The goal of this study is to propose the first direct comparison of Ga-68-DOTATATE PET/CT or PET/MR and Ga-68-DOTATOC PET/CT in patients with meningioma.

开始日期2026-01-01

申办/合作机构

Weill Medical College of Cornell University

[+1]

NCT04529044

/ Not yet recruiting临床2期IIT

A Phase II Pilot Study of (Lutetium (177Lu)-DOTATATE in Patients With Metastatic Breast Cancer

This phase II trial investigates how well 177Lu-DOTATATE works in treating patients with breast cancer that is stage IV or has come back (recurrent). 177Lu-DOTATATE may shrink or destroy the tumor or circulating breast cancer stem cells if they show evidence of the SSTR2. 177Lu-DOTATATE is a targeted therapy that uses DOTATATE, linked to a radioactive agent called 177Lu. DOTATATE attaches to tumor cells with SSTR2 and delivers 177Lu to kill them. Giving 177Lu-DOTATATE may help decrease the number and size of tumors and the number of circulating cancer stem cells in patient's blood for the treatment of patients with breast cancer positive for SSTR2.

开始日期2025-12-01

申办/合作机构

OHSU Knight Cancer Institute

[+3]

NCT06479811

/ Recruiting临床1期IIT

Phase I Trial of [212Pb]VMT-Alpha-NET in Metastatic or Inoperable Somatostatin-Receptor Positive Gastrointestinal Neuroendocrine Tumors, Pheochromocytoma/Paragangliomas, Small Cell Lung, Renal Cell, and Head and Neck Cancers

Background:
Some cancers have high levels of proteins called somatostatin receptors (SSTRs) on the surface of the tumors. These tumors can be in the lung, head and neck, digestive tract, kidneys, and in or near the adrenal glands. Researchers want to know if drug treatments that target SSTRs can help shrink these types of tumors.
Objective:
To test a study drug ([212Pb]VMT-Alpha-NET) in people with tumors that have SSTRs.
Eligibility:
People aged 18 years and older with tumors of the lung, kidneys, head and neck, digestive tract, or adrenal glands that have SSTRs. Their tumors must have spread to other organs and cannot be removed with surgery.
Design:
Participants will be screened. They will have a physical exam with blood and urine tests. They will have imaging scans and a test of their heart function. A sample of tumor tissue may be collected if one is not already available.
[212Pb]VMT-Alpha-NET is given through a tube attached to a needle inserted into a vein. The drug will be given on the first day of four 8-week cycles. Participants will stay in the hospital for a few nights after each dose. They will have blood tests once a week during each cycle.
Some participants will also get a related study drug ([203Pb]VMT-Alpha-NET). They will receive this drug a few days before the first 2 cycles. At 4, 24, and 48 hours after each infusion, they will have whole body scans. These scans will show where the study drug went in their body.
Follow-up visits will continue up to 6 years after the last treatment.

开始日期2025-08-19

申办/合作机构

National Cancer Institute

100 项与镓[68Ga]多特安肽相关的临床结果

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100 项与镓[68Ga]多特安肽相关的转化医学

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100 项与镓[68Ga]多特安肽相关的专利（医药）

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245

项与镓[68Ga]多特安肽相关的文献（医药）

2026-01-01·JOURNAL OF NEURO-ONCOLOGY

SUV-max of 68Ga-DOTATATE PET/CT correlates with WHO grade and RNA risk classification in meningioma

Article

作者: Deng, Jiaojiao ; Xie, Qing ; Xu, Juefeng ; Ren, Leihao ; Hua, Lingyang ; Chan, Louman ; Wakimoto, Hiroaki ; Gong, Ye

BACKGROUND:

⁶⁸Ga-DOTATATE binds to somatostatin receptors (SSTR) and is used for PET/CT imaging for diagnosing meningioma and guiding postoperative radiotherapy. However, the relationship between the clinicopathological characteristics and the imaging features of ⁶⁸Ga-DOTATATE PET/CT in meningioma remains undetermined.

METHODS:

We conducted a retrospective study at a single neurosurgical center. Semiquantitative indices of ⁶⁸Ga-DOTATATE PET/CT, including maximum standardized uptake value (SUV-max), median standardized uptake value (SUV-median), mean standardized uptake value (SUV-mean), and metabolic tumor volume (MTV), were measured. The correlations between these parameters and clinicopathological characteristics were analyzed.

RESULTS:

Eighty patients were retrospectively analyzed, including 45 with WHO grade 1 meningiomas, 33 with grade 2, and 2 with grade 3. The median SUV-max value was significantly higher in meningiomas with high WHO grade (P = 0.017), positive SSTR2a expression (P = 0.023), and in male patients (P = 0.002). Bulk RNA data was available in forty patients. RNA expression of SSTR2 was significantly elevated in the SSTR2a-positive group and correlated positively with SUV-max, SUV-median, and SUV-mean. Furthermore, the high RNA scores risk group exhibited significantly higher SUV-max compared to the intermediate- and low-risk groups. Of note, an SUV-max > 15.55 (P = 0.014) was independently associated with high WHO grade. Lastly, a nomogram incorporating SUV-max, gender, and surgical history demonstrated robust performance in preoperatively identifying patients at risk for high WHO grade, offering the potential utility of ⁶⁸Ga-DOTATATE PET/CT in clinical practice.

