Gozetotide

Gallium Ga 68 gozetotide binds to PSMA. It binds to cells that express PSMA, including malignant prostate cancer cells, which usually overexpress PSMA.

• GOZELLIX, after radiolabeling with Ga 68, is indicated for positron emission tomography (PET) of prostate-specific membrane antigen (PSMA) positive lesions in men with prostate cancer: With suspected metastasis who are candidates for initial definitive therapy. With suspected recurrence based on elevated serum prostate-specific antigen (PSA) level.ICD-10: C61

• None None ( 4 )contraindicated

Use appropriate aseptic technique and radiation safety handling measures in the manipulation and administration of Gallium Ga 68 Gozetotide Injection. ( 2.1 ) The recommended amount of radioactivity for adults is 111 MBq to 259 MBq (3 mCi to 7 mCi) as a bolus intravenous injection. ( 2.2 ) A diuretic expected to act within the uptake time period may be administered at the time of radiotracer injection. ( 2.2 ) Initiate imaging 50 minutes to 100 minutes after administration. The patient should void immediately prior to initiation of imaging. The scan should begin caudally and proceed cranially. ( 2.10 ) See full prescribing information for additional preparation, administration, imaging, and radiation dosimetry information. ( 2 ) 2.1 Radiation Safety - Drug Handling After radiolabeling of GOZELLIX, the vial contains Gallium Ga 68 Gozetotide Injection. Handle Gallium Ga 68 Gozetotide Injection with appropriate safety measures to minimize radiation exposure [see Warnings and Precautions (5.2) ] . Use waterproof gloves, effective radiation shielding, and other appropriate safety measures when preparing and handling Gallium Ga 68 Gozetotide Injection. Radiopharmaceuticals should be used by or under the control of healthcare providers who are qualified by specific training and experience in the safe use and handling of radionuclides, and whose experience and training have been approved by the appropriate governmental agency authorized to license the use of radionuclides.

Risk for Misinterpretation: Gallium Ga 68 gozetotide uptake can be seen in a variety of tumor types and in non-malignant processes. Clinical correlation, which may include histopathological evaluation of the suspected prostate cancer site, is recommended. ( 5.1 ) Radiation Risks: Ensure safe handling to protect patients and health care providers from unintentional radiation exposure. ( 2.1 , 5.2 ) Hypersensitivity Reactions to Sulfites: Ascorbic Acid Stabilizer contains sodium metabisulfite, a sulfite that may cause life-threatening hypersensitivity reactions including anaphylaxis. ( 5.3 ) 5.1 Risk for Misinterpretation Image interpretation errors can occur with GOZELLIX PET. A negative image does not rule out the presence of prostate cancer and a positive image does not confirm the presence of prostate cancer. Gallium Ga 68 gozetotide uptake is not specific for prostate cancer and may occur with other types of cancer as well as non-malignant processes such as Paget's disease, fibrous dysplasia, and osteophytosis. The performance of GOZELLIX for imaging of biochemically recurrent prostate cancer seems to be affected by serum PSA levels and by site of disease. The performance of GOZELLIX for imaging of metastatic pelvic lymph nodes prior to initial definitive therapy seems to be affected by Gleason score [ see Clinical Studies (14.1 , 14.2) ] . Clinical correlation, which may include histopathological evaluation of the suspected prostate cancer site, is recommended.

The most commonly reported adverse reactions include nausea, diarrhea, and dizziness. ( 6 ) To report SUSPECTED ADVERSE REACTIONS, contact Telix Pharmaceuticals (US) Inc. at 1-844-455-8638 or contact FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The safety of GOZELLIX has been established based on two prospective studies of another formulation of gallium Ga 68 gozetotide in patients with prostate cancer [see Clinical Studies (14.1 , 14.2) ] . Below is a display of the adverse reactions in these studies. The safety of gallium Ga 68 gozetotide was evaluated in 960 patients in the PSMA-PreRP and PSMA-BCR studies, each receiving one dose of gallium Ga 68 gozetotide. The average injected activity was 188.7 ± 40.7 MBq (5.1 ± 1.1 mCi) [see Clinical Studies (14.1 , 14.2) ] . The most commonly reported adverse reactions were nausea, diarrhea, and dizziness, occurring at a rate of <1%.

8.1 Pregnancy Risk Summary GOZELLIX is not indicated for use in females. There are no available data with gallium Ga 68 gozetotide injection use in pregnant women to evaluate for a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes. All radiopharmaceuticals, including GOZELLIX, have the potential to cause fetal harm depending on the fetal stage of development and the magnitude of the radiation dose. Animal reproduction studies have not been conducted with gallium Ga 68 gozetotide. 8.2 Lactation Risk Summary GOZELLIX is not indicated for use in females. There are no data on the presence of gallium Ga 68 gozetotide in human milk, the effect on the breastfed infant, or the effect on milk production. 8.4 Pediatric Use The safety and effectiveness of gallium Ga 68 gozetotide in pediatric patients have not been established. 8.5 Geriatric Use The efficacy of gallium Ga 68 gozetotide PET in geriatric patients with prostate cancer is based on data from two prospective studies [see Clinical Studies (14.1 , 14.2) ]. Of the total number of subjects in the PSMA-PreRP and PSMA-BCR studies, 691 of 960 (72%) patients were 65 years of age and older while 195 (20%) were 75 years of age and older.

