at Caris. "The ability to identify PTEN loss through IHC testing brings a new level of precision to treatment selection, helping ensure that the right patients can be matched with biomarker-driven therapies at a critical point in their disease." Key Highlights of Caris PTEN IHC Testing: Expanded IHC Capabilities: Caris continues to build one of the most comprehensive IHC testing portfolios in the industry, supporting critical biomarker identification across tumor types. Support for Biomarker-Driven Therapy Selection: PTEN IHC testing enables identification of PTEN-deficient tumors, supporting treatment decisions in mAPMN/S prostate cancer where FDA-approved biomarker-targeted therapy is now available. In-House Testing for Faster Results: By performing testing within Caris' CAP-accredited, CLIA-certified laboratories, results can be delivered efficiently to help inform timely clinical decision-making. Advancing Personalized Care: Integration of PTEN IHC with Caris' broader multi-platform molecular profiling approach including next-generation sequencing (NGS) provides a more complete understanding of tumor biology to guide therapy selection. The introduction of PTEN IHC testing reflects a broader evolution in prostate cancer care, as the field transitions toward biomarker-driven treatment strategies that align therapy with the molecular drivers of disease. By enabling identification of patients who are eligible for these therapies, Caris is helping advance more precise, individualized treatment decisions that may improve clinical outcomes. Caris' comprehensive molecular profiling portfolio includes MI Cancer Seek®, Caris Assure®, Caris MI Clarity™, Caris Chromoseq™ and Caris Detect™. MI Cancer Seek is a tissue-based assay with FDA-approved companion diagnostic indications for molecular profiling of solid tumors, while Caris Assure is a blood-based assay designed to identify tumor-derived alterations through comprehensive sequencing approaches. Caris MI Clarity is the first prognostic test designed to deliver insight into both early and late distant recurrence risk for postmenopausal patients with HR-positive/HER2-negative, node-negative early-stage breast cancer at the time of diagnosis. Caris Chromoseq is a Whole Genome Sequencing (WGS) assay designed to support the comprehensive clinical genomic evaluation of myeloid malignancies. Caris Detect™ , is a groundbreaking multi-cancer early detection blood test designed to accurately find cancer signals early, at stage I and stage II, when treatment is more effective. Caris remains committed to advancing precision medicine through innovative diagnostics, robust molecular data and clinically actionable insights that help transform cancer care. About Caris Life Sciences Caris Life Sciences® (Caris) is a leading, patient-centric, next-generation AI TechBio company and precision medicine pioneer actively developing and commercializing innovative solutions to transform healthcare. Through comprehensive molecular profiling (Whole Genome, Whole Exome and Whole Transcriptome Sequencing), advanced AI and machine learning, Caris has created the large-scale, multimodal clinico-genomic database and computing capability needed to analyze and further unravel the molecular complexity of disease. This convergence of next-generation sequencing, AI and machine learning technologies and high-performance computing provides a differentiated platform for developing the latest generation of advanced precision medicine diagnostic solutions for early detection, diagnosis, monitoring, therapy selection and drug development.  Caris was founded with a vision to realize the potential of precision medicine to improve the human condition. Headquartered in Irving, Texas, Caris has offices in Phoenix, New York, Cambridge (MA), Tokyo, Japan and Basel, Switzerland. Caris or its distributor partners provide services in the U.S. and other international markets.  Forward Looking Statements This press release contains forward-looking statements, within the meaning of the Private Securities Litigation Reform Act of 1995 and other federal securities laws. All statements other than statements of historical facts contained in this press release are forward-looking statements, including statements regarding our business, solutions, plans, objectives, goals, industry trends, financial outlook and guidance. In some cases forward-looking statements can be identified by words such as "may," "will," "should," "would," "expect," "plan," "anticipate," "could," "intend," "target," "project," "potential," "contemplate," "believe," "estimate," "predict," or "continue" or similar expressions. You should not rely upon forward-looking statements as predictions of future events. Although we believe that the expectations reflected in these forward-looking statements are reasonable based on information currently available to us, we cannot guarantee that the future results, discoveries, levels of activity, performance or events and circumstances reflected in forward-looking statements will be achieved or occur. Forward-looking statements involve known and unknown risks and uncertainties, some of which are beyond our control. Risks and uncertainties that could cause our actual results to differ materially from those indicated or implied by the forward-looking statements in this press release include, among other things: our future financial performance, results of operations or other operational results or metrics; development, analytical and clinical validation, timing and performance of future solutions by us and our competitors; commercial market acceptance for our solutions, including acceptance of preventive as well as diagnostic testing paradigms, and our ability to meet resulting demand; the rapidly evolving competitive environment in which we operate; third-party payer reimbursement and coverage decisions related to our solutions; risks related to data management, storage, and processing capabilities and our ability to integrate and deploy artificial intelligence and advanced data analytics technologies; our ability to protect and enhance our intellectual property; regulatory requirements, decisions or approvals (including the timing and conditions thereof) related to our solutions, including our application for New York State Department of Health approval for Caris Assure; reliance on third-party suppliers; risks related to data security, patient privacy, and compliance with healthcare data protection regulations as well as potential cybersecurity threats to our data platforms; our compliance with laws and regulations; the outcome of government investigations and litigation; risks related to our indebtedness; and our ability to hire and retain key personnel as well as risks, uncertainties; and other factors described in the section titled "Risk Factors" and elsewhere in our Annual Report on Form 10-K filed on March 3, 2026, and in our other filings we make with the SEC from time to time. We undertake no obligation to update any forward-looking statements to reflect changes in events, circumstances or our beliefs after the date of this press release, except as required by law. Caris Life Sciences Media: Corporate Communications CorpComm@CarisLS.com 214.294.5606 Investor Relations: IR@CarisLS.com 917.689.3511 View original content to download multimedia: SOURCE Caris Life Sciences

