更新于：2024-09-27

Oxycodone

羟考酮

更新于：2024-09-27

概要

概要

基本信息

简介Oxycodone是一种阿片类止痛药物，有时也被称为麻醉剂。它是一种通过结合大脑和脊髓中的μ、κ和δ受体来缓解疼痛的阿片类药物。Oxycodone的化学名称为4,5 α-环氧-14-羟基-3-甲氧基-17-甲基吗啡酮-6-酮。该药物在美国和中国获得批准，并由Collegium制药公司生产。Oxycodone是一种高效的止痛药物，常用于管理中度到重度疼痛，如癌症、手术或创伤引起的疼痛。然而，由于其成瘾和滥用的潜在风险，它被列为受控物质，只能在医疗专业人士的指导下使用。

药物类型

小分子化药

别名

(-)-14-Hydroxydihydrocodeinone、4,5-Epoxy-14-hydroxy-3-methoxy-17-methylmorphinan-6-one、4,5alpha-Epoxy-14-hydroxy-3-methoxy-17-methylmorphinan-6-one

+ [21]

靶点

Opioid receptors

作用机制

Opioid receptors激动剂(阿片样受体激动剂)

治疗领域

神经系统疾病其他疾病

在研适应症

疼痛术后疼痛药物滥用

非在研适应症

癌症疼痛慢性疼痛腰痛+ [5]

原研机构

Collegium Pharmaceutical, Inc.

在研机构

Ensysce Biosciences, Inc.Napp Pharmaceutical Holdings Ltd.

Collegium Pharmaceutical, Inc.

非在研机构

Mundipharma Research GmbH & Co. KG

US Food & Drug Administration

萌蒂（中国）制药有限公司

+ [1]

最高研发阶段批准上市

首次获批日期

中国 (2004-01-21),

疼痛

最高研发阶段(中国)批准上市

特殊审评突破性疗法 (美国)、快速通道 (美国)

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结构

分子式C18H21NO4

InChIKeyBRUQQQPBMZOVGD-XFKAJCMBSA-N

CAS号76-42-6

关联

428

项与羟考酮相关的临床试验

NCT06602271 / Not yet recruiting临床3期

A Multicenter, Randomized, Double-Blind, Placebo- and Active-Controlled Study to Evaluate the Efficacy and Safety of PF614 for the Treatment of Moderate to Severe Pain After Abdominoplasty

The goal of this clinical trial is to evaluate the analgesic activity of PF614 (an oral oxycodone prodrug extended-release analgesic) for control of postsurgical pain in subjects scheduled for abdominoplasty surgery. The main question to be answered is:
• To assess the analgesic efficacy of PF614 compared to oxycodone hydrochloride (an immediate-release opioid analgesic) and placebo in subjects with moderate to severe pain following abdominoplasty Participants will be asked to take oral blinded doses of study medication at about one hour before surgery starts, and then every 6 hours after surgery for up to 4 days.
Participants will be asked to:
* Rate their pain on a 0-10 numerical rating scale (NRS) at various timepoints up to 5 days following surgery;
* Tell us about the need for rescue medication if they continue to have moderate-to-severe pain;
* Tell us about any side effects or adverse effects that they may experience to help us understand the safety and tolerability of the test medications;
* Provide periodic blood samples to help us understand how much study drug is in their system.
Participants will stay in a clinic setting and be monitored for safety for 5 days following surgery. We anticipate that participants will be discharged on Day 5, pending medical review, and then keep a diary to record study-related pain and adverse effects for an additional 2-4 days after discharge.

开始日期2025-03-01

申办/合作机构

Ensysce Biosciences, Inc.

NCT06539741 / Not yet recruitingN/AIIT

Mechanisms of Variability in the Analgesic Response to Ibuprofen Following Third Molar Extraction

Nonsteroidal anti-inflammatory drugs (NSAIDs), like ibuprofen, are recommended as first-line treatment for post-surgical dental pain. However, there is variability in analgesic response, and some patients require supplemental opioids for adequate pain relief. The goal of this study is to identify the factors that contribute to the need for opioid after third molar extraction to help limit unnecessary opioid prescriptions in patients who will have good pain relief with ibuprofen alone.

开始日期2024-10-01

申办/合作机构

University of Pennsylvania

[+1]

ChiCTR2400089641 / SuspendedN/AIIT

Oxycodone combined with pulsed radiofrequency technology for the management of refractory cancer pain in patients with spinal metastases

开始日期2024-10-01

申办/合作机构-

100 项与羟考酮相关的临床结果

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100 项与羟考酮相关的转化医学

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100 项与羟考酮相关的专利（医药）

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4,848

项与羟考酮相关的文献（医药）

2025-02-01·BIOMATERIALS

The immunological and pharmacokinetic evaluation of Lipid-PLGA hybrid nanoparticle-based oxycodone vaccines

Article

作者: Pravetoni, Marco ; Hamid, Fatima A ; Rostamizadeh, Kobra ; Walter, Debra L. ; Runyon, Scott ; Vigliaturo, Jennifer R ; Zhang, Chenming ; Vigliaturo, Jennifer R. ; DeHority, Riley ; Hamid, Fatima A. ; Bian, Yuanzhi ; Hu, He ; Ehrich, Marion ; Walter, Debra L

