EMI-137(EMI-137) - 药物靶点：c-Met_在研适应症：诊断试剂_专利_临床

概要

基本信息

药物类型

多肽偶联药物（PDC）、荧光偶联药物

别名

靶点

c-Met

作用机制

c-Met调节剂(肝细胞生长因子受体调节剂)

治疗领域

在研适应症

非在研适应症

原研机构

在研机构

Edinburgh Molecular Imaging Ltd.初创企业

非在研机构

Netherlands Cancer Insitute

University Medical Center of Utrecht

最高研发阶段临床2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

使用我们的XDC技术数据为新药研发加速。

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序列信息

Sequence Code 1277664502

来源: *****

关联

7

项与 EMI-137 相关的临床试验

ISRCTN97555789 / CompletedN/AIIT

Investigation of novel molecular imaging techniques for precision surgery and genomic characterisation of high-risk prostate cancer using EMI-137

开始日期2019-10-22

申办/合作机构

University of Oxford

NCT03360461 / Completed临床2期IIT

Intraoperative Imaging of Colon Cancer Using a Fluorescent Peptide (EMI-137) Against the c-Met Receptor

EMI-137 in laparoscopic colonic resections is a single-centre stage IIa developmental study.
Ten adult participants with a diagnosis of colon adenocarcinoma undergoing laparoscopic colonic will be recruited to the trial. Participants will receive a single intravenous dose of the IMP - EMI-137 1 to 3 hours before surgery. The ability of EMI-137 to produce visible intra-operative fluorescence of primary colon cancer and lymph node metastases will be explored and evaluated.

开始日期2018-02-14

申办/合作机构

University of Leeds

[+1]

EUCTR2016-003128-22-GB / Not yet recruiting临床2期IIT

Intraoperative imaging of colon cancer using a fluorescent peptide (EMI-137) against the c-Met receptor

开始日期2017-10-19

申办/合作机构

University of Leeds

100 项与 EMI-137 相关的临床结果

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100 项与 EMI-137 相关的转化医学

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100 项与 EMI-137 相关的专利（医药）

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7

项与 EMI-137 相关的文献（医药）

2022-08-01·European Journal of Nuclear Medicine and Molecular Imaging

Intraoperative MET-receptor targeted fluorescent imaging and spectroscopy for lymph node detection in papillary thyroid cancer: novel diagnostic tools for more selective central lymph node compartment dissection

Article

作者: van Hemel, Bettien M ; Links, Thera P ; Sondorp, Luc H J ; Coppes, Robert P ; Metman, Madelon J H ; Nguyen, Anh H ; Gill, Anthony J ; van Diest, Paul J ; Jonker, Pascal K C ; Löwik, Clemens W G M ; van Ginhoven, Tessa M ; Jansen, Liesbeth ; Fehrmann, Rudolf S N ; van Dam, Gooitzen M ; Robinson, Dominic J ; Kruijff, Schelto ; Sywak, Mark S

Abstract PurposePatients undergoing prophylactic central compartment dissection (PCLND) for papillary thyroid cancer (PTC) are often overtreated. This study aimed to determine if molecular fluorescence-guided imaging (MFGI) and spectroscopy can be useful for detecting PTC nodal metastases (NM) and to identify negative central compartments intraoperatively.MethodsWe used a data-driven prioritization strategy based on transcriptomic profiles of 97 primary PTCs and 80 normal thyroid tissues (NTT) to identify tumor-specific antigens for a clinically available near-infrared fluorescent tracer. Protein expression of the top prioritized antigen was immunohistochemically validated with a tissue microarray containing primary PTC (n = 741) and NTT (n = 108). Staining intensity was correlated with 10-year locoregional recurrence-free survival (LRFS). A phase 1 study (NCT03470259) with EMI-137, targeting MET, was conducted to evaluate safety, optimal dosage for detecting PTC NM with MFGI, feasibility of NM detection with quantitative fiber-optic spectroscopy, and selective binding of EMI-137 for MET.ResultsMET was selected as the most promising antigen. A worse LRFS was observed in patients with positive versus negative MET staining (81.9% versus 93.2%; p = 0.02). In 19 patients, no adverse events related to EMI-137 occurred. 0.13 mg/kg EMI-137 was selected as optimal dosage for differentiating NM from normal lymph nodes using MFGI (p < 0.0001) and spectroscopy (p < 0.0001). MFGI identified 5/19 levels (26.3%) without NM. EMI-137 binds selectively to MET.ConclusionMET is overexpressed in PTC and associated with increased locoregional recurrence rates. Perioperative administration of EMI-137 is safe and facilitates NM detection using MFGI and spectroscopy, potentially reducing the number of negative PCLNDs with more than 25%.Clinical trial registration.NCT03470259.