上市批准

2026-07-13

·今日头条

陈守臻教授：氘代策略在新药研发中的应用

前言氘代策略通过将药物分子中的氢原子替换为其稳定重同位素氘，利用动力学同位素效应改善药物的药代动力学和安全性特征。这一策略经历了从早期偶然探索、到“氘代开关”改良老药、再到“从头设计”新药的演进历程。截至目前，全球已有氘代丁苯那嗪、多纳非尼、氘可来昔替尼、氘代恩扎卢胺等多款氘代药物获批上市，在亨廷顿病、肝细胞癌、银屑病及前列腺癌等领域展现出临床优势。山东大学齐鲁医院陈守臻教授在本文中系统梳理氘代策略的化学基础、发展脉络，尤其在前列腺癌领域已取得的突破性进展，并展望此类新型药物研发所面临的机遇和挑战。氘代：开辟药物优化新策略在新药研发的历史长河中，对先导化合物的结构优化始终是核心挑战之一。传统的生物电子等排体策略，如引入卤素原子（尤其是氟），通过改变分子的电子云分布和脂溶性来调节药物活性与代谢稳定性。然而，氟原子等修饰往往带来不可预见的毒性风险或代谢通路偏移，且较大体积的取代基可能干扰药物与靶点的精确识别 [1] 。相较之下，氘代策略提供了一种“最小结构修饰”的独特路径。氘（²H）是氢的稳定非放射性重同位素，由一个质子、一个中子和一个电子组成。当药物分子中的碳-氢（C-H）键被碳-氘（C-D）键取代时，分子的立体结构、电子性质和脂溶性几乎不受影响（氘代后摩尔体积仅变化约0.140 cm³/mol，AlogP变化约-0.006） [2,3] 。然而，由于氘原子质量是氢的两倍，C-D键的振动伸缩频率显著降低，基态能量更低，因此断裂C-D键所需的活化能高于C-H键，反应速率相应减慢（速率常数kH > kD） [4] 。这种动力学同位素效应（Kinetic Isotope Effect, KIE）如同为药物分子中特定部位“穿上盔甲”，使其对代谢酶的攻击具有更强的抵抗力，从而为调控药物体内命运提供了精妙的工具。 △原型药和氘代药的主要差异从“氘代开关”到“从头设计” 氘代在药物领域的探索可追溯至20世纪60年代。1961年，Belleau等对d2-酪胺和d3-吗啡的研究首次揭示了氘代可能改变药物的体内代谢行为，但此后相当长时间内相关研究进展缓慢 [5] 。直到近二十年，随着对药物代谢机制的深入理解和分析技术的进步， “氘代开关”（Deuterium Switch）策略逐渐兴起 ——即在已上市药物的易代谢位点选择性引入氘原子，以改善其药代动力学缺陷 [6] 。这一策略的标志性突破是2017年氘代丁苯那嗪（Deutetrabenazine）获美国FDA批准，成为全球首个上市的氘代药物。相比原药丁苯那嗪，氘代版本显著优化了给药方案，将每日三次服药减少为两次。此后，中国原研的多纳非尼（Donafenib）于2021年获批用于肝细胞癌治疗，成为全球第二个、中国第一个获批的氘代药物。真正的范式转变发生在2022年，氘可来昔替尼（Deucravacitinib）获得FDA批准，这不仅是全球第三个上市的氘代药物，更是首个从药物发现早期即“从头设计” 的氘代新药 [8] 。它标志着氘代策略从被动地改良老药，升级为主动参与新药分子设计的关键环节——研究者通过对代谢软点的精准预测，在候选化合物优化阶段即引入氘原子，以规避有害代谢物的生成，实现对靶点的高选择性抑制。这一转变深刻体现了从“经验性应用”到“理性设计”的方法学跃迁。 △氘代技术药物研发历程前列腺癌氘代药物的中国创新突破氘恩扎鲁胺（Deutenzalutamide, HC-1119）是恩扎卢胺的氘代类似物，在酰胺N-甲基基团引入三个氘原子 [8] 。恩扎卢胺的代谢途径包括水解生成非活性羧酸代谢物M1，以及经CYP2C8和CYP3A4/5介导的N-去甲基化生成活性代谢物M2，后者被认为与癫痫风险增加相关。临床前研究显示，氘代后原药M0的代谢减慢，M1和M2的生成均显著减少，且相同剂量下氘恩扎鲁胺在血浆中的M0浓度更高，脑组织中M0、M1和M2浓度均更低。在10 mg/kg剂量下，氘恩扎鲁胺可抑制80%的肿瘤生长，显示了积极的抗肿瘤活性和安全性 [8] 。在中国进行的多中心、随机、双盲、安慰剂对照III期临床试验（HC-1119-04研究，NCT03851640） [9] 进一步验证了氘恩扎鲁胺的临床疗效和安全性。该研究共入组417例转移性去势抵抗性前列腺癌（mCRPC）患者。主要终点显示，氘恩扎鲁胺组中位影像学无进展生存期（rPFS）显著延长至5.55个月，相比对照组降低疾病进展或死亡风险42%（HR=0.58, p=0.0001）。OS敏感性分析同样显示全因死亡风险降低。尤为值得关注的是，该研究中未见癫痫、跌倒、骨折等中枢神经系统相关不良事件，≥3级乏力发生率仅为3.6%。 △HC-1119-04研究主要终点rPFS及亚组分析基于上述证据，2026年《CSCO前列腺癌诊疗指南》和《CACA指南》均将氘恩扎鲁胺纳入mCRPC多个治疗阶段的推荐方案。该药物作为国产1.1类创新药，也是2025年国家医保谈判入选品种，其在中枢神经系统安全性、皮疹发生率和药物相互作用方面的显著优势，使其成为中国mCRPC患者的安心之选。【总结和展望：机遇与挑战并存】氘代策略为新药研发带来了独特机遇：在代谢调控层面，它可延长半衰期、减少给药频率、提高患者依从性；在安全性层面，它可减少有毒代谢物生成或避免药物相互作用。除了肝癌、前列腺癌等领域已取得突破性进展以外，氘代类似物有望拓展至神经退行性疾病、代谢性疾病等新适应症。然而，氘代药物的发展亦面临多重挑战。首先，合成高同位素纯度（>98%）的氘代药物难度较大，氘代试剂成本高昂，且控制H/D交换过程易导致欠氘代或过氘代，增加合成步骤与成本。其次，FDA等监管机构目前尚缺乏针对氘代药物同位素杂质的专项指南，这对审批路径和安全性评估带来不确定性。