CONCLUSION:

SUV-max of ⁶⁸Ga-DOTATATE PET/CT was significantly higher in high grade and high RNA score risk groups of meningioma. Of note, an SUV-max > 15.55 was independently associated with high WHO grade.

2025-11-01·Diagnostic and Interventional Imaging

Molecular imaging of neuroendocrine tumors: Current applications and future trends

Review

作者: Brooks, Allen F ; Scott, Peter J H ; Werner, Rudolf A ; Rowe, Steven P ; Viglianti, Benjamin L ; Wang, Ivan E ; SaTsu, Helen A

The prevalence of neuroendocrine neoplasms (NEN), which include neuroendocrine tumors (NET) and neuroendocrine carcinomas (NEC), has increasing during recent years. The approval of diagnostic single-photon emission computed tomography and positron emission tomography imaging agents for NEN is an important factor in pushing the development of additional agents using new targets to develop patient-specific, targeted, radiopharmaceuticals. Numerous NEN-specific targets exist, including somatostatin receptors, norepinephrine transport substrates, amino acid transport substrates, and glucagon-like peptide-1 receptor analogues, as well as non-specific targets, such as glucose metabolism. Additionally, there are targets that can be used in combination with current agents to further personalize NEN imaging. In well-differentiated gastroenteropancreatic NET, [⁶⁸Ga]DOTATATE is the first line agent. In pheochromocytoma, paraganglioma, and neuroblastomas [¹³¹I]MIBG can also be considered for imaging. [¹⁸F]FDOPA is mainly used for midgut NETs but is second line if access to [⁶⁸Ga]DOTATATE is difficult. In insulinomas, glucagon like peptide-1 receptor agents can be considered with [⁶⁸Ga]DOTATATE. In medullary thyroid carcinomas, [¹⁸F]FDOPA is preferred with or without [⁶⁸Ga]DOTATATE imaging. In poorly-differentiated NEN/NEC, non-specific agents such as [¹⁸F]Fluoro-2-deoxy-d-glucose and [⁶⁸Ga]fibroblast activation protein inhibitor-04 can be used if somatostatin imaging is insufficient. Urokinase plasminogen activator receptor targeting has been used as a method for risk stratification and can be used in combination with [⁶⁸Ga]DOTATATE. The use of somatostatin receptor antagonists, bombesin receptor 2, C-X-C motif chemokine receptor-4, and glucose-dependent insulinotropic polypeptide receptor agents are currently in development - with all of them requiring further studies to determine their potential utility. This review analyzes the current landscape of NEN imaging and discusses the emerging agents that can potentially contribute to NEN imaging in the future.

2025-10-01·NEURORADIOLOGY

Incidental detection of anterior clinoid meningioma on [⁶⁸Ga]Ga-DOTATATE PET/CT in a patient with suspected neuroendocrine tumor

Article

作者: Atalay, Başak ; Tatoğlu, Mehmet Tarık

Meningiomas are the most common extra-axial tumors of the central nervous system. They are slow-growing, benign lesions usually originating from the dura. They are usually detected incidentally. Anterior clinoid meningiomas are important because of their proximity to critical structures such as the optic canal and internal carotid artery. Due to their somatostatin receptor expression, especially SSTR2, ⁶⁸Ga-DOTA0-Tyr3-octreotate ([⁶⁸Ga]Ga-DOTATATE) positron emission tomography/computed tomography (PET/CT) imaging has been used in both the diagnosis and follow-up of meningiomas. We report a rare case of anterior clinoid meningioma detected incidentally on [⁶⁸Ga]Ga-DOTATATE PET/CT.

项与镓[68Ga]多特安肽相关的新闻（医药）

2025-10-27

·搜狐新闻

DOTA-TATE;DOTA-奥曲肽;DOTA-Octreotide;177943-89-4;大环配体；常用于医学领域诊断和治疗神经内分泌肿瘤靶向、示踪、成像配体

