Technetium Tc 99m trofolastat(Technetium Tc 99m trofolastat) - 药物靶点：PSMA_在研适应症：前列腺癌_专利_临床

概要

基本信息

药物类型

诊断用放射药物、核素偶联药物

别名

99mTc-trofolastat、Technetium Tc 99M Trofolastat Chloride

+ [5]

靶点

PSMA

作用机制

PSMA抑制剂(前列腺癌特异性膜抗原抑制剂)、SPECT(单光子发射计算机断层成像术增强剂)

治疗领域

肿瘤泌尿生殖系统疾病

在研适应症

前列腺癌

非在研适应症

造影剂先天性甲肥厚

原研机构

Progenics Pharmaceuticals, Inc.

在研机构

PDRadiopharma, Inc.Lantheus Medical Imaging, Inc.

非在研机构

Progenics Pharmaceuticals, Inc.

FUJIFILM Toyama Chemical Co., Ltd.

Molecular Insight Pharmaceuticals, Inc.

+ [1]

最高研发阶段临床3期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构

分子式C40H42N10O23Tc

InChIKeySEMUBPUAWVZHAS-INZTZQCYSA-F

CAS号1333204-77-5

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关联

14

项与 Technetium Tc 99m trofolastat 相关的临床试验

EUCTR2021-001059-15-SE / Unknown status临床2期IIT

The value of 99mTc-MIP-1404 SPECT/CT Veriton CZT for staging ofprostate cancer and before primary therapy and in biochemical recurrenceafter radical prostatectomy. Fase II study.

开始日期2022-04-05

申办/合作机构-

EUCTR2021-000486-33-FI / Unknown status临床3期IIT

99mTc-MIP-1404 SPECT/CT for primary PROstate cancer STAging: comparative prospective, randomized trial to present guideline imaging

开始日期2022-03-21

申办/合作机构

Turku University Hospital

JPRN-JapicCTI-163190 / Completed临床2期

Phase IIb Study of F-1311 in Patients with Prostate Cancer

开始日期2016-05-24

申办/合作机构

PDRadiopharma, Inc.

100 项与 Technetium Tc 99m trofolastat 相关的临床结果

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100 项与 Technetium Tc 99m trofolastat 相关的转化医学

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100 项与 Technetium Tc 99m trofolastat 相关的专利（医药）

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12

项与 Technetium Tc 99m trofolastat 相关的文献（医药）

2023-02-01·Journal of Nuclear Medicine

Eligibility for¹⁷⁷Lu-PSMA Therapy Depends on the Choice of Companion Diagnostic Tracer: A Comparison of⁶⁸Ga-PSMA-11 and^99mTc-MIP-1404 in Metastatic Castration-Resistant Prostate Cancer

Article

作者: Leaning, Darren ; Cook, Gary J R ; Wong, Wai-Lup ; Mangar, Stephen ; Challapalli, Amarnath ; Bassett, Paul ; Bahl, Amit ; Schmidkonz, Christian ; Sanghera, Bal

¹⁷⁷Lu-prostate-specific membrane antigen-617 (¹⁷⁷Lu-PSMA-617) is an effective therapy for metastatic castration-resistant prostate cancer (mCRPC), with evidence of improved survival over standard care. The VISION trial inclusion criteria required a metastatic lesion-to-liver ratio of greater than 1 on ⁶⁸Ga-PSMA-11 PET scans. We aimed to determine whether an equivalent ratio is suitable for a SPECT tracer, ^99mTc-MIP-1404, and to compare lesion and lesion-to-normal-organ ratios between the 2 radiotracers. Methods: Two cohorts of patients with mCRPC matched for age, prostate-specific antigen level, and total Gleason score, with either ^99mTc-MIP-1404 SPECT/CT (n = 25) or ⁶⁸Ga-PSMA-11 PET/CT (n = 25) scans, were included for analysis. Up to 3 lesions in each site (prostate/prostate bed, lymph nodes, bone and soft-tissue metastases) as well as normal liver, parotid gland, spleen, and mediastinal blood-pool SUV_max were measured. Results: ^99mTc-MIP-1404 SPECT lesion SUV_max was not significantly different from ⁶⁸Ga-PSMA-11 PET (median, 18.2 vs. 17.3; P = 0.93). However, ^99mTc-MIP-1404 liver SUV_max was higher (median, 8.5 vs. 5.8; P = 0.002) and lesion-to-liver ratios were lower (median, 2.7 vs. 3.5; P = 0.009). There was no significant difference in parotid gland or splenic SUV_max or lesion-to-parotid gland ratios between the 2 tracers although there was a small difference in lesion-to-spleen ratios (P = 0.034). Conclusion: There are differences in biodistribution and, in particular, liver activity, between ⁶⁸Ga-PSMA-11 and ^99mTc-MIP-1404. Therefore, if ^99mTc-MIP-1404 is used to assess eligibility for ¹⁷⁷Lu-PSMA-617 therapy, a lower adjusted lesion-to-liver ratio should be used.