最后，氘代药物的市场接受度取决于其成本效益比——尽管多纳非尼在疗效和安全性上具有优势，但药物经济学分析显示其当前定价的成本效益欠佳，影响了市场推广。总之，氘代策略正从“经验性氘代开关”迈向“理性设计”的新阶段。随着结构生物学和代谢预测技术的发展，研究者能够在分子设计早期精准识别代谢软点，并通过氘代实现代谢流的人工引导。氘代有望在提升药物疗效、安全性和患者生活质量方面发挥更为广泛的作用，为未被满足的临床需求提供新的解决方案。专家简介陈守臻教授山东大学齐鲁医院泌尿外科副主任副教授、硕士研究生导师泰山学者青年专家山东大学齐鲁医院优秀临床教师 CSCO前列腺癌诊疗指南执笔专家组成员中国医师协会泌尿外科医师分会膀胱癌学组委员山东省医学会泌尿男生殖系肿瘤多学科联合委员会青委组长山东省医学会泌尿外科分会青委副组长以第一或通讯作者在 PNAS、Cancer Research、Advanced Science 等杂志发表SCI文章20余篇主持国家自然科学基金、省重点研发计划等项目获得山东省科技进步一等奖参考文献： [1]Meanwell NA. Synopsis of some recent tactical application of bioisosteres in drug design. J Med Chem. 2011;54(8):2529-2591. doi:10.1021/jm1013693 [2]Atzrodt J, Derdau V, Kerr WJ, Reid M. Deuterium- and Tritium-Labelled Compounds: Applications in the Life Sciences. Angew Chem Int Ed Engl. 2018;57(7):1758-1784. doi:10.1002/anie.201704146 [3]Atzrodt J, Derdau V, Kerr WJ, Reid M. Deuterium- and Tritium-Labelled Compounds: Applications in the Life Sciences. Angew Chem Int Ed Engl. 2018;57(7):1758-1784. doi:10.1002/anie.201704146 [4]Relative Stability of Hydrogen and Deuterium Bonds S. Scheiner, M. Cuma J. Am. Chem. Soc. 1996 118 (6), 1511-1521. [5]Belleau B, Burba J, Pindell M, Reiffenstein J. Effect of Deuterium Substitution in Sympathomimetic Amines on Adrenergic Responses. Science. 1961;133(3446):102-104. doi:10.1126/science.133.3446.102 [6]Di Martino RMC, Maxwell BD, Pirali T. Deuterium in drug discovery: progress, opportunities and challenges. Nat Rev Drug Discov. 2023;22(7):562-584. doi:10.1038/s41573-023-00703-8 [7]Mullard A. First de novo deuterated drug poised for approval. Nat Rev Drug Discov. 2022;21(9):623-625. doi:10.1038/d41573-022-00139-6 [8]Li X, Cheng K, Li X, et al. Phase I clinical trial of HC-1119: A deuterated form of enzalutamide. Int J Cancer. 2021;149(7):1473-1482. doi:10.1002/ijc.33706 [9]Wu J, Li X, Gu C, et al. Deutenzalutamide, a novel androgen receptor inhibitor, after progression on docetaxel and abiraterone in metastatic castration-resistant prostate cancer: results from the randomized phase III HC-1119-04 trial.Signal Transduction and Targeted Therapy. 2026;11:131. doi:10.1038/s41392-026-02618-3 编辑：Peng 审校：陈守臻教授排版：Mercury 执行：Roberta 医脉通是专业的在线医生平台，“感知世界医学脉搏，助力中国临床决策”是平台的使命。医脉通旗下拥有「临床指南」「用药参考」「医学文献王」「医知源」「e研通」「e脉播」等系列产品，全面满足医学工作者临床决策、获取新知及提升科研效率等方面的需求。本平台旨在为医疗卫生专业人士传递更多医学信息。本平台发布的内容，不能以任何方式取代专业的医疗指导，也不应被视为诊疗建议。如该等信息被用于了解医学信息以外的目的，本平台不承担相关责任。本平台对发布的内容，并不代表同意其描述和观点。若涉及版权问题，烦请权利人与我们联系，我们将尽快处理。

