Lutetium (177Lu) chloride

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).[4][5] It is an isotopomer of lutetium(III) chloride containing the radioactive isotope 177Lu, which undergoes beta decay with a half-life of 6.65 days.

Lutetium (177Lu) chloride
Clinical data
Trade namesLumark, EndolucinBeta
AHFS/Drugs.comLumark UK Drug Information
EndolucinBeta UK Drug Information
License data
Pregnancy
category
  • AU: X (High risk)[1]
ATC code
  • None
Legal status
Legal status
  • AU: Unscheduled [2][3]
  • EU: Rx-only
  • In general: ℞ (Prescription only)
Identifiers
  • (177Lu)lutetium(3+) trichloride
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
CompTox Dashboard (EPA)
Chemical and physical data
FormulaCl3Lu
Molar mass281.32 g·mol−1
3D model (JSmol)
  • [Cl-].[Cl-].[Cl-].[177Lu+3]
  • InChI=1S/3ClH.Lu/h3*1H;/q;;;+3/p-3/i;;;1+2
  • Key:AEDROEGYZIARPU-SUNKFXMWSA-K

Medical uses

Lutetium (177Lu) chloride is a radiopharmaceutical precursor and is not intended for direct use in patients.[4] 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.[4] 177Lu has been used with both small molecule therapeutic agents (such as 177Lu-DOTATATE) and antibodies for targeted cancer therapy[6][7]

Contraindications

Medicines radiolabeled with lutetium (177Lu) chloride must not be used in women unless pregnancy has been ruled out.[4]

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.[4]

Society and culture

Lutetium (177Lu) chloride (Lumark) was approved for use in the European Union in June 2015.[4] Lutetium (177Lu) chloride (EndolucinBeta) was approved for use in the European Union in July 2016.[5]

References
  1. "Lutetium (177Lu) Chloride". Therapeutic Goods Administration (TGA). 21 January 2022. Retrieved 5 February 2022.
  2. "TGA eBS - Product and Consumer Medicine Information Licence".
  3. http://www.ebs.tga.gov.au/servlet/xmlmillr6?dbid=ebs/PublicHTML/pdfStore.nsf&docid=1C7A40803A3A3F94CA2587D4003CE48A&agid=(PrintDetailsPublic)&actionid=1
  4. "Lumark EPAR". European Medicines Agency (EMA). Retrieved 7 May 2020. Text was copied from this source under the copyright of the European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
  5. "EndolucinBeta EPAR". European Medicines Agency (EMA). Retrieved 7 May 2020. Text was copied from this source under the copyright of the European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
  6. Lundsten S, Spiegelberg D, Stenerlöw B, Nestor M (December 2019). "The HSP90 inhibitor onalespib potentiates 177Lu‑DOTATATE therapy in neuroendocrine tumor cells". International Journal of Oncology. 55 (6): 1287–1295. doi:10.3892/ijo.2019.4888. PMC 6831206. PMID 31638190.
  7. Michel RB, Andrews PM, Rosario AV, Goldenberg DM, Mattes MJ (April 2005). "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. doi:10.1016/j.nucmedbio.2005.01.003. PMID 15820762.
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