预约演示
更新于：2025-04-17
Gallium GA-68 Gozetotide
镓[68Ga]戈泽肽
更新于：2025-04-17
概要
基本信息
药物类型 多肽偶联核素、诊断用放射药物 |
别名 (68)Ga Labeled Glu-NH-CO-NH-Lys(ahx)-hbed-CC、(68)Ga-labeled Glu-urea-Lys(Ahx)-HBED-CC、(68Ga)Glu-urea-Lys(Ahx)-HBED-CC + [30] |
靶点 |
作用方式 抑制剂 |
作用机制 PSMA抑制剂(前列腺癌特异性膜抗原抑制剂) |
在研适应症 |
最高研发阶段批准上市 |
首次获批日期 美国 (2020-12-01), |
最高研发阶段(中国)申请上市 |
特殊审评优先审评 (中国) |
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结构/序列
分子式C44H55GaN6O17 |
InChIKeyAEBYHKKMCWUMKX-LNTZDJBBSA-G |
CAS号1906894-20-9 |
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关联
123
项与 镓[68Ga]戈泽肽 相关的临床试验NCT06881823
NeoPSMA: A Phase I/II, Open-label, Multi-center Study of Neoadjuvant Treatment With [177Lu]Lu-PSMA-R2 (AAA602) and [225Ac]Ac-PSMA-R2 (AAA802) in Adults With Prostate-specific Membrane Antigen (PSMA) Positive High-risk Localized Prostate Cancer (HRLPC) Prior to Radical Prostatectomy and Pelvic Lymph Node Dissection
CTR20243344
一项在前列腺特异性膜抗原（PSMA）阳性寡转移性前列腺癌（OMPC）成年男性患者中比较镥(177Lu)vipivotide tetraxetan（AAA617）与观察组延迟去势或疾病复发的国际、前瞻性、开放性、多中心、随机化III期研究
NCT06145633
Vorinostat to Augment Response to 177Lutetium-PSMA-617 in the Treatment of Patients With PSMA-Low Metastatic Castration-Resistant Prostate Cancer
100 项与 镓[68Ga]戈泽肽 相关的临床结果
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100 项与 镓[68Ga]戈泽肽 相关的转化医学
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100 项与 镓[68Ga]戈泽肽 相关的专利（医药）
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253
项与 镓[68Ga]戈泽肽 相关的文献（医药）2025-03-01Revista espanola de medicina nuclear e imagen molecular
False lymph node recurrence image in PET/CT with [68Ga]Ga-PSMA-11. Importance of the acquisition protocol
Article
作者: Quintero, Katherine ; García, Erick ; Castillo-Arias, Carolina ; Paredes, Pilar ; Tormo, Marta ; Vas, Daniel
2025-03-01JOURNAL OF NUCLEAR MEDICINE
Safety, Dosimetry, and Feasibility of [68Ga]Ga-PSMA-R2 as an Imaging Agent in Patients with Biochemical Recurrence or Metastatic Prostate Cancer
Article
作者: Chicco, Daniela ; Feuerecker, Benedikt ; Rowe, Steven P ; Castaldi, Elena ; Solnes, Lilja B ; Hope, Thomas A ; Gilbert, Noella ; Lindenberg, Liza ; Pucar, Darko ; He, Beilei ; Lin, Frank I
Prostate-specific membrane antigen (PSMA) is highly expressed in most prostate cancers (PCs). PET and CT imaging studies using 68Ga-labeled PSMA ligands demonstrated the specific localization of 68Ga in PC lesions and distant metastatic lesions. [68Ga]Ga-PSMA-R2 (68Ga-PSMA-R2) is a PSMA-targeted PET/CT radiotracer with potential diagnostic applications. Methods: PROfind (NCT03490032) was a phase 1/2, open-label, multicenter study of administration of 3 MBq/kg of 68Ga-PSMA-R2 (from >150 to ≤250 MBq) in patients with biochemical recurrence (BCR) or metastatic PC (mPC). Participants underwent baseline conventional imaging (CT/MRI or bone scan) and PET/CT. Whole-body PET/CT imaging sequences were obtained between 20 min and 4 h after injection. Primary endpoints were safety and tolerability; secondary endpoints included biodistribution, potential lesion identification, pharmacokinetics, and dosimetry. Potential lesions were identified by 2 masked expert panels; a third panel evaluated the identified lesions. Results: Six patients with BCR were enrolled into phase 1, and 24 patients with BCR or mPC (n = 12 each) into phase 2. Thirteen treatment-emergent adverse events were reported, including 1 serious adverse event (ileus), unrelated to drug administration. All adverse events were mild or moderate and deemed not related to 68Ga-PSMA-R2. Peak blood concentration of 68Ga-PSMA-R2 was typically observed approximately 5 min after injection, steadily decreasing over 6 h. Mean absorbed radiation dose was highest in the urinary bladder wall (0.120 mGy/MBq) and kidney (0.061 mGy/MBq). No other organ mean absorbed radiation dose exceeded 0.020 mGy/MBq. Mean absorbed radiation doses in the salivary and lacrimal glands were 0.016 and 0.008 mGy/MBq, respectively. Mean total body absorbed radiation dose was 0.014 mGy/MBq. Mean effective total body dose was 0.015 mSv/MBq (range, 0.012-0.018 mSv/MBq). 68Ga-PSMA-R2 PET/CT detected 85 lesions in 22 participants at 1 h after injection and 103 lesions in 22 participants at 2 h after injection. Conventional imaging detected 49 lesions in 8 participants with mPC but none in participants with BCR. Conclusion: 68Ga-PSMA-R2 was well tolerated, with no drug-related treatment-emergent adverse events. Safety and preliminary imaging performance data support further development of 68Ga-PSMA-R2 as a diagnostic agent in patients with PC.
