NODAGA-exendin-4
Exendin-4 turned into a scan agent that finds insulin-making tumours and beta cells
NODAGA-exendin-4 is exendin-4, the lizard-venom peptide that also forms the diabetes drug exenatide, with a chelator that holds gallium-68. Because beta cells carry the GLP-1 receptor and benign insulinomas carry it in large amounts, the scan finds small insulin-secreting tumours that other imaging misses, and shows whether a child's congenital hyperinsulinism comes from one spot. Researchers also use it to estimate beta-cell mass in diabetes. It is investigational.
Used in human trials: 100 MBq, Single injection, Intravenous (Gallium-68 NODAGA-exendin-4 PET, adults) Details ↓
Recommended Dosing
Used in human trials
No manufacturer dose exists for this use: these are amounts given in published trials, not recommendations.
What is it?
Insulinomas are tumours of the pancreas that make insulin and cause attacks of low blood sugar. Surgery cures the benign ones, but only if the surgeon knows where the tumour is, and CT, MRI and somatostatin receptor PET often miss them. Insulinomas carry the GLP-1 receptor in very large numbers. Exendin-4, the GLP-1 receptor agonist from lizard venom that also forms exenatide, binds that receptor, so attaching a radioactive label to it makes a receptor scan. Several versions exist with different chelators; this entry covers the NODAGA version, studied mostly at Radboud University Medical Center in the Netherlands.
Its main evidence is in localising insulinomas. In a prospective multicentre study of 69 adults with proven hyperinsulinaemic hypoglycaemia, accuracy was 94.4% against 64.8% for somatostatin receptor PET, 83.3% for CT or MRI and 82.8% for endoscopic ultrasound, and 13% of patients only got the right diagnosis after the exendin scan. Readers agreed perfectly. In France, 50 scans in patients whose earlier imaging was negative led to 29 successful operations, every positive scan was confirmed, and a negative scan helped abandon the diagnosis in most others. In young people with multiple endocrine neoplasia type 1, who often have several pancreatic tumours, it allowed surgeons to remove just the culprit lesion.
In congenital hyperinsulinism, infants whose low blood sugar comes from a single focal lesion can be cured by removing it. In 19 children, the exendin scan found focal disease with 100% sensitivity against 71% for the standard fluorine-18 DOPA scan, with better contrast and readers' agreement. Some clinicians have asked for replication of that result.
Because healthy beta cells also carry the receptor, pancreatic uptake can serve as a rough measure of beta-cell mass. Radboud studies have used it to compare people with type 1 diabetes of short and long duration, people with stable and unstable glucose, people whose type 2 diabetes did or did not remit after gastric bypass, and people with or without hypoglycaemia after bypass, and to see surviving islets after transplantation into the liver. These are small research studies. In the brain, it showed the pituitary but no other GLP-1 receptor signal in obese adults.
Radiation doses are low: about 0.7 mSv for a standard adult scan, with the kidneys most exposed. NODAGA-exendin-4 has no FDA or EMA approval, is made in hospital radiopharmacies and is used only for scans. It has nothing to do with taking exenatide as a medicine.
Mechanism of Action
It is a scan agent. Exendin-4 finds the GLP-1 receptor; gallium-68 shows where it is on PET.
GLP-1 receptor binding
Exendin-4 binds the GLP-1 receptor on beta cells, and insulinomas carry it in excess (2022 and 2024 studies).
Gallium-68 PET
Gives high lesion contrast; insulinoma-to-background ratio was about 15 against 5 for somatostatin PET (2024 study).
Beta-cell mass estimate
Pancreatic uptake is used as a proxy for beta-cell mass in diabetes research (2023 and 2026 studies).
Kidney exposure
The kidneys clear and retain the tracer and receive the highest dose (2020 study).
Published Research
These studies were read from their PubMed abstracts on October 29, 2026: eleven in people and three in animals. Five human studies titled for beta-cell mass and one rat study titled with the full chemical name are carded because their abstracts name gallium-68 NODAGA-exendin-4. Studies of other exendin tracers (DOTA-, NOTA- and DO3A-exendin-4) concern different molecules and are not included.
