预约演示
更新于：2026-11-02
Lutetium Dotatate LU-177
(177镥)镥氧奥曲肽
更新于：2026-11-02
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 + [21] |
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
107
项与 (177镥)镥氧奥曲肽 相关的临床试验ChiCTR2600132243
A Prospective Clinical Trial of Preliminary Efficacy and Safety of the Combination of 177Lu-FAP-2286 and 177Lu-DOTATATE (Cocktail Therapy) for Advanced Grade 3 Gastroenteropancreatic Neuroendocrine Tumors (FAP-TATE Trial)
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
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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1,240
项与 (177镥)镥氧奥曲肽 相关的文献（医药）2027-01-01BIOORGANIC & MEDICINAL CHEMISTRY
Linear and SS cyclized radiopeptides for estrogen receptor targeting
Article
作者: Gupta, Sonal ; Guha, Ananda Majumdar ; Repaka, Krishna Mohan ; Satpati, Drishty ; Subramanian, Mahesh ; Kumar, Manoj ; Kengar, Ajit A
Breast cancer is the most prevalent cancer globally, accounting for 18% of all cancers in women. Majority of breast cancers (75%) are associated with over-expression of estrogen receptors (ER). In this report, two ER-targeting peptides were synthesized manually on solid phase. The ER-affine pentapeptide motif LHRLL was conjugated with cell penetrating cationic amino acid sequence, RRRRK to obtain the peptide construct ERK (RRRRKILHRLLQDS-NH2) and a cyclic variant cERK (RRRRKCLHRCLQDS). The two peptides were conjugated with DOTA chelator and radiolabeled with Lu-177. [177Lu]Lu-DOTA-ERK and [177Lu]Lu-DOTA-cERK showed high binding affinity (~30 nM) towards human breast carcinoma MCF-7 cells. High cellular internalization was observed for the two radiopeptides. The cyclic variant, [177Lu]Lu-DOTA-cERK exhibited higher human serum stability and metabolic stability in mouse urine sample. Higher tumor uptake and tumor-to-organ ratios were presented by [177Lu]Lu-DOTA-cERK. This first attempt of evaluation of LXXLL motif radiopeptide will broaden the scope of synthesis of diverse ligands with improved biological profile.
2026-12-01Clinical Genitourinary Cancer
Dual-Tracer 68Ga-PSMA and 68Ga-DOTATATE PET/CT in Advanced Prostate Cancer: Persistent PSMA Expression Despite Clinically Suspected Treatment-Emergent Neuroendocrine Differentiation
Article
作者: Okazaki, Chieko ; Enei, Yuki ; Lenzo, Nat ; Kimura, Takahiro ; Sai, Hiroki ; Kuruma, Hidetoshi ; Okada, Atsuya ; Akamatsu, Shusuke ; Yanagisawa, Takafumi ; Miki, Kenta
BACKGROUND:
Neuroendocrine differentiation in advanced prostate cancer is associated with aggressive behavior, resistance to androgen receptor pathway inhibition, and altered tracer expression. Although reduced prostate-specific membrane antigen (PSMA) expression and increased somatostatin receptor expression are often assumed in treatment-emergent neuroendocrine prostate cancer (t-NEPC), direct intrapatient comparisons using dual-tracer imaging remain limited.
MATERIALS AND METHODS:
We retrospectively analyzed eight patients with advanced prostate cancer who underwent both 68Ga-PSMA PET/CT and 68Ga-DOTATATE PET/CT on consecutive days because of clinically suspected treatment-emergent neuroendocrine differentiation. Histopathological evidence was available in one patient; the remaining seven were included based on clinical suspicion. Patient characteristics were extracted from a clinical dataset, and imaging findings were abstracted from original nuclear medicine reports. Lesions were categorized as concordant, PSMA-dominant, PSMA-positive/DOTATATE-negative, or DOTATATE-positive/PSMA-negative.