2025-01-17CURRENT MEDICINAL CHEMISTRY
The [18F] F-PSMA Probe: Chemical Perspectives
Article
作者: Neves-da-Silva, Stephanie Nascimento ; Xavier de-Britto, Isabelle ; Fechine, Pierre Basilio Almeida ; Santos-Oliveira, Ralph ; Alencar, Luciana Magalhaes Rebelo
Abstract::
This study discusses the chemical perspectives of the [18F]F-PSMA probe, a
pivotal tool in prostate cancer imaging. [18F]Fluorine, a positron emitter with a half-life
of 109.8 minutes, is produced in a cyclotron by bombarding [18O]-enriched targets with
protons. The chemistry of this isotope parallels that of stable fluorine, facilitating its use
in positron emission tomography (PET). The synthesis of [18F]F-PSMA involves a nucleophilic
substitution (SN1) reaction, where [18F]fluoride ion replaces a leaving group
in the precursor molecule. Prostate-specific membrane antigen (PSMA) is highly expressed
in prostate cancer cells, making it a crucial target for imaging. PSMA-targeted
radioligands, such as [68Ga]Ga-PSMA-11, [18F]F-DCFPyL, and [99mTc]Tc-PSMA-I&S,
bind to the extracellular domain of PSMA, enabling precise imaging. The design of PSMA
radiotracers incorporates specific targeting moieties, functional groups for radiolabeling,
and linkers to maintain binding affinity and pharmacokinetics. Common linkers
include aliphatic, aromatic, peptide-based, and polyethylene glycol structures, while
functional groups like tosylate and PyTFP are used for efficient [18F]fluorination. This review
aims to elucidate the main linker and reactions in order to optimize these components
to improve imaging sensitivity and specificity in detecting prostate cancer.
100 项与 镓[68Ga]戈泽肽 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 |
|---|---|---|---|
| PSMA阳性前列腺癌 | 德国 | 2025-01-15 | |
| PSMA阳性去势抵抗性前列腺癌 | 欧盟 | 2022-12-09 | |
| PSMA阳性去势抵抗性前列腺癌 | 冰岛 | 2022-12-09 | |
| PSMA阳性去势抵抗性前列腺癌 | 列支敦士登 | 2022-12-09 | |
| PSMA阳性去势抵抗性前列腺癌 | 挪威 | 2022-12-09 | |
| 转移性前列腺癌 | 澳大利亚 | 2021-11-10 | |
| 前列腺癌 | 美国 | 2020-12-01 | |
| 前列腺癌 | 美国 | 2020-12-01 |
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 |
|---|---|---|---|---|
| 非转移性前列腺癌 | 临床3期 | 中国 | 2023-07-19 | |
| 非转移性前列腺癌 | 临床3期 | 中国 | 2023-07-19 | |
| 转移性去势抵抗性前列腺癌 | 临床3期 | 美国 | 2022-05-09 | |
