Researchers want to learn if MK-5684 (the study medicine) can treat breast cancer, ovarian cancer, and endometrial cancer. MK-5684, the study medicine, is designed to treat cancer by blocking the body from making steroid hormones.
Researchers will compare MK-5684 to the standard treatments for each cancer type in this study.
The goal of this study is to learn if people who receive MK-5684 live longer without the cancer growing or spreading compared to people who receive a standard treatment.

开始日期2025-08-11

申办/合作机构

Merck Sharp & Dohme LLC

NCT06863272

/ Recruiting临床1/2期

MK-2400-01A Substudy: A Phase 1/2, Open-label Umbrella Substudy of MK-2400-U01 Master Protocol to Evaluate the Safety and Efficacy of Ifinatamab Deruxtecan-based Treatment Combinations or Ifinatamab Deruxtecan Alone in Participants With Metastatic Castration-resistant Prostate Cancer (mCRPC) (IDeate-Prostate02)

The purpose of this substudy is to assess the efficacy and safety of ifinatamab deruxtecan (I-DXd), given alone or with other treatments in participants with metastatic castration-resistant prostate cancer (mCRPC). The goals of this study are to learn about:
* The safety of the study treatment and if people tolerate it.
* A safe dose level of I-DXd that can be used with other treatments.
* Participant levels of prostate specific antigen (PSA) during treatment.

开始日期2025-07-03

申办/合作机构

Merck Sharp & Dohme LLC

[+1]

NCT06860243

/ Recruiting临床1期

An Open-Label, Single-Dose Study to Evaluate the Pharmacokinetics of MK-5684 in Male Participants With Moderate Hepatic Impairment

Researchers have designed a study medicine called opevesostat as a new way to treat prostate cancer.
The purpose of this study is to learn what happens to opevesostat in a person's body over time (a pharmacokinetic [PK] study). Researchers will compare what happens to opevesostat in the body when it is given to healthy participants and participants with moderate hepatic (liver) impairment.

开始日期2025-05-13

申办/合作机构

Merck Sharp & Dohme LLC

100 项与 Opevesostat 相关的临床结果

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100 项与 Opevesostat 相关的转化医学

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100 项与 Opevesostat 相关的专利（医药）

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项与 Opevesostat 相关的文献（医药）

2024-05-01·Current opinion in oncology

Targeting androgen biosynthesis in prostate cancer: implications on endocrine physiology

Review

作者: Malek, Rana ; Hussain, Arif ; Kango, Ghazal ; Mannuel, Heather

Purpose of review:

Targeting specific steroidogenic enzymes is effective in decreasing testosterone synthesis, resulting in significant antitumor effects in prostate cancer. Such treatments result in disruptions of complicated and intertwining pathways with systemic physiologic consequences via effects on the adrenal gland and renin–angiotensin–aldosterone axis. This review highlights some of these aspects that need to be taken into consideration when treating patients with androgen biosynthesis inhibitors.

Recent findings:

Targeting CYP17A1, a key enzyme involved in androgen biosynthesis, is a well established treatment in prostate cancer. More recently, efforts are underway to target a gatekeeper enzyme of steroidogenesis, CYP11A1. This enzyme mediates conversion of cholesterol to pregnenolone, the first step in steroid hormone biogenesis. Studies are beginning to demonstrate antitumor effects of ODM-208, a CYP11A1 inhibitor in prostate cancer. Although anticipated to have a therapeutic role in prostate cancer, there are potential downstream effects of CYP11A1 targeting arising from suppression of the entire adrenal cortex, including long-term adrenal insufficiency and possibly cardiovascular dysregulation.

Summary:

Agents targeting androgen biosynthesis can have systemic implications. Balancing management of prostate cancer with better understanding of the mechanisms associated with potential side effects will allow for patients to obtain improved antitumor benefit while mitigating against treatment-associated adverse effects.