DOTA-奥曲肽（DOTA-TATE）的基本性质、应用领域及应用原理一、基本性质DOTA-奥曲肽（DOTA-TATE）是由大环配体DOTA（1,4,7,10-四氮杂环十二烷-1,4,7,10-四乙酸）与奥曲肽（Octreotide）通过共价键偶联形成的多肽衍生物，兼具靶向识别活性与核素螯合功能，是神经内分泌肿瘤诊断与治疗的核心分子探针，其关键基本性质如下：英文名称：DOTA-TATE（全称：DOTA-D-Phe1-Tyr3-Octreotide）中文名称：DOTA-奥曲肽；DOTA-酪氨酸3-奥曲肽（系统命名）CAS登录号：177943-89-4分子结构特征：以奥曲肽为母体骨架，奥曲肽是一种由8个氨基酸残基组成的环状多肽（序列：D-Phe-Cys-Phe-D-Trp-Lys-Thr-Cys-Thr-ol），通过第2位和第7位半胱氨酸形成二硫键环化；在奥曲肽的第3位酪氨酸（Tyr3）残基上通过酰胺键与DOTA分子偶联。整体分子由靶向识别单元（奥曲肽）、连接结构（酪氨酸侧链）及螯合单元（DOTA）构成，分子量约为1313.5 Da。等电点：经实验测定，等电点约为6.2-6.8，因DOTA分子含4个羧基（酸性基团），奥曲肽分子含1个赖氨酸氨基（碱性基团），整体呈弱酸性，等电点较单纯奥曲肽（约6.5-7.0）略有降低。靶向活性：修饰后仍保留奥曲肽对生长抑素受体2（SSTR2）的高特异性与高亲和力，体外受体结合实验显示其与SSTR2的解离常数（Kd值）约为0.1-0.5 nM，与未修饰奥曲肽（Kd值约0.2 nM）活性相当，DOTA偶联未破坏奥曲肽与受体结合的关键结构域。螯合特性：核心螯合单元DOTA具有12元环结构及4个氮原子、4个羧基氧原子的多齿配位位点，可与多种放射性核素形成稳定螯合物，尤其对正电子显像核素（如68Ga）及治疗性核素（如177Lu、90Y）螯合稳定性优异，体内脱核率＜2%，保障诊断准确性与治疗安全性。稳定性：在中性pH环境（pH 6.5-7.5）及4℃冷藏条件下稳定性良好，可保存1-2周；对蛋白酶（如胰蛋白酶、胃蛋白酶）耐受性较强，二硫键环化结构及DOTA修饰增强了抗降解能力；但强酸（pH＜3.0）、强碱（pH＞9.0）或高温（＞60℃）会导致肽键断裂或螯合物解离，需严格控制储存与使用条件。水溶性：因DOTA分子含多个羧基（解离后带负电），整体水溶性优异，在生理盐水中溶解度可达5 mg/mL以上，完全满足体内注射给药需求。二、应用领域DOTA-奥曲肽的应用核心在于其“靶向SSTR2-核素螯合”的双重特性，基于生长抑素受体2（SSTR2）在神经内分泌肿瘤等疾病细胞中的高表达特征，已形成“诊断-治疗-疗效监测”的完整应用体系，具体领域如下：2.1 神经内分泌肿瘤（NETs）诊断领域这是DOTA-奥曲肽最核心的应用领域，神经内分泌肿瘤（尤其是胃肠胰神经内分泌肿瘤GEP-NETs、类癌、嗜铬细胞瘤等）细胞普遍高表达SSTR2，为靶向诊断提供分子基础。将DOTA-奥曲肽与68Ga等正电子核素螯合后，通过正电子发射断层显像（PET/CT或PET/MRI）实现多维度诊断：一是原发灶定位，精准识别常规影像学（CT、MRI）难以发现的微小原发灶（直径＜1cm），尤其对原发灶不明的NETs诊断价值显著；二是分期诊断，清晰显示全身范围内的淋巴结转移、肝转移、骨转移等远处转移灶，为临床TNM分期提供关键依据；三是靶点评估，通过显像量化肿瘤SSTR2表达水平，筛选适合SSTR2靶向治疗（如177Lu-DOTA-TATE治疗）的患者。临床数据显示，其对SSTR2阳性NETs的检出灵敏度达90%-95%，显著优于传统生长抑素受体闪烁显像（SRS）。