Advances in 177Lu-PSMA and 225Ac-PSMA Radionuclide Therapy for Metastatic Castration-Resistant Prostate Cancer

Sui Wai Ling; Erik de Blois; Eline Hooijman; Astrid van der Veldt; Tessa Brabander

doi:10.3390/pharmaceutics14102166

Advances in ¹⁷⁷Lu-PSMA and ²²⁵Ac-PSMA Radionuclide Therapy for Metastatic Castration-Resistant Prostate Cancer

Sui Wai Ling^*
, Erik de Blois
, Eline Hooijman
, Astrid van der Veldt
, Tessa Brabander

^*Corresponding author for this work

Research output: Contribution to journal › Review article › Academic › peer-review

59 Citations (Scopus)

572 Downloads (Pure)

Abstract

For patients with metastatic castration-resistant prostate cancer (mCRPC), the survival benefit of classic treatment options with chemotherapy and drugs targeting androgen signaling is limited. Therefore, beta and alpha radionuclide therapy (RNT) have emerged as novel treatment options for patients with mCRPC. Radioligands target the prostate-specific membrane antigen (PSMA) epitopes, which are upregulated up to a thousand times more in prostate cancer cells compared to the cells in normal tissues. For this reason, PSMA is an excellent target for both imaging and therapy. Over the past years, many studies have investigated the treatment effects of lutetium-177 labeled PSMA (¹⁷⁷Lu-PSMA) and actinium-225 labeled PSMA (²²⁵Ac-PSMA) RNT in patients with mCRPC. While promising results have been achieved, this field is still in development. In this review, we have summarized and discussed the clinical data of ¹⁷⁷Lu-PSMA and ²²⁵Ac-PSMA RNT in patients with mCRPC.

Original language	English
Article number	2166
Journal	Pharmaceutics
Volume	14
Issue number	10
DOIs	https://doi.org/10.3390/pharmaceutics14102166
Publication status	Published - 11 Oct 2022

Bibliographical note

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

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Cite this

@article{eff19403299f4271b4f6c57f93adcac1,

title = "Advances in 177Lu-PSMA and 225Ac-PSMA Radionuclide Therapy for Metastatic Castration-Resistant Prostate Cancer",

abstract = "For patients with metastatic castration-resistant prostate cancer (mCRPC), the survival benefit of classic treatment options with chemotherapy and drugs targeting androgen signaling is limited. Therefore, beta and alpha radionuclide therapy (RNT) have emerged as novel treatment options for patients with mCRPC. Radioligands target the prostate-specific membrane antigen (PSMA) epitopes, which are upregulated up to a thousand times more in prostate cancer cells compared to the cells in normal tissues. For this reason, PSMA is an excellent target for both imaging and therapy. Over the past years, many studies have investigated the treatment effects of lutetium-177 labeled PSMA (177Lu-PSMA) and actinium-225 labeled PSMA (225Ac-PSMA) RNT in patients with mCRPC. While promising results have been achieved, this field is still in development. In this review, we have summarized and discussed the clinical data of 177Lu-PSMA and 225Ac-PSMA RNT in patients with mCRPC.",

author = "Ling, \{Sui Wai\} and \{de Blois\}, Erik and Eline Hooijman and \{van der Veldt\}, Astrid and Tessa Brabander",

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year = "2022",

month = oct,

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doi = "10.3390/pharmaceutics14102166",

language = "English",

volume = "14",

journal = "Pharmaceutics",

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T1 - Advances in 177Lu-PSMA and 225Ac-PSMA Radionuclide Therapy for Metastatic Castration-Resistant Prostate Cancer

AU - Ling, Sui Wai

AU - de Blois, Erik

AU - Hooijman, Eline

AU - van der Veldt, Astrid

AU - Brabander, Tessa

PY - 2022/10/11

Y1 - 2022/10/11

N2 - For patients with metastatic castration-resistant prostate cancer (mCRPC), the survival benefit of classic treatment options with chemotherapy and drugs targeting androgen signaling is limited. Therefore, beta and alpha radionuclide therapy (RNT) have emerged as novel treatment options for patients with mCRPC. Radioligands target the prostate-specific membrane antigen (PSMA) epitopes, which are upregulated up to a thousand times more in prostate cancer cells compared to the cells in normal tissues. For this reason, PSMA is an excellent target for both imaging and therapy. Over the past years, many studies have investigated the treatment effects of lutetium-177 labeled PSMA (177Lu-PSMA) and actinium-225 labeled PSMA (225Ac-PSMA) RNT in patients with mCRPC. While promising results have been achieved, this field is still in development. In this review, we have summarized and discussed the clinical data of 177Lu-PSMA and 225Ac-PSMA RNT in patients with mCRPC.

AB - For patients with metastatic castration-resistant prostate cancer (mCRPC), the survival benefit of classic treatment options with chemotherapy and drugs targeting androgen signaling is limited. Therefore, beta and alpha radionuclide therapy (RNT) have emerged as novel treatment options for patients with mCRPC. Radioligands target the prostate-specific membrane antigen (PSMA) epitopes, which are upregulated up to a thousand times more in prostate cancer cells compared to the cells in normal tissues. For this reason, PSMA is an excellent target for both imaging and therapy. Over the past years, many studies have investigated the treatment effects of lutetium-177 labeled PSMA (177Lu-PSMA) and actinium-225 labeled PSMA (225Ac-PSMA) RNT in patients with mCRPC. While promising results have been achieved, this field is still in development. In this review, we have summarized and discussed the clinical data of 177Lu-PSMA and 225Ac-PSMA RNT in patients with mCRPC.

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