68Ga-NeoBOMB1(68Ga-NeoBOMB1) - 药物靶点：GRPR_在研适应症：ER阳性/PR阳性/HER2阳性乳腺癌，晚期恶性实体瘤，神经内分泌前列腺癌_专利_临床

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

[68Ga]Ga-NeoB

靶点

GRPR

作用方式

拮抗剂

作用机制

GRPR拮抗剂(胃泌素释放肽前体受体拮抗剂)

治疗领域

肿瘤泌尿生殖系统疾病皮肤和肌肉骨骼疾病

在研适应症

ER阳性/PR阳性/HER2阳性乳腺癌晚期恶性实体瘤神经内分泌前列腺癌+ [2]

非在研适应症

结直肠癌非小细胞肺癌小细胞肺癌

原研机构

Erasmus Universiteit Rotterdam Holding BV

在研机构

Advanced Accelerator Applications SA

Novartis Pharmaceuticals Corp.

Novartis AG

+ [2]

非在研机构-

权益机构-

最高研发阶段临床2期

首次获批日期-

最高研发阶段(中国)临床申请批准

特殊审评-

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结构/序列

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关联

11

项与 68Ga-NeoBOMB1 相关的临床试验

CTR20241939

/ Recruiting临床1/2期

一项在既往内分泌治疗联合CDK4/6抑制剂治疗后进展的胃泌素释放肽受体阳性、雌激素受体阳性、人表皮生长因子受体-2阴性、转移性乳腺癌成人患者中评价 [177Lu]Lu-NeoB联合卡培他滨的开放标签、多中心、I/II期试验

I期部分旨在确定在既往内分泌治疗联合CDK4/6抑制剂治疗后进展的胃泌素释放肽受体阳性、雌激素受体阳性、人表皮生长因子受体-2阴性转移性乳腺癌成人患者中 [177Lu]Lu-NeoB联合卡培他滨治疗的推荐剂量（RD）和给药方案。II期部分旨在评价 [177Lu]Lu-NeoB两种不同剂量/方案联合卡培他滨治疗的初步抗肿瘤活性（剂量优化）。

开始日期2025-03-20

申办/合作机构

Advanced Accelerator Applications SA

[+2]

CTR20250047

/ Recruiting临床1期

一项评估 [177Lu]Lu-NeoB联合瑞波西利和氟维司群在（新）辅助内分泌治疗后早期复发或内分泌治疗联合CDK4/6抑制剂治疗晚期疾病后进展的ER阳性、HER2阴性和GRPR阳性晚期乳腺癌参与者中的安全性和活性的Ib期剂量探索研究

估计 [177Lu]Lu-NeoB联合瑞波西利和氟维司群在（新）辅助内分泌治疗后早期复发或内分泌治疗联合CDK4/6抑制剂治疗晚期疾病后进展的雌激素受体（ER）阳性（ER+）、人表皮生长因子受体-2（HER2）阴性（HER2-）和胃泌素释放肽受体（GRPR）阳性（GRPR+）晚期乳腺癌参与者中的推荐剂量（RD）。

开始日期2025-03-17

申办/合作机构

诺华中国

[+1]

NCT06247995

/ Recruiting临床1/2期

A Phase I/II, Open-label, Multi-center Trial of [177Lu]Lu-NeoB in Combination With Capecitabine in Adult Patients With Gastrin Releasing Peptide Receptor Positive, Estrogen Receptor-positive, Human Epidermal Growth Factor Receptor-2 Negative Metastatic Breast Cancer After Progression on Previous Endocrine Therapy in Combination With a CDK4/6 Inhibitor.

In the phase I part, to determine the recommended doses (RD) and dosing regimens of [177Lu]Lu-NeoB in combination with capecitabine in adult patients with gastrin releasing peptide receptor positive, estrogen receptor-positive, human epidermal growth factor receptor-2 negative metastatic breast cancer after progression on previous endocrine therapy in combination with a CDK4/6 inhibitor. In the phase II part, to evaluate the preliminary anti-tumor activity of two different doses/regimens of [177Lu]Lu-NeoB in combination with capecitabine (dose optimization).

开始日期2024-08-14

申办/合作机构

Novartis Pharmaceuticals Canada, Inc.

