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更新于：2026-01-13
Lutetium Dotatate LU-177
(177镥)镥氧奥曲肽
更新于：2026-01-13
概要
基本信息
药物类型 多肽偶联核素、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)临床3期 |
特殊审评快速通道 (美国)、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
101
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
NCT06955169
MOMENTUM-1: A Multicenter, Randomized, Open-Label, Phase II Study of [177LU]LU-DOTATATE in Adults With Progressive Intracranial Grade 1-3 Meningioma
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
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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1,054
项与 (177镥)镥氧奥曲肽 相关的文献（医药）2026-02-01NUCLEAR MEDICINE COMMUNICATIONS
Threshold optimization for lesion size in lutetium-177 single-photon emission computed tomography imaging: a phantom-based evaluation
Article
作者: Kuyumcu, Serkan ; Demir, Bayram ; Kovan, Bilal ; Mutlu, Eda ; Şenişik, Ahmet Murat
Background:
Accurate lesion volume estimation is essential for reliable voxel-based dosimetry in Lu-177 radionuclide therapy. Conventional fixed-threshold segmentation—particularly the commonly used 40% threshold—can markedly underestimate small lesions due to partial volume effects, leading to substantial errors in quantitative SPECT-based dosimetry.
Purpose:
This study systematically evaluated the relationship between lesion size and optimal threshold values in Lu-177 SPECT/CT imaging, quantified deviations introduced by the fixed 40% threshold, and established size-specific adaptive thresholds to improve segmentation and activity recovery accuracy.
Methods:
A NEMA IEC body phantom with six spherical inserts (0.52–26.5 cm³) was filled with 20 mCi (740 MBq) Lu-177 at an 8 : 1 lesion-to-background ratio. SPECT/CT data were acquired using 60–90 projections with 10–20 s per frame. Images were reconstructed under 180 parameter combinations varying iterations, subsets, and filters. For each sphere, segmentation was performed using the fixed 40% threshold (40%ThS) and an adaptive, volume-matched threshold (AV%ThS) that reproduced the true physical volume.
Results:
Optimal thresholds showed a strong inverse correlation with lesion size, decreasing from ~83% (1.15 cm³) to ~42% (26.5 cm³). The fixed 40% threshold substantially underestimated volumes less than 25 cm³, with quantitative deviations reaching 45% compared to AV%ThS. Best quantitative recovery was achieved with 90 projections × 20 s and OSEM 10 × 10 iterations/subsets with Butterworth filtering (0.45 cycles/cm, order 10).
Conclusion:
A single fixed threshold is insufficient for accurate Lu-177 SPECT/CT dosimetry across diverse lesion sizes. Size-adaptive thresholding combined with optimized reconstruction parameters improves lesion delineation, enhances quantitative accuracy, and reduces dosimetric uncertainty in clinical practice.
2026-01-14PHYSICS IN MEDICINE AND BIOLOGY
Absorbed doses to single cells from radionuclides Tb-161, Pd-103, Pd-109, and Er-165 in different cellular compartments and neighbour cells
Article
作者: Peterson, S W ; Zeevaart, J R ; Bolcaen, J ; Fourie, H
Abstract:
Objective.
Targeted radionuclide therapy using Auger electron (AE) emitting radionuclides is promising for the treatment of small tumour lesions and metastases. However, selecting the optimal AE emitting radionuclide and its ideal targeting cell compartment is necessary to reach their full potential. The aim of this study was to compare the absorbed doses in single cells and from neighbouring cells from emerging AE-emitting radionuclides targeting different cellular compartments.
Approach.
We computed
S
-values in concentric water spheres of unit density, using simulations with Geant4-DNA (v. 11.1.1) and MIRDcell (v. 3.13), for the radionuclides Pd-103 (including its Rh-103 m daughter), Pd-109, Tb-161, Er-165, and commonly studied radionuclides like Lu-177, I-123, I-125, I-131, In-111, and Y-90, focusing on the cell nucleus, cytoplasm, and the cell membrane as target regions; alongside cross-dose effects representing neighbouring cells.
Main Results.
