Tracer library / [223Ra]Ra-RaCl2

[223Ra]Ra-RaCl2

Also written as [Ra-223]RaCl2
Radionuclide
Ra-223 t½ 16459 min
Modality
Therapy
Production route
—
Stage
Approved
Syntheses indexed
3

What it is

Compound class
bone-seeking radiopharmaceutical (radium dichloride, calcium-mimetic alpha emitter)
Target / mechanism
Calcium-mimetic alpha-emitter that localizes to bone metastases (bone-seeker) PMID 34163647
Clinical application
Treatment of bone metastases in metastatic castration-resistant prostate cancer PMID 36687439
Theranostic pair
—

Regulatory status

FDA
Yes — 2013; Xofigo (radium Ra 223 dichloride); sponsor BAYER HLTHCARE; NDA 203971 Drugs@FDA / openFDA drug registry, NDA 203971, original approval 2013-05-15, marketing status 'Prescription' — https://api.fda.gov/drug/drugsfda.json?search=application_number:%22NDA203971%22 (queried 2026-09-18)
EMA (centralised)
Yes — 2013; Xofigo (radium (223Ra) dichloride); Bayer AG; EMEA/H/C/002653 EMA medicines register (JSON export 2026-09-18), EPAR Xofigo: status 'Authorised', marketing authorisation date 2013-11-13 — https://www.ema.europa.eu/en/medicines/human/EPAR/xofigo
Other approvals
—
Brand names
—

Published syntheses

ModuleCassettePurificationYield %RCP %Precursor / supplierSource
Manual synthesis—none95 ± 1.05%>95%macropa34163647
2021 Chem Sci
The reaction was carried out at room temperature by mixing a solution of macropa with 3.7 kBq (0.1 μCi) of [223Ra]Ra2+ - Within 5 min at room temperature, [223Ra][Ra(macropa)] was formed with a radiolabeling efficiency (RL% ± SD) of 95 ± 1.05% (n = 5) (Fig. 2a)
————>94%UiO-66-NH2 MOF (mMOF)41452472
2026 ACS Appl Mater Interfaces
————>94%UiO-66-NH2 MOF (nMOF)41452472
2026 ACS Appl Mater Interfaces

Clinical literature

Clinical studies in the indexed corpus, ordered by design (multicentre, prospective, retrospective, others, case reports last) and then by year. Titles and links only, as published; this is not a summary of the evidence.

  1. Large Italian Multicenter Study on Prognostic Value of Baselines Variables in mCRPC Patients Treated with 223RaCl2: Ten Years of Clinical Experience.
    2025 · Diagnostics (Basel) · Clinical study
  2. Radiation Safety Considerations and Clinical Advantages of α-Emitting Therapy Radionuclides.
    2022 · J Nucl Med Technol · Clinical study
  3. Radium Ra 223 dichloride injection: U.S. Food and Drug Administration drug approval summary.
    2014 · Clin Cancer Res · Clinical study

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Notes

Added at stage 21 from therapy-discovered.xlsx (bulk PubMed search by isotope/therapy-type/known-agent, not individually researched yet) -- 6 articles found. Target/mechanism, clinical application, indications, approval and precursor fields still need per-agent research and are intentionally left empty. Stage set/updated at stage 23 from PMID 42149170: 'The radiopharmaceutical 223Ra-dichloride (Xofigo®) has been approved for palliative treatment of metastatic castration-resistant prostate cancer.'.
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