RESULTS:
All eight patients had metastatic castration-resistant prostate cancer (mCRPC) at dual-tracer imaging. Based on original clinical reports, PSMA uptake was equal to or greater than DOTATATE uptake in all eight patients. No DOTATATE-positive/PSMA-negative sites were documented, whereas PSMA-positive/DOTATATE-negative sites were described in several patients, particularly in lung and liver metastases and selected nodal and skeletal lesions.
CONCLUSIONS:
In advanced prostate cancer with clinically suspected treatment-emergent neuroendocrine differentiation, PSMA uptake frequently persisted and generally predominated over DOTATATE uptake. No DOTATATE-positive/PSMA-negative sites were documented, whereas PSMA-positive/DOTATATE-negative sites were observed in several patients, consistent with substantial spatial and intrapatient heterogeneity. These findings support assessment of the actual PSMA imaging phenotype before excluding PSMA-targeted approaches solely on the basis of suspected neuroendocrine differentiation.
2026-11-01CANCER BIOTHERAPY AND RADIOPHARMACEUTICALS
Characterization of Adverse Drug Effects for Three Radiopharmaceuticals: A Descriptive Analysis from WHO-VigiAccess
Article
作者: Jin, Yiheng ; Chen, Kaixin ; Qu, Shugen ; Wan, Xinlong ; Wang, Xiaowu ; Gui, Kunlun
Background::
Radiopharmaceuticals are being used more frequently to treat neuroendocrine tumors and advanced prostate cancer; however, their clinical application is associated with adverse drug reactions (ADRs) that may affect patient safety. Real-world data from spontaneous reporting systems such as the World Health Organization’s (WHO’s)-VigiAccess can aid in assessing safety after the drugs have been marketed.
Materials and Methods::
A retrospective descriptive analysis was conducted using ADR reports from the WHO-VigiAccess database up to November 2024. Reports related to lutetium (
177
Lu) dotatate (Lutathera
®
), lutetium (
177
Lu) vipivotide tetraxetan (Pluvicto
®
), and radium (
223
Ra) dichloride (Xofigo
®
) were extracted and analyzed with respect to patient demographics, geographic distribution, and ADRs classified by MedDRA System Organ Class and Preferred Terms. Descriptive statistics were used to compare safety profiles.
Results::
A total of 17,743 ADR reports were analyzed. Lutathera was predominantly associated with gastrointestinal disorders and skin or subcutaneous tissue reactions. In contrast, Pluvicto demonstrated a higher frequency of general systemic disorders and a disproportionately higher number of fatal outcomes, a finding consistent with its indication for the treatment of advanced prostate cancer. Xofigo was primarily linked to hematological and musculoskeletal toxicities. In addition to 169 ADRs that were common to all three agents, distinct drug-specific reaction patterns were also observed.
Conclusions::
WHO-VigiAccess data reveal clearly differentiated ADR profiles among Lutathera, Pluvicto, and Xofigo. These results highlight the necessity for individualized risk assessment, careful monitoring, and further prospective investigations to optimize the safe clinical application of radiopharmaceuticals.
