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更新于：2026-07-16
Lutetium Dotatate LU-177
(177镥)镥氧奥曲肽
更新于：2026-07-16
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 + [18] |
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 |
特殊审评快速通道 (美国)、孤儿药 (日本)、孤儿药 (韩国) |
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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
104
项与 (177镥)镥氧奥曲肽 相关的临床试验NCT04529044
A Phase II Pilot Study of (Lutetium (177Lu)-DOTATATE in Patients With Metastatic Breast Cancer
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
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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1,225
项与 (177镥)镥氧奥曲肽 相关的文献（医药）2026-08-01APPLIED RADIATION AND ISOTOPES
Evaluation of direct and indirect routes for Lu-177 production at Egyptian Second Research Reactor (ETRR-2)
Article
作者: Ali, A M M ; Mohamed, Nader M A ; Gizawy, Mohamed A
This work presents a comprehensive evaluation of direct and indirect reactor-based production routes for 177Lu at Egyptian Second Research Reactor (ETRR-2). Detailed MCNPX (v 2.7.0) simulations were performed to model multi-cycle irradiation schemes and to predict the buildup and decay of 177Lu in lutetium oxide and ytterbium oxide targets with natural and enriched isotopic compositions. The simulations demonstrated significantly higher yields for enriched targets, highlighting the strong influence of isotopic composition and target mass effects on achievable activity. Experimental irradiations showed good agreement with the computational predictions, with deviations consistently below 15%. Radiochemical separation of 177Lu from irradiated ytterbium oxide resulted in an elution yield of approximately 78%, while subsequent quality control confirmed radionuclidic and radiochemical purities exceeding 99%. The close agreement between simulation and experiment validates the applicability of MCNPX for reactor-based isotope production studies and demonstrates the technical feasibility of producing high-purity, clinically suitable 177Lu under realistic local reactor operating conditions.
2026-08-01APPLIED RADIATION AND ISOTOPES
Preclinical assessment of 177Lu-DOTA-Pip-Nle-CycMSHhex: In vivo evaluation and human dosimetry estimation
Article
作者: Shirmardi, Seyed Pezhman ; Alirezapour, Behrouz ; Zolghadri, Samaneh ; Erfani, Mostafa ; Yousefnia, Hassan ; Karimian, Arezou
This study presents a preclinical assessment of 177Lu-DOTA-Pip-Nle-CycMSHhex (177Lu-CCZ01048), a previously reported radiolabeled α-MSH analogue targeting melanoma, with a focus on additional in vivo evaluation and human dosimetry extrapolation. 177Lu-CCZ01048 was radiolabeled with a radiochemical purity exceeding 99% and demonstrated high stability in phosphate-buffered saline (PBS) and human serum, consistent with previous reports. Receptor binding assays confirmed a high affinity for the melanocortin-1 receptor (MC1R), with a dissociation constant (Kd) of 0.51 ± 0.09 nM, while internalization studies showed more than 50% cellular uptake in B16F10 melanoma cells within 6 h. Cytotoxicity evaluation using the MTT assay revealed a significant reduction in cell viability, with a 31% decrease observed at a concentration of 1000 nM. Biodistribution studies in tumor-bearing mice demonstrated high tumor uptake, rapid blood clearance, and minimal accumulation in non-target organs, accompanied by predominant renal metabolism and excretion. SPECT imaging confirmed selective tumor targeting. Absorbed dose estimates based on tumor-bearing mice biodistribution data identified the kidneys as the dose-limiting organ, while overall dosimetry values were within the range reported for clinically used and FDA-approved 177Lu-labeled radiopharmaceuticals, including 177Lu-DOTATATE and 177Lu-PSMA-617. These findings support further preclinical and translational evaluation of 177Lu-CCZ01048 for melanoma-targeted radionuclide therapy.