Multicentre insulinoma localisation
Sixty-nine adults with proven endogenous hyperinsulinaemic hypoglycaemia had the exendin scan and all routine imaging. Accuracy was 94.4% against 64.8% for somatostatin PET, 83.3% for CT/MRI and 82.8% for endoscopic ultrasound. Tumour-to-background ratio was about three times higher than somatostatin PET; readers agreed fully.
Occult insulinomas in France
Fifty scans in 44 patients with negative or unclear imaging were positive in 62%, and all 29 resulting resections confirmed an insulinoma. After 14 of 19 negative scans the diagnosis was dropped. One patient had symptomatic low blood sugar after injection.
Conservative surgery in MEN1
Five young patients had single-lesion laparoscopic enucleation guided by the scan; none had recurrence or pancreatic insufficiency over a median 48 months. Of 15 operated on conventional imaging, 80% needed more extensive surgery and a third developed pancreatic insufficiency.
Focal congenital hyperinsulinism
Nineteen children had both scans before surgery; 14 with focal lesions were operated. Sensitivity was 100% for the exendin scan and 71% for fluorine-18 DOPA, with higher lesion contrast (2.02 vs 1.40) and reader agreement (0.91 vs 0.56). Surgeons rated it better for finding the lesion.
Human radiation dosimetry
Six patients received 100 MBq and four scans over 4 hours. Effective dose was 0.71 mSv for adults, with the kidney the most exposed organ (47.3 mGy per 100 MBq). Estimated doses for children were 0.59-2.32 mSv for 20-30 MBq, lower than for somatostatin tracers.
Brain imaging in obesity
In ten obese adults before bariatric surgery, there was clear uptake in the pituitary area but none elsewhere in the brain, so the authors concluded it cannot measure brain GLP-1 receptors.
Islets after liver transplantation
Thirteen people with type 1 diabetes, nine with functioning intrahepatic islet grafts, had scans repeated over time. Liver hotspots took up more tracer in transplanted patients than controls (median 0.55 vs 0.43), and graft islets carried the receptor on staining.
Beta-cell mass and glucose variability
Sixteen people with type 1 diabetes were grouped by glucose variability. Pancreatic uptake was higher in the low-variability group (5.1 vs 2.9), who also had lower HbA1c and more time in range; uptake correlated with time in range (r 0.64).
Short vs long type 1 diabetes
In 26 people, estimated total beta-cell mass was higher with diabetes under 7 years than longer (4.4 vs 2.8 kBq/MBq), with larger pancreases and better beta-cell function; mass correlated with pancreatic volume (r 0.91).
Diabetes remission after gastric bypass
Seventeen people received about 100 MBq. Those whose type 2 diabetes remitted had better beta-cell function, but beta-cell mass did not differ from non-remitters (3.6 vs 3.8 kBq/MBq), arguing against new beta-cell growth.
Hypoglycaemia after gastric bypass
Nineteen people, ten with postbariatric hypoglycaemia, received about 102 MBq. Beta-cell mass did not differ between groups, though those with hypoglycaemia had smaller pancreases, arguing against beta-cell expansion as the cause.
Gallium-68 and copper-64 forms in rats
Both forms labelled pancreatic islets specifically on autoradiography, but the pancreas could not be seen on rat PET. Kidneys took up the most. Projected effective doses were 0.012 mSv per MBq for gallium-68 and 0.144 for copper-64, whose kidney dose may limit clinical use.
Heart repair after infarction in rats
Uptake rose in infarcted heart muscle, peaking at 3 days and persisting at 1 week, and was blocked by unlabelled exendin. It was 8.6 times higher than in sham hearts on autoradiography and tracked macrophage numbers.
Atherosclerotic plaques in mice
In hypercholesterolaemic mice with and without diabetes, the tracer detected GLP-1 receptor in inflamed plaques, where staining placed the receptor mainly on M2 macrophages.
Clinical imaging protocol
A methods chapter describing gallium-68 labelling of the NODAGA-exendin conjugate, quality control and PET/CT. It notes the scan's sensitivity for insulinomas comes from their very high GLP-1 receptor expression, and its use for beta-cell mass research and congenital hyperinsulinism.
Dosing Data
NODAGA-exendin-4 has no approved label. It is dosed by radioactivity for a single scan; rows are from the carded human studies.
Educational information, not medical advice. Each dose above is tagged with its source: an approved label, a published human study, animal data, or amounts reported by users. None is a recommendation for you. An unapproved compound has no established safe or effective human dose, and products sold for “research use only” are not made or tested for people. Talk to a doctor before acting on anything on this site, including before you start, stop or change any medicine or dose. Full medical disclaimer.
