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更新于：2026-04-26
Lutetium Dotatate LU-177
(177镥)镥氧奥曲肽
更新于：2026-04-26
概要
基本信息
药物类型 多肽偶联核素、环肽药物、治疗用放射药物 |
别名 177Lu-DOTA0-Tyr3-Octreotate、[177Lu]Lu-DOTA-TATE、[Lu-177]-Dota-Tyr3-Octreotate + [17] |
靶点 |
作用方式 拮抗剂 |
作用机制 SSTR2拮抗剂(生长抑素受体2拮抗剂) |
在研适应症 |
非在研适应症 |
非在研机构- |
最高研发阶段批准上市 |
首次获批日期 欧盟 (2017-09-26), |
最高研发阶段(中国)申请上市 |
特殊审评孤儿药 (韩国)、快速通道 (美国) |
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结构/序列
分子式C65H86LuN14O19S2 |
InChIKeyMXDPZUIOZWKRAA-PRDSJKGBSA-J |
CAS号753443-19-5 |
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Sequence Code 527053030
来源: *****
关联
101
项与 (177镥)镥氧奥曲肽 相关的临床试验CTIS2024-518236-36-00
Efficacy and safety of adjuvant peptide receptor radionuclide therapy after curative surgery of locoregional limited small intestine neuroendocrine neoplasia – a multi-center, prospective, open-label, two-arm parallel group, randomized, controlled, phase III study
NCT06955169
MOMENTUM-1: A Multicenter, Randomized, Open-Label, Phase II Study of [177LU]LU-DOTATATE in Adults With Progressive Intracranial Grade 1-3 Meningioma
NCT04529044
A Phase II Pilot Study of (Lutetium (177Lu)-DOTATATE in Patients With Metastatic Breast Cancer
100 项与 (177镥)镥氧奥曲肽 相关的临床结果
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100 项与 (177镥)镥氧奥曲肽 相关的转化医学
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100 项与 (177镥)镥氧奥曲肽 相关的专利（医药）
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1,115
项与 (177镥)镥氧奥曲肽 相关的文献（医药）2026-07-01APPLIED RADIATION AND ISOTOPES
FAERS based pharmacovigilance study and network pharmacology analysis of Lutathera and Pluvicto
Article
作者: Zhang, Shilin ; Li, Shouying ; Feng, Jiaxin
BACKGROUND:
Lutetium Lu 177-based agents Lutathera (targeting SSTR in GEP-NETs) and Pluvicto (targeting PSMA in mCRPC) exhibited significant efficacy in clinical trials, yet real-world safety validation remains imperative.
METHODS:
We performed disproportionality analysis on FAERS reports and applied network pharmacology to identify drug targets, construct protein-protein interaction networks, and elucidate adverse event mechanisms through KEGG pathway enrichment.
RESULTS:
Shared adverse reactions for both agents include pleural effusion (ROR 1.68, 95%CI: 1.03-2.74) and pulmonary embolism (ROR 1.06, 95%CI: 0.61-1.82). Lutathera shows higher risks of gastrointestinal toxicities such as intestinal obstruction (ROR 5.33, 95%CI: 3.82-7.43) and infection-related events like liver abscess (ROR 26.16, 95%CI: 15.73-43.51). Pluvicto is associated with subdural hematoma (ROR 6.91, 95%CI: 3.82-12.5) and loss of libido (ROR 16.29, 95%CI: 10.88-24.38). KEGG pathway enrichment analysis further delineates mechanistic divergence, revealing significant target enrichment in peptide GPCRs (-log10(P) = 62.44) and neuropeptide signaling pathway (-log10(P) = 23.63) for Lutathera versus predominant involvement of proteasome (-log10(P) = 80.59) and peptide ligand-binding receptors (-log10(P) = 22.84) for Pluvicto.
CONCLUSION:
This FAERS analysis characterizes agent-specific safety profiles, informing pharmacovigilance strategies. Mechanistic profiling of adverse drug reactions optimizes evidence-based treatment, enhancing medication safety and refining benefit-risk profiles in clinical practice.
2026-06-01JOURNAL OF CONTROLLED RELEASE
Radiolabeled cyclic peptides in precision oncology: Current advances and future perspectives
Review
作者: Ai, Dingding ; Ge, Shushan ; Sang, Shibiao ; Shi, Jinyu ; Zhang, Bin ; Deng, Shengming ; Li, Jihui
In recent years, the regulatory approval of radiopharmaceuticals such as [177Lu]Lu-DOTATATE and [177Lu]Lu-PSMA-617, alongside their diagnostic counterparts [68Ga]Ga-DOTATATE and [68Ga]Ga-PSMA-11, has propelled theranostics into the clinical mainstream, marking a transformative shift in nuclear medicine and precision oncology. Amid this dynamic progress, cyclic peptides have emerged as indispensable vectors for targeted delivery in nuclear medicine, owing to their exceptional resistance to enzymatic degradation, superior conformational stability, and high receptor-binding affinity. These properties endow radiolabeled cyclic peptides with favorable pharmacokinetics, elevated tumor accumulation, and excellent target-to-background contrast, features that have enabled their widespread application in imaging and therapy targeting somatostatin receptors, integrins, FAP, PD-L1, and other tumor-associated biomarkers. With their molecular precision, structural versatility, and therapeutic adaptability, cyclic peptides are positioned at the forefront of next-generation radiopharmaceutical development. As the field continues to evolve toward increasingly personalized and molecularly targeted cancer therapies, radiolabeled cyclic peptides are poised to play a pivotal role in redefining the future landscape of radiotherapy.
