Delving into the Latest Updates on 68Ga-NOTA-exendin-4 with Synapse

Overview

Basic Info

Drug Type

Peptide Conjugate Radionuclide, Diagnostic radiopharmaceuticals

Synonyms-

Target

GLP-1R

Action

agonists

Mechanism

GLP-1R agonists(Glucagon-like peptide 1 receptor agonists)

Therapeutic Areas

NeoplasmsDigestive System DisordersEndocrinology and Metabolic Disease+ [1]

Active Indication

Insulinoma

Inactive Indication

Nesidioblastosis

Originator Organization-

Active Organization

First Affiliated Hospital Of Fujian Medical University

Inactive Organization

Peking Union Medical College Hospital

License Organization-

Drug Highest PhasePhase 1

First Approval Date-

Regulation-

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Structure/Sequence

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Sequence Code 751

The sequence is quoted from: *****

Glucagon-like peptide-1 receptor (GLP-1R)-targeted PET imaging with 68Ga-labeled compounds is able to provide superior sensitivity and specificity to detect insulinoma, like the widely studied [68Ga]Ga-NOTA-exendin-4. This pilot study was prospectively designed to evaluate the early dynamic distribution of [68Ga]Ga-HBED-CC-exendin-4, a novel radiopharmaceutical targeting GLP-1R, which was compared with [68Ga]Ga-NOTA-exendin-4 in the same group of insulinoma patients.

Start Date01 Oct 2021

Sponsor / Collaborator

Peking Union Medical College Hospital

NCT04979611

/ RecruitingPhase 1IIT

The Clinical Application of 68Ga-NOTA-exendin-4 PET/CT in Detecting Insulinoma

The small insulinoma can not be detected by the CT or MRI. We use 68Ga-NOTA-exendin-4 positron emission tomography/computed tomography (PET/CT) to detect the insulinoma for the patient diagnosed with endogenous hyperinsulinemic hypoglycaemia. And the diagnostic value will be performed. A single dose of 37-111 Mega-Becquerel (MBq) 68Ga-NOTA-exendin-4 will be injected intravenously. Visual and semiquantitative method will be used to assess the PET/CT images.

Start Date01 Aug 2020

Sponsor / Collaborator

First Affiliated Hospital Of Fujian Medical University

NCT02560376

/ Unknown statusEarly Phase 1IIT

68Ga-NOTA-exendin-4 PET/CT for the Localization of Insulinoma and Diagnosis of Nesidioblastosis

This is an open-label positron emission tomography/computed tomography (PET/CT) study to investigate the diagnostic performance and evaluation efficacy of 68Ga-NOTA-exendin-4 in insulinoma and nesidioblastosis patients. A single dose of 55.5-111 Mega-Becquerel (MBq) 68Ga-NOTA-exendin-4 will be injected intravenously. Visual and semiquantitative method will be used to assess the PET/CT images.

Start Date01 Feb 2014

Sponsor / Collaborator

Peking Union Medical College Hospital

[+1]

100 Clinical Results associated with 68Ga-NOTA-exendin-4

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100 Translational Medicine associated with 68Ga-NOTA-exendin-4

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100 Patents (Medical) associated with 68Ga-NOTA-exendin-4

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4

Literatures (Medical) associated with 68Ga-NOTA-exendin-4

01 Jan 2025·CLINICAL NUCLEAR MEDICINE

Glucagon-Like Peptide-1 Receptor–Targeted PET/CT With 68Ga-HBED-CC-Exendin-4 in Localizing Insulinoma

Article

Author: Wang, Rongxi ; Zhu, Lin ; Pan, Qingqing ; Zhu, Zhaohui ; Wang, Guochang ; Ma, Heng ; Hong, Haiyan ; Wang, Jiarou ; Li, Linlin ; Chen, Jingci ; Luo, Yaping ; Kung, Hank F. ; Jin, Wenbin

Purpose:

Modifying glucagon-like peptide-1 receptor (GLP-1R)–targeted PET agent to achieve faster renal clearance and preserved high affinity to GLP-1R is clinically relevant. The aim of this study is to assess the performance of a newly developed GLP-1R–targeted agent, 68Ga-HBED-CC-exendin-4 in localizing insulinoma, and its biodistribution, as compared with previously introduced 68Ga-NOTA-exendin-4.

Patients and Methods:

Nineteen patients with endogenous hyperinsulinemic hypoglycemia were enrolled and referred for 68Ga-HBED-CC-exendin-4 PET/CT and 68Ga-NOTA-exendin-4 PET/CT within 2 consecutive days. Diagnostic performance of the 2 tracers in localizing insulinoma was evaluated, and SUV of the lesion, normal pancreas background, kidneys, and bladder were measured.

Results:

68Ga-HBED-CC-exendin-4 and 68Ga-NOTA-exendin-4 PET/CT exhibited an equivalent efficacy in detection rate (both sensitivity of 100%). Although SUVmax of the tumor in 68Ga-HBED-CC-exendin-4 was significantly lower than that in 68Ga-NOTA-exendin-4 (20.01 ± 9.41 vs 31.78 ± 15.46, P < 0.001) at 50 minutes postinjection, there was no significant difference in the tumor-to-background ratio between the 2 agents (8.61 ± 3.57 vs 8.18 ± 3.38, P = 0.326), and the lesions could be visible as early as 4 minutes postinjection for both agents in patients who underwent dynamic PET/CT. In addition, 68Ga-HBED-CC-exendin-4 exhibited approximately 30% decrease of the renal accumulation compared with 68Ga-NOTA-exendin-4 (SUVmean, 42.21 ± 5.79 vs 58.58 ± 10.06 at 50 minutes, P < 0.001).

