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

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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 Sep 2025·European Journal of Nuclear Medicine and Molecular Imaging

Comparison of PET/CT using 68Ga-NOTA-Exendin-4 with 68Ga-DOTATATE, 18F-FDG, and conventional imaging in the localization of insulinomas

Article

Author: Bao, Xiangyuan ; He, Qing ; Li, Dong ; Pan, Meijie ; Chen, Qiusong ; Gu, Yian ; Yu, Haonan ; Yao, Shaobo

PURPOSE:

Accurate preoperative localization is particularly important for surgical treatment of insulinomas. Current imaging methods, including ¹⁸F-FDG (FDG) PET/CT, ⁶⁸Ga-DOTATATE (TATE) PET/CT, CE-CT, and CE-MRI, have limitations. This prospective study provides a direct comparison of ⁶⁸Ga-NOTA-Exendin-4 (Ex4) PET/CT with other imaging techniques.

METHOD:

47 patients with biochemically proven endogenous hyperinsulinemic hypoglycemia underwent Ex4 PET/CT and other imaging methods. Sensitivity and accuracy of all imaging procedures for localizing insulinoma were calculated at the patient level and lesion level. Both clinical (>10 years experience) and junior (< 2 years experience) nuclear medicine physician readings were used to assess the diagnostic efficacy. We compared the SUV_max and tumor-to-background ratio (TBR) of three tracers and analyzed the values with Ki-67, maximum tumor diameter, and glucose metabolism indicators.

RESULTS:

In patient level, the sensitivity and accuracy of Ex4 PET/CT (94.11% and 95.74%) were higher than TATE PET/CT (70.59%, p = 0.026; 78.72%, p = 0.030), FDG PET/CT (50.00%, p < 0.001; 63.83%, p < 0.001), CE-CT (77.77%, p = 0.135; 72.22%, p = 0.007), and CE-MRI (63.64%, p = 0.135; 43.75%, p < 0.001), respectively. Interobserver agreement was higher for Ex4 PET/CT than TATE PET/CT and FDG PET/CT (Cohen κ, 0.839 vs. 0.707 and 0.784, respectively). SUV_max and TBR of Ex4 and TATE PET/CT were significantly higher than FDG PET/CT (p < 0.01). Negative correlations of tumor Ki-67 with TATE PET/CT were observed with SUV_max (r = -0.637, p < 0.001). SUV_max and TBR of three molecular imaging methods had positive correlations with the maximum tumor diameter (p < 0.05), except TBR of FDG PET/CT. Semi-quantitative values of the three tracers showed no correlation with the lowest blood glucose level, corresponding insulin, and C-peptide level. TBR of TATE PET/CT showed a positive correlation with C-peptide (r = 0.393, p = 0.043).

CONCLUSION:

Ex4 PET/CT showed superior characteristics in localization compared to routine imaging modalities in benign insulinomas. Ex4 PET/CT demonstrates better imaging quality and interpretability than FDG PET/CT and TATE PET/CT. Combined Ex4 and TATE PET/CT could provide a comprehensive evaluation/localization of insulinoma.

TRIAL REGISTRATION:

The trial was retrospectively registered at ClinitalTrial.gov (NCT06690957 and NCT06725693) on November 14, 2024 and December 5, 2024.

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 ; Xue, Huadan ; Yao, Shaobo ; 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.

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


Pubmed \| Eur J Nucl Med Mol Imaging	Not Applicable	Insulinoma Ki-67 \| maximum tumor diameter \| glucose metabolism indicators	47	68Ga-NOTA-Exendin-4 PET/CT	zrjuwlzois(alhgfvjoen) = gnchlcjglj tfdvwqepxa (ilpsmdcujr ) View more	Positive	22 Apr 2025
				68Ga-DOTATATE PET/CT	zrjuwlzois(alhgfvjoen) = blogujpyol tfdvwqepxa (ilpsmdcujr ) View more
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	kxyxaqmjwk(nhtkviqigx) = etnjaiqxid pjqmepfrgw (caqxlrmaql )	Positive	08 Nov 2024
				68Ga-NOTA-exendin-4	kxyxaqmjwk(nhtkviqigx) = bywuvwrfmy pjqmepfrgw (caqxlrmaql )