A thorough comparison showed our Geant4-DNA
S
-values align within 10% of other Monte Carlo methods for well-studied geometries (e.g. nucleus, cytoplasm, and the entire cell as targets). When nucleus-bound, Tb-161 showed a 5-fold higher and Pd-103 a 3-fold higher nuclear dose compared to Lu-177. The dose to the cell membrane increased 9-fold for Lu-177, 17-fold for Tb-161, and 30-fold for Pd-103 when the radionuclides are bound to the cell surface compared to their cytoplasmic counterparts. Nuclear dose differences up to 30% from literature values were observed for surface-bound sources and were particularly dependent on the computational method employed. No significant cross-irradiation contributions were seen for the pure AE-emitter Er-165; whereas the nuclear dose doubled due to cross-dose from Tb-161 and Pd-103 located on the surfaces of neighbouring cells in the micrometastasis-mimicking model, mainly from their conversion electron emissions.
Significance.
This study contributes new
S
-values for novel AE-emitters and illustrates the value of cellular dosimetry methods to investigate the optimal cellular target for AE-emitting radionuclides and their potential for treating micrometastasis.
2026-01-01CLINICAL NUCLEAR MEDICINE
Current Status and Future Perspectives of CXCR4-based Radio-theranostics in Human Cancers
Review
作者: Singh, Baljinder ; Dhingra, Kirti ; Nayeem, Muazzam ; Watts, Ankit ; Kaur, Harneet ; Kumar, Suraj ; Malhotra, Pankaj
Among the class of chemokine receptors, the G-protein coupled CXCR4 receptors are overexpressed in more than 30 human cancers. These receptors have been recognized as potential disease targets both for imaging and therapy. CXCR4 receptors are associated with tumor aggressiveness, increased risk of metastasis, and a higher probability of recurrence, which in turn leads to a poor prognosis. Ga-68 Pentixafor PET/CT has been reported to have a high affinity for CXCR4 receptors and offers efficient in vivo imaging suitable for the whole body CXCR4 disease mapping. Ga-68 Pentixafor, as a high throughput PET probe targeting CXCR4 receptors, has provided important diagnostic and prognostic information in human cancers. This PET radioligand provides favorable radiolabelling efficiency, stability, and safety profiling data. This review article discusses the Ga-68 Pentixafor PET/CT and Lu-177/Y-90 Pentixather as “theranostics pair” and their potential applications in hematological and solid cancers.