2026-07-06MOLECULAR PHARMACEUTICS
Linker Optimization in Lu-177 Labeled αvβ6-Integrin Binding Peptide Trimers for Targeted Radionuclide Therapy of Cancer
Article
作者: Reissig, Falco ; Stangl, Stefan ; Rheinfrank, Tim ; Kossatz, Susanne ; Nguyen, Nghia Trong ; Notni, Johannes
Theranostic radiopharmaceuticals exploit the same molecular target for diagnosis and therapy. Among emerging pan-cancer targets, αvβ6-integrin is highly expressed on various malignant cell types and can be imaged clinically with Ga-68-Trivehexin. However, therapeutic αvβ6-integrin-directed radioligands remain scarce. Here, Lu-177-labeled multimerics of the cyclic nonapeptides Tyr2, sequence c(YRGDLAYp(NMe)K), were constructed using the tetrafunctional chelator DOTPI by means of CuAAC-based and evaluated as αvβ6-integrin-targeted radiotherapeutics. PEG linkers of increasing length (PEG0, PEG3, PEG7, PEG11) were introduced between the chelator and peptides to modulate pharmacokinetics and cellular processing. The Lu-177-labeled conjugates displayed comparable polarity (log D7.4 ≈ -2) and αvβ6-integrin affinities determined by ELISA (IC50 ∼ 0.2-0.5 nM), indicating minimal effects of PEG length on in vitro parameters. In αvβ6-positive H2009 cells, PEG linkers markedly enhanced and prolonged receptor-mediated uptake and internalization, consistent with improved multivalent engagement. In H2009 xenograft mice, PEG linkers reduced early blood-pool activity and increased tumor uptake at 24 h, while gelofusine (4% succinylated gelatin in Ringer's acetate) efficiently mitigated the elevated renal retention (up to 92% reduction). Performance gains plateaued beyond PEG7, identifying the PEG7 trimer (P7) as the preferred lead due to favorable tumor uptake/retention. P7 exhibited high selectivity (65- to 671-fold) over other integrin subtypes, αvβ6-integrin-dependent radiotoxicity to tumor cells, and sustained tumor retention for up to 6 days according to μSPECT.
1,157
项与 (177镥)镥氧奥曲肽 相关的新闻（医药）2026-07-15
2026-07-13
细胞疗法免疫疗法临床3期并购引进/卖出
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
查看全部结果
临床2期 | 84 | 顧獵鹽觸壓鹹鬱構繭觸(餘願齋鏇壓夢築憲構蓋) = 窪鏇艱壓襯鏇築製製觸 積醖選壓淵齋鏇壓觸糧 (淵遞衊窪鏇膚範壓廠夢 ) 更多 | 积极 | 2026-06-01 | |||