2025-01-01·CLINICA CHIMICA ACTA

Direct analysis in real time mass spectrometry (DART-MS/MS) for rapid urine opioid detection in a clinical setting

Article

作者: El-Khoury, Joe M ; Tran, Minh Nguyet ; Cassella-McLane, Gina ; Shang, Emily ; Choucair, Ibrahim

BACKGROUND AND AIMS:

Current laboratory methods for opioid detection involve an initial screening with immunoassays which offers efficient but non-specific results and a subsequent liquid chromatography-tandem mass spectrometry (LC-MS/MS) confirmation which offers accurate results but requires extensive sample preparation and turnaround time. Direct Analysis in Real Time (DART) tandem mass spectrometry is evaluated as an alternative approach for accurate opioid detection with efficient sample preparation and turnaround time.

MATERIALS AND METHODS:

DART-MS/MS was optimized by testing the method with varying temperatures, operation modes, extraction methods, hydrolysis times, and vortex times. The method was evaluated for 12 opioids by testing the analytical measurement range, percent carryover, precision studies, stability, and method-to-method comparison with LC-MS/MS.

RESULTS:

DART-MS/MS shows high sensitivity and specificity for the detection of 6-acetylmorphine, codeine, hydromorphone, oxymorphone, hydrocodone, naloxone, buprenorphine, norfentanyl, and fentanyl in urine samples. However, its performance was suboptimal for norbuprenorphine, morphine and oxycodone.

CONCLUSION:

In this proof-of-concept study, DART-MS/MS is evaluated for its rapid quantitative definitive testing of opioids drugs in urine. Further research is needed to expand its application to other areas of drug testing.

2024-12-31·Gut microbes

Prescription opioids induced microbial dysbiosis worsens severity of chronic pancreatitis and drives pain hypersensitivity

Article

作者: Jalodia, Richa ; Dawra, Rajinder ; Roy, Sabita ; Ghosh, Nillu ; Tao, Junyi ; Kesh, Kousik ; Singh, Salma

Opioids, such as morphine and oxycodone, are widely used for pain management associated with chronic pancreatitis (CP); however, their impact on the progression and pain sensitivity of CP has never been evaluated. This report investigates the impact of opioid use on the severity of CP, pain sensitivity, and the gut microbiome. C57BL/6 mice were divided into control, CP, CP with morphine/oxycodone, and either morphine or oxycodone alone groups. CP was induced by administration of caerulein (50ug/kg/h, i.p. hourly x7, twice a week for 10 weeks). The mouse-to-pancreas weight ratio, histology, and Sirius red staining were performed to measure CP severity. Tail flick and paw pressure assays were used to measure thermal and mechanical pain. DNA was extracted from the fecal samples and subjected to whole-genome shotgun sequencing. Germ-free mice were used to validate the role of gut microbiome in sensitizing acute pancreatic inflammation. Opioid treatment exacerbates CP by increasing pancreatic necrosis, fibrosis, and immune-cell infiltration. Opioid-treated CP mice exhibited enhanced pain hypersensitivity and showed distinct clustering of the gut microbiome compared to untreated CP mice, with severely compromised gut barrier integrity. Fecal microbiota transplantation (FMT) from opioid-treated CP mice into germ-free mice resulted in pancreatic inflammation in response to a suboptimal caerulein dose. Together, these analyses revealed that opioids worsen the severity of CP and induce significant alterations in pain sensitivity and the gut microbiome in a caerulein CP mouse model. Microbial dysbiosis plays an important role in sensitizing the host to pancreatic inflammation.