100 项与醋酸阿比特龙相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D09701	醋酸阿比特龙	L02BX03	DB05812

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	巴西	Libbs Farmacêutica Ltda.	2018-12-24
神经内分泌前列腺癌	日本	Janssen Pharmaceutical KK	2018-02-16
去势抵抗性前列腺癌	澳大利亚	Janssen-Cilag Pty Ltd.	2012-03-01
激素依赖性前列腺癌	澳大利亚	Janssen-Cilag Pty Ltd.	2012-03-01
转移性去势抵抗性前列腺癌	美国	Janssen Biotech, Inc.	2011-04-28

未上市

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适应症	最高研发状态	国家/地区	公司	日期
前列腺腺癌	临床3期	美国	Tavanta Therapeutics, Inc.	2021-05-05
前列腺腺癌	临床3期	法国	Tavanta Therapeutics, Inc.	2021-05-05
前列腺腺癌	临床3期	匈牙利	Tavanta Therapeutics, Inc.	2021-05-05
前列腺腺癌	临床3期	波兰	Tavanta Therapeutics, Inc.	2021-05-05
前列腺腺癌	临床3期	西班牙	Tavanta Therapeutics, Inc.	2021-05-05
前列腺腺癌	临床3期	瑞典	Tavanta Therapeutics, Inc.	2021-05-05
前列腺腺癌	临床3期	英国	Tavanta Therapeutics, Inc.	2021-05-05
去势敏感前列腺癌	临床3期	美国	Tavanta Therapeutics, Inc.	2021-05-05
去势敏感前列腺癌	临床3期	法国	Tavanta Therapeutics, Inc.	2021-05-05
去势敏感前列腺癌	临床3期	匈牙利	Tavanta Therapeutics, Inc.	2021-05-05

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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


