Lutetium Lu-177 vipivotide tetraxetan

DB16778ApprovedInvestigationalSmall moleculeRadioligand Therapeutic Agent

Lutetium Lu-177 vipivotide tetraxetan is a radioligand therapeutic agent used to treat prostate-specific membrane antigen (PSMA)-positive metastatic castration-resistant prostate cancer in adults. It consists of a radionuclide, lutetium Lu-177, linked to a moiety that binds to PSMA, a transmembrane protein that is expressed in prostate cancer.

Mechanism: Prostate‐specific membrane antigen (PSMA) is a transmembrane glycoprotein involved in various cellular functions, such as cellular uptake of folate, cell migration, and cell survival. Due to its overexpression on the surface of prostate cancer cells, PMSA remains a useful protein target for targeted diagnostic processes and radionuclide therapy in prostate cancer.
Lutetium Lu 177 vipivotide tetraxetan consists of lutetium Lu-177, a radionuclide and an active moiety of the drug, linked to a moiety that binds to PSMA. Once administered, lutetium Lu 177 vipivotide tetraxetan binds to PSMA-expressing cells. The beta-minus emission from lutetium Lu-177 delivers radiation to PSMA-expressing cells, as well as to surrounding cells, and induces DNA damage which can lead to cell death.
Curator reviewed · 2 references
Primary indication: Lutetium Lu 177 vipivotide tetraxetan is a radioligand therapeutic agent indicated for the treatment of adult patients with prostate-specific membrane antigen (PSMA)-positive metastatic castration-resistant prostate cancer (mCRPC) who have been treated with androgen receptor (AR)...Curator reviewed · 3 structured indications
Formula / weight: C₄₉H₆₈LuN₉O₁₆ · 1216.074 g/mol (avg)
First approval: United States, 2022 · European Union, 2023
Also known as: 177Lu-labeled PSMA-617 · 177Lu-PSMA-617 · 177Lutetium -PSMA 617 · 177Lutetium-PSMA-617
Code names: [177Lu]Lu-PSMA-617 · AAA-617 · Lu-177 PSMA-617
Brand names: Pluvicto

Resolves to

Compound

UNIIG6UF363ECXCAS1703749-62-5

Clinical / RWD

RxNorm2597053ATCV10XX05

Structure

InChIKeyRSTDSVVLNYFDHY-BGOLSCJMSA-KSMILES

[177Lu+3].OC(=O)CC[C@H](NC(=O)N[C@@H](CCCCNC(=O)[C@H](CC1=CC2=CC=CC=C2C=C1)NC(=O)[C@H]1CC[C@H](CNC(=O)CN2CCN(CC([O-])=O)CCN(CC([O-])=O)CCN(CC([O-])=O)CC2)CC1)C(O)=O)C(O)=O

Targets

P07288KLK3Q04609FOLH1

What you can answer from here — as of September 24, 2026

2Protein targetsEach mapped to UniProt, with action and pharmacological action

Listed above

71Clinical trialsPhase, status and sponsor resolved per trial

3Structured indicationsCondition, population, route and combination as fields, not prose

2ContraindicationsEach with its own population and attribute set

3Marketed productsAcross 2 countries and 3 labellers

1ATC codeIncluding every combination product, plus 10 drug categories

10+ReferencesStructured and connected to the statements they support

Which drugs share a target with Lutetium Lu-177 vipivotide tetraxetan, and which of those have an active Phase 3 trial?

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