Lutetium (177Lu) vipivotide tetraxetan Peptide: Structure, Research & Science Guide

By The Peptides Codex Editorial TeamReviewed September 8, 2026

Page data last changed: 2026-10-05. Registry refreshes and identity assessments are separate from scientific content review.

Reference backbone length

n/a

Class

PSMA-targeting peptidomimetic radioligand therapy

Function

A PSMA-binding peptidomimetic that delivers beta radiation from lutetium-177 to prostate cancer cells

Context

Approved (FDA, 23 March 2022) for PSMA-positive metastatic castration-resistant prostate cancer after androgen-receptor pathway inhibition and taxane chemotherapy

Not a classical peptide but a peptidomimetic: a small PSMA-binding ligand that turns a prostate-cancer surface enzyme into a target for internal radiation.

Also known as: 177Lu-PSMA-617 · PSMA-617 · Pluvicto (brand) · lutetium Lu 177 vipivotide tetraxetan

Part of the Foundational & therapeutic peptides cluster

Overview

Lutetium (177Lu) vipivotide tetraxetan, marketed as Pluvicto and formerly 177Lu-PSMA-617, is a radioligand therapy in which a peptidomimetic ligand for prostate-specific membrane antigen (PSMA) carries the beta-emitting isotope lutetium-177 into PSMA-expressing prostate cancer cells. The FDA approved it on 23 March 2022, on the basis of the phase 3 VISION trial, for adults with PSMA-positive metastatic castration-resistant prostate cancer previously treated with androgen-receptor pathway inhibition and taxane chemotherapy.

Source & context

Biological / chemical source: Synthetic PSMA-targeting peptidomimetic ligand conjugated through a linker to a radionuclide chelator carrying lutetium-177

Primary research or clinical context: Approved (FDA, 23 March 2022) for PSMA-positive metastatic castration-resistant prostate cancer after androgen-receptor pathway inhibition and taxane chemotherapy

What Pluvicto is

Lutetium (177Lu) vipivotide tetraxetan is a radioligand therapeutic developed by Advanced Accelerator Applications, a Novartis subsidiary, under the earlier name 177Lu-PSMA-617. Its active part is lutetium-177, linked to a ligand that binds prostate-specific membrane antigen (PSMA), a transmembrane enzyme overexpressed in primary and metastatic prostate cancers (Keam, Molecular Diagnosis & Therapy 2022). The FDA's own approval summary describes it as lutetium-177 linked to a peptide, vipivotide tetraxetan, that binds PSMA-expressing cells, with cell death resulting from the radiation (Fallah et al., Clinical Cancer Research 2023; Morrison and Holle, Journal of Oncology Pharmacy Practice 2026).

Peptide or peptidomimetic?

Strictly, the targeting part is a peptidomimetic: a patent analysis describes the drug as a PSMA-targeting peptidomimetic moiety conjugated to a radionuclide chelator via a linker (Chia, ACS Medicinal Chemistry Letters 2023). It is built from amino-acid-derived units that mimic PSMA's natural substrate rather than from a hormone-like chain, which is why regulatory documents call it a peptide and chemists call it a peptidomimetic. Either way it belongs to the same theranostic family as lutetium dotatate: a small targeting molecule, a chelator, and a beta-emitting metal.

Mechanism

PSMA is present at low levels in normal tissue and at high levels on prostate cancer cells, including metastases. Vipivotide tetraxetan binds PSMA, is internalised, and the lutetium-177 it carries delivers beta radiation that kills the cell and its immediate neighbours (Shah et al., Expert Review of Anticancer Therapy 2022). Because the isotope is excreted by the kidneys, renal exposure and potential renal toxicity are a recognised concern (Morrison and Holle 2026). Patient selection uses PSMA imaging to confirm that the tumours express the target.

Evidence and approval

Extensive experience outside the United States and randomised phase 2 and phase 3 data showed the drug to be safe, generally well tolerated and effective in men with metastatic castration-resistant prostate cancer (Shah et al. 2022). On 23 March 2022 the FDA approved it for adults with PSMA-positive metastatic castration-resistant prostate cancer previously treated with androgen-receptor pathway inhibition and taxane-based chemotherapy, on the basis of the phase 3 VISION trial, at a recommended activity of 7.4 gigabecquerels per dose (Fallah et al., Clinical Cancer Research 2023; Liu et al., Drugs of Today 2023). The phase 2 TheraP trial in Australia had compared 177Lu-PSMA-617 with cabazitaxel; a 2024 individual-participant analysis of TheraP and VISION examined why their overall-survival effects differed, including crossover after progression (Soon et al., JAMA Network Open 2024).

