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Pluvicto

lutetium Lu 177 vipivotide tetraxetan
Radioligand Therapy (PSMA-targeted) Novartis FDA Approved 2022
Indications Dosing Forms Contraindications Warnings Adverse Reactions Pharmacology Clinical Studies Tumor Types
1. Indications and Usage

PSMA-positive metastatic castration-resistant prostate cancer (mCRPC) in adult patients who have been treated with androgen receptor pathway inhibition and taxane-based chemotherapy.

2. Dosage and Administration

7.4 GBq (200 mCi) IV every 6 weeks for up to 6 doses
Infused slowly over approximately 3-5 minutes
Pre-treatment PSMA-positive imaging required (gallium Ga 68 gozetotide PET scan or similar)
Continue LHRH analogue or have had orchiectomy
Hydration: Encourage adequate hydration and frequent voiding for 48 hours post-dose

3. Dosage Forms and Strengths

Injection: 7.4 GBq (200 mCi) per single-dose vial at calibration date and time

4. Contraindications

Pregnancy.

5. Warnings and Precautions
  • Myelosuppression: Grade 3-4 anemia (13%), thrombocytopenia (8%), lymphopenia (8%), neutropenia (4%). Monitor CBC every 2 weeks × first 3 months, then every 4 weeks. Withhold for Grade ≥3.
  • Renal Toxicity: Radiation to kidneys. Monitor creatinine and BUN regularly. D/C for Grade 3+ nephrotoxicity.
  • Dry Mouth (Xerostomia): In 39%. Due to radiation to salivary glands (physiologic PSMA expression).
  • Radiation Safety Precautions: Patient is radioactive post-dose. Minimize contact with others for 48 hours. Avoid pregnancy for 14 weeks post-last dose (males).
  • Secondary Malignancies: Myelodysplastic syndrome and acute leukemia reported.
6. Adverse Reactions
Most Common Adverse Reactions

Fatigue (43%), dry mouth (39%), nausea (35%), anemia (32%), decreased appetite (21%), constipation (20%), vomiting (19%), musculoskeletal pain (18%), renal impairment (11%), thrombocytopenia (16%)

Fatigue
43%
Dry Mouth
39%
Nausea
35%
Anemia
32%
Decreased Appetite
21%
Constipation
20%
Vomiting
19%
Musculoskeletal Pain
18%
Thrombocytopenia
16%
Renal Impairment
11%

Consult the complete prescribing information for a comprehensive list of adverse reactions and their frequencies.

12. Clinical Pharmacology
Mechanism of Action

Pluvicto is a radioligand therapy consisting of a PSMA-targeting ligand (vipivotide tetraxetan) conjugated to the beta-emitting radionuclide lutetium-177. PSMA (prostate-specific membrane antigen) is highly expressed on the surface of prostate cancer cells. Upon binding to PSMA, the radioligand is internalized, and lutetium-177 emits beta radiation (maximum energy 0.497 MeV, mean tissue penetration ~0.67 mm) that causes DNA double-strand breaks and cell death in PSMA-expressing cells and the surrounding microenvironment (crossfire effect).

Pharmacokinetics

Lu-177 physical half-life: 6.647 days. After IV administration, rapidly distributes to PSMA-expressing tissues. Approximately 60% of injected activity excreted in urine within 24 hours. Highest radiation-absorbed doses to salivary glands, kidneys, and bone marrow. Residual activity in tumor measurable on SPECT imaging for 1-2 weeks.

14. Clinical Studies

Clinical efficacy and safety data supporting the approval are available in the full prescribing information and from the clinical trials listed below.

Pivotal Clinical Trials
Additional Resources
Approved Tumor Types
External Resources