249

项与羟考酮相关的新闻（医药）

2024-09-19

·BioSpace

Ensysce Biosciences Submits Phase 3 Protocol to the FDA

Phase 3 Study to Assess PF614 Efficacy in Treating Post-Surgical Pain SAN DIEGO, CA / ACCESSWIRE / September 19, 2024 / Ensysce Biosciences, Inc. (NASDAQ:ENSC) (“Ensysce” or the “Company”), a clinical-stage pharmaceutical company developing innovative solutions for severe pain relief while reducing the potential for opioid abuse and overdose, today announced it has submitted to the FDA its PF614-301 protocol of the study, “A Multicenter, Randomized, Double-Blind, Placebo-and Active-Controlled Study to Evaluate the Efficacy and Safety of PF614 for the Treatment of Moderate to Severe Pain after Abdominoplasty”. Included in the Phase 3 study is the Company’s statistical analysis plan for review and input by the FDA. The study, once finalized with the FDA, will be conducted through four to six clinical sites in the United States, and is designed to assess the analgesic efficacy of PF614 compared to placebo in subjects with moderate-to-severe pain following abdominoplasty. Additionally, Ensysce will evaluate PF614 versus an active comparator, the use of rescue medication and the safety and tolerability of PF614. Dr. Bill Schmidt, Chief Medical Officer of Ensysce, commented, “The review of this study protocol represents another key milestone that brings us one step closer to executing the last clinical phase of evaluation for PF614. We anticipate the results of this Phase 3 trial will continue to prove the positive qualities of PF614 over existing oxycodone products. We remain dedicated to bringing PF614, a ‘next-generation opioid’, to market.” Dr. Lynn Kirkpatrick, CEO of Ensysce, offered, “We believe that the features of PF614 will be a game changer for the treatment of short-term severe pain. The fact that PF614 delivers the pain-relieving qualities of OxyContin but lasts twice as long, should alleviate the common problem of recurring breakthrough pain between dosing. In parallel with its reduced abuse potential, PF614 is anticipated to offer this market a superior pain product. We look forward to conducting this trial and expect results in late 2025.” About Ensysce Biosciences Ensysce Biosciences is a clinical-stage company using its proprietary technology platforms to develop safer prescription drugs. Leveraging its Trypsin-Activated Abuse Protection (TAAP TM ) and Multi-Pill Abuse Resistance (MPAR®) platforms, the Company is developing unique, tamper-proof treatment options for pain that minimize the risk of both drug abuse and overdose. Ensysce’s products are anticipated to provide safer options to treat patients suffering from severe pain and assist in preventing deaths caused by medication abuse. The platforms are covered by an extensive worldwide intellectual property portfolio for a wide array of prescription drug compositions. For more information, please visit . Forward-Looking Statements Statements contained in this press release that are not purely historical may be deemed to be forward-looking statements for the purposes of the safe harbor provisions under The Private Securities Litigation Reform Act of 1995 and other federal securities laws. Without limiting the foregoing, the use of words such as “may,” “intends,” “can,” “might,” “will,” “expect,” “plan,” “possible,” “believe” and other similar expressions are intended to identify forward-looking statements. The product candidates discussed are in clinic and not approved and there can be no assurance that the clinical programs will be successful in demonstrating safety and/or efficacy, that Ensysce will not encounter problems or delays in clinical development, or that any product candidate will ever receive regulatory approval or be successfully commercialized. All forward-looking statements are based on estimates and assumptions by Ensysce’s management that, although Ensysce believes to be reasonable, are inherently uncertain. All forward-looking statements are subject to risks and uncertainties that may cause actual results to differ materially from those that Ensysce expected. In addition, Ensysce’s business is subject to additional risks and uncertainties, including among others, the initiation and conduct of preclinical studies and clinical trials; the timing and availability of data from preclinical studies and clinical trials; expectations for regulatory submissions and approvals; potential safety concerns related to, or efficacy of, Ensysce’s product candidates; the availability or commercial potential of product candidates; the ability of Ensysce to fund its continued operations, including its planned clinical trials; the dilutive effect of stock issuances from our fundraising; and Ensysce’s and its partners’ ability to perform under their license, collaboration and manufacturing arrangements. These statements are also subject to a number of material risks and uncertainties that are described in Ensysce’s most recent quarterly report on Form 10-Q and current reports on Form 8-K, which are available, free of charge, at the SEC’s website at Any forward-looking statement speaks only as of the date on which it was made. Ensysce undertakes no obligation to publicly update or revise any forward-looking statement, whether as a result of new information, future events or otherwise, except as required under applicable law. Ensysce Biosciences Company Contact: Lynn Kirkpatrick, Ph.D. Chief Executive Officer (858) 263-4196 Ensysce Biosciences Investor Relations Contact: Shannon Devine MZ North America Main: 203-741-8811 ENSC@mzgroup.us SOURCE: Ensysce Biosciences Inc. View the original press release on accesswire.com

临床3期

2024-09-12

·drugs

Racial Differences Seen in Pain Rx for Older Adults With Hip Fracture

THURSDAY, Sept. 12, 2024 -- Racial differences exist in opioid pain management for Medicare beneficiaries after a hip fracture, according to a study published online Sept. 11 in the Journal of the American Geriatrics Society . Kaleen N. Hayes, Pharm.D., Ph.D., from Brown University in Providence, Rhode Island, and colleagues assessed whether the receipt and dose of opioids differed between Black and White older adult U.S. Medicare beneficiaries with a hip fracture as they transitioned back to the community setting. The analysis included 164,170 older adults (mean age, 82.7 years) with hip fracture. The researchers found that overall use of opioids in the community was similar between Black and White Medicare beneficiaries. However, Black beneficiaries had lower average doses in their first 90 days in both total cumulative doses (institutional postacute care [PAC] group, 165 fewer milligram morphine equivalents [MMEs]; no PAC, 167 fewer MMEs) and average MME per days' supply of medication (PAC, –3.0 fewer MMEs per day; no PAC, –4.7 fewer MMEs per day). In secondary analyses, the greatest differences were seen among Asian beneficiaries (e.g., 617 to 653 fewer cumulative mg oxycodone). “Future work should examine whether these differences result in disparities in short- and long-term health outcomes,” the authors write. Several authors disclosed ties to relevant organizations. Abstract/Full Text Whatever your topic of interest, subscribe to our newsletters to get the best of Drugs.com in your inbox.

