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
- Curator reviewed · 2 references
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.
- 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
- 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
Resolves to
What you can answer from here — as of August 31, 2026
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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