Gozetotide
The PSMA PET imaging agent that maps prostate cancer and picks patients for Pluvicto
Gozetotide, or PSMA-11, carries radioactive gallium-68 to prostate cancer cells that display PSMA, so a PET scan can show where the cancer is. First approved in 2020, it finds spread that CT and bone scans miss and is used to select patients for PSMA-targeted therapy.
What is it?
Finding exactly where prostate cancer has spread changes treatment: whether surgery or radiotherapy can cure it, where to aim radiation, and whether a patient can receive PSMA-targeted therapy. CT and bone scans miss small deposits. Gozetotide, developed as PSMA-11, binds prostate-specific membrane antigen on cancer cells and carries gallium-68, a positron emitter, so a PET scanner can see even small clusters of PSMA-expressing cells.
Like vipivotide tetraxetan, it is built on a peptidomimetic glutamate-urea-lysine motif rather than a natural peptide chain, here joined to an HBED-CC chelator that holds the gallium. Gallium-68 decays within hours, so the tracer is prepared shortly before each scan. It is taken up in the liver, kidneys, spleen and salivary glands as well as in tumours; about 14% of the dose leaves in the urine within two hours.
In a 2026 randomised trial, a scan-guided pathway avoided biopsy in about half of men with an equivocal MRI while finding a similar share of significant cancers. In men whose cancer had returned, positive findings were confirmed by tissue in 84% of cases. It was first approved in December 2020 for the UCLA and UCSF programmes that developed it, then as the kits Illuccix (2021), Locametz (2022) and Gozellix (2025). The labels warn that images can be misread, because PSMA uptake is not specific to prostate cancer, and of radiation risk.
At a Glance
Every value in this table is printed from the Grey Peptides dataset, the same record the compound explorer and comparison tool read, so the three can never disagree.
Educational information, not medical advice. The doses on this page come from approved labels, published studies and, where no study exists, 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.
Published Research
The studies behind gozetotide, read from their PubMed abstracts.
Pharmacokinetics and radiation dose
In Japanese patients given 111 to 259 MBq before lutetium-177 PSMA-617 therapy, the tracer cleared from the blood in two phases with a terminal half-life of about 3.9 hours; the kidneys received the largest absorbed dose, and the effective dose was 0.030 mSv per MBq.
Recurrent cancer, 635 men
In men whose cancer had returned after prostatectomy or radiotherapy, the scan located recurrence in 75%, rising from 38% at PSA below 0.5 ng/mL to 97% at 5 ng/mL or more. Positive findings were confirmed by tissue in 84%, and no serious adverse events were linked to the tracer.
Replacing some biopsies
In 660 men with high-risk features but an equivocal or non-suspicious MRI, a PSMA PET-guided pathway found clinically significant cancer in 12% against 16% with systematic biopsy, meeting non-inferiority, and avoided biopsy in 49%.
EMPIRE-2: guiding salvage radiotherapy
In 140 men with recurrence after prostatectomy, PET-guided radiotherapy with dose escalation gave 87% two-year event-free survival against 80% in the earlier EMPIRE-1 comparison cohort.
EMPIRE-2: changes to radiotherapy plans
Scans changed salvage radiotherapy decisions in 42% of men imaged with PSMA-11 and 29% with fluciclovine, with no clear difference between the tracers.
Predicting benefit in VISION
In 826 men from the VISION trial, the average PSMA uptake across all tumours on the baseline scan best predicted benefit from lutetium-177 PSMA-617: each one-unit rise cut the risk of progression by 12% and of death by 10%, though benefit was seen at every uptake level.
Side Effects & Contraindications
Reported Side Effects
From the studies and labels.
Contraindications & Cautions
Warnings from the Locametz (DailyMed, effective January 15, 2026) and Illuccix (effective June 15, 2026) labels.
Legal Status
Gozetotide is approved in the US as several products, all prepared and given in nuclear medicine departments.
Frequently Asked Questions
?What is a PSMA PET scan?
A scan that uses a PSMA-binding tracer, such as gallium Ga 68 gozetotide, to show where prostate cancer cells are in the body. It finds spread that CT and bone scans often miss.
?How does it relate to Pluvicto?
Both bind PSMA. Gozetotide carries an imaging isotope and is used to confirm PSMA-positive disease; Pluvicto carries a treatment isotope and is given to patients whose scans show the target.
?Is the scan specific to prostate cancer?
No. Its labels warn that PSMA uptake also occurs in other cancers and some benign conditions, so images need careful interpretation.
References
- [fda] US FDA, Drugs@FDA (openFDA): gallium Ga 68 gozetotide, NDA 212642 (UCLA) and NDA 212643 (UCSF), approved December 1, 2020; ILLUCCIX NDA 214032 (December 17, 2021); LOCAMETZ NDA 215841 (March 23, 2022); GOZELLIX NDA 219592 (March 20, 2025). Read October 3, 2026.
- [fda-pi] FDA. Locametz (kit for gallium Ga 68 gozetotide) US prescribing information (DailyMed set 8683b06e-4901-4526-89ad-23a8fe2d1331, effective January 15, 2026). Read October 3, 2026.
- [fda-pi] FDA. Illuccix (kit for gallium Ga 68 gozetotide) US prescribing information (DailyMed set d4643b31-9b4f-673f-e053-2a95a90a559d, effective June 15, 2026). Read October 3, 2026.
- [clinical-trial] Takano S, et al. "Pharmacokinetics and dosimetry of [(177)Lu]Lu-PSMA-617 and [(68)Ga]Ga-PSMA-11 in Japanese patients with PSMA-positive mCRPC." Ann Nucl Med, 2025;39(11):1201-1212. PMID: 40638023.
- [clinical-trial] Fendler WP, et al. "Assessment of 68Ga-PSMA-11 PET Accuracy in Localizing Recurrent Prostate Cancer: A Prospective Single-Arm Clinical Trial." JAMA Oncol, 2019;5(6):856-863. PMID: 30920593.
- [clinical-trial] Buteau JP, et al. "Effect of [(68)Ga]Ga-PSMA-11 PET-CT in the diagnosis of prostate cancer in men with equivocal or clinically high-risk non-suspicious findings on multiparametric MRI (PRIMARY2): a multicentre, non-inferiority, phase 3, randomised controlled trial." Lancet Oncol, 2026;27(7):839-848. PMID: 42269655.
- [clinical-trial] Jani AB, et al. "[(18)F]-Fluciclovine or [(68)Ga]-PSMA-11 Molecular Imaging To Guide Dose Escalation of Salvage Radiotherapy After Radical Prostatectomy for Prostate Cancer: The EMPIRE-2 Trial." Eur Urol, 2026;89(4):368-377. PMID: 41412908.
- [clinical-trial] Abiodun-Ojo OA, et al. "(18)F-Fluciclovine or (68)Ga-PSMA-11 PET/CT-guided Salvage Radiotherapy Changes in Postprostatectomy Biochemical Recurrence: Secondary Analysis of the EMPIRE-2 Trial." Radiology, 2026;319(3):e251874. PMID: 42377125.
- [pubmed] Kuo PH, et al. "Quantitative (68)Ga-PSMA-11 PET and Clinical Outcomes in Metastatic Castration-resistant Prostate Cancer Following (177)Lu-PSMA-617 (VISION Trial)." Radiology, 2024;312(2):e233460. PMID: 39162634.
Sources & Citations
Studies were read from their PubMed records; regulatory sources are listed below, read October 3, 2026.
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. Consult a licensed healthcare provider before making health decisions.