==== Reference: Usmani SS, Bedi G, Samuel JS, Singh S, Kalra S, Kumar P, et al. (2017) THPdb: Database of FDA-approved peptide and protein therapeutics. PLoS ONE 12(7) e0181748.====

Detailed description page of THPdb

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1412 details
Primary information
ThPP IDTh1068
Therapeutic Peptide/Protein NameTositumomab
SequenceHeavy Chain 1: QAYLQQSGAELVRPGASVKMSCKASGYTFTSYNMH view full sequnce in fasta
Functional ClassificationIIb
Molecular Weight143859.7
Chemical FormulaC6416H9874N1688O1987S44
Isoelectric Point8.68
Hydrophobicity-0.4144
Melting Point (℃)61 (FAB f
Half Life0.8 hours (mammalian reticulocytes, in vitro)
DescriptionMurine IgG2a lambda monoclonal antibody against CD20 antigen (2 heavy chains of 451 residues, 2 lambda chains of 220 residues). It is produced in an antibiotic-free culture of mammalian cells. It can be covalently linked to Iodine 131 (a radioactive isotope of iodine).
Indication/DiseaseFor treatment of non-Hodgkin's lymphoma (CD20 positive, follicular)
PharmacodynamicsTositumomab binds to the CD20 antigen, which is predominantly expressed on mature B cells and on >90% of B-cell non-Hodgkin's lympohomas. The antibody leads to selective killing of B-cells.
Mechanism of ActionBinds to the CD20 antigen which is found on mature B lymphocytes. The antibody binding appears to induce apoptosis, complement-dependent cytotoxicity and cell death through ionizing radiation.
ToxicityN.A.
MetabolismMost likely removed by opsonization via the reticuloendothelial system when bound to B lymphocytes, or by human antimurine antibody production
AbsorptionN.A.
Volume of DistributionN.A.
Clearance68.2 mg/hr [patients with NHL]
CategoriesN.A.
Patents NumberN.A.
Date of IssueN.A.
Date of ExpiryN.A.
Drug InteractionNatalizumab with immunosuppressant, Tositumomab, may increase the adverse effects. Increased risk of Progressive Multifocal Leukoencephalopathy (PML) and other infections. Concurrent therapy should be avoided
TargetN.A.
Information of corresponding available drug in the market
Brand NameBexxar
CompanyGalaxo Smith Kline
Brand DiscriptionThe BEXXAR therapeutic regimen is composed of the monoclonal antibody tositumomab, and the radiolabeled monoclonal antibody, I-131 tositumomab
Prescribed forThe BEXXAR therapeutic regimen (Tositumomab and Iodine I 131 Tositumomab) is indicated for the treatment of patients with CD20 antigen-expressing relapsed or refractory, low grade, follicular, or transformed non-Hodgkin's lymphoma, including patients with Rituximab-refractory non-Hodgkin’s lymphoma. Determination of the effectiveness of the BEXXAR therapeutic regimen is based on overall response rates in patients whose disease is refractory to chemotherapy alone or to chemotherapy and Rituximab. The effects of the BEXXAR therapeutic regimen on survival are not known.
Chemical NameN.A.
FormulationThe formulation contains 100 mg/mL maltose, 8.5 mg/mL sodium chloride, 1 mg/mL phosphate, 1 mg/mL potassium hydroxide, and Water for Injection, USP. The pH is approximately 7.2.
Physcial AppearnceTositumomab is supplied as a Sterile, pyrogen-free, clear to opalescent, colorless to slightly yellow, preservative-free solution 
Route of AdministrationIntravenous (Intravenous) administration
Recommended DosageThe BEXXAR therapeutic regimen consists of 2 separate components (tositumomab and iodine I 131 tositumomab) administered in 2 separate steps (dosimetric dose and therapeutic dose) separated by 7 to 14 days.Tositumomab 450 mg by Intravenous infusion.I-131 tositumomab (5 mCi I-131 and 35 mg protein) by Intravenous infusion
ContraindicationThe BEXXAR therapeutic regimen is contraindicated in patients with known hypersensitivity to murine proteins or any other component of the BEXXAR therapeutic regimen.
Side EffectsSerious Allergic Reactions, Including Anaphylaxis, Prolonged and Severe Cytopenias, Secondary malignancies, Hypothyroidism, neutropenia, thrombocytopenia, anemia, infections (including pneumonia, bacteremia, septicemia, bronchitis, and skin infections), infusion reactions, asthenia, fever, and nausea.
Useful Linkhttp://dailymed.nlm.nih.gov/dailymed/archives/fdaDrugInfo.cfm?archiveid=11680 http://www.rxlist.com/bexxar-drug.htm
PubMed ID16179960, 15071612, 27195659, 25568316, 22531442, 21355777, 21225019, 19649342, 19455266
3-D StructureTh1068 (View) or (Download)