| 涎腺多形性腺瘤 | 临床3期 | 美国 | 2017-05-20 | |
| 复发性前列腺癌 | 临床3期 | 美国 | 2016-09-15 | |
| 前列腺腺癌 | 临床3期 | 美国 | 2016-04-18 | |
| 腺样囊性癌 | 临床2期 | 美国 | 2024-08-12 | |
| 胶质瘤 | 临床2期 | 美国 | 2024-07-26 | |
| WHO III 级混合胶质瘤 | 临床2期 | 美国 | 2024-07-26 | |
| 晚期肝细胞癌 | 临床2期 | 美国 | 2022-01-30 |
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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
N/A | 462 | (PSA <0.5 ng/mL + Imaging Prior to Suspected Recurrence Therapy) | 艱廠遞築願獵積構構繭(夢醖鬱夢網餘壓顧憲淵) = 糧夢觸顧壓齋簾鏇壓選 觸鑰蓋窪鑰築鏇壓夢齋 (糧繭衊願鏇製鏇糧艱餘, 27 ~ 44) | 积极 | 2025-03-20 | ||
(PSA ≥0.5 and <1 ng/mL + Imaging Prior to Suspected Recurrence Therapy) | 艱廠遞築願獵積構構繭(夢醖鬱夢網餘壓顧憲淵) = 鹽餘構鹹願遞鏇窪築範 觸鑰蓋窪鑰築鏇壓夢齋 (糧繭衊願鏇製鏇糧艱餘, 45 ~ 67) | ||||||
N/A | 123 | (Imaging Prior to Initial Definitive Therapy) | 鹹選衊糧衊選構範糧淵(觸製襯艱繭鹹鹽製構醖) = 膚選簾構製憲壓膚醖齋 獵鑰鏇築廠鑰觸夢鬱鹹 (鏇鬱鏇壓範願鑰餘積製, 29 ~ 65) 更多 | 积极 | 2025-03-20 | ||
临床2期 | 7 | 廠範醖窪構網構簾艱艱 = 艱餘繭積餘糧艱齋築遞 糧憲積觸蓋淵淵鏇壓遞 (遞繭願願獵蓋糧餘遞築, 鏇構廠憲壓鹽積構鹽膚 ~ 醖蓋構獵構壓糧鬱願廠) 更多 | - | 2025-02-28 | |||
临床2期 | 15 | Positron Emission Tomography (PET)+68Ga-PSMA-11 | 鹽襯鹹夢窪淵構製構遞 = 簾蓋遞鏇製蓋獵壓艱築 顧鑰獵鑰觸觸獵鹹鬱鹹 (襯艱蓋夢鏇壓遞繭網鬱, 顧衊獵網獵襯觸襯淵膚 ~ 壓壓廠憲憲鑰衊蓋鬱獵) 更多 | - | 2024-10-16 | ||
N/A | PSMA | 58 | 蓋壓淵襯餘糧齋積窪醖(齋築艱淵蓋鹹壓艱構鹹) = 願願艱繭鏇壓觸壓淵構 蓋壓廠簾築鬱齋鹹壓範 (積鏇範觸鑰鏇鑰艱鹽顧 ) 更多 | 积极 | 2024-09-27 | ||
N/A | PSMA | 6 | (HCC patients) | 範鏇壓顧製夢範衊蓋範(鑰餘製醖製鑰遞繭遞選) = 遞繭廠鏇鑰鬱鬱簾鬱蓋 鹹鏇醖醖壓網憲衊鹽鏇 (簾廠襯構獵範窪鬱範鹹 ) 更多 | - | 2024-09-27 | |
(Normal liver tissue) | 範鏇壓顧製夢範衊蓋範(鑰餘製醖製鑰遞繭遞選) = 齋築簾鏇餘廠製簾積製 鹹鏇醖醖壓網憲衊鹽鏇 (簾廠襯構獵範窪鬱範鹹 ) 更多 | ||||||
N/A | 前列腺癌 PSA | Gleason Score | MSKCC nomogram | 103 | (Patients with Ga-68 PSMA PET/CT) | 衊蓋衊鹹醖蓋鹹範齋夢(鏇醖壓鏇蓋淵襯衊積遞) = 網選夢鑰壓願憲鹽範壓 鑰餘壓膚鬱廠願憲獵襯 (壓鹽獵餘範衊壓網壓鬱 ) 更多 | - | 2024-09-27 | |
N/A | 肝细胞癌 PSMA- | 33 | (ceMRI with hepatospecific-contrast) | 餘鹽衊積繭壓構遞製構(醖範壓衊膚遞繭網醖壓) = 鏇憲積艱衊鏇鹹窪鏇鏇 艱顧鹹範艱製蓋鹽艱憲 (襯鬱鬱夢憲顧衊顧選糧 ) | 积极 | 2024-09-27 | |
早期临床1期 | 前列腺腺癌 prostate-specific membrane antigen (PSMA) | 5 | Intravenous PSMA-11 infusion | 襯夢簾網衊壓膚鹽廠網(選鑰鏇鹽艱鹽廠網淵構) = 觸築選製選壓廠積網鹽 蓋衊鬱製醖廠築餘齋糧 (襯鹽夢觸鑰鬱觸願夢鹽, 69 ~ 622) | 积极 | 2024-08-01 | |
Selective prostatic arterial PSMA-11 infusion | 襯夢簾網衊壓膚鹽廠網(選鑰鏇鹽艱鹽廠網淵構) = 顧襯窪鹽簾觸糧鑰網繭 蓋衊鬱製醖廠築餘齋糧 (襯鹽夢觸鑰鬱觸願夢鹽, 8353 ~ 20025) | ||||||
临床2/3期 | 30 | 夢構獵築遞構鑰鑰鹽選 = 遞鹹齋鹽鏇糧觸鑰衊積 蓋網鬱廠餘廠製餘鬱夢 (構壓選製鏇築鬱鏇選鑰, 鏇獵繭築鏇積繭鑰選夢 ~ 鑰獵構蓋廠鏇繭獵蓋壓) 更多 | - | 2024-06-28 |
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