Metabolism

Distribution Intravenously injected gallium Ga 68 gozetotide is cleared from the blood and is accumulated preferentially in the liver (15%), kidneys (7%), spleen (2%), and salivary glands (0.5%). Gallium Ga 68 gozetotide uptake is also seen in the adrenals and prostate.

In the event of an overdose of gallium Ga68 gozetotide, reduce the radiation absorbed dose to the patient where possible by increasing the elimination of the drug from the body using hydration and frequent bladder voiding. A diuretic might also be considered. If possible, an estimate of the radiation effective dose given to the patient should be made.

• Dec 1, 2020NDANDA212642Univ Ca Los Angeles
• Dec 1, 2020NDANDA212643Univ Of Ca San Fran
• Dec 17, 2021NDANDA214032Telix
• Mar 23, 2022NDANDA215841Novartis
• Mar 20, 2025NDANDA219592Telix Innovations
• May 14, 2026ANDAANDA219189Ionetix

1. 1Injection Site Pain13732%
2. 2Hot Flush337.8%
3. 3Erectile Dysfunction255.9%
4. 4Fatigue174.0%
5. 5Death112.6%
6. 6Burning Sensation92.1%
7. 7Muscular Weakness92.1%
8. 8Overdose92.1%
9. 9Pathological Fracture92.1%
10. 10Rash92.1%
11. 11Asthenia81.9%
12. 12Injection Site Discomfort81.9%
13. 13Positron Emission Tomogram Abnormal81.9%
14. 14Anaemia71.7%
15. 15Cerebral Amyloid Angiopathy71.7%

The 10 most recently updated of 30 ClinicalTrials.gov registrations naming Gozetotide as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• NEPC Study: An Exploratory Safety and Efficacy Study With PSMA, SSTR2 and GRPR Targeted Radioligand Therapy in Metastatic Neuroendocrine Prostate Cancer.
  Active not recruiting · Phase 1 · Interventional · 31 enrolled · Novartis Pharmaceuticals
  NCT06379217updated 2026-06-10
• An Open-label Study Comparing Lutetium (177Lu) Vipivotide Tetraxetan Versus Observation in PSMA Positive OMPC.
  Recruiting · Phase 3 · Interventional · 450 enrolled · Novartis Pharmaceuticals
  NCT05939414updated 2026-06-10
• A Study to Evaluate the Efficacy, Safety, Pharmacokinetics and Dosimetry of [177Lu]Lu-PSMA-617 in Chinese Adult Male Patients With Progressive PSMA-Positive mCRPC
  Completed · Phase 2 · Interventional · 62 enrolled · Novartis Pharmaceuticals
  NCT05670106updated 2026-06-08
• A Phase II Study of AAA617 Alone and AAA617 in Combination With ARPI in Patients With PSMA PET Scan Positive CRPC
  Active not recruiting · Phase 2 · Interventional · 49 enrolled · Novartis Pharmaceuticals
  NCT05849298updated 2026-05-27
• 68Ga-PSMA-11 PET for the Diagnosis of Metastatic Castration Resistant Prostate Cancer
  Terminated · Phase 2 · Interventional · 15 enrolled · Thomas Hope
  NCT04716725updated 2026-05-15
• Re-treatment With 177Lu-PSMA-617 for the Treatment of Metastatic Castration-Resistant Prostate Cancer, RE-LuPSMA Trial
  Recruiting · Phase 2 · Interventional · 40 enrolled · Jonsson Comprehensive Cancer Center
  NCT06288113updated 2026-03-13
• Phase 2 Randomized Trial of Flexible Dosing Schedule of 177Lu-PSMA-617 for the Treatment of Metastatic Castration-Resistant Prostate Cancer (FLEX-MRT)
  Recruiting · Phase 2 · Interventional · 90 enrolled · Jonsson Comprehensive Cancer Center
  NCT06216249updated 2026-03-10
• Image-Guided (68Ga-PSMA-11 PET/CT) Prostate Biopsy for the Diagnosis of Prostate Cancer in Men With Prior Negative/Inconclusive Biopsy
  Active not recruiting · Early phase 1 · Interventional · 30 enrolled · Jonsson Comprehensive Cancer Center
  NCT05160597updated 2026-02-12
• 68Ga PSMA PET Imaging for the Treatment of Advanced Liver Cancer
  Completed · Phase 2 · Interventional · 29 enrolled · Mayo Clinic
  NCT05176223updated 2026-02-05
• Vorinostat and 177Lu-PSMA-617 for the Treatment of PSMA-Low Metastatic Castration-Resistant Prostate Cancer
  Recruiting · Phase 2 · Interventional · 15 enrolled · Fred Hutchinson Cancer Center
  NCT06145633updated 2026-01-28

Frequently asked questions

How does Gozetotide work?

Gallium Ga 68 gozetotide binds to PSMA. It binds to cells that express PSMA, including malignant prostate cancer cells, which usually overexpress PSMA.

What is Gozetotide used for?

According to FDA labeling, Gozetotide carries indications including: GOZELLIX, after radiolabeling with Ga 68, is indicated for positron emission tomography (PET) of prostate-specific membrane antigen (PSMA) positive lesions in men with prostate cancer: With suspected metastasis who are candidates for initial definitive therapy. With suspected recurrence based on elevated serum prostate-specific antigen (PSA) level.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What are the contraindications for Gozetotide?

Gozetotide labeling lists contraindications including: None None ( 4 ). Always consult the full prescribing information and a clinician.