NCT02789878 (NeoPRO, ASCO2026)	临床2期	局限性前列腺癌新辅助	62	goserelin+abiraterone acetate+prednisone	糧夢夢餘襯構鏇簾鑰繭(願獵膚遞糧糧獵襯衊選) = 夢憲獵蓋淵鬱鬱顧艱淵築觸遞鹽蓋網窪齋鏇蓋 (鏇襯壓鹹膚襯網鬱獵壓 ) 更多	不佳	2026-05-29
				goserelin+abiraterone acetate+prednisone+apalutamide	糧夢夢餘襯構鏇簾鑰繭(願獵膚遞糧糧獵襯衊選) = 簾鏇糧壓積醖獵壓窪範築觸遞鹽蓋網窪齋鏇蓋 (鏇襯壓鹹膚襯網鬱獵壓 ) 更多
NCT01949337 (Alliance A031201, ASCO2026)	临床3期	转移性去势抵抗性前列腺癌一线	776	enzalutamide + abiraterone acetate + prednisone	選醖襯餘觸網蓋糧鬱選(鬱鏇膚夢艱齋觸齋獵壓) = 鏇遞襯憲顧獵窪淵獵鬱範製糧遞壓網壓壓範構 (構範製窪構網鑰築艱選 ) 更多	积极	2026-05-29
				enzalutamide	選醖襯餘觸網蓋糧鬱選(鬱鏇膚夢艱齋觸齋獵壓) = 鏇鹽廠鑰淵齋廠蓋顧積範製糧遞壓網壓壓範構 (構範製窪構網鑰築艱選 )
ASCO2026	N/A	去势敏感前列腺癌	726	Abiraterone + ADT	繭蓋築範顧鹽膚選廠遞(網繭願糧醖艱鑰觸膚鑰) = All-cause mortality was also higher in the abiraterone group (OR 3.4; 95% CI, 2.3-5.1) 襯鹹廠廠衊製鹹願艱襯 (鑰積簾艱糧鏇簾築壓顧 ) 更多	不佳	2026-05-29
				Darolutamide + ADT
ASCO2026	N/A	转移性去势敏感性前列腺癌	11,588	Darolutamide (doublet therapy)	艱構蓋壓憲繭構築糧鬱(壓範築蓋窪積製衊壓選) = 壓餘淵鬱構淵蓋鬱淵淵觸構製觸鹽齋簾淵鹹選 (蓋簾簾製願襯製築選選, 5.6 ~ 9.0) 更多	积极	2026-05-29
				Abiraterone (doublet therapy)	艱構蓋壓憲繭構築糧鬱(壓範築蓋窪積製衊壓選) = 鬱鬱壓壓衊蓋網獵製餘觸構製觸鹽齋簾淵鹹選 (蓋簾簾製願襯製築選選, 10.0 ~ 11.4) 更多
NCT03934840 (CASCARA, CTgov)	临床2期	转移性去势敏感性前列腺癌	61	Cabazitaxel+Carboplatin+prednisone+Abiraterone	獵選積齋膚鹹鹽膚蓋鹽 = 鹹選網衊窪構艱鹹艱蓋餘膚鏇網範獵範觸鹽製 (窪簾繭齋觸齋醖遞壓鬱, 衊鹽齋範遞築積鏇夢簾 ~ 鹹膚糧鑰積鹽遞蓋鏇壓) 更多	-	2026-05-26