2.2 神经内分泌肿瘤（NETs）治疗领域基于靶向富集特性，DOTA-奥曲肽与治疗性核素螯合后可实现SSTR2阳性NETs的靶向放射性核素治疗（PRRT），核心应用场景包括：一是晚期转移性NETs治疗，针对无法手术切除或已发生远处转移的SSTR2阳性NETs患者，177Lu-DOTA-TATE是一线治疗方案之一，可显著延长患者无进展生存期；二是术后残留或复发肿瘤治疗，用于手术无法完全切除或术后复发的患者，通过局部靶向放疗清除残留病灶；三是症状控制，对伴有类癌综合征（如潮红、腹泻）的患者，治疗性核素可抑制肿瘤细胞活性，减轻激素过度分泌导致的临床症状。目前177Lu-DOTA-TATE已在全球多个国家获批用于NETs治疗，临床疗效明确。2.3 “诊疗一体化”应用领域DOTA-奥曲肽是“诊断-治疗-疗效监测”一体化的核心载体，形成标准化诊疗流程：诊断阶段，通过68Ga-DOTA-TATE PET显像明确肿瘤位置、分期及SSTR2表达水平；治疗阶段，采用177Lu-DOTA-TATE进行靶向核素治疗，每4-8周一次，共3-4个疗程；疗效监测阶段，每个疗程结束后通过68Ga-DOTA-TATE PET显像评估肿瘤摄取变化，若SUVmax下降＞30%提示治疗有效，根据显像结果调整治疗方案。该模式实现了“精准定位-精准治疗-精准评估”的闭环管理，显著提升NETs治疗效果。2.4 其他SSTR2阳性疾病的潜在应用领域除神经内分泌肿瘤外，部分非神经内分泌肿瘤及良性疾病也存在SSTR2表达，为应用拓展提供可能：在肿瘤领域，对小细胞肺癌、乳腺癌、胰腺癌等SSTR2低至中度表达的肿瘤，68Ga-DOTA-TATE显像可用于微小转移灶检出及异质性评估；在良性疾病领域，用于肢端肥大症（垂体生长激素瘤高表达SSTR2）的诊断与疗效监测，显像可评估肿瘤对药物的应答情况。目前这些应用多处于临床研究阶段，前景可期。2.5 基础医学与药物研发领域在基础研究中，DOTA-奥曲肽是SSTR2相关研究的重要工具：一是用于SSTR2组织分布与表达调控研究，明确其在正常组织及疾病模型中的分布特征；二是用于NETs动物模型构建与验证，通过显像验证模型有效性及疾病进展；三是作为药物研发对照，评估新型SSTR2靶向探针或药物的亲和力、特异性及体内效果。此外，在核医学技术研发中，常作为标准化探针用于PET设备性能校准。三、应用原理DOTA-奥曲肽的各类应用均基于“靶向富集-核素显像/治疗”的协同作用，其核心是奥曲肽与SSTR2的特异性结合及DOTA与核素的稳定螯合，不同应用领域的原理既具共性又有特异性，具体如下：2.1 靶向结合核心原理示踪剂/治疗药物的靶向性源于奥曲肽与SSTR2的特异性高亲和力结合。SSTR2是G蛋白偶联受体，广泛分布于NETs细胞、垂体瘤细胞等目标细胞表面，奥曲肽作为生长抑素的人工类似物，其环状多肽结构可与SSTR2的胞外结构域精准匹配，形成稳定的受体-配体复合物。DOTA偶联于奥曲肽的酪氨酸残基，远离受体结合位点，不影响结合活性。结合后，复合物通过细胞内吞作用进入目标细胞，使核素在细胞内富集，目标区域与正常组织的放射性活度比值（T/N比值）可达10:1以上，为显像与治疗提供基础。2.2 核素显像与治疗的核心原理DOTA-奥曲肽的显像与治疗功能均依赖其螯合单元与放射性核素的稳定作用，具体分为两类场景：显像原理：将DOTA-奥曲肽与68Ga等正电子核素螯合后，核素在衰变过程中释放正电子，正电子与体内电子发生湮灭反应，产生一对能量均为511 keV、方向相反的γ光子。PET设备通过探测γ光子的发射时间与空间位置，经计算机断层重建生成三维断层影像。因示踪剂已靶向富集于SSTR2高表达区域（如NETs病灶），该区域放射性活度显著高于周围组织，在影像上表现为高摄取灶，实现定位；通过标准化摄取值（SUVmax、SUVmean）定量评估SSTR2表达水平，为治疗方案选择提供依据。申明：仅实验室科研，不适应于人体，后果自负相关其他产品：Exendin-4 NOTA-exendin-4 DOTA-MAL-Cys39-exendin-4 NOTA-MAL-Cys39-exendin-4 DOTA-TATE供应商：上海楚肽生物科技有限公司返回搜狐，查看更多

