==== 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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1005 details
Primary information
ThPP IDTh1002
Therapeutic Peptide/Protein NameCetuximab
SequenceHeavy chain:QVQLKQSGPGLVQPSQSLSITCTVSGFSLTNYGVHWVR view full sequnce in fasta
Functional ClassificationIIIc
Molecular Weight145781.6
Chemical FormulaC6484H10042N1732O2023S36
Isoelectric Point8.48
Hydrophobicity-0.413
Melting Point (℃)71
Half Life114 hours
DescriptionIt is an epidermal growth factor receptor which binds to FAB region. Cetuximab consists of the variable antigen-binding regions of the 225 murine EGFr monoclonal antibody that is specific for N-terminal part of human EGFr with human IgG1 heavy chain and kappa light chain constant regions.
Indication/DiseaseUsed to treat EGFR-expressing metastatic colorectal cancer in patients resistant to irinotecan based chemotherapy regimens. Also used to treat squamous cell carcinoma of the head and neck in combination with radiation therapy.
PharmacodynamicsCetuximab specifically binds to the epidermal growth factor receptors (EGFr, HER1, c-ErbB-1) on both normal and tumor cells(EGFr is over-expressed in many colorectal cancers). Cetuximab competitively inhibits the binding of epidermal growth factor (EGF) and other ligands, such as transforming growth factor–alpha. Binding of cetuximab to the EGFr blocks phosphorylation and activation of receptor-associated kinases, resulting in inhibition of cell growth, induction of apoptosis, decreased matrix metalloproteinase secretion and reduced vascular endothelial growth factor production.
Mechanism of ActionCetuximab binds to EGFr (over-expressed in many colorectal cancers) on both normal and tumor cells. Cetuximab competitively inhibits the binding of epidermal growth factor (EGF) and TGF alpha, thereby reducing their effects on cell growth and metastatic spread.
ToxicitySingle doses of cetuximab more than 500 mg/m2 have'nt been tested. There is no report of overdosage in human clinical trials.
MetabolismN.A.
AbsorptionN.A.
Volume of DistributionN.A.
ClearanceN.A.
CategoriesAntineoplastic Agents
Patents NumberCA1340417
Date of Issue02/03/99
Date of Expiry02/03/16
Drug InteractionThalomid (thalidomide)
TargetEpidermal growth factor receptor,Low affinity immunoglobulin gamma Fc region receptor III-B,Complement C1r subcomponent,Complement C1q subcomponent subunit A,Complement C1q subcomponent subunit B,Complement C1q subcomponent subunit C,Low affinity immunoglobulin gamma Fc region receptor III-A,Complement C1s subcomponent,High affinity immunoglobulin gamma Fc receptor I,Low affinity immunoglobulin gamma Fc region receptor II-a,Low affinity immunoglobulin gamma Fc region receptor II-b,Low affinity immunoglobulin gamma Fc region receptor II-c
Information of corresponding available drug in the market
Brand NameErbitux
CompanyImClone Systems Inc
Brand DiscriptionIt's a targeted therapy, classified as a monoclonal antibody and signal transduction inhibitor. Erbitux binds to epidermal growth factor receptors (EGFR).
Prescribed forUsed for treatment of metastatic colorectal cancer (cancer spread beyond the colon or rectum) that over-expresses the epidermal growth factor receptor (EGFR). Aapproved for the treatment of squamous cell carcinoma of the head and neck.
Chemical NameN.A.
FormulationFormulated in a solution with no preservatives, which contains 8.48 mg/mL sodium chloride, 1.88 mg/mL sodium phosphate dibasic heptahydrate, 0.41 mg/mL sodium phosphate monobasic monohydrate, and Water for Injection, USP.
Physcial AppearnceSterile, clear, colorless liquid of pH 7.0-7.4, which may contain a small amount of easily visible, white, amorphous cetuximab particulates
Route of AdministrationIntravenous infusion
Recommended DosageGenerally given once every week for 6 to 7 weeks. And supplied at a concentration of 2 mg/mL in either 100 mg (50 mL) or 200 mg (100 mL), single-use vials.
Contraindicationallergic
Side EffectsRash (Acne like), Generalized weakness, malaise, Fever, Low magnesium level are commom (occurring in greater than 30%) for patients taking Erbitux. And less coomon side effects (occurring in about 10-29%) of patients receiving Erbitux are; Nausea and vomitting.
Useful Linkhttp://chemocare.com/chemotherapy/drug-info/erbitux.aspx
PubMed ID28222590, 28069552, 27033349, 26254368, 26119717, 25512619, 24990295, 24175095, 24105075
3-D StructureTh1002 (View) or (Download)