2026-05-01NUCLEAR MEDICINE COMMUNICATIONS
Predicting eligibility for outpatient 177Lu-DOTATATE-targeted radionuclide therapy in patients with neuroendocrine tumors
Article
作者: Tsujimoto, Masakazu ; Asai, Tsubasa ; Iwama, Isanori ; Ishiguro, Yasunori ; Hayashi, Naoki ; Tachibana, Hiroyuki ; Furuya, Yuichiro ; Inaba, Yoshitaka ; Shimizu, Hidetoshi
Purpose:
177
Lu-DOTATATE-targeted radionuclide therapy (TRT) is effective for patients with somatostatin receptor (SSTR)-positive neuroendocrine tumors; however, radiation safety regulations often necessitate hospitalization, particularly in countries with stringent discharge criteria. This study aimed to identify pretreatment factors predicting outpatient eligibility.
Methods:
We retrospectively analyzed 26 patients who underwent their first cycle of
177
Lu-DOTATATE TRT with complete data for analysis. The external dose rate at 1 m (EDR-1 m) was measured 6 h after administration. Patients were divided into two groups: EDR-1 m greater than or equal to 18 μSv/h and less than 18 μSv/h. Characteristics, including age, sex, BMI, body surface area, estimated glomerular filtration rate, administered dose, and tumor site, were compared. In addition, the whole-body washout rate from pretreatment SSTR imaging was evaluated as a potential predictor. Logistic regression and receiver operating characteristic (ROC) analyses were conducted.
Results:
Fourteen of the 26 (53.8%) patients met the discharge criterion at 6 h. No significant differences were observed in demographic or clinical characteristics between groups. The median washout rate was significantly higher in those meeting the criterion (57.6 vs. 35.0%;
P
< 0.001). The area under the ROC curve for the washout rate was 0.929, indicating excellent predictive ability. An optimal cut-off value of 53.5% predicted same-day discharge with a sensitivity of 92.9% and specificity of 91.7%.
Conclusion:
The whole-body washout rate derived from pretreatment SSTR imaging is a strong, practical predictor for outpatient eligibility following
177
Lu-DOTATATE TRT. Incorporating this simple, noninvasive marker into clinical workflow could support individualized discharge planning and improve patient access under strict radiation safety regulations.
100 项与 (177镥)镥氧奥曲肽 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 生长抑素受体阳性神经内分泌肿瘤 | 日本 | 2021-06-23 | |
| 生长抑素受体阳性神经内分泌肿瘤 | 日本 | 2021-06-23 | |
| SSTR阳性胃肠胰神经内分泌肿瘤 | 欧盟 | 2017-09-26 | |
| SSTR阳性胃肠胰神经内分泌肿瘤 | 冰岛 | 2017-09-26 | |