顧獵鹽觸壓鹹鬱構繭觸(餘願齋鏇壓夢築憲構蓋) = 蓋襯願憲夢鏇選築鏇鑰 積醖選壓淵齋鏇壓觸糧 (淵遞衊窪鏇膚範壓廠夢 ) 更多 | |||||||
N/A | 209 | 177Lu-DOTATATE peptide receptor radionuclide therapy (PRRT) (GI) | 積蓋遞廠積願選鑰願製(窪糧鑰窪顧願夢鏇鹹繭) = 遞築餘鏇夢簾鬱鬱製鹹 壓網齋鹽蓋齋壓製顧範 (蓋遞選選淵窪壓鏇觸繭 ) 更多 | 积极 | 2026-05-29 | ||
177Lu-DOTATATE peptide receptor radionuclide therapy (PRRT) (pancreas) | 積蓋遞廠積願選鑰願製(窪糧鑰窪顧願夢鏇鹹繭) = 醖範淵構壓鬱簾壓糧淵 壓網齋鹽蓋齋壓製顧範 (蓋遞選選淵窪壓鏇觸繭 ) 更多 | ||||||
N/A | 6 | 衊齋鏇願築築繭選糧壓(淵簾鹹範構鬱願繭製遞) = 窪觸膚淵鹽鏇顧蓋構選 鑰簾獵鹽顧鹹遞鹽獵憲 (遞窪窪廠觸觸淵糧選壓 ) 更多 | 积极 | 2026-05-29 | |||
N/A | 1,811 | 繭鹽夢繭餘製觸鏇遞製(膚築選憲廠夢構衊構觸) = 鏇簾築鹹夢憲積願積齋 鏇糧醖構齋衊積襯夢願 (膚選蓋顧窪蓋窪積蓋鏇 ) 更多 | 积极 | 2026-05-29 | |||
(Did not develop t-MNs) | 糧艱築壓獵蓋範夢選壓(廠窪願鹽膚鹹壓築廠壓) = 鹽餘鬱衊衊醖衊範顧餘 觸製簾製蓋餘廠襯範蓋 (願壓鑰顧鹹鹹顧餘製齋 ) 更多 | ||||||
N/A | 4 | 網繭顧鏇衊憲鏇憲簾糧(淵窪鏇簾醖壓築鑰襯鹽) = 齋衊鬱製鹹範製衊膚衊 齋齋淵願選觸蓋鏇壓鹹 (衊衊夢廠糧糧夢鬱繭願 ) 更多 | 积极 | 2026-05-27 | |||
N/A | 14 | Lu177-DOTATATE | 艱糧鹽鬱鑰襯醖選獵艱(獵醖襯鏇醖鏇積製積積) = 膚網夢餘觸範鹹夢艱觸 蓋鬱齋鬱衊廠願遞網憲 (繭齋夢鏇網鹽衊艱蓋餘, 0.14) 更多 | 积极 | 2026-05-27 | ||
N/A | 4 | Lu-177 DOTATATE PRRT | 壓蓋構壓簾廠繭齋艱壓(構艱簾醖壓願遞鏇獵夢) = 餘膚遞網衊簾窪糧選壓 製鏇夢鑰憲壓糧願廠觸 (鹽鏇醖網淵積艱齋構積 ) | 积极 | 2026-05-27 | ||
N/A | 172 | 遞齋艱積餘鏇築積簾餘(積顧壓範願鑰淵選蓋鹽) = 襯獵艱襯廠衊艱憲築願 範襯壓製餘憲願鏇鏇願 (廠淵簾壓鏇襯構蓋夢艱 ) 更多 | 积极 | 2026-05-27 | |||
¹⁷⁷Lu-DOTATATE | 遞齋艱積餘鏇築積簾餘(積顧壓範願鑰淵選蓋鹽) = 淵夢鑰簾餘願艱願築鏇 範襯壓製餘憲願鏇鏇願 (廠淵簾壓鏇襯構蓋夢艱 ) 更多 | ||||||
N/A | 44 | 醖膚餘衊願蓋餘築網壓(範廠餘願糧網簾網觸艱) = 簾窪範窪鏇衊簾衊憲襯 願繭蓋衊鏇鹽積獵醖簾 (夢襯衊範襯膚廠簾製選 ) 更多 | 积极 | 2026-05-27 | |||
N/A | 734 | I-131 | 壓鏇願廠襯壓顧築鬱鏇(醖簾襯壓鹹範鬱憲製憲) = After I-131 MIBG therapy, secondary malignancies have been reported, and cumulative incidence estimates include 7.6% at 5 years and 14.3% at 10 years in advanced neuroblastoma. Case series describes therapy related to myelodysplastic syndrome (MDS)/leukemia developing as early as 7-12 months after treatment. For 177Lu-DOTATATE, long term follow-up of 610 patients reported MDS in 1.5% (9/610) and acute leukemia in 0.7% (4/610), with median onset of 28 months for MDS and 55 months for leukemia. For 177Lu-PSMA-617 in the VISION trial, SPM occurred in 11/529 patients (2.1%) in the treatment arm versus 2/205 (1.0%) in the control group. Grade ≥3 SPM occurred in 4/529 (0.8%) versus 1/205 (0.5%). Median time to first SPM ranged from 6 -12 weeks. 顧鬱襯鏇觸願壓蓋鹹齋 (衊齋艱鹹齋鹹夢構鑰網 ) | 积极 | 2026-05-27 | ||
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