2024-01-23·NEJM evidence

Targeted Inhibition of CYP11A1 in Castration-Resistant Prostate Cancer

Article

In the Original Article, "Targeted Inhibition of CYP11A1 in Castration-Resistant Prostate Cancer", originally published December 26, 2023 (DOI: https://doi.org/10.1056/EVIDoa2300171), in the Abstract, under "Background", the sentence "ODM-208, a novel inhibitor of cytochrome P450 17A1 …" should have read "ODM-208, a novel inhibitor of cytochrome P450 11A1…" A corrected version of the article has been posted at evidence.nejm.org.

2023-12-26·NEJM evidence

Targeted Inhibition of CYP11A1 in Castration-Resistant Prostate Cancer

Article

作者: Ikonen, Tarja ; Fléchon, Aude ; Cook, Natalie ; Barthélémy, Philippe ; van der Voet, Johannes ; Roubaud, Guilhem ; Antonarakis, Emmanuel S. ; Pohjanjousi, Pasi ; Garratt, Chris ; Utriainen, Tapio ; Baldini, Capucine ; Peters, Niamh ; Ratta, Raffaele ; Parikh, Omi ; Tanner, Minna ; Bernard-Tessier, Alice ; Fizazi, Karim ; Gravis, Gwenaëlle ; Jones, Robert ; Joensuu, Heikki

BACKGROUND: Prostate cancer is regulated by steroid hormones, even in castration-resistant disease. ODM-208, a novel inhibitor of cytochrome P450 11A1 (which catalyzes the first step of steroid-hormone biosynthesis), was investigated in patients with heavily pretreated metastatic castration-resistant prostate cancer (mCRPC). METHODS: CYPIDES is a first-in-human phase 1 (3 + 3 design) and phase 2 study. We administered ODM-208 twice daily with glucocorticoid/mineralocorticoid replacement and ongoing androgen deprivation therapy to adults with previously treated mCRPC, regardless of androgen receptor gene (AR) ligand-binding domain mutations (phase 1) and with activating AR ligand-binding domain mutations (ARmut; phase 2). Safety, pharmacokinetics, steroid-hormone pharmacodynamics, and preliminary efficacy were the key outcomes. RESULTS: Ninety-two patients received one or more doses of ODM-208: 47 in phase 1 (20 [42.6%] with ARmut) and 45 in phase 2 (all ARmut). A dose of ODM-208 of 5 mg twice a day with dexamethasone 1 mg/fludrocortisone 0.1 mg provided a balance between decreased steroidogenesis and toxicity. Treatment-related adrenal insufficiency was the most common toxicity in phase 1 (n=17, 36.2%; necessitating ODM-208 discontinuation in one patient); this toxicity occurred in six patients (13.3%) at 5 mg twice a day in phase 2. Median circulating testosterone levels declined from 3.0 ng/dl (interquartile range, 1.3 to 6.2 ng/dl) at baseline to undetectable levels within the first week of ODM-208 5 mg twice a day treatment in 46 of 53 (87%) patients. A decrease in prostate-specific antigen levels of 50% or more occurred in 14 of 19 (73.7%) patients with ARmut and 2 of 23 (8.7%) patients with AR wild type in phase 1 and in 24 of 45 (53.3%) patients with ARmut in phase 2. CONCLUSIONS: ODM-208 potently inhibited steroid-hormone biosynthesis with the expected toxicity of adrenal insufficiency. Evidence of antitumor activity was observed in this heavily pretreated mCRPC population, especially in those with ARmut. (Funded by Orion Pharma; ClinicalTrials.gov number, NCT03436485.)

