Lutetium (177Lu) chloride
塩化ルテチウム (177Lu)
Formula | Lu. 3Cl |
---|---|
CAS | 16434-14-3 |
Mol weight | 281.326 |
2022/9/15 EMA 2022, Illuzyce
EndolucinBeta
(177Lu)lutetium(3+) trichloride
Diagnostic aid, Radioactive agent |
Lutetium 177 is an isotope of a rare-earth lanthanide metal lutetium. Radioactive decay of Lu 177 produces electrons with low energies making the isotope suitable for treatment of metastatic disease. A complex of Lu177 and somatostatin analog DOTA-TATE was approved by the FDA for the treatment of somatostatin receptor-positive gastroenteropancreatic neuroendocrine tumors, including foregut, midgut, and hindgut neuroendocrine tumors in adults. It is marketed under a tradename Lutathera. Lutetium in the complex with other carriers – phosphonates and monoclonal antibodies – was investigated in clinical trials as radiotherapy to prostate, ovarian, renal and other types of cancer.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.
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]
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Clinical data | |
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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 [3][4]EU: Rx-only [5][6][7]In general: ℞ (Prescription only) |
Identifiers | |
showIUPAC name | |
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−1 |
3D model (JSmol) | Interactive image |
hideSMILES[Cl-].[Cl-].[Cl-].[177Lu+3] |
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
- ^ “Lutetium (177Lu) Chloride”. Therapeutic Goods Administration (TGA). 21 January 2022. Archived from the original on 5 February 2022. Retrieved 5 February 2022.
- ^ “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.
- ^ “TGA eBS – Product and Consumer Medicine Information Licence”. Archived from the original on 5 February 2022. Retrieved 5 February 2022.
- ^ http://www.ebs.tga.gov.au/servlet/xmlmillr6?dbid=ebs/PublicHTML/pdfStore.nsf&docid=1C7A40803A3A3F94CA2587D4003CE48A&agid=(PrintDetailsPublic)&actionid=1 Archived 30 July 2022 at the Wayback Machine[bare URL PDF]
- ^ Jump up to:a b c d e f g “Lumark EPAR”. European Medicines Agency (EMA). 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.
- ^ Jump up to:a b c “EndolucinBeta EPAR”. European Medicines Agency (EMA). 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.
- ^ Jump up to:a b “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.
- ^ 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.
- ^ 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.
- ^ Jump up to:a b c “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.
External links
- “Lutetium chloride Lu-177”. Drug Information Portal. U.S. National Library of Medicine.
.///////////Lutetium (177Lu) chloride, EMA 2022, EU 2022, APPROVALS 2022, Illuzyce, EndolucinBeta, 塩化ルテチウム (177Lu),