Approval facts (Fallah et al., Clinical Cancer Research 2023)
Item	Detail
Approval date	23 March 2022 (US FDA)
Indication	PSMA-positive mCRPC after androgen-receptor pathway inhibition and taxane chemotherapy
Pivotal trial	VISION (phase 3, n = 831)
Recommended activity	7.4 GBq per dose

Safety in practice

The cited literature identifies kidney excretion and possible renal toxicity as the main pharmacological concern (Morrison and Holle 2026). A 2026 pharmacovigilance study of the FDA Adverse Event Reporting System compared reporting profiles for enzalutamide, olaparib and lutetium vipivotide tetraxetan in prostate cancer from approval through the third quarter of 2025, using four disproportionality algorithms (Li et al., World Journal of Urology 2026). Reviews position PSMA-directed radioligand therapy alongside PARP inhibition and androgen-receptor blockade as the three targeted strategies reshaping advanced prostate cancer (Kawczak and Bączek, Journal of Clinical Medicine 2026).

Ongoing research and relation to other profiles

ClinicalTrials.gov lists 39 registered studies as of September 2026, including a phase 3 comparison of dosing schedules (NCT07200830), a phase 3 open-label comparison in a broader population (NCT05939414), a phase 1 comparison of 177Lu-PSMA-617 with an actinium-225 version (NCT07054346) and combinations with bispecific antibodies (NCT05818683). On this site the closest relative is lutetium dotatate, the somatostatin-receptor radioligand for neuroendocrine tumours that established the approach; octreotide and edotreotide supply the peptide lineage. Pluvicto is a hospital-administered approved medicine, not a research peptide. This profile is educational and is not medical advice.

Structure & chemistry

Molecular identity & reference confidence

Source-supported reference

FDA explicitly identifies the radiolabeled177Lu complex and reports molecular mass1216.06. GSRS independently identifies the exact trans-cyclohexyl molecular form with five specified centers and the177Lu isotope. This value is isotope-specific, not a natural-lutetium average or a claimed monoisotopic mass. Export average_mass_da must remain null while reference_mass_da and mass_basis carry the documented value. This is unmetallated vipivotide tetraxetan/PSMA-617, C49H71N9O16, mass1042.1. It has no177Lu and is not the radiolabeled drug complex. Qualified related record only: GSRS cross-references it and its elemental formula/isotope agree, but its standard InChI leaves two cyclohexyl centers unspecified (/t32?,35?), whereas GSRS specifies the trans form. It is not selected as an exact full stereochemical identifier.

Molecular form: Lutetium(177Lu) vipivotide tetraxetan radiolabeled complex
Species: Synthetic radiolabeled peptidomimetic; species is not applicable
Termini (N / C): Not applicable to this linked peptidomimetic-chelator complex / Not applicable to this linked peptidomimetic-chelator complex

Reference mass (isotope-specific) · Molecular identity assessment: 2026-10-05

Reference policy updated: 2026-10-05

FDA PLUVICTO label, March2022, Section11 · 2026-10-05
NIH NCATS/FDA GSRS, UNII G6UF363ECX · 2026-10-05
PubChem PUG molecular properties, CID 122706785 · 2026-10-05
PubChem PUG molecular properties, CID 122706786 · 2026-10-05

Full sequence with modifications

Not applicable: PSMA-binding urea peptidomimetic and linker joined to a DOTA chelator containing lutetium-177; trans-cyclohexyl form defined by GSRSG6UF363ECX.

Molecular formula: C49H68[177Lu]N9O16
Reference mass (isotope-specific): ≈ 1,216.1
Receptors: Prostate-specific membrane antigen (PSMA), a transmembrane enzyme overexpressed in primary and metastatic prostate cancer
Backbone: Lutetium(177Lu) vipivotide tetraxetan radiolabeled complex
C-terminus: Not applicable to this linked peptidomimetic-chelator complex
Status: Approved: FDA (23 March 2022) for PSMA-positive metastatic castration-resistant prostate cancer after ARPI and taxane therapy

Identifiers

CAS RN: 1703749-62-5
UNII: G6UF363ECX

Chemistry values: curated profile.

Clinical development snapshot

ClinicalTrials.gov lists 42 registered studies with “Lutetium vipivotide tetraxetan” as an intervention (snapshot 2026-10-01). A registry footprint is not evidence of efficacy or approval.