2023-01-01·Journal of Nuclear Medicine

Feasibility of^99mTc-MIP-1404 for SPECT/CT Imaging and Subsequent PSMA-Radioguided Surgery in Early Biochemically Recurrent Prostate Cancer: A Case Series of 9 Patients

Article

作者: Koehler, Daniel ; Apostolova, Ivayla ; Klutmann, Susanne ; Maurer, Tobias ; Lehnert, Wencke ; Sauer, Markus ; Knipper, Sophie ; Budäus, Lars

This case series evaluated the feasibility of prostate-specific membrane antigen (PSMA)-radioguided surgery (RGS) with ^99mTc-MIP-1404 in recurrent prostate cancer. Methods: Nine patients with PSMA-positive lesions on PET/CT received ^99mTc-MIP-1404 (median, 747 MBq; interquartile range [IQR], 710-764 MBq) 17.2 h (IQR, 16.9-17.5 h) before SPECT/CT and 22.3 h (IQR, 20.8-24.0 h) before RGS. Results: Seventeen PSMA-positive lesions were detected on PET/CT (median short-axis diameter, 4 mm; IQR, 3-6 mm; median SUV_max, 8.9; IQR, 5.2-12.6). Nine of 17 (52.9%) were visible on SPECT/CT (median SUV_max, 13.8; IQR, 8.0-17.9). Except for 2 foci, all PET/CT-positive findings demonstrated intraoperative count rates above the background level (median count, 31; IQR, 17-89) and were lymph node metastases. Moreover, PSMA-RGS identified 2 additional metastases compared with PET/CT. Prostate-specific antigen values decreased after RGS in 6 of 9 patients (67%). Conclusion: PSMA-RGS with ^99mTc-MIP-1404 identified lymph node metastases in all patients, including 2 additional lesions compared with PET/CT.

2020-03-02·Molecular Pharmaceutics2区 · 医学

Development of ¹⁸F-Fluoroglycosylated PSMA-Ligands with Improved Renal Clearance Behavior

2区 · 医学

Article

作者: Kuwert, Torsten ; Strauch, Brigitte ; Maschauer, Simone ; Potemkin, Roman ; Prante, Olaf