临床结果

2025-08-29

·EINPresswire

July - September 2021 | Potential Signals of Serious Risks/New Safety Information Identified by the FDA Adverse Event Reporting System (FAERS)

Ajovy (fremanezumab-vfrm) Emgality (galcanezumab-gnlm) Nurtec ODT (rimegepant) Ubrelvy (ubrogepant) Vyepti (eptinezumab-jjmr) Hypertension The "Warnings and Precautions", "Adverse Reactions", "Patient Counseling Information", and "Patient Information" sections of the labeling were updated in March 2025 to include information about the risk of hypertension. Example: Ajovy labeling Apriso (mesalamine) Asacol (mesalamine) Asacol HD (mesalamine) Azulfidine (sulfasalazine) Azulfidine EN-Tabs (sulfasalazine) Canasa (mesalamine) Colazal (balsalazide disodium) Delzicol (mesalamine) Dipentum (osalazine sodium) Giazo (balsalazide disodium) Lialda (mesalamine) Rowasa (mesalamine) Pentasa (mesalamine) Severe cutaneous adverse reactions The Warnings and Precautions section of the labeling was updated November 2021 to include severe cutaneous adverse reactions. Example: Delzicol labeling Avastin (bevacizumab) Mvasi (bevacizumab-awwb) Zirabev (bevacizumab-bvzr) Pancreatitis FDA determined that no action is necessary at the time based on available information. Avastin (bevacizumab) Mvasi (bevacizumab-awwb) Zirabev (bevacizumab-bvzr) Anaphylactic shock The "Warnings and Precautions" section of the labeling was updated between September 2022 and February 2023 to include anaphylactoid/anaphylactic reactions. Example: Avastin labeling Ayvakit (avapritinib) Photosensitivity reaction The "Warnings and Precautions", "Adverse Reactions", "Patient Counseling Information", and "Patient Information" sections of the labeling were updated in March 2023 to include information about photosensitivity. Ayvakit labeling Azacitidine Onureg (azacitidine) Vidaza (azacitidine) Generic products containing azacitidine Pericarditis The "Adverse Reactions" section of the labeling was updated between September 2022 and June 2023 to include pericarditis. Example: Vidaza labeling FDA determined that no action is necessary at the time based on available information for Onureg. Bavencio (avelumab) Imfinzi (durvalumab) Libtayo (cemiplimab-rwlc) Keytruda (pembrolizumab) Opdivo (nivolumab) Tecentriq (atezolizumab) Yervoy (ipilimumab) Tumour lysis syndrome FDA determined that no action is necessary at the time based on available information. Cymbalta (duloxetine hydrochloride) Drizalma Sprinkle (duloxetine hydrochloride) Generic products containing duloxetine hydrochloride Anosmia, Hyposmia This issue is posted as two individual newly identified safety signal (NISS) entries in the January-March 2022 quarter, to reflect the focus on the potential signals of anosmia and hyposmia, separately. Darzalex (daratumumab) Darzalex Faspro (daratumumab and hyaluronidase-fihj) Blood stem cell transplant failure FDA determined that no action is necessary at the time based on available information. Dipeptidyl peptidase-4 (DPP-4) inhibitors Glyxambi (empagliflozin and linagliptin) Janumet (metformin hydrochloride and sitagliptin phosphate) Janumet XR (metformin hydrochloride and sitagliptin phosphate) Jentadueto (linagliptin and metformin hydrochloride) Jentadueto XR (linagliptin and metformin hydrochloride) Kazano (alogliptin and metformin hydrochloride) Kombiglyze XR (metformin hydrochloride and saxagliptin) Nesina (alogliptin) Onglyza (saxagliptin) Oseni (alogliptin and pioglitazone) Steglujan (ertugliflozin and sitagliptin) Tradjenta (linagliptin) Trijardy XR (empagliflozin, linagliptin and metformin hydrochloride) Qtern (saxagliptin and dapagliflozin) Generic products containing dipeptidyl peptidase-4 inhibitors Tubulointerstitial nephritis The "Adverse Reactions" section of the labeling was updated between March 2022 and June 2022 for products containing alogliptin and sitagliptin to include tubulointerstitial nephritis. Example: Janumet labeling FDA determined that no action is necessary for products containing linagliptin and saxagliptin at the time based on available information. *An administrative error resulted in the omission of Januvia from the list of product names after the initial quarterly report was posted. Dupixent (dupilumab) Angioedema The "Warnings and Precautions" and "Adverse Reactions" sections of the labeling were updated in December 2021 to include angioedema. Dupixent labeling Glucagon-like peptide-1 (GLP-1) analogues Adlyxin (lixisenatide) Bydureon (exenatide) Bydureon BCise (exenatide) Byetta (exenatide) Ozempic (semaglutide) Rybelsus (semaglutide) Saxenda (liraglutide) Soliqua 100/33 (insulin glargine and lixisenatide injection) Trulicity (dulaglutide) Victoza (liraglutide) Wegovy (semaglutide) Xultophy 100/3.6 (insulin degludec and liraglutide injection) Generic products containing glucagon-like peptide-1 analogues Gallbladder related disorders The "Warnings and Precautions", "Adverse Reactions", and "Patient Counseling Information" sections of the GLP-1 analogues labeling were updated between March 2022 and June 2022 to include information about acute gallbladder disease. Example: Adlyxin labeling FDA has determined that the last