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Lutetium (177Lu) chloride

Clinical data
Trade names	Lumark, EndolucinBeta, Illuzyce
AHFS/Drugs.com	Lumark UK Drug Information EndolucinBeta UK Drug Information
Pregnancy category	AU: X (High risk)
ATC code	None
Legal status
Legal status	AU: Unscheduled EU: Rx-only In general: ℞ (Prescription only)
Identifiers
IUPAC name (Lu)lutetium(3+) trichloride
CAS Number	16434-14-3
PubChem CID	71587001
DrugBank	DBSALT002634
ChemSpider	32700269
UNII	1U477369SN
KEGG	D10828
CompTox Dashboard (EPA)	DTXSID20167745
Chemical and physical data
Formula	Cl3Lu
Molar mass	281.32 g·mol
3D model (JSmol)	Interactive image
SMILES ...
InChI InChI=1S/3ClH.Lu/h3*1H;/q;;;+3/p-3/i;;;1+2 Key:AEDROEGYZIARPU-SUNKFXMWSA-K

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

Medical uses

Lutetium (Lu) 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. Lu has been used with both small molecule therapeutic agents (such as Lu-DOTATATE) and antibodies for targeted cancer therapy

Contraindications

Medicines radiolabeled with lutetium (Lu) 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 (Lu) chloride (Lumark) was approved for use in the European Union in June 2015. Lutetium (Lu) 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 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 (Lu) chloride. The applicant for this medicinal product is Billev Pharma ApS. Illuzyce was approved for medical use in the European Union in September 2022.

In September 2024, the CHMP adopted a positive opinion, recommending the granting of a marketing authorization for the medicinal product Theralugand, a radiopharmaceutical precursor. Theralugand 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 Eckert & Ziegler Radiopharma GmbH.

References

1. ^ "Lutetium (177Lu) Chloride APMDS". Therapeutic Goods Administration (TGA). 21 January 2022. Archived from the original on 5 February 2022. Retrieved 5 February 2022.
2. "Updates to the Prescribing Medicines in Pregnancy database". Therapeutic Goods Administration (TGA). 12 May 2022. Archived from the original on 3 April 2022. Retrieved 13 May 2022.
3. "TGA eBS - Product and Consumer Medicine Information Licence". Archived from the original on 5 February 2022. Retrieved 5 February 2022.
4. "ANSTO Lutetium (177Lu) Chloride Radiochemical Solution for injection vial". Archived from the original (PDF) on 30 July 2022.
5. ^ "Lumark EPAR". European Medicines Agency (EMA). 17 September 2018. Archived from the original on 25 October 2020. 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. ^ "EndolucinBeta EPAR". European Medicines Agency (EMA). 17 September 2018. Archived from the original on 28 October 2020. 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.
7. ^ "Illuzyce EPAR". European Medicines Agency (EMA). 18 July 2022. Archived from the original on 22 September 2022. Retrieved 21 September 2022. Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
8. Ladrière T, Faudemer J, Levigoureux E, Peyronnet D, Desmonts C, Vigne J (April 2023). "Safety and Therapeutic Optimization of Lutetium-177 Based Radiopharmaceuticals". Pharmaceutics. 15 (4): 1240. doi:10.3390/pharmaceutics15041240. PMC 10145759. PMID 37111725.
9. 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.
10. 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.
11. ^ "Illuzyce: Pending EC decision". European Medicines Agency. 21 July 2022. Archived from the original on 30 July 2022. Retrieved 30 July 2022. Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
12. ^ "Theralugand EPAR". European Medicines Agency (EMA). 19 September 2024. Retrieved 21 September 2024. Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.

• Medicine

• Drugs not assigned an ATC code
• Radiopharmaceuticals
• Lutetium compounds
• Chlorides
• Orphan drugs