Registered studies

Highest phase reached

Phase 4

Active in latest 100

Most recent update

2026-10-01

Most recently updated studies
NCT	Title	Phase	Status	Updated
NCT07852195	Testing the Use of High Dose Testosterone Followed by Darolutamide Compared to the Usual Care for Patients Wit	Phase 3	not yet recruiting	2026-10-01
NCT07843758	An External Control Arm Study Comparing Survival Among Metastatic Castration-Resistant Prostate Cancer (mCRPC)	—	completed	2026-10-01
NCT07226986	A Phase Ib/II Open-label Study of AMO959 With Lutetium (177Lu) Vipivotide Tetraxetan (AAA617) in Combination W	Phase 2	recruiting	2026-10-01
NCT06095089	A Study of JNJ-87189401 Combined With JNJ-78278343 for Advanced Prostate Cancer	Phase 1	recruiting	2026-09-28
NCT05818683	A Study of Pasritamig (JNJ-78278343) in Combination With Other Agents for Metastatic Prostate Cancer	Phase 1	recruiting	2026-09-25
NCT06379217	NEPC Study: An Exploratory Safety and Efficacy Study With PSMA, SSTR2 and GRPR Targeted Radioligand Therapy in	Phase 1	active not recruiting	2026-09-22

See all on ClinicalTrials.gov →

Concentration math

Lutetium (177Lu) vipivotide tetraxetan — reconstitution calculator

Enter how much peptide is in the vial and how much diluent (e.g. bacteriostatic water) is added. The tool returns the resulting solution concentration — and, for any amount you type, the volume it corresponds to. This is educational arithmetic, not a dosing recommendation.

Reference form: Lutetium(177Lu) vipivotide tetraxetan radiolabeled complexReference mass (isotope-specific): 1,216.06 Da

Peptide in vial (mg)

Diluent added (mL)

Syringe graduation

Solution concentration

5 mg/mL5,000 mcg/mL

Amount to measure (optional)

mcg

Enter an amount to see the volume it corresponds to.

Educational concentration mathematics only. This tool does not recommend a dose, amount, or protocol, and nothing here is medical advice. Many peptides are not authorized by Health Canada for human use — see our reconstitution and bacteriostatic-water guides for context.

Open the Lutetium (177Lu) vipivotide tetraxetan calculator on its own page →

Change log

Dated observations from the data pipeline (registry flags, trial footprints, identifiers) and editorial reviews of this profile.

2026-10-01ChemistryPubChem formula updated to C49H68LuN9O16.
2026-10-01Trials2 registered studies added on ClinicalTrials.gov (now 42).
2026-09-08IdentifiersCross-linked to IUPHAR ligand 11982 and PubChem CID 122706786.
2026-09-08TrialsClinicalTrials.gov snapshot added: 40 registered studies, highest phase 4.
2026-09-08EditorialProfile content reviewed and updated by the editorial team.

FAQ about Lutetium (177Lu) vipivotide tetraxetan

What is Lutetium (177Lu) vipivotide tetraxetan?+

What Canadian product status is recorded for Lutetium (177Lu) vipivotide tetraxetan?+

Canadian product status for Lutetium (177Lu) vipivotide tetraxetan has not been verified in this profile. No verified record here does not mean no authorization exists. Status depends on the product, formulation and use; consult Health Canada's product records.

What is the length of the selected reference form for Lutetium (177Lu) vipivotide tetraxetan?+

The selected reference form (Lutetium(177Lu) vipivotide tetraxetan radiolabeled complex) is a peptidomimetic without a conventional peptide chain; an amino-acid length does not apply.

What is Pluvicto?+

Lutetium (177Lu) vipivotide tetraxetan, a radioligand therapy: a PSMA-binding peptidomimetic carrying the beta-emitter lutetium-177 into prostate cancer cells.

Is vipivotide tetraxetan a peptide?+

Regulators call it a peptide; chemists describe it as a PSMA-targeting peptidomimetic built from amino-acid-derived units. It is not a hormone-like chain.

When was Pluvicto approved?+

The FDA approved it on 23 March 2022 for PSMA-positive metastatic castration-resistant prostate cancer after androgen-receptor pathway inhibition and taxane chemotherapy, based on the VISION trial.

How does Pluvicto work?+

The ligand binds PSMA on prostate cancer cells and is internalised; the attached lutetium-177 delivers beta radiation that kills the cell.

What is the main safety concern?+

Kidney excretion of the radioisotope, with possible renal toxicity; pharmacovigilance analyses of reported adverse events were published in 2026.

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References & further reading

Disclaimer: Educational content only. Not medical advice. Not instructions for human use. Research peptides and unapproved products may be restricted or illegal to market for human consumption in your jurisdiction. Consult qualified professionals and applicable law.

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