797
项与 (177镥)镥氧奥曲肽 相关的新闻（医药）2026-01-13
2026-01-13
放射疗法并购临床2期临床结果
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3期 | 生长抑素受体阳性神经内分泌肿瘤 somatostatin receptor-positive | 209 | 齋廠蓋獵鹽鹹窪構鑰夢(鏇襯獵簾艱廠遞簾網獵) = 構鏇齋繭繭鹹鬱襯鏇繭 網積窪窪繭鹽築築餘鬱 (網積積蓋醖築憲構鹹窪, 16.49 ~ NR) | 积极 | 2025-12-06 | ||
齋廠蓋獵鹽鹹窪構鑰夢(鏇襯獵簾艱廠遞簾網獵) = 膚鏇繭醖憲鏇夢廠鹽夢 網積窪窪繭鹽築築餘鬱 (網積積蓋醖築憲構鹹窪, 3.12 ~ 5.65) 更多 | |||||||
临床3期 | 196 | XTR008 four cycles every 8 weeks | 窪選膚衊鬱顧憲繭廠顧(鹹鹹艱觸衊鑰餘襯顧鬱) = 製製鹹製齋淵鏇鹽壓廠 鹹醖範淵夢願願築繭艱 (鹽鑰糧願選艱鑰獵構醖, 16.13 ~ NE) 更多 | 积极 | 2025-10-18 | ||
Octreotide 60 mg every 4 weeks | 窪選膚衊鬱顧憲繭廠顧(鹹鹹艱觸衊鑰餘襯顧鬱) = 憲鑰壓壓鬱鹹製獵繭鑰 鹹醖範淵夢願願築繭艱 (鹽鑰糧願選艱鑰獵構醖, 5.65 ~ 8.41) 更多 | ||||||
临床3期 | 196 | 鹹鑰艱網鏇餘窪衊範選(壓鑰觸艱憲餘鑰壓觸繭) = 壓遞壓鏇鑰鬱製糧醖夢 願鏇夢鹽鑰鹽構衊觸蓋 (糧壓願廠構淵構夢壓鬱, 22.14 ~ NE) 更多 | 积极 | 2025-10-17 | |||
LAR (60 mg q4w) | 鹹鑰艱網鏇餘窪衊範選(壓鑰觸艱憲餘鑰壓觸繭) = 廠鑰糧夢淵壓鑰構襯窪 願鏇夢鹽鑰鹽構衊觸蓋 (糧壓願廠構淵構夢壓鬱, 5.65 ~ 8.41) 更多 | ||||||
N/A | 383 | 淵齋鬱選憲願獵網膚構(艱鏇襯簾廠顧齋糧簾繭) = 觸糧遞廠鑰餘鑰齋艱襯 壓鹹簾觸膚襯窪衊餘窪 (鏇顧艱選艱遞糧膚願齋 ) 更多 | 积极 | 2025-10-17 | |||
N/A | - | 鏇淵鏇淵遞鏇製蓋鏇蓋(窪製衊繭憲鏇鬱糧淵衊) = 壓積鹽齋衊糧淵淵遞鏇 衊繭積願餘鑰範觸積獵 (窪窪糧廠廠築衊夢選網, 8.29 ~ NE) | 积极 | 2025-05-30 | |||
临床3期 | 226 | (Lutathera® Plus Octreotide LAR 30 mg (Investigational Arm)) | 鑰願簾鹹齋鹽膚範積築(構襯製餘艱鬱齋蓋範觸) = 齋膚齋憲廠獵鏇繭鹽衊 窪築憲範窪繭衊構獵網 (艱選餘醖壓願餘範齋艱, 遞製憲簾繭鏇構鏇蓋選 ~ 蓋鑰糧製糧窪願糧鏇壓) 更多 | - | 2024-10-10 | ||
(Octreotide LAR 60 mg (Control Arm)) | 鑰願簾鹹齋鹽膚範積築(構襯製餘艱鬱齋蓋範觸) = 遞構網顧憲蓋觸廠憲築 窪築憲範窪繭衊構獵網 (艱選餘醖壓願餘範齋艱, 繭壓餘繭網憲襯網選觸 ~ 壓鬱簾餘憲襯觸網鹹襯) 更多 | ||||||
N/A | - | 憲憲構網膚鹹鑰鬱製艱(鑰鹽願鑰鏇鹹繭衊鹽襯) = 製願顧醖襯鬱窪選願膚 顧構範膚簾鹽齋獵夢製 (淵齋夢範餘糧製廠繭鹹 ) | - | 2024-10-01 | |||
临床2期 | 195 | (177Lu-D >880 mCi) | 壓艱襯衊鹹壓餘艱淵構(醖艱襯壓膚網網顧膚襯) = 積鏇遞積鏇廠築窪繭夢 觸獵壓簾網衊鑰積簾簾 (製餘衊膚廠窪鑰鹹範廠, 90 ~ 100) 更多 | 不佳 | 2024-10-01 | ||
(177Lu-D 800 ± 10%) | 壓艱襯衊鹹壓餘艱淵構(醖艱襯壓膚網網顧膚襯) = 鬱鏇鬱鹽範餘窪淵範餘 觸獵壓簾網衊鑰積簾簾 (製餘衊膚廠窪鑰鹹範廠, 73 ~ 100) 更多 | ||||||
临床2期 | 脑膜瘤 somatostatin receptors | 20 | 177Lu-Dotatate 7.4 GBq | 網憲範繭製鏇觸鹹願餘(鬱顧觸醖糧鹽艱淵憲繭) = 夢窪網餘餘齋繭鑰簾憲 淵壓襯憲糧鏇構網衊衊 (選積築願構蓋蓋憲構繭, 52 ~ 94) 更多 | 积极 | 2024-10-01 | |
N/A | - | 33 | 構窪膚鹹鬱獵夢夢遞願(餘醖顧繭築遞鏇選選廠) = 願餘淵製醖壓選淵獵遞 餘鑰鏇觸夢餘蓋鏇蓋醖 (繭衊鹹夢憲繭鹹蓋衊簾, 0.87) 更多 | 积极 | 2024-10-01 | ||
68Ga-DOTATATE | 構窪膚鹹鬱獵夢夢遞願(餘醖顧繭築遞鏇選選廠) = 製窪憲齋積遞簾構顧憲 餘鑰鏇觸夢餘蓋鏇蓋醖 (繭衊鹹夢憲繭鹹蓋衊簾, 0.87) 更多 |
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