临床结果

2024-09-10

·华昊中天

优替德隆破解化疗周期限制难题，谱写晚期乳腺癌长期高质量生存篇章

以下文章来源于医脉通肿瘤科，作者医脉通 // 随着医疗技术水平的进步，乳腺癌患者的长期预后得到了极大改善。然而对于转移性乳腺癌患者而言，预后依旧不容乐观，且治疗难度相对较大。化疗作为乳腺癌治疗中最常用的治疗手段之一，能有效控制病灶，最大限度地延长生存。但是随着紫杉类和/或蒽环类药物在早期乳腺癌治疗中的广泛使用，患者后续治疗的交叉耐药和多重耐药的问题愈加凸显¹,²。这使既往紫杉类治疗失败的晚期乳腺癌患者后续可选化疗药物选择有限。2021年，我国首个自主研发的埃坡霉素类抗肿瘤药物优替德隆上市，打破了既往晚期乳腺癌紫杉类治疗失败后的选择限制。多项研究表明，优替德隆具有抗肿瘤活性强、安全性良好的特点，可为紫杉类治疗失败的患者带来疗效获益，为晚期乳腺癌患者带来新的希望³-⁵。本期佳木斯市肿瘤医院芦明月主治医师将为我们分享一例接受优替德隆治疗的晚期乳腺癌诊疗病例，并邀请到佳木斯市肿瘤医院孙红梅教授深入剖析并解读病例。该患者为伴有多发转移的HR+/HER2-晚期乳腺癌，在五线接受了优替德隆联合方案治疗后，取得了显著疗效，缓解了临床症状，生活质量显著提高。病例分享病例:HR+晚期乳腺癌患者伴双肺转移、胸膜转移、多发骨转移癌专家简介芦明月主治医师佳木斯市肿瘤医院肿瘤内一科主治医师佳木斯市医学会化疗专业委员会秘书佳木斯市抗癌协会消化道肿瘤MDT委员会委员黑龙江省抗癌协会第二届淋巴瘤委员会委员黑龙江省医学会靶向治疗专业委员会委员黑龙江省医师协会肺癌青年委员会委员黑龙江省医疗保健国际交流促进会肿瘤放射治疗专业委员会委员黑龙江省慢性病肺癌专业委员会委员中国老年医学学会肿瘤康复委员会委员 ① 患者基本信息患者，女，42岁，以“右乳癌术后”为主诉入院治疗。否认高血压、冠心病、糖尿病等慢性病史，否认乳腺癌家族史。ECOG评分1分。 ② 诊疗过程（外院治疗）手术治疗 2012年10月19日，于中国人民解放军空军总医院行右乳腺癌改良根治术。术后病理提示：浸润性导管癌（直径1.5cm），腋窝淋巴结可见癌转移（1/25）；免疫组化提示：PR（2+），ER（+），HER2（-）。术后辅助治疗 2012年11月1日开始行表柔比星联合环磷酰胺序贯紫杉醇脂质体（AC-T）方案治疗，共8个周期。 2013年7月开始口服他莫昔芬内分泌治疗，患者因个人原因未遵医嘱，仅口服1年，定期复查病情稳定。疾病进展 2016年9月就诊于天津医科大学肿瘤医院，行相关检查提示双肺转移；后自行口服中药1年，未经系统治疗。无疾病生存期（DFS）47个月。 2017年9月患者开始出现腰痛，双下肢轻度活动受限；同年12月病情加重，伴憋喘，进一步就诊于我院。 ③ 相关检查及诊断完善相关抽血检验及影像学检查。抽血检验提示CEA、CA15-3升高，雌二醇未达到绝经。影像学检查提示双侧胸腔积液，肺转移，多发骨转移。余未见明显异常。胸腔积液沉渣病理提示：见恶性肿瘤细胞，符合乳腺癌来源。临床诊断：右侧乳腺浸润性癌（T1cN1M1 Ⅳ期）、多发骨转移癌、双肺转移癌、胸膜转移癌、恶性胸腔积液、癌性疼痛（8分）。 ④ 晚期诊疗过程（本院治疗）晚期一线 2017年12月27日开始行吉西他滨联合顺铂（GP）方案治疗，共6个周期，其中前2个周期顺铂为胸腔灌注。治疗2周后憋喘等症状均缓解，疼痛控制尚可，生活质量明显改善。同时给予唑来膦酸骨保护治疗，以及羟考酮镇痛治疗，以及放疗。放疗结束后，疼痛控制良好，可停用吗啡类止痛药物。治疗期间定期复查，疗效评估为部分缓解（PR）；第5周期、第6周期化疗结束后出现Ⅲ度骨髓抑制，无法耐受化疗。 2018年6月14日开始氟维司群维持治疗，因患者未绝经，给予醋酸戈舍瑞林抑制卵巢功能。 2019年1月9日内分泌维持治疗6个月，疗效评估为PR。 2019年1月19日，患者因“胸闷、气短症状”入院，完善胸部超声提示：右侧大量胸腔积液，考虑疾病进展（PD）。无进展生存期（PFS）13个月。晚期二线 2019年2月2日，开始行哌柏西利联合来曲唑方案治疗，同时给予醋酸戈舍瑞林抑制卵巢功能。治疗期间定期复查，未见新增病灶，胸腔积液缓慢增多，最佳疗效为疾病稳定（SD）。 2021年12月15日，出现乏力、胸闷、气短、呼吸困难症状。完善相关检查提示：胸腔积液较前增多，新增肝脏病灶。PFS 34个月。晚期三线 2022年1月7日，开始行西达本胺联合依西美坦方案治疗，治疗后出现血红蛋白65g/l，血小板71*10^9/l，对症治疗。患者无法耐受治疗。 2022年2月18日复查血红蛋白78g/l，血小板73*10^9/l。完善骨穿，活检病理提示：未见异常。 2022年4月13日西达本胺联合依西美坦治疗2个月后，完善相关检查，提示PD。PFS 3个月。4月14日，患者出现全程肉眼血尿半个月，血块堵塞尿道致排尿困难（尿潴留），病情危重；对症支持治疗；血常规：血红蛋白59g/l，血小板63*10^9/l。晚期四线 2022年4月25日开始口服卡培他滨治疗，同时给予2次顺铂膀胱灌注治疗。治疗后排尿困难及血尿症状缓解，期间反复出现中/重度贫血，给予输血治疗。 2023年3月20日出现心悸、呼吸困难加重，（吸氧）血氧饱和度83%，心率112次/分；饮食差。 2023年3月24日，复查发现左侧胸腔积液增多，心包积液明显增多，新增肝脏病灶，疗效评估为PD。PFS 11个月。 