NCT02772588 (CTgov)	临床2期	前列腺癌 \| 前列腺腺癌	64	stereotactic, ultra-fractionated radiotherapy+ARN-509+Abiraterone+Leuprolide	積襯選鑰窪網顧繭積糧 = 憲齋鹹糧獵膚遞糧遞憲範艱廠壓窪製艱齋鹽膚 (鑰獵鬱積願糧積築鑰夢, 顧積廠獵繭範壓簾蓋糧 ~ 製廠膚獵範顧夢構範壓) 更多	-	2026-04-13
NCT00268476 (STAMPEDE, Pubmed \| J Clin Invest)	临床3期	转移性前列腺癌 Ki-67	1,605	Abiraterone + ADT	築窪憲艱鹹夢遞蓋襯艱(簾製憲糧餘願觸淵壓夢) = 鏇遞觸窪憲鹹製觸積襯蓋窪夢鬱願獵築夢糧積 (衊繭觸簾窪觸鹽繭積鏇 )	积极	2026-03-31
NCT03012321 (BRCAAway, ASCO_GU2026) 人工标引	临床2期	转移性去势抵抗性前列腺癌一线 DNA repair defects	61	Abiraterone 1000 mg QD + prednisone 5 mg BID	蓋憲蓋鹹蓋餘膚醖餘憲(糧憲醖製簾鬱鏇遞觸憲) = 簾餘觸醖鑰醖艱廠顧鏇廠艱廠鬱積鬱齋糧製願 (製蓋選範憲鹹夢膚齋鹹, 13 ~ NR) 更多	积极	2026-02-26
				Olaparib 300 mg BID	蓋憲蓋鹹蓋餘膚醖餘憲(糧憲醖製簾鬱鏇遞觸憲) = 醖艱積膚鹽窪膚衊蓋鹹廠艱廠鬱積鬱齋糧製願 (製蓋選範憲鹹夢膚齋鹹, 26 ~ NR) 更多
ASCO_GU2026	N/A	前列腺癌	195	Abiraterone acetate	衊鬱糧艱願襯衊築衊築(廠鹽襯觸壓鹹鑰齋壓蓋) = 壓築鏇獵顧觸衊夢鹹簾簾壓醖淵顧壓齋簾顧積 (築壓鏇鬱襯遞繭壓鏇憲 ) 更多	不佳	2026-02-26
				Apalutamide	衊鬱糧艱願襯衊築衊築(廠鹽襯觸壓鹹鑰齋壓蓋) = 夢願淵鹹觸積鹽襯顧網簾壓醖淵顧壓齋簾顧積 (築壓鏇鬱襯遞繭壓鏇憲 ) 更多
ASCO_GU2026	N/A	转移性前列腺癌	344	Enzalutamide (Charlson Comorbidity Index ≥3)	廠鏇簾獵夢鑰憲膚鬱壓(製齋淵網遞醖鑰積築餘) = 齋憲構齋積積膚選淵夢選壓築艱鹽廠繭憲築壓 (憲膚鑰膚廠壓齋壓積廠, 25.9 ~ 55.1) 更多	积极	2026-02-26
				Abiraterone (Charlson Comorbidity Index ≥3)	廠鏇簾獵夢鑰憲膚鬱壓(窪糧範構築餘製醖積製) = 獵餘鏇繭獵遞顧簾鑰鏇餘鬱網獵襯夢夢製憲艱 (窪鏇鏇膚醖獵築鹹廠簾 )