Conclusions:

68Ga-HBED-CC-exendin-4 is an effective agent for localizing insulinoma showing similar detectability and tumor-to-background ratio compared with 68Ga-NOTA-exendin-4. Notably, 68Ga-HBED-CC-exendin-4 exhibits significantly lower renal uptake than 68Ga-NOTA-exendin-4, which might potentially benefit the detection of the tumors adjacent to the left kidneys.

01 May 2016·Journal of nuclear medicine : official publication, Society of Nuclear MedicineQ1 · MEDICINE

Glucagon-Like Peptide-1 Receptor PET/CT with ⁶⁸Ga-NOTA-Exendin-4 for Detecting Localized Insulinoma: A Prospective Cohort Study

Q1 · MEDICINE

Article

Author: Zhu, Zhaohui ; Chen, Xiaoyuan ; Luo, Yaping ; Li, Fang ; Yu, Miao ; Wu, Wenming ; Zhao, Yupei ; Yao, Shaobo ; Xue, Huadan ; Pan, Qingqing ; Kiesewetter, Dale O

METHODS:

In our prospective cohort study, patients with endogenous hyperinsulinemic hypoglycemia were enrolled. CT, MRI, endoscopic ultrasound, and (99m)Tc-hydrazinonicotinamide-TOC SPECT/CT were done according to standard protocols. GLP-1R PET/CT was performed 30-60 min after the injection of (68)Ga-NOTA-exendin-4. The gold standard for diagnosis was the histopathologic results after surgery.

RESULTS:

Of 52 recruited patients, 43 patients with histopathologically proven insulinomas were included for the imaging studies. Nine patients did not undergo surgical intervention. (68)Ga-NOTA-exendin-4 PET/CT correctly detected insulinomas in 42 of 43 patients with high tumor uptake (mean SUVavg ± SD, 10.2 ± 4.9; mean SUVmax ± SD, 23.6 ± 11.7), resulting in sensitivity of 97.7%. In contrast, (99m)Tc-hydrazinonicotinamide-TOC SPECT/CT showed a low sensitivity of 19.5% (8/41) in this group of patients; however, it successfully localized the tumor that was false-negative with GLP-1R PET/CT. The sensitivities of CT, MR, and endoscopic ultrasonography were 74.4% (32/43), 56.0% (14/25), and 84.0% (21/25), respectively.

CONCLUSION:

(68)Ga-NOTA-exendin-4 PET/CT is a highly sensitive imaging technique for the localization of insulinoma.

01 Apr 2016·Clinical nuclear medicineQ3 · MEDICINE

68Ga-NOTA-Exendin-4 PET/CT in Localization of an Occult Insulinoma and Appearance of Coexisting Esophageal Carcinoma

Q3 · MEDICINE

Article

Author: Dale O. Kiesewetter ; Fang Li ; Xiaoyuan Chen ; Naishi Li ; Yaping Luo

A 61-year-old woman with biochemically proven endogenous hyperinsulinemic hypoglycemia and negative conventional imaging underwent 68Ga-NOTA-exendin-4 PET/CT for localization of insulinoma. Focal intense radioactivity in the tail of the pancreas was observed that was subsequently confirmed as insulinoma pathologically after surgical resection. In addition, esophageal carcinoma with lymph node and hepatic metastases was found by FDG PET/CT in the same patient. Neither the primary carcinoma nor the metastases showed increased radioactivity on 68Ga-NOTA-exendin-4 PET/CT.

100 Deals associated with 68Ga-NOTA-exendin-4

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Insulinoma	Phase 1	China	Peking Union Medical College Hospital	01 Feb 2014
Nesidioblastosis	Phase 1	China	Peking Union Medical College Hospital	01 Feb 2014

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT05034783 (A Head-to-Head Comparison to 68Ga-NOTA-Exendin-4, Pubmed \| Clin Nucl Med)	Early Phase 1	Insulinoma GLP-1R	-	68Ga-HBED-CC-exendin-4	qakcobnsmt(mopxujvfxa) = mjawhmmonz mrfkydaqpj (gpmbpxjxro )	Positive	08 Nov 2024
				68Ga-NOTA-exendin-4	qakcobnsmt(mopxujvfxa) = nyskskizff mrfkydaqpj (gpmbpxjxro )
EANM2019	Not Applicable	Multiple Endocrine Neoplasia Type 1	6	68Ga-DOTA-exendin-4 PET/CT	nvawgyxqbe(knpcdyynhe) = kmqafftmkc fgfbbughgw (zkunipdlcr, 54.6 - 98.1)	-	18 Sep 2019
				68Ga-DOTA-exendin-4 (MRI)	nvawgyxqbe(knpcdyynhe) = wvcawgrwib fgfbbughgw (zkunipdlcr, 13.9 - 68.4)

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Biosimilar

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