2023年3月28日给予心包积液穿刺引流术，病理回报提示：（心包积液）见腺癌细胞，提示乳腺导管癌来源。晚期五线 2023年4月3日开始给予贝伐珠单抗联合优替德隆治疗。治疗1~2个周期后心包积液，逐渐吸收，生活质量明显改善；治疗期间手足麻木，考虑周围神经毒性，给予氨磷汀、维生素B12。 2023年5月14日，优替德隆联合方案治疗2个周期后，心包积液较前减少，肝脏病灶较前减少，膀胱病灶消失，疗效评估为PR。后续治疗期间定期复查。 2024年6月10日，优替德隆联合方案治疗18个周期后，疗效评估为持续PR。目前患者无贫血，手足麻木，ECOG评分1分，心包积液明显吸收，症状缓解。2024年7月10日，行第19个周期优替德隆联合方案治疗，治疗仍在继续，PFS＞15个月。图1 优替德隆联合治疗期间疗效评估（肝脏病灶）图2 优替德隆联合治疗期间疗效评估（膀胱病灶) 图3 优替德隆联合治疗期间疗效评估（心包积液/胸腔积液） ⑤ 治疗回顾图4 诊疗过程回顾专家点评：突破桎梏，持之以恒，优替德隆为长期用药打下坚实基础专家简介孙红梅教授佳木斯市肿瘤医院肿瘤内一科主任主任医师黑龙江省医学会化疗专业委员会副主任委员黑龙江省医师协会消化道肿瘤MDT专业委员会副主任委员黑龙江省医师协会中西医结合肿瘤专业委员会常委黑龙江省老年学学会老年肿瘤专业委员会常委黑龙江省医学会靶向治疗专业委员会委员 CSCO化疗专业委员会委员 CSCO中西医结合专家委员会委员中国老年医学学会肿瘤康复专业委员会委员佳木斯市医学会化疗专业委员主任委员佳木斯市抗癌协会消化道肿瘤MDT专业委员会主任委员该患者为HR+/HER2-晚期乳腺癌，并伴有骨转移、双肺转移、胸膜转移、恶性胸腔积液，在接受了包括铂类、吉西他滨、卡培他滨、哌柏西利、氟维司群、来曲唑等多种药物的多线治疗后再次PD，出现了呼吸困难、心悸等心包积液症状。并且该患者在既往治疗过程中多次出现无法耐受治疗的情况，这使得选择后续治疗方案时，不仅要保证疗效以控制疾病，还要充分考量药物安全性及患者耐受性以保障患者可以坚持治疗。对于有内脏转移、内分泌耐药或不耐受的HR+/HER2-的患者来说，CSCO BC指南推荐首选化疗⁶。但考虑到该患者既往已接受过紫杉类治疗，此时在选择化疗方案时应考虑选择可回避紫杉类耐药机制的化疗药物，为患者创造获得更优疗效和更长PFS的机会。相关研究表明，多药耐药是导致肿瘤化疗失败的原因之一，其中P-糖蛋白（P-gp）是一种典型的多药耐药转运蛋白，可介导主动转运将如紫杉烷类的P-gp底物类药物转运至细胞外，降低药物在细胞内的积累，导致药物疗效降低并最终发生耐药⁷。优替德隆是新一代的埃坡霉素类微抑制剂，虽然其作用机制与紫杉类相似，但优替德隆不是P-gp底物，不会与肿瘤细胞膜上高表达的P-gp结合，可避免因活性药物成分被转运至细胞外导致的药物浓度降低的问题⁷。基于此作用机制，多药耐药的肿瘤依然可对优替德隆敏感。优替德隆的关键性Ⅲ期临床研究BG01-1323L研究显示，优替德隆联合卡培他滨在紫杉类和蒽环类耐药的乳腺癌患者中疗效显著³。这一研究也证明了，优替德隆的作用机制优势可转化为患者的疗效获益。目前，该方案已在中国获批用于既往接受过至少一种化疗方案的复发或转移性乳腺癌患者，但该患者为卡培他滨经治且PD，因此需要个体化调整优替德隆治疗方案。根据中国晚期乳腺癌规范诊疗指南推荐，贝伐珠单抗联合化疗方案可改善晚期乳腺癌PFS，对于多药耐药的患者，化疗联合贝伐珠单抗可为患者带来疗效获益⁸。因此该病例中采用了优替德隆联合贝伐珠单抗方案，以求通过抗血管生成剂和新型微管抑制剂的协同作用提升治疗疗效。该患者接受优替德隆联合贝伐珠单抗的治疗疗效显著，在接受治疗1~2个周期后心包积液逐渐吸收，临床症状得到了明显改善，生活质量得到了显著提高。在接受优替德隆联合贝伐珠单抗治疗2个周期后，患者心包积液及肝脏转移灶较前明显减少，膀胱病灶消失，疗效评估为PR。该患者在五线接受优替德隆联合方案治疗后快速获得PR也进一步在真实世界中证明了，优替德隆优越作用机制可转化为良好临床疗效。除了优越疗效外，从安全性的角度来看，患者在接受优替德隆联合方案治疗过程中耐受性良好，仅发生手足麻木的周围神经毒性，在接受氨磷汀对症治疗后好转。优替德隆关键性Ⅲ期临床研究结果提示，尽管优替德隆联合卡培他滨治疗中有部分患者会出现周围神经毒性，但经过对症治疗或调整剂量等临床处理后，96%的患者可恢复至0~Ⅰ级，中位恢复时间仅为3.1周³。良好的安全性使乳腺癌患者更易于坚持优替德隆治疗，并从中持续获益。CSCO BC指南提出，持续的化疗相对短期化疗（6~8个周期）更能延长患者PFS和总生存期（OS）⁶。在BG01-1323L研究中优替德隆联合卡培他滨方案最长使用到了34个周期，这进一步为患者持续接受优替德隆治疗提供了循证医学证据³。在此病例中，患者已接受19个周期优替德隆联合方案治疗，已突破传统化疗周期，并且目前患者疗效评估为持续PR，仍在继续接受优替德隆联合方案治疗，PFS已超过15个月。由此可见，优替德隆不仅能快速控制控制病灶，缓解患者临床症状，还能从长期治疗中为患者提供持久获益并改善生活质量。该病例证明了优替德隆联合贝伐珠单抗方案的优异疗效和良好安全性，为目前正在进行的优替德隆联合贝伐珠单抗治疗晚期乳腺癌的临床研究提供了真实世界证据。期待相关研究能够取得积极结果，进一步为优替德隆联合方案治疗乳腺癌提供更多循证医学证据，使更多乳腺癌患者能够从优替德隆治疗中获益。