Iodine-131 tositumomab
A cancer-targeting antibody carrying a radioactive form of iodine was used, as a single course, to treat a type of blood cancer called non-Hodgkin lymphoma. The manufacturer stopped selling it in 2014 because too few patients were using it.
Overview
The Bexxar therapeutic regimen combined tositumomab, an anti-CD20 murine IgG2a monoclonal antibody, with the same antibody radiolabelled with iodine-131. It was approved by the FDA in 2003 (and in Canada in 2005) for CD20-positive relapsed or refractory low-grade, follicular or transformed non-Hodgkin lymphoma in patients who had progressed during or after rituximab therapy, including rituximab-refractory disease. It was given as a single course only, comprising an unlabelled predose followed by a dosimetric and then a therapeutic dose of 131I-tositumomab, with activity individualised to deliver a specified total-body radiation dose.
Bexxar competed with the similar CD20-targeted radioimmunotherapy ibritumomab tiuxetan (Zevalin, labelled with yttrium-90). Despite comparable efficacy, Bexxar's use declined steadily after a 2006 peak: by 2012 only about 75 US patients received it in a year. GlaxoSmithKline announced in August 2013 that it would discontinue manufacture and sale of the regimen, citing projected declining sales and the availability of alternative therapies; marketing was formally withdrawn on 20 February 2014.
Bexxar is a useful cautionary example in the graph: an approved, effective radiopharmaceutical regimen withdrawn for commercial rather than safety reasons, illustrating how logistics (dosimetry visits, hospital nuclear-medicine capacity, competition from simpler agents) can end a therapy's market life even when clinical data support it.
- Chelated Lu-177 / Ac-225
- Antigen-positive cell
- Radiation, not chemistry
An unlabelled anti-CD20 murine monoclonal antibody (tositumomab) dosing step to saturate normal B-cell sinks, followed by the same antibody labelled with iodine-131, which delivers combined beta and gamma radiation directly to CD20-expressing lymphoma cells as well as an antibody-dependent immune effect. Connects to CD20.
- PSMA / SSTR-positive cell
1.Iodine-131 tositumomab slips into a pocket on CD20.
- 6 Aug 2013WithdrawalUS/CA
GlaxoSmithKline announced it would discontinue manufacture and sale of the Bexxar regimen, citing declining use (about 75 US patients in 2012) and available alternative therapies. source
- 20 Feb 2014WithdrawalUS/CA
Marketing of the Bexxar therapeutic regimen formally discontinued. source
Approvals
| Region | Year | Indication |
|---|---|---|
| US | 2003 | CD20-positive relapsed or refractory, low-grade, follicular, or transformed non-Hodgkin lymphoma progressing during or after rituximab therapy |
| CA | 2005 | Same indication as the US approval |
Trials
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Latest papers
topQuery for this drug: (TITLE:"Iodine-131 tositumomab" OR ABSTRACT:"Iodine-131 tositumomab" OR TITLE:"Bexxar" OR ABSTRACT:"Bexxar" OR TITLE:"tositumomab and I-131 tositumomab" OR ABSTRACT:"tositumomab and I-131 tositumomab") 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 Iodine-131 tositumomab, not a curated reading list.
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