Lutetium (177Lu) chloride explained

Tradename:Lumark, EndolucinBeta, Illuzyce
Drugs.Com:Lumark
EndolucinBeta
Pregnancy Au:X
Pregnancy Au Comment:[1] [2]
Atc Prefix:None
Legal Au:Unscheduled
Legal Au Comment:[3] [4]
Legal Eu:Rx-only
Legal Eu Comment:[5]
Legal Status:Rx-only
Cas Number:16434-14-3
Pubchem:71587001
Drugbank:DBSALT002634
Chemspiderid:32700269
Unii:1U477369SN
Kegg:D10828
Iupac Name:(177Lu)lutetium(3+) trichloride
Cl:3
Lu:1
Smiles:[Cl-].[Cl-].[Cl-].[177Lu+3]
Stdinchi:1S/3ClH.Lu/h3*1H;/q;;;+3/p-3/i;;;1+2
Stdinchikey:AEDROEGYZIARPU-SUNKFXMWSA-K

Lutetium (177Lu) chloride is a radioactive compound used for the radiolabeling of pharmaceutical molecules, aimed either as an anti-cancer therapy or for scintigraphy (medical imaging).[6] [7] It is an isotopomer of lutetium(III) chloride containing the radioactive isotope 177Lu, which undergoes beta decay with a half-life of 6.64 days.[8]

Medical uses

Lutetium (177Lu) chloride is a radiopharmaceutical precursor and is not intended for direct use in patients. It is used for the radiolabeling of carrier molecules specifically developed for reaching certain target tissues or organs in the body. The molecules labeled in this way are used as cancer therapeutics or for scintigraphy, a form of medical imaging. 177Lu has been used with both small molecule therapeutic agents (such as 177Lu-DOTATATE) and antibodies for targeted cancer therapy[9] [10]

Contraindications

Medicines radiolabeled with lutetium (177Lu) chloride must not be used in women unless pregnancy has been ruled out.

Adverse effects

The most common side effects are anaemia (low red blood cell counts), thrombocytopenia (low blood platelet counts), leucopenia (low white blood cell counts), lymphopenia (low levels of lymphocytes, a particular type of white blood cell), nausea (feeling sick), vomiting and mild and temporary hair loss.

Society and culture

Legal status

Lutetium (177Lu) chloride (Lumark) was approved for use in the European Union in June 2015. Lutetium (177Lu) chloride (EndolucinBeta) was approved for use in the European Union in July 2016.

In July 2022, the Committee for Medicinal Products for Human Use (CHMP) of the European Medicines Agency (EMA) adopted a positive opinion, recommending the granting of a marketing authorization for the medicinal product Illuzyce, a radiopharmaceutical precursor. Illuzyce is not intended for direct use in patients and must be used only for the radiolabelling of carrier medicines that have been specifically developed and authorized for radiolabelling with lutetium (177Lu) chloride. The applicant for this medicinal product is Billev Pharma ApS.[11] Illuzyce was approved for medical use in the European Union in September 2022.

Notes and References

  1. Web site: Lutetium (177Lu) Chloride APMDS . Therapeutic Goods Administration (TGA) . 21 January 2022 . 5 February 2022 . 5 February 2022 . https://web.archive.org/web/20220205214734/https://www.tga.gov.au/apm-summary/lutetium-177lu-chloride . live .
  2. Web site: Updates to the Prescribing Medicines in Pregnancy database . Therapeutic Goods Administration (TGA) . 12 May 2022 . 13 May 2022 . 3 April 2022 . https://web.archive.org/web/20220403064059/https://www.tga.gov.au/updates-prescribing-medicines-pregnancy-database . live .
  3. Web site: TGA eBS - Product and Consumer Medicine Information Licence. 5 February 2022. 5 February 2022. https://web.archive.org/web/20220205213233/https://www.ebs.tga.gov.au/ebs/picmi/picmirepository.nsf/pdf?OpenAgent&id=CP-2022-PI-01059-1. live.
  4. Web site: ANSTO Lutetium (177Lu) Chloride Radiochemical Solution for injection vial . https://web.archive.org/web/20220730051623/https://www.ebs.tga.gov.au/servlet/xmlmillr6?dbid=ebs%2FPublicHTML%2FpdfStore.nsf&docid=1C7A40803A3A3F94CA2587D4003CE48A&agid=%28PrintDetailsPublic%29&actionid=1 . 30 July 2022 . dead.
  5. Web site: Illuzyce EPAR . European Medicines Agency (EMA) . 18 July 2022 . 21 September 2022 . 22 September 2022 . https://web.archive.org/web/20220922033419/https://www.ema.europa.eu/en/medicines/human/EPAR/illuzyce . live . Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
  6. Web site: Lumark EPAR . European Medicines Agency (EMA) . 17 September 2018 . 7 May 2020 . 25 October 2020 . https://web.archive.org/web/20201025033334/https://www.ema.europa.eu/en/medicines/human/EPAR/lumark . live . Text was copied from this source under the copyright of the European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
  7. Web site: EndolucinBeta EPAR . European Medicines Agency (EMA) . 17 September 2018 . 7 May 2020 . 28 October 2020 . https://web.archive.org/web/20201028053253/https://www.ema.europa.eu/en/medicines/human/EPAR/endolucinbeta . live . Text was copied from this source under the copyright of the European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
  8. Ladrière T, Faudemer J, Levigoureux E, Peyronnet D, Desmonts C, Vigne J . Safety and Therapeutic Optimization of Lutetium-177 Based Radiopharmaceuticals . Pharmaceutics . 15 . 4 . April 2023 . 37111725 . 10.3390/pharmaceutics15041240 . 1240 . free . 10145759 .
  9. Lundsten S, Spiegelberg D, Stenerlöw B, Nestor M . The HSP90 inhibitor onalespib potentiates 177Lu‑DOTATATE therapy in neuroendocrine tumor cells . International Journal of Oncology . 55 . 6 . 1287–1295 . December 2019 . 31638190 . 10.3892/ijo.2019.4888 . 6831206 .
  10. Michel RB, Andrews PM, Rosario AV, Goldenberg DM, Mattes MJ . 177Lu-antibody conjugates for single-cell kill of B-lymphoma cells in vitro and for therapy of micrometastases in vivo . Nuclear Medicine and Biology . 32 . 3 . 269–78 . April 2005 . 15820762 . 10.1016/j.nucmedbio.2005.01.003 .
  11. Web site: Illuzyce: Pending EC decision . European Medicines Agency . 21 July 2022 . 30 July 2022 . 30 July 2022 . https://web.archive.org/web/20220730022025/https://www.ema.europa.eu/en/medicines/human/summaries-opinion/illuzyce . live . Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.

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