参考文献： 1. Rivera E, Gomez H. Chemotherapy resistance in metastatic breast cancer: the evolving role of ixabepilone[J]. Breast Cancer Research : BCR, 2010, 12(Suppl 2): S2. 2. Bashmail H A, Alamoudi A A, Noorwali A, et al. Thymoquinone Enhances Paclitaxel Anti-Breast Cancer Activity via Inhibiting Tumor-Associated Stem Cells Despite Apparent Mathematical Antagonism[J]. Molecules, 2020, 25(2): 426. 3. Xu B, Sun T, Zhang Q, et al. Efficacy of utidelone plus capecitabine versus capecitabine for heavily pretreated, anthracycline- and taxane-refractory metastatic breast cancer: final analysis of overall survival in a phase III randomised controlled trial[J]. Annals of Oncology: Official Journal of the European Society for Medical Oncology, 2021, 32(2): 218-228. 4. Shi Y, Wang P, Zhu Y, et al. 401P Utidelone in combination with etoposide and bevacizumab in HER2-negative breast cancer with brain metastasis (UTOBIA-BM): A prospective, single-arm, phase II trial[J]. Annals of Oncology, 2023, 34: S349-S350. 5. Gangloff A, Hsueh W A, Kesner A L, et al. Estimation of paclitaxel biodistribution and uptake in human-derived xenografts in vivo with (18)F-fluoropaclitaxel[J]. Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine, 2005, 46(11): 1866-1871. 6. 中国临床肿瘤学会指南工作委员会 . 中国临床肿瘤学会（CSCO）乳腺癌诊疗指南 2023[M]. 北京: 人民卫生出版社, 2023. 7. Zhang P, Sun M, Qiu R, et al. Phase I clinical and pharmacokinetic study of UTD1, a genetically engineered epothilone analog in patients with advanced solid tumors[J]. Cancer Chemotherapy and Pharmacology, 2011, 68(4): 971-978. 8. 国家肿瘤质控中心乳腺癌专家委员会, 中国抗癌协会乳腺癌专业委员会, 中国抗癌协会肿瘤药物临床研究专业委员会. 中国晚期乳腺癌规范诊疗指南(2022版)[J]. 中华肿瘤杂志, 2022, 44(12): 1262-1287. 往期推荐 “优”效例证｜疗效、安全双优，优替德隆实现乳腺癌治疗长期持久获益有“例”可循｜从临床研究到临床实践，优替德隆为晚期消化道肿瘤患者带来新选择 ASCO中国之声 | 史艳侠教授：曙光已现，未来可期，优替德隆破解晚期前列腺癌治疗困局更“优”选择，护尔安康，优替德隆为晚期卵巢癌患者带来生存获益求解更要“优”解｜挑战多线！优替德隆为多线经治的乳腺癌脑转移患者带来获益寻“优”入微，启迪新思，优替德隆点亮晚期实体瘤患者希望之光潘跃银教授：新一代微管抑制剂优替德隆或将成为晚期乳腺癌一线化疗“新秀” 多线治疗再获益——看优替德隆如何为伴内脏转移的HR+/HER2-乳腺癌患者带来更长生存 “胰腺”生机，优替德隆注射液联合吉西他滨为晚期胰腺癌治疗带来更“优”获益 ESMO中国之声｜姜愚教授：捷报频传，优替德隆单药治疗为晚期软组织肉瘤提供化疗新方案 ESMO新声，破局“优”选 | 优替德隆突破晚期乳腺癌脑转移治疗瓶颈以“优”解忧，共赴卓越丨突破化疗使用周期限制，优替德隆为晚期乳腺癌患者带来持续生存获益排兵布局，更“优”生机｜CDK4/6抑制剂进展后，优替德隆为HR+/HER2-晚期乳腺癌患者提供治疗新选择曲径通“优”，优替德隆助力ADC药物治疗失败后晚期乳腺癌后线治疗再获益优替德隆治疗多线经治激素受体阳性肝转移晚期乳腺癌患者带来长生存获益欧阳取长教授：二十年磨一剑，优替德隆进医保为乳腺癌治疗利刃添光！王树森教授：原创新药优替德隆进入国家医保目录，传统细胞毒药物再添利器！