approved labeling for Saxenda and Wegovy is adequately labeled for acute gallbladder disease, and that no further regulatory action is needed at this time. Gonadotropin releasing hormone (GnRH) analogues Fensolvi (leuprolide acetate) Lupron Depot-PED (leuprolide acetate) Supprelin LA (histrelin acetate) Synarel (nafarelin acetate) Triptodur (triptorelin) Idiopathic intracranial hypertension The "Warnings", "Precautions", and "Adverse Reactions" sections of the labeling were updated in April 2022 to include idiopathic intracranial hypertension. Example: Fensolvi labeling Jakafi (ruxolitinib phosphate) Herpes simplex virus (HSV) reactivation and/or disseminated HSV The "Dosage and Administration", "Warnings and Precautions", and "Adverse Reactions" sections of the labeling were updated in January 2023 to include information about herpes simplex and herpes zoster infections. Jakafi labeling Ibrance (palbociclib) Kisqali (ribociclib) Kisqali Femara Co-Pack (letrozole and ribociclib) Embolic and thrombotic events, venous The "Adverse Reactions" section of the Ibrance labeling was updated in December 2024 to include venous thromboembolism. Ibrance labeling FDA determined that no action is necessary at the time for Kisqali and Kisqali Femara Co-Pack based on available information. Ocrevus (ocrelizumab) Myocardial infarction FDA determined that no action is necessary at the time based on available information. Potassium Chloride Product preparation error The “Warnings” section of the labeling was updated in December 2022 to include information about fatal cardiac adverse reactions with intravenous administration of undiluted potassium chloride. Praxbind (idarucizumab) Wrong dose errors The carton labeling and "Dosage and Administration" sections of the labeling were revised in February 2022 to clarify the number of vials included in each carton and the recommended dosing. Praxbind labeling Qbrexza (glycopyrronium tosylate) Accidental exposure to product The container label, carton labeling, "Dosage and Administration", "Warnings and Precautions", "Patient Counseling Information", and "Patient Information" sections of the labeling were updated in October 2022 to include information about accidental exposure. Qbrexza labeling Qbrexza (glycopyrronium tosylate) Urinary retention The “Warnings and Precautions”, “Adverse Reactions”, and “Patient Counseling Information” sections of the labeling were updated in October 2022 to include information about new or worsening urinary retention. Qbrexza labeling Sodium-glucose cotransporter-2 (SGLT-2) inhibitors Farxiga (dapagliflozin) Glyxambi (empagliflozin and linagliptin) Invokamet (canagliflozin and metformin hydrochloride) Invokamet XR (canagliflozin and metformin hydrochloride) Invokana (canagliflozin) Jardiance (empagliflozin) Qtern (saxagliptin and dapagliflozin) Steglatro (ertugliflozin) Steglujan (ertugliflozin and sitagliptin) Segluromet (ertugliflozin and metformin hydrochloride) Synjardy (empagliflozin and metformin hydrochloride) Synjardy XR (empagliflozin and metformin hydrochloride) Trijardy XR (empagliflozin, linagliptin and metformin hydrochloride) Xigduo XR (dapagliflozin and metformin) Generic products containing sodium-glucose cotransporter-2 (SGLT-2) inhibitors Tubulointerstitial nephritis FDA determined that no action is necessary at the time based on available information. Somatostatin Receptor Imaging Agents Detectnet (copper Cu-64 dotatate injection) Gallium Dotatoc (GA 68) Octreoscan (Indium In 111 Pentetreotide) Netspot (Gallium GA 68 Dotatate) Hypersensitivity The "Warnings and Precautions" and "Adverse Reactions" sections of the labeling were updated in December 2021 to include hypersensitivity reactions. Example: Netspot labeling Stromectol (ivermectin) Generic products containing ivermectin Off label use FDA determined that no action is necessary at the time based on available information. Stromectol (ivermectin) Generic products containing ivermectin Neurotoxicity The "Warnings", "Adverse Reactions", and "Overdosage" sections of the labeling were updated in March 2022 to include neurotoxicity. Example: Stromectol labeling Sunosi (solriamfetol hydrochloride) Hypersensitivity FDA determined that no action is necessary at the time based on available information. Vivitrol (naltrexone) Incorrect route of product administration The container label (vial), carton labeling, "Dosage and Administration", "Warnings and Precautions", and "Description", sections of the labeling were revised in September 2022 to emphasize the appropriate route and site of administration. Vivitrol labeling Xcopri (cenobamate) Psychiatric disorders The "Adverse Reactions" section of the labeling was updated in June 2022 to include psychiatric disorders. Xcopri labeling Legal Disclaimer: EIN Presswire provides this news content "as is" without warranty of any kind. We do not accept any responsibility or liability for the accuracy, content, images, videos, licenses, completeness, legality, or reliability of the information contained in this article. If you have any complaints or copyright issues related to this article, kindly contact the author above.

