Lutetium (177Lu) chloride

Short description: Radioactive compound used for radiopharmaceutical labeling

Lutetium (177Lu) chloride

Clinical data
Trade names| Lumark, EndolucinBeta, Illuzyce
AHFS/Drugs.com| Lumark UK Drug Information
EndolucinBeta UK Drug Information
License data|

* EU EMA: by INN

Pregnancy
category|

* AU: X (High risk)[1][2]

ATC code|

* None

Legal status
Legal status|

* AU: Unscheduled [1][3][4]
* EU: Rx-only [5][6][7]
* In general: ℞ (Prescription only)

Identifiers

IUPAC name

* (177Lu)lutetium(3+) trichloride

CAS Number|

* 16434-14-3

PubChem CID|

* 71587001

DrugBank|

* DBSALT002634

ChemSpider|

* 32700269

UNII|

* 1U477369SN

KEGG|

* D10828

Chemical and physical data
Formula| Cl3Lu
Molar mass| 281.32 g·mol−1
3D model (JSmol)|

* Interactive image

SMILES

* [Cl-].[Cl-].[Cl-].[177Lu+3]

InChI

* InChI=1S/3ClH.Lu/h3*1H;/q;;;+3/p-3/i;;;1+2

* Key: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).[5][6] 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.

## Contents

* 1 Medical uses
* 2 Contraindications
* 3 Adverse effects
* 4 Society and culture
* 4.1 Legal status
* 5 References

## Medical uses

Lutetium (177Lu) chloride is a radiopharmaceutical precursor and is not intended for direct use in patients.[5] 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.[5] 177Lu has been used with both small molecule therapeutic agents (such as 177Lu-DOTATATE) and antibodies for targeted cancer therapy[8][9]

## Contraindications

Medicines radiolabeled with lutetium (177Lu) chloride must not be used in women unless pregnancy has been ruled out.[5]

## 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.[5]

## Society and culture

### Legal status

Lutetium (177Lu) chloride (Lumark) was approved for use in the European Union in June 2015.[5] Lutetium (177Lu) chloride (EndolucinBeta) was approved for use in the European Union in July 2016.[6]

On 21 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.[10] 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.[10] The applicant for this medicinal product is Billev Pharma ApS.[10] Illuzyce was approved for medical use in the European Union in September 2022.[7]

## References

1. ↑ 1.0 1.1 "Lutetium (177Lu) Chloride APMDS". 21 January 2022. https://www.tga.gov.au/resources/auspmd/lutetium-177lu-chloride.
2. ↑ "Updates to the Prescribing Medicines in Pregnancy database". 12 May 2022. https://www.tga.gov.au/resources/resource/guidance/updates-prescribing-medicines-pregnancy-database.
3. ↑ "TGA eBS - Product and Consumer Medicine Information Licence". https://www.ebs.tga.gov.au/ebs/picmi/picmirepository.nsf/pdf?OpenAgent&id=CP-2022-PI-01059-1.
4. ↑ http://www.ebs.tga.gov.au/servlet/xmlmillr6?dbid=ebs/PublicHTML/pdfStore.nsf&docid=1C7A40803A3A3F94CA2587D4003CE48A&agid=(PrintDetailsPublic)&actionid=1 [bare URL PDF]
5. ↑ 5.0 5.1 5.2 5.3 5.4 5.5 5.6 "Lumark EPAR". 17 September 2018. https://www.ema.europa.eu/en/medicines/human/EPAR/lumark. Text was copied from this source under the copyright of the European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
6. ↑ 6.0 6.1 6.2 "EndolucinBeta EPAR". 17 September 2018. https://www.ema.europa.eu/en/medicines/human/EPAR/endolucinbeta. Text was copied from this source under the copyright of the European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
7. ↑ 7.0 7.1 "Illuzyce EPAR". 18 July 2022. https://www.ema.europa.eu/en/medicines/human/EPAR/illuzyce. Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
8. ↑ "The HSP90 inhibitor onalespib potentiates 177Lu‑DOTATATE therapy in neuroendocrine tumor cells". International Journal of Oncology 55 (6): 1287–1295. December 2019. doi:10.3892/ijo.2019.4888. PMID 31638190.
9. ↑ "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. doi:10.1016/j.nucmedbio.2005.01.003. PMID 15820762.
10. ↑ 10.0 10.1 10.2 "Illuzyce: Pending EC decision". 21 July 2022. https://www.ema.europa.eu/en/medicines/human/summaries-opinion/illuzyce. Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.

* v
* t
* e

Therapeutic radiopharmaceuticals (ATC: V10)

Pain palliation|

* 153Sm
* Lexidronam
* 89Sr (Strontium chloride)

Adrenergic tumors|

* 131I
* Iobenguane

CD20 antibodies|

* 90Y
* Ibritumomab tiuxetan
* 131I
* Tositumomab

Radionuclides|

| alpha emitters|

* 223Ra (Radium chloride)

|

beta emitters|

* 32P
* 89Sr
* 90Y
* 131I
* 153Sm
* 165Dy
* 169Er
* 177Lu (Oxodotreotide)
* 186Re
* 198Au

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