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technologiesTechnologyApproved

Radioligand therapy (beta emitters)

A drug that finds tumour cells and carries a radioactive atom that irradiates them from inside the body.

177Lu-DOTATATE (Lutathera, 2018) in neuroendocrine tumours and 177Lu-PSMA-617 (Pluvicto, 2022; pre-chemotherapy label 2025; 2026 label expansion) in prostate cancer are the approved beta-emitter therapies. Pipeline: 177Lu-FAP, 177Lu-PSMA-I&T, 177Lu-NeoB (GRPR), 177Lu-labelled antibodies. Dosimetry-guided personalised dosing is emerging.

Schematic · not to scale
PSMA / SSTR-positive cell

How it works

177Lu emits beta particles with ~2 mm range and gamma photons for SPECT imaging; the ligand determines biodistribution.

Strengths
  • Systemic, whole-body targeting of microscopic disease
  • Crossfire kills antigen-negative neighbours
  • Imaging companion selects patients
Limitations
  • Marrow and kidney dose
  • Isotope logistics (6.7-day half-life)
  • Not curative alone
Since
2018

Products

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EstablishedRadioligand therapy (beta, norepinephrine transporter)
131I-MIBG (iobenguane I-131) therapy

High-dose radioactive MIBG delivers radiation from inside neuroblastoma cells that take up noradrenaline; used for relapsed disease and tested in upfront therapy.

Phase 3Radioligand therapy (beta)
177Lu-edotreotide

A second lutetium radioligand for neuroendocrine tumours that beat the standard pill everolimus in a head-to-head trial and is awaiting an FDA decision.

Phase 3Radioligand therapy (beta)
177Lu-PSMA-I&T

177Lu-PSMA-I&T is a second PSMA radioligand, chemically different from Pluvicto, that has passed two phase 3 trials on progression but has not yet shown a survival benefit.

Phase 2Theranostic pair (peptide radioligand)
FAP-2286 (177Lu / 68Ga)

A FAP-targeted theranostic pair: one version images almost any solid tumour, the other treats it with radiation.

Not mapped herePET radiotracer (somatostatin receptor ligand)
Gallium-68 DOTATATE (and Cu-64 DOTATATE) · Netspot / Detectnet

The PET scan for neuroendocrine tumours that finds far more disease than older scans and confirms eligibility for lutetium radioligand therapy (the theranostic pair).

ApprovedRadioligand therapy (beta)
Lutetium-177 dotatate · Lutathera

Lutetium-177 dotatate was the first modern radioligand therapy (2018), for neuroendocrine tumours, and is now used in first line.

ApprovedRadioligand therapy (beta)
Lutetium-177 vipivotide tetraxetan · Pluvicto

A radioactive drug that seeks out PSMA on prostate cancer cells; the best-selling radiopharmaceutical ever.

ApprovedRadiopharmaceutical (beta/gamma emitter, natural uptake)
Radioactive iodine (I-131) · Sodium iodide I-131

The original targeted radiotherapy: thyroid cells soak up iodine, so radioactive iodine destroys leftover thyroid tissue and metastases while sparing everything else.

Key papers

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Latest papers

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Literature trend791 papers in the last 12 months+23% vs prior 12How this is computed
Latest papers · live from Europe PMC
Open in Europe PMC

Query for this technology: (TITLE:"radioligand therapy" OR ABSTRACT:"radioligand therapy" OR TITLE:"peptide receptor radionuclide therapy" OR ABSTRACT:"peptide receptor radionuclide therapy" OR TITLE:"lutetium-177" OR ABSTRACT:"lutetium-177" OR TITLE:"177Lu" OR ABSTRACT:"177Lu"). Results are unfiltered search hits about Radioligand therapy (beta emitters), not a curated reading list.

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