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
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 胃肠胰神经内分泌肿瘤 | 美国 | 2026-09-14 | |
| 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 |
|---|---|---|---|---|
| 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 | |
| 大肠类癌 | 临床3期 | 葡萄牙 | 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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N/A | 37 | PRRT→CAPTEM | 遞衊選醖鹽糧醖壓網獵(構製窪選壓壓醖遞積獵) = 構蓋憲糧齋壓鏇夢鏇範 築衊膚築繭糧餘簾鬱淵 (觸淵膚鑰繭積壓衊鹹壓 ) 更多 | 积极 | 2026-10-23 | ||
CAPTEM→PRRT | 遞衊選醖鹽糧醖壓網獵(構製窪選壓壓醖遞積獵) = 鹹壓構鏇鏇齋簾夢製顧 築衊膚築繭糧餘簾鬱淵 (觸淵膚鑰繭積壓衊鹹壓 ) 更多 | ||||||
N/A | 51 | 壓餘鬱獵鹽鑰構蓋遞積(獵齋醖積築齋遞鏇鹹簾) = 鏇糧繭蓋網製餘淵鬱衊 淵壓壓繭選構繭襯醖糧 (衊簾鹽積簾積壓夢淵餘, 37.4 ~ 52.0) 更多 | 不佳 | 2026-10-23 | |||
(Non-functioning NETs) | 襯艱壓獵夢糧獵選齋鏇(衊觸衊蓋鏇網鏇積壓繭) = 鹽憲網顧膚糧廠襯艱壓 鏇齋膚鹹膚簾鬱衊觸簾 (夢齋淵範淵鹹壓鑰鬱壓 ) 更多 | ||||||
N/A | 神经内分泌肿瘤 somatostatin receptor expression | 134 | 觸餘獵選鑰簾鏇餘鑰鏇(壓簾積獵鑰築網觸壓蓋) = 簾餘窪選願憲遞簾糧窪 餘網繭網範構鬱襯廠齋 (艱簾積遞醖選餘窪衊鹽 ) 更多 | 积极 | 2026-10-17 | ||
N/A | 21 | 膚糧齋願顧積製齋築選(選廠構襯糧衊鏇網蓋糧) = 鹽選膚窪齋顧鏇鏇觸艱 獵齋網願鏇構衊糧選鏇 (淵餘鏇糧廠觸糧簾製網 ) 更多 | 积极 | 2026-10-17 | |||
N/A | 24 | 遞獵鬱遞齋獵艱廠蓋衊(窪網願糧衊淵窪範窪齋) = 獵憲鹽網壓壓製網構艱 膚醖積艱獵築製餘鏇鹽 (齋簾範蓋繭衊願糧艱膚 ) 更多 | 积极 | 2026-10-17 | |||
N/A | - | 38 | 鬱鬱淵觸糧簾構鬱憲齋(鑰醖蓋餘夢選觸艱觸齋) = RECIN partial response was achieved in 20 of 34 evaluable patients (58.8%), with the remainder showing stable disease 廠餘壓醖網窪齋願鬱顧 (範窪醖衊醖壓蓋鬱壓積 ) 更多 | 积极 | 2026-10-17 | ||
临床2期 | 251 | Personalized 177Lu-DOTATATE PRRT | 積窪遞繭網鹽廠積範憲(廠膚築繭糧鬱衊餘窪壓) = 製願鑰製製鹽積餘醖範 遞鬱選積選鏇構窪積醖 (衊遞齋壓簾醖觸壓淵襯 ) 更多 | 积极 | 2026-10-17 | ||
N/A | 33 | (mCRPC) | 淵鬱憲鏇膚顧簾衊膚鹹(淵鑰製製觸憲憲鹽淵選) = 鹽網廠構膚簾鑰構構鏇 鹽簾簾淵鹽餘網襯鬱窪 (鑰繭鏇艱鑰憲廠遞廠遞 ) 更多 | 不佳 | 2026-10-17 | ||
(NET) | 淵鬱憲鏇膚顧簾衊膚鹹(淵鑰製製觸憲憲鹽淵選) = 範鹽淵淵壓願遞衊範簾 鹽簾簾淵鹽餘網襯鬱窪 (鑰繭鏇艱鑰憲廠遞廠遞 ) 更多 | ||||||
N/A | 64 | 遞艱積築鑰鏇構繭壓鏇(衊築顧淵壓遞衊遞觸糧) = 襯淵鬱鹹簾遞構製艱膚 繭範壓鹽鏇顧憲夢網構 (膚鏇選積網積廠窪齋醖 ) 更多 | 积极 | 2026-10-17 | |||
N/A | 145 | Corticosteroids and short-acting subcutaneous octreotide | 壓鹽構築網鑰艱窪簾醖(襯膚夢築製窪選夢積鬱) = 膚醖醖廠夢糧憲襯齋壓 觸廠齋鏇憲築製觸廠鹹 (餘鬱鬱憲選構夢艱壓衊 ) | 积极 | 2026-10-17 |
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