项与 Opevesostat 相关的新闻（医药）

2025-06-05

·PipelineReview

Acerand Therapeutics Initiates First-in-Human Phase I Clinical Trial of ACE-232, a Novel CYP11A1 Inhibitor for Advanced Prostate Cancer

SHANGHAI, China & INDIANAPOLIS, IN, USA I June 04, 2025 I Acerand Therapeutics, a clinical-stage biotech company focusing on the discovery and development of innovative small-molecule therapies in oncology, today announced the dosing of the first patient in its first-in-human Phase I clinical trial (NCT06801236) of ACE-232, a novel oral inhibitor of CYP11A1. The trial is being conducted in patients with metastatic castration-resistant prostate cancer (mCRPC). This multicenter Phase I study is being conducted in both the United States and China. The study comprises two parts: a dose-escalation phase (Phase IA) and a dose-optimization phase (Phase IB). The primary objectives are to evaluate the safety, tolerability, pharmacokinetics (PK), pharmacodynamics (PD), as well as preliminary clinical activity of ACE-232, and to determine the recommended Phase II dose (RP2D). Professor Emmanuel Antonarakis, Director of Genitourinary Oncology at Masonic Cancer Center, University of Minnesota, is serving as the global coordinating Principal Investigator for the study. “I would like to congratulate the Acerand team, the research staff, and the first patient for helping us to reach this important milestone,” says Dr. Antonarakis. Preclinical data demonstrated that ACE-232 possesses superior potency, efficacy, and pharmacokinetic properties (flat PK curve and long half-life profile) compared to other investigational CYP11A1 inhibitors, including MK-5684 (Opevesostat, formerly known as ODM-208). ACE-232 showed excellent tolerability in preclinical models, presenting a wide therapeutic window for clinical development. The initiation of this trial marks a significant milestone for Acerand, representing its first clinical study in the United States and highlighting its strategic commitment to the global development of innovative cancer therapies that address major unmet medical needs. About ACE-232 ACE-232 is a highly potent and selective small-molecule inhibitor of CYP11A1, a key adrenal enzyme involved in the first and rate-limiting step of steroid hormone biosynthesis. By targeting CYP11A1, ACE-232 aims to suppress the production of androgens and other steroid hormones, offering a novel therapeutic mechanism for the treatment of androgen-dependent (including enzalutamide or abiraterone-resistant) prostate cancer. About Acerand Therapeutics Acerand Therapeutics is a biotech company dedicated to discovering and developing novel small-molecule therapies for oncology and metabolic diseases. With research and development hubs in Shanghai, China, and Indianapolis, USA, ACE-232 leverages its proprietary innovation platform and operational efficiency to deliver a highly differentiated pipeline of drug candidates from discovery to clinical trials. http://acerand.com/ SOURCE: Acerand Therapeutics

临床1期

2025-05-21

·GlobeNewswire-Health Care

Orion’s collaborator, MSD, expands clinical development program for opevesostat to women’s cancers

ORION CORPORATION INVESTOR NEWS 21 MAY 2025 at 07.30 EEST Orion’s collaborator, MSD, expands clinical development program for opevesostat to women’s cancers Orion’s collaborator, MSD, has expanded the development program for opevestostat (MK-5684) to now include women’s cancers. A new Phase 2 clinical trial evaluating the safety and efficacy of opevesostat for the treatment of breast, endometrial and ovarian cancers has been posted to ClinicalTrials.gov database. The study is not yet recruiting patients. Further information is available on ClinicalTrials.gov: A Study of MK-5684 in People With Certain Solid Tumors (study identifier: NCT06979596) MSD has global exclusive rights to opevesostat which is an oral, non-steroidal and selective inhibitor of CYP11A1 discovered and developed by Orion. MSD is currently evaluating opevesostat in several clinical trials, including two Phase 3 trials, for the treatment of metastatic castration-resistant prostate cancer. Contact person:Tuukka Hirvonen, Investor Relations, Orion Corporation tel. +358 10 426 2721 Publisher:Orion CorporationCommunicationsOrionintie 1A, FI-02200 Espoo, Finlandwww.orionpharma.com Orion is a globally operating Nordic pharmaceutical company – a builder of well-being for over a hundred years. We develop, manufacture and market human and veterinary pharmaceuticals and active pharmaceutical ingredients. Orion has an extensive portfolio of proprietary and generic medicines and consumer health products. The core therapy areas of our pharmaceutical R&D are oncology and pain. Proprietary products developed by Orion are used to treat cancer, neurological diseases and respiratory diseases, among others. In 2024 Orion's net sales amounted to EUR 1,542 million and the company employed about 3,700 professionals worldwide, dedicated to building well-being. Orion's A and B shares are listed on Nasdaq Helsinki.