The prostate-specific membrane antigen (PSMA) is a type II transmembrane glycoprotein that is highly expressed in the malignant human prostate epithelium. Therefore, PSMA has emerged as a very attractive target for developing radiopharmaceuticals for the diagnosis, e.g., by positron emission tomography (PET) imaging, and radiotherapy of prostate cancer. The aim of this study was to develop ¹⁸F-labeled PSMA ligands bearing different ¹⁸F-glycosyl moieties to study the effect on the in vivo clearance behavior of radiotracers in addition to their tumor binding ability. Therefore, we applied click chemistry-based ¹⁸F-fluoroglcosylation using 2-deoxy-2-[¹⁸F]fluoroglucosyl azide or 6-deoxy-6-[¹⁸F]fluoroglucosyl azide as prosthetic groups for the radiosynthesis of the ¹⁸F-fluoroglycosylated glutamate-urea-lysine-based PSMA inhibitors 2-[¹⁸F]FGlc-PSMA ([¹⁸F]7) and 6-[¹⁸F]FGlc-PSMA ([¹⁸F]8). The PSMA inhibitory potencies were determined by competitive radioligand binding assays using ^99mTc-MIP-1404 and PSMA-expressing PC-3 PIP cells, revealing moderate PSMA inhibitory potencies for [¹⁸F]7 (IC₅₀ = 234 nM) and [¹⁸F]8 (IC₅₀ = 59 nM). Biodistribution and small-animal PET studies were performed using PSMA-positive PC-3 PIP and PSMA-negative PC-3 tumor-bearing nude mice. PSMA inhibitors [¹⁸F]7 and [¹⁸F]8 were obtained in high radioactivity yields of 19-22% (nondecay-corrected, referred to [¹⁸F]fluoride) and with molar activities of 71-136 GBq/μmol. In the biodistribution studies, the uptake levels of [¹⁸F]7 and [¹⁸F]8 in PC-3 PIP tumors were 13 ± 3%ID/g and 6 ± 5%ID/g at 60 min p.i., respectively. PSMA-negative PC-3 tumors and all other tissues had negligible low uptake values. Interestingly, [¹⁸F]7 had high uptake in the kidneys, with remarkable retention from 30 to 60 min p.i. (74 to 72%ID/g). In contrast, [¹⁸F]8 revealed a low uptake of 7.5%ID/g in the kidneys at 30 min p.i. and was rapidly cleared through the kidney (0.9%ID/g at 120 min p.i.). In direct comparison to a ⁶⁸Ga-PSMA-11 PET scan of the same mouse, [¹⁸F]7 and [¹⁸F]8 showed 2- to 3-fold higher uptake values in PC-3 PIP tumors. Both radiotracers were solely cleared via the kidneys and not via the hepatobiliary pathway. The regional kidney distribution pattern of the tracers in the kidneys revealed that ⁶⁸Ga-PSMA-11 and 2-[¹⁸F]FGlc-PSMA([¹⁸F]7) mainly accumulated in the cortex of the kidneys, whereas 6-[¹⁸F]FGlc-PSMA([¹⁸F]8) showed a 10-fold lower kidney uptake with accumulation in the inner medulla or pelvis of the kidneys. Overall, the developed 6-fluoroglucosyl derivative [¹⁸F]8, with its considerably low kidney uptake and fast clearance, demonstrated high uptake in PSMA-positive tumors in vivo. This candidate could, therefore, be valuable for translation into the clinic.

100 项与 Technetium Tc 99m trofolastat 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
前列腺癌	临床3期	美国	Lantheus Medical Imaging, Inc.	-
先天性甲肥厚	临床1期	俄罗斯	Molecular Insight Pharmaceuticals, Inc.	2012-08-01
先天性甲肥厚	临床1期	美国	Molecular Insight Pharmaceuticals, Inc.	2012-08-01
先天性甲肥厚	临床1期	荷兰	Molecular Insight Pharmaceuticals, Inc.	2012-08-01
先天性甲肥厚	临床1期	意大利	Molecular Insight Pharmaceuticals, Inc.	2012-08-01
先天性甲肥厚	临床1期	捷克	Molecular Insight Pharmaceuticals, Inc.	2012-08-01
造影剂	临床前	-	FUJIFILM Corp.	-
造影剂	临床前	-	Progenics Pharmaceuticals, Inc.	-
先天性甲肥厚	药物发现	匈牙利	Molecular Insight Pharmaceuticals, Inc.	2012-08-01
先天性甲肥厚	药物发现	波兰	Molecular Insight Pharmaceuticals, Inc.	2012-08-01

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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


NCT01667536 (Pubmed \| J Nucl Med) 人工标引	临床2期	前列腺癌	105	99m Tc-Trofolastat	(範積製簾襯顧餘壓夢網) = 鑰膚膚鬱壓艱憲鏇鬱膚願鹽壓簾壓範鑰網壓遞 (簾餘窪衊鏇鏇鏇製鹽鹽 ) 更多	积极	2017-09-01
NCT01667536 (CTgov)	临床2期	先天性甲肥厚 \| 前列腺癌	105	Drug: 99mTc-MIP-1404	積築醖鬱壓製蓋觸膚壓(醖淵餘簾糧醖醖構窪鬱) = 鬱膚獵糧網膚窪衊網艱網簾衊壓鬱憲齋構顧鏇 (積製窪獵鏇鑰製夢衊鏇, 築鹽鹹繭遞鹽餘簾壓壓 ~ 蓋築齋觸觸觸廠鏇餘齋) 更多	-	2016-03-30