The Evolution of Radioligand Therapy: Next-Generation Strategies to Expand the Therapeutic Window

The design and application of radioactively labeled drugs for cancer treatment are experiencing a rebirth, led in part by new advances in radioligand therapies (RLTs) like 177 Lu-PSMA-617 and 177 Lu-DOTATATE that specifically and potently bind to proteins highly upregulated in cancer. This review discusses the latest advances in RLT design that aim to maximize radiation delivery to tumor tissue while sparing normal tissues from greater than minimal radioactive dose.

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Publication Details

Journal
Annual Review of Cancer Biology
Published
2025-11-21
DOI
https://doi.org/10.1146/annurev-cancerbio-070524-031441
Primary Topic
Radiopharmaceutical Chemistry and Applications
Type
article
Field-Weighted Citation Impact
0.00
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article

The Evolution of Radioligand Therapy: Next-Generation Strategies to Expand the Therapeutic Window

Apurva Pandey, Michael J. Evans, Luke N. Jaskowski
Annual Review of Cancer Biology
Radiopharmaceutical Chemistry and Applications
article

The Evolution of Radioligand Therapy: Next-Generation Strategies to Expand the Therapeutic Window

Apurva Pandey, Michael J. Evans, Luke N. Jaskowski
article en

Abstract

The design and application of radioactively labeled drugs for cancer treatment are experiencing a rebirth, led in part by new advances in radioligand therapies (RLTs) like 177 Lu-PSMA-617 and 177 Lu-DOTATATE that specifically and potently bind to proteins highly upregulated in cancer. This review discusses the latest advances in RLT design that aim to maximize radiation delivery to tumor tissue while sparing normal tissues from greater than minimal radioactive dose.

Annual Review of Cancer Biology
University of California, San Francisco (US), University of California System (US), UCSF Helen Diller Family Comprehensive Cancer Center (US)
Openalex Percentile: Top 49%
Radiopharmaceutical Chemistry and Applications
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