临床2期临床3期临床终止

2025-04-25

·微信

AACR「最新突破性研究」，君实、恒瑞、信达、再鼎、海思科等新药入选

当地时间 2025 年 4 月 25 日至 30 日，美国癌症研究协会（AACR）年会将在芝加哥盛大召开。作为癌症领域规模最大、最权威的学术会议之一，每年都会有众多最新研究成果在此亮相。据不完全统计，今年有超过 120 家中国药企亮相 AACR 会议，带来了近 300 项新药研究结果。其中，更是有 24 项中国新药研究入选了「Late-breaking Abstracts（最新突破性研究）」。本文将节选其中 8 项入选「Late-Breaking Research: Clinical Research」的中国新药研究进行简单介绍，仅供读者参阅。君实生物：JS015截图来源：AACR 官网，下同JS015 是君实生物开发的一款重组人源化抗 DKK1 单克隆抗体，主要用于治疗晚期恶性实体瘤，目前处于 Ⅱ 期临床阶段。君实将在此次大会上首次公布 JS015 的初步临床研究数据，这也是国内首个公布临床数据的 DKK1 抑制剂。JS015 能以高亲和力结合肿瘤微环境中分泌的 DKK1，阻断 DKK1 与其配体 LRP5/6 的相互作用，从而激活 Wnt 信号通路。同时，JS015 还能够通过结合 DKK1 促进 NK 细胞活化、抑制髓源性抑制细胞的活性，抑制免疫抑制信号的传导，进而发挥抗肿瘤作用。恒瑞医药：CTLA-4×TIGIT 双抗恒瑞将在本次大会上首次披露其潜在「first-in-class」CTLA-4×TIGIT 双抗的研究数据。安全性和一系列免疫相关的副作用是 CTLA-4 抗体研发中面临的一个挑战。CTLA-4×TIGIT 双抗有望提高 CTLA-4 靶向治疗的安全性。Insight 数据库显示，全球目前还没 CTLA-4×TIGIT 双抗获批，恒瑞之外，赛金生物、免疫方舟也有开发 CTLA-4×TIGIT 双抗，目前都在临床前研究阶段。信达生物：IBI3010IBI3010 是一款靶向 FRα的双表位抗体偶联药物（ADC），信达将在本次大会上公布其用于治疗 FRα表达肿瘤的临床前特性研究数据。今年 1 月，该药首次在国内获批临床，适应症为不可切除、局部晚期或转移性实体瘤。Insight 数据库显示，全球目前仅有 1 款 FRα ADC 获批，即艾伯维/华东医药/武田的索米妥昔单抗。此外，还有 11 款 FRα ADC 正在临床开发阶段。再鼎医药：ZL-1222ZL-1222 是再鼎开发的一款新一代靶向 PD-1 的 IL-12 免疫细胞因子癌症免疫疗法，目前在临床前研究阶段。该药本次入选 LBA 的摘要标题为：通过抗 PD-1 单链抗体顺式递送效力降低的 IL-12 显示出强大的抗肿瘤活性。在多个癌症类型中，IL-12 疗法已展现出可以提供治疗获益的潜力，但因治疗窗口较窄和毒性问题，应用受限。再鼎医药正在评估 ZL-1222 在多个适应证中的效果，该药有望在增强抗肿瘤活性的同时改善全身安全性。海思科：HSK46575SK46575 片是海思科自主研发的一种口服、强效和高选择性的小分子 CYP11A1 抑制剂，拟用于治疗前列腺癌。目前，海思科正在国内开展一项Ⅰ期临床研究，以评估 HSK46575 片在转移性去势抵抗性前列腺癌（mCRPC）患者中的安全性、药代动力学和有效性。本次大会上，海思科将公布该药用于治疗 CRPC 的研究数据。Insight 数据库显示，全球尚无 CYP11A1 抑制剂获批，进度最快的是默沙东的 Opevesostat，在 Ⅲ 期研究阶段。此外，还有四款 CYP11A1 抑制剂在早期临床阶段，其中 2 款是国产药，分别来自海思科（SK46575）、原力生命科学（INV-9956）。原力生命科学：INV-6452INV-6452 是原力生命科学开发的一款 CDK2/4 抑制剂，拟开发用于治疗对当前 CDK4/6 疗法具有耐药性的 HR+/HER2- 乳腺癌。原力生命科学正在国内开展一项多中心、开放性首次人体Ⅰ期研究，以评估 INV-6452 在 HR+/HER2-晚期/转移性乳腺癌或局部晚期/转移性实体瘤成人患者中的安全性、药代动力学和初步抗肿瘤活性。普济远成：CT1113CT1113 是一种双重 USP25/28 抑制剂。普济远成正在国内开展一项开放性、剂量递增的 Ⅰ 期临床研究，以评估 CT1113 治疗复发/难治性急性髓系白血病患者的安全性、耐受性、药代动力学、药效动力学与初步疗效。根据 Insight 数据库，该药是全球首款且目前唯一的 USP25/28 抑制剂。USP25/28 对多种蛋白，特别是 MYC 和 RAS 的稳定表达具有重要维持作用。抑制 USP25/28 可导致这些癌蛋白经由蛋白酶体降解而不能发挥促癌功能，产生抗肿瘤效果。CT1113 可通过阻止 YTHDF2 介导的补体激活来促进抗肿瘤免疫，并增强抗 PD-1 疗法的效果。截图来源：普济远成官微高田生物：HF1K16HF1K16 是高田生物开发的一种注射用全反式维甲酸 (ATRA) 脂质体。高田生物将在本次大会上公布 HF1K16 的Ⅰ期研究（NCT05388487）最新数据。ATRA 是维生素 A 的小分子代谢物，HF1K16 可穿过血管并渗透到肿瘤微环境，释放 ATRA 并促进骨髓源性抑制细胞的成熟，进而发挥杀伤肿瘤细胞的作用。该药已在国内获批开展 Ⅱ 期临床研究，以评估 HF1K16 联合标准治疗在局部晚期或转移性胰腺癌、非小细胞肺癌、脑胶质瘤中的安全耐受性和有效性。除了上述药物，还有一些其它中国公司的新药也入选了 Late-Breaking Research 的其它专题，限于篇幅本文不再一一介绍。数据来源：AACR 官网，Insight 数据库制图封面来源：Insight 制图免责声明：本文仅作信息分享，不代表 Insight 立场和观点，也不作治疗方案推荐和介绍。如有需求，请咨询和联系正规医疗机构。编辑：馨药PR 稿对接：微信 insightxb投稿：微信 insightxb；邮箱 insight@dxy.cn