2022-03-01·Surgical Oncology3区 · 医学

A novel fluorescent c-met targeted imaging agent for intra-operative colonic tumour mapping: Translation from the laboratory into a clinical trial

3区 · 医学

Article

作者: Nick P. West ; Gemma R. Armstrong ; David G. Jayne ; Christophe Portal ; Mohammed I. Khot ; Damian J. Tolan ; Thomas A. Hughes ; Sarah L. Perry ; Tom I. Maisey ; Jim P. Tiernan

BACKGROUNDThe c-Met protein is overexpressed in many gastrointestinal cancers. We explored EMI-137, a novel c-Met targeting fluorescent probe, for application in fluorescence-guided colon surgery, in HT-29 colorectal cancer (CRC) cell line and an in vivo murine model.METHODSHT-29 SiRNA transfection confirmed specificity of EMI-137 for c-Met. A HT-29 CRC xenograft model was developed in BALB/c mice, EMI-137 was injected and biodistribution analysed through in vivo fluorescent imaging. Nine patients, received a single intravenous EMI-137 bolus (0.13 mg/kg), 1-3 h before laparoscopic-assisted colon cancer surgery (NCT03360461). Tumour and LN fluorescence was assessed intraoperatively and correlated with c-Met expression in eight samples by immunohistochemistry.FINDINGSc-Met expression HT-29 cells was silenced and imaged with EMI-137. Strong EMI-137 uptake in tumour xenografts was observed up to 6 h post-administration. At clinical trial, no serious adverse events related to EMI-137 were reported. Marked background fluorescence was observed in all participants, 4/9 showed increased tumour fluorescence over background; 5/9 had histological LN metastases; no fluorescent LN were detected intraoperatively. All primary tumours (8/8) and malignant LN (15/15) exhibited high c-Met protein expression.INTERPRETATIONEMI-137, binds specifically to the human c-Met protein, is safe, and with further refinement, shows potential for application in fluorescence-guided surgery.

2022-01-01·Journal of Nuclear Medicine1区 · 医学

c-MET Receptor–Targeted Fluorescence on the Road to Image-Guided Surgery in Penile Squamous Cell Carcinoma Patients

1区 · 医学

Article

作者: Vries, Hielke M de ; Poel, der ; Bekers, Elise ; Buckle, Tessa ; van Oosterom, Matthias N ; Karakullukcu, M Baris ; Brouwer, Oscar R ; van Leeuwen, Fijs W B ; van, Henk G

In penile squamous cell carcinoma (pSCC), primary surgery aims to obtain oncologically safe margins while minimizing mutilation. Surgical guidance provided by receptor-specific tracers could potentially improve margin detection and reduce unnecessary excision of healthy tissue. Here, we present the first results of a prospective feasibility study for real-time intraoperative visualization of pSCC using a fluorescent mesenchymal-epithelial transition factor (c-MET) receptor targeting tracer (EMI-137). Methods: EMI-137 tracer performance was initially assessed ex vivo (n = 10) via incubation of freshly excised pSCC in a solution containing EMI-137 (500 nM). The in vivo potential of c-MET targeting and intraoperative tumor visualization was assessed after intravenous administration of EMI-137 to 5 pSCC patients scheduled for surgical resection using a cyanine-5 fluorescence camera. Fluorescence imaging results were related to standard pathologic tumor evaluation and c-MET immunohistochemistry. Three of the 5 in vivo patients also underwent a sentinel node resection after local administration of the hybrid tracer indocyanine green- ^99mTc-nanocolloid, which could be imaged using a near-infrared fluorescence camera. Results: No tracer-related adverse events were encountered. Both ex vivo and in vivo, EMI-137 enabled c-MET-based tumor visualization in all patients. Histopathologic analyses showed that all pSCCs expressed c-MET, with expression levels of at least 70% in 14 of 15 patients. Moreover, the highest c-MET expression levels were seen on the outside rim of the tumors, and a visual correlation was found between c-MET expression and fluorescence signal intensity. No complications were encountered when combining primary tumor targeting with lymphatic mapping. As such, simultaneous use of cyanine-5 and indocyanine green in the same patient proved to be feasible. Conclusion: Fluorescence imaging of c-MET receptor- expressing pSCC tumors after intravenous injection of EMI-137 was shown to be feasible and can be combined with fluorescence-based lymphatic mapping. This combination is unique and paves the way toward further development of this surgical guidance approach.

100 项与 EMI-137 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
诊断试剂	临床2期	-	GE Healthcare, Inc.	-
诊断试剂	临床2期	-	Edinburgh Molecular Imaging Ltd.初创企业	-
阴茎肿瘤	临床前	荷兰	Netherlands Cancer Insitute	2019-10-12
舌肿瘤	临床前	荷兰	Netherlands Cancer Insitute	2019-10-11
前列腺癌	临床前	英国	Edinburgh Molecular Imaging Ltd.初创企业	2019-09-09
结肠癌	临床前	英国	Edinburgh Molecular Imaging Ltd.初创企业	2018-02-14
淋巴转移	临床前	英国	Edinburgh Molecular Imaging Ltd.初创企业	2018-02-14
乳腺癌	临床前	英国	-	2015-11-13
巴雷特食管	临床前	荷兰	University Medical Center of Utrecht	-
甲状腺癌	临床前	荷兰	Edinburgh Molecular Imaging Ltd.初创企业	-