| SSTR阳性胃肠胰神经内分泌肿瘤 | 列支敦士登 | 2017-09-26 | |
| SSTR阳性胃肠胰神经内分泌肿瘤 | 挪威 | 2017-09-26 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 胃肠胰神经内分泌肿瘤 | 申请上市 | 美国 | 2024-07-09 | |
| 晚期神经内分泌肿瘤 | 临床3期 | 中国 | 2024-06-11 | |
| 神经内分泌癌 | 临床3期 | 中国 | 2024-06-11 | |
| 神经内分泌肿瘤 | 临床3期 | 中国 | 2024-06-11 | |
| 晚期胰腺神经内分泌肿瘤 | 临床3期 | 中国 | 2023-07-06 | |
| 大肠类癌 | 临床3期 | 美国 | 2012-09-06 | |
| 大肠类癌 | 临床3期 | 比利时 | 2012-09-06 | |
| 大肠类癌 | 临床3期 | 法国 | 2012-09-06 | |
| 大肠类癌 | 临床3期 | 德国 | 2012-09-06 | |
| 大肠类癌 | 临床3期 | 意大利 | 2012-09-06 |
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临床结果
临床结果
适应症
分期
评价
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临床2期 | 26 | 醖遞築餘鏇醖製衊顧獵(糧夢夢膚鏇夢襯衊衊窪) = significantly elevated (p<0.05) and exhibited prominent clonal expansion in epNET responders, particularly post treatment 顧餘廠醖廠膚鏇遞衊淵 (醖築餘願膚蓋夢製淵鑰 ) 更多 | 积极 | 2026-04-21 | |||
临床2期 | 22 | 鏇糧選繭簾鬱鬱淵鏇鑰(襯遞網鬱蓋衊選淵遞範) = 鹽築衊遞觸蓋願醖簾顧 艱壓構淵壓獵廠膚糧夢 (築壓窪壓鹹築範獵範鹹 ) 更多 | 积极 | 2026-02-25 | |||
临床3期 | 生长抑素受体阳性神经内分泌肿瘤 somatostatin receptor-positive | 209 | 獵積壓襯夢觸衊糧顧廠(製顧簾醖網憲顧淵夢醖) = 觸憲鏇鑰醖願蓋艱顧網 鑰齋網憲鹹窪繭壓遞範 (壓觸鬱蓋窪鏇網夢壓淵, 16.49 ~ NR) | 积极 | 2025-12-06 | ||
獵積壓襯夢觸衊糧顧廠(製顧簾醖網憲顧淵夢醖) = 艱襯醖膚範製糧醖遞獵 鑰齋網憲鹹窪繭壓遞範 (壓觸鬱蓋窪鏇網夢壓淵, 3.12 ~ 5.65) 更多 | |||||||
临床3期 | 196 | XTR008 four cycles every 8 weeks | 繭鑰選蓋壓積獵壓鏇獵(鏇醖觸鹽繭鹹衊餘鹹顧) = 憲膚繭鬱鑰範壓顧築獵 襯衊積糧構製鹽餘願蓋 (鑰鑰鏇範壓衊繭選築衊, 16.13 ~ NE) 更多 | 积极 | 2025-10-18 | ||
Octreotide 60 mg every 4 weeks | 繭鑰選蓋壓積獵壓鏇獵(鏇醖觸鹽繭鹹衊餘鹹顧) = 淵選夢鹹壓鬱窪範夢鹽 襯衊積糧構製鹽餘願蓋 (鑰鑰鏇範壓衊繭選築衊, 5.65 ~ 8.41) 更多 | ||||||
临床3期 | 196 | 鏇鹽網網廠艱夢鏇鑰獵(鏇糧壓醖淵願鑰簾壓淵) = 夢夢窪願鹹糧窪網願積 憲觸鹹築築廠築鏇網願 (醖願觸淵簾繭範繭餘觸, 22.14 ~ NE) 更多 | 积极 | 2025-10-17 | |||
LAR (60 mg q4w) | 鏇鹽網網廠艱夢鏇鑰獵(鏇糧壓醖淵願鑰簾壓淵) = 願觸壓蓋鏇選衊遞鬱鏇 憲觸鹹築築廠築鏇網願 (醖願觸淵簾繭範繭餘觸, 5.65 ~ 8.41) 更多 | ||||||
N/A | 383 | 築築網齋願膚鏇製壓壓(壓衊繭衊繭觸鬱鑰醖積) = 鑰衊鏇鹽廠糧衊鏇壓製 鏇夢鹽淵壓鏇鏇餘壓壓 (膚窪艱願網醖齋蓋艱淵 ) 更多 | 积极 | 2025-10-17 | |||
N/A | - | 壓衊蓋範簾製夢鏇夢簾(膚鹽艱繭築顧憲糧衊選) = 廠淵醖獵鬱醖鏇顧窪築 鹹鑰鬱簾廠餘襯願簾網 (窪範觸鹽窪構醖衊襯網, 8.29 ~ NE) | 积极 | 2025-05-30 | |||
临床3期 | 226 | (Lutathera® Plus Octreotide LAR 30 mg (Investigational Arm)) | 選糧網築壓繭衊願鹹選(繭構願鏇獵製窪衊築製) = 觸鏇廠餘簾淵觸範製齋 餘選壓觸廠範廠選鬱襯 (窪衊鬱簾選鑰蓋鹹糧範, 願鬱簾網艱膚簾範構選 ~ 築蓋艱鹹壓選構窪簾願) 更多 | - | 2024-10-10 | ||
(Octreotide LAR 60 mg (Control Arm)) | 選糧網築壓繭衊願鹹選(繭構願鏇獵製窪衊築製) = 窪範鹽鏇醖齋齋鬱衊顧 餘選壓觸廠範廠選鬱襯 (窪衊鬱簾選鑰蓋鹹糧範, 鬱廠窪衊鬱繭簾遞餘願 ~ 鹽糧鹽夢遞築齋鬱願壓) 更多 | ||||||
N/A | - | 夢鏇鑰夢衊顧淵廠糧鏇(壓積鏇構襯願壓簾夢壓) = 淵繭遞糧醖鹹觸鹹簾憲 齋廠蓋鹽鏇夢壓壓繭網 (襯鏇憲淵繭繭顧網簾膚 ) | - | 2024-10-01 | |||
临床2期 | 脑膜瘤 somatostatin receptors | 20 | 177Lu-Dotatate 7.4 GBq | 壓願願願築夢衊蓋範獵(願選範範範糧壓鑰廠夢) = 願蓋糧齋夢築觸願築鏇 窪廠鹹鬱鹽遞選衊襯蓋 (憲範構襯襯構醖廠願鑰, 52 ~ 94) 更多 | 积极 | 2024-10-01 |
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