AACR会议抗体药物偶联物临床结果突破性疗法免疫疗法

100 项与 Opevesostat 相关的药物交易

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研发状态

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适应症	最高研发状态	国家/地区	公司	日期
转移性前列腺癌	临床3期	美国	Merck Sharp & Dohme LLC	2023-12-31
转移性前列腺癌	临床3期	中国台湾	Merck Sharp & Dohme LLC	2023-12-31
转移性前列腺癌	临床3期	英国	Merck Sharp & Dohme LLC	2023-12-31
去势抵抗性前列腺癌	临床3期	西班牙	Merck Sharp & Dohme LLC	2023-12-18
转移性去势抵抗性前列腺癌	临床3期	美国	Orion Oyj	2023-12-18
转移性去势抵抗性前列腺癌	临床3期	美国	默沙东研发（中国）有限公司	2023-12-18
转移性去势抵抗性前列腺癌	临床3期	美国	Merck Sharp & Dohme LLC	2023-12-18
转移性去势抵抗性前列腺癌	临床3期	中国	Merck Sharp & Dohme LLC	2023-12-18
转移性去势抵抗性前列腺癌	临床3期	中国	Orion Oyj	2023-12-18
转移性去势抵抗性前列腺癌	临床3期	日本	Orion Oyj	2023-12-18