What a Buyer Needs to Know
What is sold, how it is mixed, stored and taken, and what is known about its safety, quality and legal status. Each part names its source. Where we have none, it says unknown.
What is sold
Unknown: we hold no regulator's label that says in what form NODAGA-exendin-4 is supplied. It is a radioactive drug: the next part says where it is prepared and given.
Mixing a vial: a worked example
Nothing to mix at home, and no syringe units to work out: NODAGA-exendin-4 is a radioactive drug, prepared and given in nuclear-medicine departments, and its dose is an amount of radioactivity (MBq or GBq), not a weight.
This page's dosing note: “Investigational radioactive imaging agent, prepared and given only in nuclear-medicine departments within studies; these are study activities, not recommendations.”
Source: this page's own note in Dosing Data below; the amount of each dose row in Dosing Data below.
Storage before and after mixing
Unknown: no label on file says how NODAGA-exendin-4 is stored. It is a radioactive drug held by the nuclear-medicine department that prepares and gives it (see the part above); the home rules for a mixed vial in the mixing guide do not apply to it.
How it is taken
As it was given in human studies: Intravenous (Single injection; Gallium-68 NODAGA-exendin-4 PET, adults).
Source: Used in human trials: the route and frequency of each row in Dosing Data below.
What to expect, and when
How long it stays in the body: not established by a measurement cited on this entry.
How long the doses were given: Gallium-68 NODAGA-exendin-4 PET, adults: Scans up to 4 hours later; Gallium-68 NODAGA-exendin-4 PET, beta-cell mass studies: One scan.
When effects appear: unknown; no source on this page gives a time to effect for NODAGA-exendin-4. Results reported in the studies are under Published Research.
Source: Used in human trials, the duration of each row in Dosing Data below.
Side effects, and when to stop or get help
From the Side Effects section: Symptomatic low blood sugar after injection in 1 of 44 patients with suspected insulinoma; Radiation: about 0.71 mSv per 100 MBq in adults, highest to the kidneys. Full list and cautions ↓
When to stop or get help: unknown; no label or trial on file sets rules for stopping NODAGA-exendin-4. Treat a severe or unexpected reaction as a reason to stop and see a doctor.
Source: the Side Effects section below (“From the human studies above”).
Interactions
Unknown: a PubMed search for human interaction studies of NODAGA-exendin-4 (reviewed 2026-10-28) found none. Unknown is not the same as safe to combine.
Every peptide's record, with its source: the interaction matrix.
Checking what you bought
Unknown: no published independent test of NODAGA-exendin-4 products is in our lab-results database yet, so how products sold under this name measure up is not known.
To read a certificate of analysis, paste it into the COA decoder. Trust & Verification explains what independent testing can and cannot show.
Legal status
US: In Clinical Trials (Not approved: Drugs@FDA and the EMA medicines list hold no record (searched October 28, 2026)). Sport: Prohibited (S0 catch-all).
Country by country ↓ · Regulatory tracker
Source: this entry's approval status and the WADA Prohibited List, as in Legal Status below.
Side Effects & Contraindications
Reported Side Effects
From the human studies above.
Contraindications & Cautions
No approved label exists, so there are no official contraindications. Points from the studies:
Legal Status
NODAGA-exendin-4 is investigational in every jurisdiction checked.
Frequently Asked Questions
?What is NODAGA-exendin-4?
Exendin-4 with a NODAGA chelator holding gallium-68, used for PET scans of GLP-1 receptors.
?Is it the same as exenatide?
It uses the same exendin-4 peptide, modified to carry a radioactive label and given once in a trace amount for a scan. It is not a diabetes treatment.
?What is it used for?
Finding small insulinomas before surgery, finding focal lesions in congenital hyperinsulinism, and research on beta-cell mass.
?Is it approved?
No.
References
- [clinical-trial] Boss M, et al. "Improved Localization of Insulinomas Using (68)Ga-NODAGA-Exendin-4 PET/CT." J Nucl Med, 2024;65(12):1959-1964. PMID: 39419553.