放射疗法

100 项与羟考酮相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D05312	羟考酮	N02AA05	DB00497

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
疼痛	中国	Napp Pharmaceutical Holdings Ltd.	2004-01-21

未上市

10 条进展最快的记录,

后查看更多信息

适应症	最高研发状态	国家/地区	公司	日期
肿瘤疼痛	临床3期	德国	Mundipharma Research GmbH & Co. KG	2014-11-01
腰痛	临床3期	美国	Collegium Pharmaceutical, Inc.	2012-08-01
术后疼痛	临床3期	-	萌蒂（中国）制药有限公司	2011-07-01
癌症疼痛	临床3期	-	萌蒂（中国）制药有限公司	2011-01-01
癌症	临床3期	-	萌蒂（中国）制药有限公司	2011-01-01
骨关节炎	临床3期	比利时	Mundipharma Research GmbH & Co. KG	2009-05-01
骨关节炎	临床3期	捷克	Mundipharma Research GmbH & Co. KG	2009-05-01
骨关节炎	临床3期	芬兰	Mundipharma Research GmbH & Co. KG	2009-05-01
骨关节炎	临床3期	德国	Mundipharma Research GmbH & Co. KG	2009-05-01
骨关节炎	临床3期	匈牙利	Mundipharma Research GmbH & Co. KG	2009-05-01

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临床结果

适应症

分期

评价

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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