上市批准

2025-01-23

·小核说核药

新核药[68Ga]Ga-DATA5m-LM4的首个临床研究！

今天因为你的分享，让小核元气满满！ FOCUS ON Xiaohe 点击蓝字.催更小核小核微信| xiaoheshuoheyao777 聚焦领域| 放射性药物与临床核医学分享一篇文献摘要与图文。文章于2025年1月20日online于Theranostics期刊，报道了一项关于新型SSTR拮抗剂68Ga-DATA5m-LM4在转移性神经内分泌肿瘤（NETs）患者中的首次临床研究！该研究的主要目的是评估68Ga-DATA5m-LM4用于PET/CT成像的可行性，并考察其安全性、生物分布和初步诊断效能。相关往期链接：JNM：靶向成纤维细胞激活蛋白(FAP):使用方酰胺偶联双功能DOTA和DATA 5m螯合剂的下一代PET放射示踪剂《Bioconjugate Chem》用于肿瘤显像和治疗的方酸类放射药物论文的通讯作者是新加坡国立大学张静静教授和德国Richard P. Baum教授。可下载原文仔细拜读doi:10.7150/thno.94521 01 摘要 Abstract 背景简介 FDA和EMA已批准68Ga标记的[68Ga]Ga-DOTA-TATE和[68Ga]Ga-DOTA-TOC用于SSTR阳性NETs的成像，SSTR2的激动剂能够轻易内化进入肿瘤细胞，从而在靶细胞中滞留。近期的研究表明SSTR拮抗剂在某些患者中，尤其是SSTR2表达较低的患者中，可能具有更好的成像效果。与SSTR2激动剂相比，SSTR2拮抗剂如68Ga标记的DOTA或NODAGA螯合物与JR11和LM3在临床前和临床研究中显示出更高的摄取。螯合剂和核素对SSTR示踪剂的亲和力和药代动力学有较大影响，例如DOTA螯合剂不太适合与相对较小的放射性金属镓螯合，且需要较高的反应温度，这对于许多抗体以及热敏感的生物分子都是不利的。此外，这类螯合通常需要较长的反应时间，还需要额外的时间进行冷却，然后才能进行静脉注射，由于68Ga的半衰期较短，也给临床应用带来了限制。DATA是一种新型螯合剂，与已有的螯合剂相比，它在68Ga标记方面具有优势：DATA可以在室温下快速定量放射性标记68Ga，此外相关的螯合剂AAZTA提供了用治疗性同位素（如177Lu）标记的可能性。从2020年9月到2022年1月，该研究共纳入27名经组织病理学确认的分化良好的转移性NETs患者。 02 正文图片 Figure DATA5m-LM4结构：研究在50°C 15分钟内实现了80-95%的放射化学产率，整个68Ga-DATA5m-LM4的标记过程大约需要20分钟，包括加热、纯化、过滤和配制。随后进行纯化、配制和无菌过滤。使用分析型高效液相色谱和薄层色谱进行质量控制，两者都显示放射化学纯度超过98%，比活度在12到17 MBq/nmol之间。 68Ga-DATA5m-LM4在患者中的生物分布如上图所示：68Ga-DATA5m-LM4在注射后1小时内从血液循环中有效清除，并主要通过肾脏和泌尿系统排泄。除肾脏和膀胱外，68Ga-DATA5m-LM4的最高正常器官摄取在肾上腺，其次是脾脏和垂体，注射后60分钟的SUVmax分别为13.16 ± 5.80、12.87 ± 9.37和10.84 ± 6.40。腮腺、甲状腺、肝和胰腺表现出中等摄取，SUVmax分别为5.29 ± 2.64、3.16 ± 1.26、3.90 ± 0.88和3.73 ± 1.13。上表显示了68Ga-DATA5m-LM4与68Ga标记的其他SSTR类似物（包括68Ga-DOTA-TATE、68Ga-DOTA-TOC、68Ga-NODAGA-JR11、68Ga-NODAGA-LM3）的分布比较。与68Ga-DOTA-TATE PET/CT相比，68Ga-DATA5m-LM4在正常肝实质中的摄取较低（3.90 ± 0.88 vs. 9.12 ± 3.64, P < 0.000001）。此外，甲状腺、胰腺和脾脏的摄取也较低（P < 0.05）。在27名患者中，14名还接受了68Ga-DOTA-TOC PET/CT，1名接受了68Ga-DOTA-TATE PET/CT，4名接受了68Ga-NODAGA-LM3 PET/CT（上表）。半定量分析显示，68Ga-DATA5m-LM4在肝脏和脾脏的摄取显著低于68Ga-DOTA-TOC（3.70 ± 0.79 vs. 5.33 ± 2.43, P = 0.0397；11.88 ± 6.88 vs. 26.55 ± 16.07, P = 0.0022）。相比之下，68Ga-DATA5m-LM4在肾脏的摄取高于68Ga-DOTA-TOC（19.40 ± 7.12 vs. 16.44 ± 6.04, P = 0.0059）。68Ga-DATA5m-LM4在垂体的摄取显著高于68Ga-NODAGA-LM3（8.87 vs. 4.79, P = 0.0183），代表性图像如下所示。下图展示了27名患者通过68Ga-DATA5m-LM4 PET/CT检测到的肿瘤的SUVmax、肿瘤与肝脏比值以及肿瘤与血池比值。数据表明68Ga-DATA5m-LM4 PET/CT能够检测到高摄取的肿瘤病变，其中最高的SUVmax达到167.93，平均值为44.47 ± 36.22，第二高的SUVmax为133.99，平均值为34.00 ± 27.43。这些结果表明68Ga-DATA5m-LM4在检测NETs患者肿瘤病变方面的高效性和敏感性，尤其是在检测微小病变和CT不可见的肿瘤方面。 Q 小核的笔记呢？声明：本公众号为科研文献分享公益公众号，小核主要分享核药、放射性药物、核医学、放射化学等公开发表的研究成果，对相关疾病的诊断及治疗方案不做推荐（也不涉及），此外本文不构成也不提供任何投资建议。非常感谢读者们的关注！因小核个人水平有限，错误不可避免，欢迎各位读者留言或私信指出，小核会及时修订，感谢！小核原创，版权所有若需转载，敬请联络文末附上了原文链接，方便请检索拜读。 ●新CLDN18.2靶向核药重磅来袭！ ●68Ga-FAP-2286精准诊断尿路上皮癌！ ●新TROP2靶向核药重磅来袭！ ●“罕见”的甲状腺髓样癌核药赛道戳“小核”一起来讨论吧!

放射疗法临床结果

100 项与镓[68Ga]多特安肽相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	-	V09	-

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
神经内分泌肿瘤	美国	Advanced Accelerator Applications USA, Inc.	2016-06-01

未上市

10 条进展最快的记录,

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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	临床3期	中国	原子高科股份有限公司	2024-01-05
鼻咽癌	临床2期	中国	福建医科大学附属第一医院（福建省皮肤病性病防治院、福建省皮肤病性病防治研究所）	2022-11-20
肿瘤	临床2期	美国	Stanford University	2014-05-27
甲状腺髓样癌	临床1期	中国	福建医科大学附属第一医院（福建省皮肤病性病防治院、福建省皮肤病性病防治研究所）	2023-06-21
神经嵴肿瘤	临床1期	中国	北京协和医院	2021-09-01
神经母细胞瘤	临床1期	中国	北京协和医院	2021-09-01
嗜铬细胞瘤	临床1期	中国	北京协和医院	2021-09-01
肿瘤源性骨软化症	临床1期	中国	北京协和医院	2020-03-15
间充质细胞肿瘤	临床1期	中国	北京协和医院	2011-12-01

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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


