Vipivotide Tetraxetan
A PSMA-seeking molecule that delivers radiation directly to prostate cancer cells
Vipivotide tetraxetan carries radioactive lutetium-177 to cells that display PSMA, a protein found on most prostate cancers. Approved as Pluvicto in 2022 after the VISION trial, it is given intravenously every six weeks to men whose PSMA PET scan shows the target.
What is it?
Prostate-specific membrane antigen (PSMA) sits on the surface of most prostate cancer cells, often at far higher levels than on normal tissue. That makes it a target for 'theranostics': one PSMA-binding molecule labelled for imaging finds the cancer on a PET scan, and a relative labelled for treatment delivers radiation to the same cells. Vipivotide tetraxetan, known in research as PSMA-617, is the treatment half; gozetotide is the imaging half.
The molecule is not a classic peptide. Its PSMA-binding part is a peptidomimetic glutamate-urea-lysine motif, joined through a linker to DOTA, a cage that holds lutetium-177. Lutetium-177 emits beta particles that travel only millimetres, damaging the cell it sits on and its neighbours. The drug leaves the body mainly through the kidneys, with a terminal elimination half-life of 41.6 hours.
In the VISION trial of 831 men with heavily pretreated metastatic castration-resistant prostate cancer, adding it to standard care extended median survival from 11.3 to 15.3 months. It was approved as Pluvicto in March 2022, and later trials moved it earlier; the current label also covers hormone-sensitive disease given with an androgen receptor pathway inhibitor. The label warns of radiation exposure, low blood counts, kidney toxicity, harm to a fetus and infertility.
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.
Half-Life: How Much Remains
The dataset records a half-life of 41.6 hours, terminal elimination (label 12.3) for Vipivotide Tetraxetan. After each half-life, half of what was in the circulation is gone, so about 3% remains after five. Real clearance varies with the person, the dose, the route and kidney or liver function; this is arithmetic on a published figure, not a dosing tool.
Published Research
The trials behind Pluvicto, read from their PubMed abstracts.
VISION phase 3, 831 men
In men with PSMA-positive metastatic castration-resistant prostate cancer after hormone tablets and chemotherapy, adding it to standard care extended median imaging-based progression-free survival from 3.4 to 8.7 months and overall survival from 11.3 to 15.3 months. Grade 3 or worse adverse events were more common (52.7% against 38.0%), but quality of life was not worsened.
PSMAfore phase 3: before chemotherapy
In 468 chemotherapy-naive men who had progressed once on a hormone tablet, median radiographic progression-free survival was 9.3 months on lutetium-177 PSMA-617 against 5.6 months on a switch of hormone tablet. Grade 3 to 5 adverse events were less common, 36% against 48%.
PSMAfore: final survival analysis
Median overall survival was 24.5 months against 23.1 months, not a significant difference; 60% of the comparison group crossed over to the drug, and adjusting for that gave a hazard ratio of 0.59. Dry mouth occurred in 59.5% and anaemia in 27.3%.
TheraP phase 2: against cabazitaxel
In 200 men who would otherwise have received cabazitaxel chemotherapy, PSA fell by at least half in 66% on lutetium-177 PSMA-617 against 37% on cabazitaxel, with fewer grade 3 or 4 adverse events (33% against 53%).
TheraP: overall survival
After a median of 35.7 months, survival was similar in the two groups (restricted mean 19.1 against 19.6 months). Men excluded because their scans showed too little PSMA did worse, with a restricted mean of 11.0 months.
ENZA-p phase 2: with enzalutamide
In 162 men starting treatment for castration-resistant disease, adding lutetium-177 PSMA-617 to enzalutamide extended median PSA progression-free survival from 7.8 to 13.0 months. Grade 3 to 5 events were similar, 40% against 41%; dry mouth affected 40% in the combination group.
Side Effects & Contraindications
Reported Side Effects
From the trials above.
Contraindications & Cautions
Warnings from the Pluvicto label (DailyMed, effective August 12, 2026).
Legal Status
Vipivotide tetraxetan is approved in the US as Pluvicto, given only by specialist centres licensed to handle radioactive drugs.
Frequently Asked Questions
?What is Pluvicto?
Lutetium Lu 177 vipivotide tetraxetan: a molecule that binds PSMA on prostate cancer cells and carries radioactive lutetium-177 to them. It is given intravenously every six weeks.
?Who can receive it?
Men with PSMA-positive metastatic prostate cancer, confirmed on a PSMA PET scan such as one using gozetotide, in the settings its label describes.
?Is it a peptide?
Not exactly. Its PSMA-binding part is a peptidomimetic glutamate-urea-lysine motif, so we class it as a peptidomimetic rather than a peptide.
References
- [fda] US FDA, Drugs@FDA (openFDA): PLUVICTO (lutetium Lu 177 vipivotide tetraxetan), NDA 215833, original approval March 23, 2022, prescription. Read October 3, 2026.
- [fda-pi] FDA. Pluvicto (lutetium Lu 177 vipivotide tetraxetan) US prescribing information (DailyMed set 14908037-2892-4d98-a053-253ce35afb1a, effective August 12, 2026). Read October 3, 2026.
- [clinical-trial] Sartor O, et al. "Lutetium-177-PSMA-617 for Metastatic Castration-Resistant Prostate Cancer." N Engl J Med, 2021;385(12):1091-1103. PMID: 34161051.
- [clinical-trial] Morris MJ, et al. "(177)Lu-PSMA-617 versus a change of androgen receptor pathway inhibitor therapy for taxane-naive patients with progressive metastatic castration-resistant prostate cancer (PSMAfore): a phase 3, randomised, controlled trial." Lancet, 2024;404(10459):1227-1239. PMID: 39293462.
- [clinical-trial] Fizazi K, et al. "Final overall survival and safety analyses of the phase III PSMAfore trial of [(177)Lu]Lu-PSMA-617 versus change of androgen receptor pathway inhibitor in taxane-naive patients with metastatic castration-resistant prostate cancer." Ann Oncol, 2025;36(11):1319-1330. PMID: 40680993.
- [clinical-trial] Hofman MS, et al. "[(177)Lu]Lu-PSMA-617 versus cabazitaxel in patients with metastatic castration-resistant prostate cancer (TheraP): a randomised, open-label, phase 2 trial." Lancet, 2021;397(10276):797-804. PMID: 33581798.
- [clinical-trial] Hofman MS, et al. "Overall survival with [(177)Lu]Lu-PSMA-617 versus cabazitaxel in metastatic castration-resistant prostate cancer (TheraP): secondary outcomes of a randomised, open-label, phase 2 trial." Lancet Oncol, 2024;25(1):99-107. PMID: 38043558.
- [clinical-trial] Emmett L, et al. "[(177)Lu]Lu-PSMA-617 plus enzalutamide in patients with metastatic castration-resistant prostate cancer (ENZA-p): an open-label, multicentre, randomised, phase 2 trial." Lancet Oncol, 2024;25(5):563-571. PMID: 38621400.
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.