NCT03859024 (CTgov)	临床4期	尿道狭窄 \| 术后疼痛	48	Acetaminophen+Ibuprofen 800 mg+Oxycodone (Standard Protocol)	鏇餘築製鏇艱顧顧廠積(廠鹹齋糧壓願鹽築廠廠) = 鏇積鏇餘遞積簾夢製憲觸製鏇蓋壓醖築鏇積膚 (鹽築餘糧築獵鹹壓網艱, 範糧鏇膚淵鑰構憲鹽糧 ~ 襯鹽壓觸壓獵獵繭遞淵) 更多	-	2024-09-19
				Acetaminophen+Ibuprofen 800 mg+celebrex+Dexamethasone+Oxycodone+Bupivacaine+Gabapentin (Enhanced Recovery Protocol)	鏇餘築製鏇艱顧顧廠積(廠鹹齋糧壓願鹽築廠廠) = 繭醖鹹鏇獵窪糧遞廠選觸製鏇蓋壓醖築鏇積膚 (鹽築餘糧築獵鹹壓網艱, 膚觸鏇簾鑰獵艱淵艱鏇 ~ 選繭顧蓋構觸艱襯鬱積) 更多
NCT04791761 (CTgov)	临床1/2期	术后疼痛	73	Opioid disposal education+Acetaminophen+Ibuprofen+Oxycodone (Opioid Pain Control)	鬱淵糧範製觸遞範觸選(壓獵憲糧淵廠鬱積觸願) = 鏇壓壓衊艱鏇鹽膚艱鬱壓鹹簾製膚選襯淵遞顧 (艱廠壓餘壓廠鏇鹹衊獵, 顧襯願築蓋艱淵網鑰醖 ~ 廠醖鹽製膚鬱鏇餘範襯) 更多	-	2024-08-16
				Acetaminophen+Ibuprofen (Non-opioid Pain Control)	鬱淵糧範製觸遞範觸選(壓獵憲糧淵廠鬱積觸願) = 艱觸夢選憲壓範構網範壓鹹簾製膚選襯淵遞顧 (艱廠壓餘壓廠鏇鹹衊獵, 衊齋簾顧襯觸艱壓膚願 ~ 衊艱壓構襯鑰願顧窪簾) 更多
NCT04015908 (CTgov)	临床4期	-	100	Pregabalin+Acetaminophen+Celecoxib+Oxycodone (Multi-modal)	積鏇鏇獵鬱選艱齋遞繭(遞鹹襯繭壓夢繭簾淵廠) = 襯蓋憲積憲願廠網壓膚觸廠遞築廠艱範遞網餘 (膚顧淵窪網遞鹽繭膚繭, 窪構壓壓窪艱窪願醖齋 ~ 夢襯顧範淵廠鏇願膚網) 更多	-	2024-07-08
				Percocet (Control)	積鏇鏇獵鬱選艱齋遞繭(遞鹹襯繭壓夢繭簾淵廠) = 顧範淵艱窪網顧醖製簾觸廠遞築廠艱範遞網餘 (膚顧淵窪網遞鹽繭膚繭, 選鏇壓簾鬱淵製選構構 ~ 齋簾齋齋願夢夢齋膚範) 更多
PF614-201 (Biospace) 人工标引	临床2期	-	-	PF614	積餘網壓築築鹹鏇顧繭(夢鹽廠淵鹽顧繭範製憲) = demonstrated time-to-efficacy onset for the analgesia effect and significant decrease of pain intensity versus placebo of PF614 at two different dose levels 積選蓋築築積網願衊齋 (遞簾鬱積鬱鬱齋艱壓願 )	积极	2023-12-14
				placebo
NCT04285853 (CTgov)	临床4期	前交叉韧带损伤	98	Oxycodone (Oxycodone Arm)	選衊範蓋築窪積憲選鏇(積鑰網範顧遞壓壓觸網) = 淵鏇糧醖餘淵蓋糧簾廠網網齋窪遞鹹觸廠壓膚 (齋醖鏇廠願鑰襯積願製, 範網膚餘鏇鏇蓋鑰齋糧 ~ 鹽簾糧選餘衊製顧鏇製) 更多	-	2023-10-11
				Placebo oral tablet (Placebo Arm)	選衊範蓋築窪積憲選鏇(積鑰網範顧遞壓壓觸網) = 鹽願鑰範淵淵製構齋衊網網齋窪遞鹹觸廠壓膚 (齋醖鏇廠願鑰襯積願製, 鑰繭鹹選觸遞鹽糧繭願 ~ 願衊製鹹窪夢獵壓廠壓) 更多
NCT04149964 (CTgov)	临床4期	瘘 \| 术后疼痛	65	Acetaminophen/Hydrocodone 325 mg/7.5 mg oral tablet+Acetaminophen 325 mg Oral Tablet (Standard of Care Arm)	膚蓋積糧廠膚壓餘齋夢(構構遞膚膚鑰顧鏇蓋築) = 壓積齋構艱遞艱範膚構壓衊衊鹽壓觸衊廠餘鹽 (夢蓋選遞範觸餘鏇糧鹹, 範廠齋餘積顧艱糧夢構 ~ 齋鏇齋選顧衊獵製積醖) 更多	-	2023-08-31
				Acetaminophen 650 mg Oral Tablet+OxyCODONE 5 mg Oral Tablet (Study Arm)	膚蓋積糧廠膚壓餘齋夢(構構遞膚膚鑰顧鏇蓋築) = 廠選鹽鹽願築襯繭網艱壓衊衊鹽壓觸衊廠餘鹽 (夢蓋選遞範觸餘鏇糧鹹, 鬱積獵遞遞製繭繭醖餘 ~ 憲製鏇獵夢夢壓廠壓鹹) 更多
NCT04429022 (RA-TLH, CTgov)	临床3期	术后疼痛	68	Local anesthetic injection+Local anesthetic injection with ropivacaine at abdominal laparoscopic port sites+Hydromorphone+Acetaminophen+Ketorolac+Celecoxib+Oxycodone+Gabapentin (Prospective Cohort)	淵網鹹積鑰遞夢鑰製製(鏇齋鹽鹹鹹鹽網積艱簾) = 繭製艱糧鹹製願襯淵憲淵簾遞鹹膚鑰夢鬱艱範 (衊鏇艱衊繭製繭餘顧艱, 簾淵壓鑰構構願願憲願 ~ 願壓夢繭膚夢製築製鹹) 更多	-	2023-08-01
				Hydromorphone (Historical Control)	淵網鹹積鑰遞夢鑰製製(鏇齋鹽鹹鹹鹽網積艱簾) = 構淵簾憲艱夢鏇構蓋蓋淵簾遞鹹膚鑰夢鬱艱範 (衊鏇艱衊繭製繭餘顧艱, 願淵夢艱窪積構壓遞鹹 ~ 夢衊鬱網窪範膚壓壓鬱) 更多
NCT02573831 (Pubmed)	临床4期	-	22	Oxycodone	淵淵簾鑰鹽選鬱網廠窪(築簾選願壓獵淵網餘選) = 餘艱獵顧構製鏇願繭壓鹽遞選窪製願憲鹹淵膚 (齋繭醖積範選蓋窪觸網 ) 更多	积极	2023-06-21
				Placebo	淵淵簾鑰鹽選鬱網廠窪(築簾選願壓獵淵網餘選) = 醖選艱鏇製繭鹹衊夢襯鹽遞選窪製願憲鹹淵膚 (齋繭醖積範選蓋窪觸網 ) 更多