- [pubmed] Aveline C, et al. "68 Ga-NODAGA-EXENDIN-4 PET/CT in the Detection or the Exclusion of Occult Sporadic Insulinomas." Clin Nucl Med, 2025;50(12):1109-1119. PMID: 41223138.
- [pubmed] Ambulkar KS, et al. "Outcomes of 68Ga-NODAGA-Exendin-4 PET/CT Guided Surgical Management of Insulinomas in MEN1: A Preliminary Study." Nuklearmedizin, 2025;64(5):301-307. PMID: 41005352.
- [clinical-trial] Boss M, et al. "(68)Ga-NODAGA-Exendin-4 PET/CT Improves the Detection of Focal Congenital Hyperinsulinism." J Nucl Med, 2022;63(2):310-315. PMID: 34215672.
- [clinical-trial] Boss M, et al. "PET-Based Human Dosimetry of (68)Ga-NODAGA-Exendin-4, a Tracer for β-Cell Imaging." J Nucl Med, 2020;61(1):112-116. PMID: 31519801.
- [pubmed] Deden LN, et al. "Brain Imaging of the GLP-1 Receptor in Obesity Using (68)Ga-NODAGA-Exendin-4 PET." Brain Sci, 2021;11(12). PMID: 34942949.
- [pubmed] Jansen TJP, et al. "Monitoring β-Cell Survival After Intrahepatic Islet Transplantation Using Dynamic Exendin PET Imaging: A Proof-of-Concept Study in Individuals With Type 1 Diabetes." Diabetes, 2023;72(7):898-907. PMID: 37068261.
- [pubmed] Jansen TJP, et al. "Importance of beta cell mass for glycaemic control in people with type 1 diabetes." Diabetologia, 2023;66(2):367-375. PMID: 36394644.
- [pubmed] Tokgöz S, et al. "β-Cell Mass and Function, Pancreatic Volume, and Fat Differences Between Short- and Long-Duration Type 1 Diabetes: A Detailed PET/CT Imaging Study." J Nucl Med, 2026. PMID: 42850044.
- [pubmed] Tokgöz S, et al. "Beta cell function and mass in individuals with and without remission of type 2 diabetes after Roux-en-Y gastric bypass." Diabetologia, 2026;69(5):1295-1300. PMID: 41555052.
- [pubmed] Tokgöz S, et al. "β-Cell Mass in Individuals With and Without Postbariatric Hypoglycemia After Roux-en-Y Gastric Bypass." Diabetes, 2025;74(12):2301-2306. PMID: 41066755.
- [pubmed] Mikkola K, et al. "64Cu- and 68Ga-labelled [Nle(14),Lys(40)(Ahx-NODAGA)NH2]-exendin-4 for pancreatic beta cell imaging in rats." Mol Imaging Biol, 2014;16(2):255-63. PMID: 24101374.
- [pubmed] Ståhle M, et al. "Glucagon-like peptide-1 receptor expression after myocardial infarction: Imaging study using (68)Ga-NODAGA-exendin-4 positron emission tomography." J Nucl Cardiol, 2020;27(6):2386-2397. PMID: 30547299.
- [pubmed] Ståhle M, et al. "Evaluation of glucagon-like peptide-1 receptor expression in nondiabetic and diabetic atherosclerotic mice using PET tracer (68)Ga-NODAGA-exendin-4." Am J Physiol Endocrinol Metab, 2021;320(5):E989-E998. PMID: 33843281.
- [review] Tokgöz S, et al. "Protocol for Clinical GLP-1 Receptor PET/CT Imaging with [(68)Ga]Ga-NODAGA-Exendin-4." Methods Mol Biol, 2023;2592:143-153. PMID: 36507990.
- [pubmed] Prasad V, et al. "Reply: (68)Ga NODAGA-Exendin-4 PET Scanning for Focal Congenital Hyperinsulinism: Need for Replication." J Nucl Med, 2022;63(3):493-494. PMID: 35232881.
Sources & Citations
Studies were read from their PubMed records on October 29, 2026. Regulatory status comes from Drugs@FDA and the EMA medicines list (searched October 28, 2026) and trial listings from ClinicalTrials.gov (October 29, 2026). Grey Peptides sells nothing and links to no vendor.
Medical Disclaimer: This content is for educational and informational purposes only. It is not medical advice, and nothing here is an instruction to obtain or use any compound. Talk to a licensed clinician about your own situation.