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适应症

分期

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT03436485 (CYPIDES, ESMO2024) 人工标引	临床2期	转移性去势抵抗性前列腺癌二线 AR-LBD mutations	134	Opevesostat 5mg BID	願糧鹹襯鹽醖廠艱鬱齋(衊網遞遞糧築築鬱壓醖) = 壓廠遞鹹遞願餘構艱襯膚鏇積顧構遞築膚獵襯 (衊網餘蓋獵醖餘獵膚夢 ) 更多	积极	2024-09-15
				Opevesostat	願糧鹹襯鹽醖廠艱鬱齋(衊網遞遞糧築築鬱壓醖) = 淵鹹顧鹹鏇觸鏇範選艱膚鏇積顧構遞築膚獵襯 (衊網餘蓋獵醖餘獵膚夢 ) 更多
NCT03436485 (CYPIDES, ASCO_GU2024) 人工标引	临床2期	转移性去势抵抗性前列腺癌 AR-LBD mutations	134	MK-5684 5mg BID (AR-LBD mutation-positive)	艱製遞願淵積範鏇襯餘(選簾醖鹹憲觸網網觸觸) = 鑰憲廠膚鬱繭築選蓋範顧鹽願蓋憲淵範積窪築 (願顧艱齋獵獵鬱鏇築襯 ) 更多	积极	2024-01-25
				MK-5684 5mg BID (AR-LBD mutation-negative)	構艱築獵構鑰鏇蓋構築(鹽鹽餘遞蓋齋膚膚網選) = 築壓膚廠構糧獵獵顧範齋夢鬱繭夢窪鹹窪憲艱 (蓋鹽簾簾範艱鏇淵網獵 ) 更多
NCT03436485 (CYPIDES , Pubmed) 人工标引	临床1/2期	去势抵抗性前列腺癌 AR Mutation	92	ODM-208+glucocorticoid/mineralocorticoid replacement+androgen deprivation therapy (ARmut in phase 1)	選鹹獵選壓鹹糧襯餘繭(遞構齋範窪選襯鏇艱選) = Treatment-related adrenal insufficiency was the most common toxicity in phase 1 (n=17, 36.2%; necessitating ODM-208 discontinuation in one patient); this toxicity occurred in six patients (13.3%) at 5 mg twice a day in phase 2. 廠醖餘艱醖糧衊願繭鹽 (醖願鏇願獵獵餘壓衊艱 )	积极	2023-12-26
				ODM-208+glucocorticoid/mineralocorticoid replacement+androgen deprivation therapy (AR wild type in phase 1)
NCT03436485 (CYPIDES, ESMO2022) 人工标引	临床2期	转移性去势抵抗性前列腺癌 AR LBD mutation	45	ODM-208+dexamethasone+fludrocortisone	糧膚選鹹選衊製鬱簾鏇(簾襯窪繭觸製鏇齋餘衊) = 夢窪鏇廠膚壓壓願選齋窪夢積鏇選夢醖積鬱壓 (艱範鹹醖衊壓餘壓鏇觸 ) 更多	积极	2022-09-11
NCT03436485 (CYPIDES, Corporate Publications) 人工标引	临床1/2期	转移性去势抵抗性前列腺癌 AR LBD mutation	44	ODM-208	蓋簾襯憲廠鏇窪鑰構憲(網憲鑰繭製範餘壓鑰艱) = severe adrenal insufficiency 32% 衊積膚淵齋選鏇艱鬱糧 (糧鹽鹽醖蓋繭鏇夢積鑰 )	积极	2022-02-18