NCT03448458 (CTgov)	临床2期	转移性去势抵抗性前列腺癌	17	CT (Computed Tomography)+Gallium Ga 68-DOTATATE	夢簾醖鏇艱繭鏇構範鏇 = 網願廠製積製範鏇範淵膚製蓋蓋鏇選製獵構築 (鹽淵鑰構蓋糧願鏇壓選, 選製壓獵糧壓憲製獵範 ~ 糧糧獵積糧膚齋蓋齋選) 更多	-	2025-07-17
NCT03736564 (CTgov)	临床1/2期	间充质细胞肿瘤 \| 肿瘤源性骨软化症	18	68Ga-DOTATATE PET/CT	醖齋淵範築製襯鏇鏇鏇 = 鹹窪積鏇窪艱顧網鏇繭醖築範製鏇構膚窪網鹹 (構齋築鏇鬱壓艱遞鑰鑰, 製餘窪願觸蓋壓醖衊構 ~ 獵餘鏇鏇觸遞鏇鑰願獵) 更多	-	2025-04-30
EANM2024	N/A	转移性甲状腺髓样癌 serum calcitonin levels	20	68Ga-DOTATATE PET/CT	襯衊廠窪簾願鏇構鬱積(鏇齋壓鹹顧壓範艱糧範) = 窪獵鏇餘鹹鹽網膚簾網鹹觸廠壓廠膚膚夢壓築 (夢獵遞廠範繭鏇淵壓顧, 5.52 ~ 29.48)	积极	2024-09-27
SNO2023 \| EANO2023	N/A	脑膜瘤 68 Ga-DOTATATE/PET	46	Positive 68Ga-DOTATATE/PET	廠齋繭選選艱範襯襯壓(鏇窪膚網糧獵網壓廠鏇) = 範鏇艱襯顧壓壓衊壓範鹹構膚鹽窪齋衊襯顧襯 (膚鬱選遞鑰艱獵鏇憲壓 )	积极	2023-11-10
SNO2023 \| EANO2023	N/A	脑膜瘤 68 Ga-DOTATATE/PET	46	Negative 68Ga-DOTATATE/PET	廠選觸製窪蓋衊艱積觸(襯顧遞遞壓願願願襯齋) = 夢壓襯鏇選願網選衊餘膚憲糧網淵糧衊艱觸選 (選醖遞鏇壓壓膚選繭構 )	积极	2023-11-10
P15.11.B (EANO2023 \| SNO2023)	N/A	脑膜瘤 68 Ga-DOTATATE/PET	46	Positive 68Ga-DOTATATE/PET	鹽範鏇顧醖膚襯構膚繭(積糧蓋鹽膚衊壓憲餘遞) = higher on PET compared to MRI 築顧憲鹹鹹遞壓網衊夢 (蓋觸鏇醖蓋齋蓋觸糧鹽 )	积极	2023-09-08
ASCO_GI2023	N/A	APUD瘤	424	Ga68-DOTATE (Patients with well-differentiated NETs of GI and pancreatic origin)	範齋衊顧窪齋網糧繭餘(餘廠觸襯選衊鑰廠糧願) = 範衊鑰廠鏇衊製簾膚窪觸觸構簾襯壓餘壓襯壓 (淵獵選獵窪遞範膚繭鏇 ) 更多	-	2023-01-24
ASCO_GI2023	N/A	APUD瘤	424	Ga68-DOTATE (Patients with lung carcinoid)	選網網齋構範襯壓淵襯(遞鹹範觸構壓憲蓋淵夢) = 願鹹簾顧餘積鏇獵壓膚廠餘齋願壓製襯壓鬱繭 (齋願廠顧憲窪遞簾膚鏇 )	-	2023-01-24
ASTRO2022	N/A	脑膜瘤	-	[Ga68]-DOTATATE (fSRS (35 Gy in 5 fractions))	遞觸積醖鏇繭膚衊遞鑰(壓壓夢鏇顧淵淵範獵願) = 廠築淵糧糧鏇鑰範顧遞膚衊簾構獵範齋鹽衊糧 (鑰鬱膚繭醖糧蓋築衊衊 )	-	2022-11-01
SNMMI2022	N/A	神经内分泌肿瘤 tumor markers	98	68Ga-DOTATATE PET/CT	選遞網衊選範鹹襯鹽網(餘構鑰壓淵醖艱齋鑰廠) = 獵積繭製築選憲築構獵餘壓壓願餘窪餘憲顧憲 (網蓋廠遞鹹憲壓獵憲窪 ) 更多	积极	2022-08-08
SNMMI2022	N/A	神经内分泌肿瘤	-	68Ga-DOTATATE (Neuroendocrine tumor patients with cardiac metastases)	淵餘襯構艱齋壓鹽簾遞(鹽憲糧積衊夢選衊願襯) = mean ± SD: 26.2 ± 31.4 鑰艱壓鬱積願廠積窪廠 (鏇繭淵築廠繭憲製顧築 ) 更多	-	2022-08-08
SNMMI2022	N/A	神经内分泌肿瘤	-	68Ga-DOTATATE (Patients with non-cardiac metastatic grade 1-2 gastroenteropancreatic NETs)		-	2022-08-08
NCT03125629 (CTgov)	临床2期	肿瘤	53	Positron Emission Tomography / Computed Tomography (PET/CT) Scan+F-18 FDG (18F-FDG PET/CT Scan)	範膚範壓窪選願艱淵製(淵衊夢觸製構觸夢網醖) = 積蓋鏇醖膚廠鏇壓夢夢廠憲艱鏇蓋繭鏇獵壓廠 (獵蓋憲糧艱艱餘艱糧獵, 0.42) 更多	-	2021-04-08
NCT03125629 (CTgov)	临床2期	肿瘤	53	Positron Emission Tomography / Magnetic Resonance Imaging (PET/MRI) Scan+F-18 FDG (18F-FDG PET/MRI Scan)	範膚範壓窪選願艱淵製(淵衊夢觸製構觸夢網醖) = 鹹選築鬱淵衊鹽遞鬱衊廠憲艱鏇蓋繭鏇獵壓廠 (獵蓋憲糧艱艱餘艱糧獵, 0.38) 更多	-	2021-04-08