100 项与 68Ga-NeoBOMB1 相关的临床结果

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100 项与 68Ga-NeoBOMB1 相关的转化医学

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100 项与 68Ga-NeoBOMB1 相关的专利（医药）

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7

项与 68Ga-NeoBOMB1 相关的文献（医药）

2021-12-01·EJNMMI Radiopharmacy and Chemistry

GMP-compliant production of [68Ga]Ga-NeoB for positron emission tomography imaging of patients with gastrointestinal stromal tumor

Article

作者: Hohenberger, Peter ; Reffert, Laura ; Schönberg, Stefan O ; Pretze, Marc ; Diehl, Steffen ; Wängler, Carmen ; Wängler, Björn

AbstractBackground[68Ga]Ga-NeoB is a novel DOTA-coupled Gastrin Releasing Peptide Receptor (GRPR) antagonist with high affinity for GRPR and good in vivo stability. This study aimed at (1) the translation of preclinical results to the clinics and establish the preparation of [68Ga]Ga-NeoB using a GMP conform kit approach and a licensed 68Ge/68Ga generator and (2) to explore the application of [68Ga]Ga-NeoB in patients with gastrointestinal stromal tumors (GIST) before and/or after interventional treatment (selective internal radiotherapy, irreversible electroporation, microwave ablation).ResultsValidation of the production and quality control of [68Ga]Ga-NeoB for patient use had to be performed before starting the GMP production. Six independent batches of [68Ga]Ga-NeoB were produced, all met the quality and sterility criteria and yielded 712 ± 73 MBq of the radiotracer in a radiochemical purity of > 95% and a molar activity of 14.2 ± 1.5 GBq/μmol within 20 min synthesis time and additional 20 min quality control. Three patients (2 females, 1 male, 51–77 yrs. of age) with progressive gastrointestinal stromal tumor metastases in the liver or peritoneum not responsive to standard tyrosine kinase inhibitor therapy underwent both [68Ga]Ga-NeoB scans prior and after interventional therapy. Radiosynthesis of 68Ga-NeoB was performed using a kit approach under GMP conditions. No specific patient preparation such as fasting or hydration was required for [68Ga]Ga-NeoB PET/CT imaging. Contrast-enhanced PET/CT studies were performed. A delayed, second abdominal image after the administration of the of [68Ga]Ga-NeoB was acquired at 120 min post injection.ConclusionsA fully GMP compliant kit preparation of [68Ga]Ga-NeoB enabling the routine production of the tracer under GMP conditions was established for clinical routine PET/CT imaging of patients with metastatic GIST and proved to adequately visualize tumor deposits in the abdomen expressing GRPR. Patients could benefit from additional information derived from [68Ga]Ga-NeoB diagnosis to assess the presence of GRPR in the tumor tissue and monitor antitumor treatment.

2020-12-01·Journal of Nuclear Medicine1区 · 医学

MITIGATE-NeoBOMB1, a Phase I/IIa Study to Evaluate Safety, Pharmacokinetics, and Preliminary Imaging of ⁶⁸Ga-NeoBOMB1, a Gastrin-Releasing Peptide Receptor Antagonist, in GIST Patients

1区 · 医学

Article

作者: Reindl, Wolfgang ; Jiménez-Franco, Luis David ; Hohenberger, Peter ; Schoenberg, Stefan O ; Virgolini, Irene ; Mariani, Maurizio ; Uprimny, Christian ; Jaschke, Werner ; Glatting, Gerhard ; Decristoforo, Clemens ; Gruber, Leonhard ; Orlandi, Francesca

Gastrin-releasing peptide receptors (GRPRs) are potential molecular imaging targets in a variety of tumors. Recently, a ⁶⁸Ga-labeled antagonist to GRPRs, NeoBOMB1, was developed for PET. We report on the outcome of a phase I/IIa clinical trial (EudraCT 2016-002053-38) within the EU-FP7 project Closed-loop Molecular Environment for Minimally Invasive Treatment of Patients with Metastatic Gastrointestinal Stromal Tumors ('MITIGATE') (grant agreement no. 602306) in patients with oligometastatic gastrointestinal stromal tumors (GIST). Methods: The main objectives were evaluation of safety, biodistribution, dosimetry, and preliminary tumor targeting of ⁶⁸Ga-NeoBOMB1 in patients with advanced tyrosine-kinase inhibitors-treated GIST using PET/CT. Six patients with histologically confirmed GIST and unresectable primary lesion or metastases undergoing an extended protocol for detailed pharmacokinetic analysis were included. ⁶⁸Ga-NeoBOMB1 was prepared using a kit procedure with a licensed ⁶⁸Ge/⁶⁸Ga generator. ⁶⁸Ga-NeoBOMB1 (3 MBq/kg of body weight) was injected intravenously, and safety parameters were assessed. PET/CT included dynamic imaging at 5, 11, and 19 min as well as static imaging at 1, 2, and 3-4 h after injection for dosimetry calculations. Venous blood samples and urine were collected for pharmacokinetic analysis. Tumor targeting was assessed on a per-lesion and per-patient basis. Results:⁶⁸Ga-NeoBOMB1 (50 μg) was prepared with high radiochemical purity (yield > 97%). Patients received 174 ± 28 MBq of the radiotracer, which was well tolerated in all patients over a follow-up period of 4 wk. Dosimetry calculations revealed a mean effective dose of 0.029 ± 0.06 mSv/MBq, with the highest organ dose to the pancreas (0.274 ± 0.099 mSv/MBq). Mean plasma half-life was 27.3 min with primarily renal clearance (mean 25.7% ± 5.4% of injected dose 4 h after injection). Plasma metabolite analyses revealed high stability; metabolites were detected only in the urine. In 3 patients, a significant uptake with increasing maximum SUVs (SUV_max at 2 h after injection: 4.3-25.9) over time was found in tumor lesions. Conclusion: This phase I/IIa study provides safety data for ⁶⁸Ga-NeoBOMB1, a promising radiopharmaceutical for targeting GRPR-expressing tumors. Safety profiles and pharmacokinetics are suitable for PET imaging, and absorbed dose estimates are comparable to those of other ⁶⁸Ga-labeled radiopharmaceuticals used in clinical routine.

