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ImmunoglobulinG2a, anti-(human CD20 (antigen)) (mouse monoclonal clone B1R1 g2a-chain),disulfide with mouse monoclonal clone B1R1 lx-chain, dimer, iodine-131I-labeled

Base Information Edit
  • Chemical Name:ImmunoglobulinG2a, anti-(human CD20 (antigen)) (mouse monoclonal clone B1R1 g2a-chain),disulfide with mouse monoclonal clone B1R1 lx-chain, dimer, iodine-131I-labeled
  • CAS No.:192391-48-3
  • Molecular Formula:I
  • Molecular Weight:130.90600
  • Hs Code.:
  • Mol file:192391-48-3.mol
ImmunoglobulinG2a, anti-(human CD20 (antigen)) (mouse monoclonal clone B1R1 g2a-chain),disulfide with mouse monoclonal clone B1R1 lx-chain, dimer, iodine-131I-labeled

Synonyms:3:PN: WO2008003319 PAGE: 45 claimed sequence; Bexxar; Iodine I131 tositumomab;Tositumab

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Chemical Property of ImmunoglobulinG2a, anti-(human CD20 (antigen)) (mouse monoclonal clone B1R1 g2a-chain),disulfide with mouse monoclonal clone B1R1 lx-chain, dimer, iodine-131I-labeled Edit
Chemical Property:
  • PSA:0.00000 
  • LogP:0.88570 
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  • Description Tositumomab was launched as a new radioimmunotherapeutic antibody for the treatment of β-cell non-Hodgkin’s lymphoma (NHL). It is specifically indicated for patients with CD20-positive, follicular NHL, with or without transformation, whose disease is refractory to rituximab and has relapsed following chemotherapy. Tositumomab is an anti-CD20 murine IgG2a lambda monoclonal antibody produced in an antibiotic-free culture of mammalian cells. The therapeutic regimen of the drug is composed of tositumomab and 131I-tositumomab. This dual-action therapy combines the tumor-targeting ability of a cytotoxic monoclonal antibody and the therapeutic potential of radiation with patient-specific dosing. The binding of tositumomab to CD20 antigen on NHL cells initiates an immune response to the cancer and the radiolabeled antibody, 131Itositumomab, delivers a dose of radiation directly to tumor cells. Iodine-131 has a physical half-life of eight days. It emits b particles and γ rays, but the primary antitumor effect results from the β particles. In contrast to the external beam radiation, 131Itositumomab delivers radiation to the tumor at a continuous low dose rate. The dose rate initially increases, as radiolabelled antibodies accumulate at the tumor site, with a maximal tumor dose rate of <0.10 Gy/h. The dose rate then decreases with physical decay of the radioisotope and clearance from the body. The tositumomab and 131Itositumomab therapeutic regimen is dosed in two steps: a dosimetric step followed 7–14 days later by a therapeutic step. The dosimetric step consists of successive infusions of tositumomab (450 mg) and 131I-tositumomab (5.0 mCi, 35 mg). The therapeutic step consists of 450 mg tositumomab infusion, followed by 131I-tositumomab as calculated to patient-specific activity. Since non-tumor localization of 131I is primarily in the thyroid, the patients are also treated with a thyro-protective agent such as potassium iodide throughout the therapeutic course. In a clinical study in patients who had an average of four prior chemotherapies and who did not respond to or relapsed from rituximab therapy, overall response to tositumomab and 131I-tositumomab treatment was achieved in 63% of the patients and complete response was achieved in 29% of the patients. The duration of response in this category of patients was 25 months. The most common adverse reactions associated tositumomab regimens are severe or life-threatening cytopenia, infections, hemorrhage, allergic reactions, secondary leukemia, and myelodysplasia.
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