Pluvicto®▼ Prescribing information

Locametz®▼ (gozetotide) Prescribing information

This page/content is for Great Britain healthcare professionals only.

Pluvicto (lutetium [177Lu] vipivotide tetraxetan) is 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) pathway inhibition and taxane-based chemotherapy or who are not medically suitable for taxanes.1

Locametz (gozetotide) is for diagnostic use only. Locametz, after radiolabelling with gallium-68, is a radioactive diagnostic agent indicated for the identification of prostate-specific membrane antigen (PSMA)-positive lesions by positron emission tomography (PET) in adult patients with prostate cancer.2

 

Pluvicto Mode of Action

Pluvicto is a PSMA-targeted radioligand therapy (RLT) that delivers DNA-damaging radiation to PSMA-positive bone, nodal, and visceral metastases.1,3–7

Pluvicto targets PSMA-positive cells, including prostate cancer cells1

The MOA of Pluvicto can be broken down into a few key steps:

Graphic to represent the composition of Pluvicto.

Pluvicto comprises 2 key components:
lutetium-177, a cytotoxic radionuclide, and PSMA-617, a PSMA-targeting ligand.1

 

Image to highlight how Pluvicto binds to PSMA on prostate cancer cells.

As determined by pre-clinical research, Pluvicto binds with high affinity to PSMA, a transmembrane protein overexpressed on prostate cancer cells.1
After binding to PSMA, PLUVICTO undergoes endocytosis and is internalised into the cell.1,8–10

 

Image to highlight how Lutetium-177 emits DNA-damaging radiation within the cell causing single- and double-stranded DNA breaks in targeted cells as well as surrounding cells.

As determined by pre-clinical research, Lutetium-177, (the cytotoxic radionuclide of Pluvicto), emits DNA-damaging radiation within the cell.1,10
The short path length of the radiation emitted by Pluvicto, (approx. 2 mm max.), causes single- and double-stranded DNA breaks in targeted cells as well as surrounding cells, which can lead to cell death.1,9–11

 

  • PSMA scanning enables you to see and target PSMA-positive mCRPC2,5,13,14
  • The high sensitivity of PSMA scanning detects PSMA-positive bone, nodal or visceral metastases13–16
  • PSMA imaging establishes patient eligibility for PSMA-targeted RLT6

The most common ADRs (≥20%) occurring at a higher incidence in patients who received Pluvicto + BSoC compared to BSoC alone include fatigue, dry mouth, nausea, anaemia, decreased appetite and constipation.1

For further information please refer to the Great Britain summary of product characteristics.1

 

ADR, adverse drug reaction; AR, androgen receptor; BSoC, best standard of care; DNA, deoxyribonucleic acid; mCRPC, metastatic castration-resistant prostate cancer; MOA, mode of action; PET, positron emission tomography; PSMA, prostate-specific membrane antigen; RLT, radioligand therapy.

References:

  1. Pluvicto® (lutetium [177Lu] vipivotide tetraxetan) GB Summary of Product Characteristics. 
  2. Locametz® (gozetotide) GB Summary of Product Characteristics.
  3. Benešová M, et al. J Nucl Med 2015;56(6):914–920.
  4. Fendler WP, et al. J Nucl Med 2017;58(11):1786–1792.
  5. Hofman MS, et al. Lancet Oncol 2018;19(6):825–833.
  6. Sartor O, et al. N Engl J Med 2021;385(12):1091–1103.
  7. Violet J, et al. J Nucl Med 2019;60(4):517–523.
  8. Liu H, et al. Cancer Res 1998;58(18):4055–4060.
  9. Rajasekaran SA, et al. Mol Biol Cell 2003;14(12):4835–4845.
  10. Ruigrok EAM, et al. Eur J Nucl Med Mol Imaging 2021;48(5):1339–1350.
  11. Sartor O, et al. N Eng J Med 2021;385(12):1091–1103. Supplementary appendix.
  12. Kassis AI, et al. Semin Nucl Med 2008;38(5):358–366.
  13. Maffey-Steffan J, et al. Eur J Nucl Med Mol Imaging 2020;47(3):695–712.
  14. Vlachostergios PJ, et al. Front Oncol 2021;11:630589.
  15. Woythal N, et al. J Nucl Med 2018;59(2):238–243.
  16. Schmuck S, et al. J Nucl Med 2017;58(12):1962–1968.
AAA-PSMA-UK-0615 | February 2024
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