2017-12-01·Journal of Nuclear Medicine1区 · 医学

Will GRPR Compete with PSMA as a Target in Prostate Cancer?

1区 · 医学

Article

作者: Iagaru, Andrei

A review discussing if GRPR competes with PSMA as target in prostate cancer.It also discusses the continued development and introduction to clin. use of GRPR-targeting PET radiopharmaceuticals and PSMA-targeting tracers as complementary diagnostic and therapeutic approaches.PET radiopharmaceuticals include ⁶⁸Ga-RM2, ⁶⁸Ga-SB3, ⁶⁸Ga-NeoBOMB1, ¹⁸F-BAY-864367, and ⁶⁴Cu-CB-TE2A-AR06.

100 项与 68Ga-NeoBOMB1 相关的药物交易

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研发状态

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
乳腺癌	药物发现	法国	Advanced Accelerator Applications SA	2018-07-03
乳腺癌	药物发现	奥地利	Advanced Accelerator Applications SA	2018-07-03
结直肠癌	药物发现	法国	Advanced Accelerator Applications SA	2018-07-03
结直肠癌	药物发现	奥地利	Advanced Accelerator Applications SA	2018-07-03
非小细胞肺癌	药物发现	法国	Advanced Accelerator Applications SA	2018-07-03
非小细胞肺癌	药物发现	奥地利	Advanced Accelerator Applications SA	2018-07-03
前列腺癌	药物发现	法国	Advanced Accelerator Applications SA	2018-07-03
前列腺癌	药物发现	奥地利	Advanced Accelerator Applications SA	2018-07-03
小细胞肺癌	药物发现	法国	Advanced Accelerator Applications SA	2018-07-03
小细胞肺癌	药物发现	奥地利	Advanced Accelerator Applications SA	2018-07-03

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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


NCT03724253 (NeoFIND, CTgov)	临床2期	小细胞肺癌 \| 乳腺癌 \| 非小细胞肺癌 \| 前列腺癌 \| 结直肠癌	19	[68Ga]-NeoBOMB1 (Breast)	衊糧製鬱糧鹹衊餘廠壓(膚齋壓製願觸顧齋鬱鏇) = 簾願蓋願鹹製蓋範餘膚構築簾築餘繭艱壓顧選 (糧範夢網憲齋鬱夢鏇簾, 獵繭襯鹽繭顧廠糧鹹醖 ~ 蓋鏇壓構襯網顧糧醖鬱) 更多	-	2020-10-23
NCT03724253 (NeoFIND, CTgov)	临床2期	小细胞肺癌 \| 乳腺癌 \| 非小细胞肺癌 \| 前列腺癌 \| 结直肠癌	19	[68Ga]-NeoBOMB1 (Prostate)	衊糧製鬱糧鹹衊餘廠壓(膚齋壓製願觸顧齋鬱鏇) = 廠顧壓鏇網艱鬱積範廠構築簾築餘繭艱壓顧選 (糧範夢網憲齋鬱夢鏇簾, 壓選簾獵範齋構憲糧願 ~ 積糧觸憲齋淵鹽鏇憲獵) 更多	-	2020-10-23
EUCTR2016-002053-38-AT (MITIGATE, EANM2019)	临床1/2期	胃肠道间质瘤 GRPRs	9	68 Ga-NeoBOMB1	築積廠鬱範膚憲製構餘(餘糧獵網範簾鑰鏇衊膚) = only transient mild adverse events (maximum CTCAE grade 1) apparent within 4 weeks after application 遞艱遞願憲醖築鏇顧壓 (淵糧願膚顧築積襯餘繭 ) 更多	积极	2019-09-18
EUCTR2016-002053-38-AT (MITIGATE project, EANM2017)	临床1/2期	胃肠道间质瘤 GRPR	12	68 Ga-NeoBOMB1	齋鏇築夢鏇憲築獵齋簾(製網遞鏇範夢壓獵製醖) = exclusive renal excretion pattern starting within few minutes after injection and a physiologic high uptake in pancreas already 30 min p.i 簾遞顧遞簾憲築積獵膚 (繭網蓋網範壓繭廠顧壓 ) 更多	积极	2017-09-11