Samarium-153 lexidronam
Quadramet (samarium-153 lexidronam) is a radioactive bone-seeking injection that lodges in bone metastases and irradiates them from inside, approved in 1997 to relieve pain from prostate, breast and other cancers spread to bone. Most patients get relief within one to two weeks, but marrow suppression follows at three to five weeks, and radium-223 and PSMA radioligands have largely replaced it.
Overview
Samarium-153 lexidronam was approved by the FDA in March 1997 and authorised in the EU in February 1998 for relief of pain in patients with confirmed osteoblastic metastatic bone lesions that take up technetium-labelled bisphosphonate on bone scan, on placebo-controlled trials in which most patients had pain relief within one to two weeks lasting for months. It and strontium-89 (Metastron) were the bone-pain radiopharmaceuticals of the 1990s; radium-223 (Xofigo), which extends survival in prostate cancer, and PSMA radioligands have since taken most of their role. A single intravenous dose is given; transient marrow suppression, with nadir at three to five weeks, is the main toxicity, and a pain flare can occur early. Distributed by Lantheus in the US and Curium in Europe.
PubChem holds the unlabelled ligand, so the radionuclide itself is not in this drawing.
Samarium-153 chelated to the tetraphosphonate EDTMP concentrates in areas of high bone turnover around osteoblastic metastases; beta emission (1.9 day half-life) irradiates the metastases and relieves pain, with gamma emission allowing imaging.
- PSMA / SSTR-positive cell
1.Samarium-153 lexidronam binds its target on the cancer cell or is taken up by it.
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Approvals
| Region | Year | Indication |
|---|---|---|
| US | 1997 | Relief of pain in patients with confirmed osteoblastic metastatic bone lesions that enhance on radionuclide bone scan |
| EU | 1998 | Relief of bone pain from multiple painful osteoblastic skeletal metastases (Quadramet) |
Trials
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Latest papers
topQuery for this drug: (TITLE:"Samarium-153 lexidronam" OR ABSTRACT:"Samarium-153 lexidronam" OR TITLE:"Quadramet" OR ABSTRACT:"Quadramet" OR TITLE:"153Sm-EDTMP" OR ABSTRACT:"153Sm-EDTMP" OR TITLE:"Samarium Sm 153 lexidronam pentasodium" OR ABSTRACT:"Samarium Sm 153 lexidronam pentasodium") AND (radiopharmaceutical OR radioligand OR radionuclide OR theranostic OR "nuclear medicine" OR "molecular imaging" OR radiotracer OR scintigraphy OR cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about Samarium-153 lexidronam, not a curated reading list.
Similar pages
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