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1474 details
Primary information
ThPP IDTh1094
Therapeutic Peptide/Protein NamePanitumumab
SequenceN.A. view full sequnce in fasta
Functional ClassificationIIa
Molecular WeightN.A.
Chemical FormulaN.A.
Isoelectric PointN.A.
HydrophobicityN.A.
Melting Point (℃)N.A.
Half Life7.5 days (range: 4-11 days)
DescriptionPanitumumab (ABX-EGF) is an anti-neoplastic agent. It is a recombinant human IgG2 monoclonal antibody that binds specifically to the human epidermal growth factor receptor (EGFR).
Indication/DiseaseFor the treatment of EGFR-expressing, metastatic colorectal carcinoma that is refractory to fluoropyrimidine-, oxaliplatin-, and irinotecan- containing chemotherapy regimens.
PharmacodynamicsPanitumumab is a recombinant, human IgG2 kappa monoclonal antibody that binds specifically to the human Epidermal Growth Factor Receptor (EGFR). EGFR is a transmembrane glycoprotein that belongs to the subfamily of type I receptor tyrosine kinases. Although EGFR is expressed in normal cells, the overexpression of EGFR is detected in many human cancers, including those of the colon and rectum. Interaction of EGFR with its normal ligands causes phosphorylation and activation of a series of intracellular proteins that will in turn regulate the transcription of genes involved with cellular growth and survival, motility, and prolieration. Signal transduction through EGFR leads to the activation of the wild type KRAS gene, but the presence of an activating somatic mutation of the KRAS gene within a cancer cell can result in the dysregulation of signaling pathways and resistance to EGFR inhibitor therapy.
Mechanism of ActionPanitumumab binds specifically to EGFR on both normal and tumor cells, and competitively inhibits the binding of ligands for EGFR. Nonclinical studies show that binding of panitumumab to the EGFR prevents ligand-induced receptor autophosphorylation and activation of receptor-associated kinases, resulting in inhibition of cell growth, induction of apoptosis, decreased pro-inflammatory cytokine and vascular growth factor production, and internalization of the EGFR.
ToxicityPanitumumab was shown to cause skin, ocular and mucosal related toxicities in 90% of patients receiving panitumumab. Subsequent to the development of severe dermatologic toxicities, infectious complications, including sepsis, septic death, and abscesses requiring incisions and drainage, were reported.
MetabolismN.A.
AbsorptionN.A.
Volume of DistributionN.A.
Clearance4.9± 1.4 mL/kg/day [Following single-dose administrations of panitumumab as 1-hour infusions]
CategoriesN.A.
Patents NumberN.A.
Date of IssueN.A.
Date of ExpiryN.A.
Drug InteractionN.A.
TargetEpidermal growth factor receptor
Information of corresponding available drug in the market
Brand NameVectibix
CompanyAmgen Inc
Brand DiscriptionVectibix (panitumumab) is a recombinant, human IgG2 kappa monoclonal antibody that binds specifically to the human epidermal growth factor receptor (EGFR). Panitumumab has an approximate molecular weight of 147 kDa. Panitumumab is produced in genetically engineered mammalian (Chinese hamster ovary) cells.
Prescribed forN.A.
Chemical NameN.A.
Formulationsingle-use 5 mL vial contains 100 mg of panitumumab, 29 mg sodium chloride, 34 mg sodium acetate, and Water for Injection, USP. Each single-use 10 mL vial contains 200 mg of panitumumab, 58 mg sodium chloride, 68 mg sodium acetate, and Water for Injection, USP. Each single-use 20 mL vial contains 400 mg of panitumumab, 117 mg sodium chloride, 136 mg sodium acetate, and Water for Injection, USP.
Physcial AppearnceSterile, colorless, pH 5.6 to 6.0 liquid for intravenous (IV) infusion, which may contain a small amount of visible translucent-to-white, amorphous, proteinaceous, panitumumab particulates
Route of AdministrationN.A.
Recommended DosageN.A.
ContraindicationN.A.
Side EffectsDermatologic toxicities occurred in 90% of patients and were severe (NCI-CTC grade 3 and higher) in 15% of patients receiving Vectibix monotherapy. hives; difficult breathing; swelling of your face, lips, tongue, or throat.
Useful Linkhttp://www.rxlist.com/vectibix-drug.htm http://www.drugs.com/vectibix.html http://www.vectibix.com/preparation-and-administration.html
PubMed ID20481659, 18343240, 17355997
3-D StructureN.A.