Primary information |
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ThPP ID | Th1094 |
Therapeutic Peptide/Protein Name | Panitumumab |
Sequence | N.A. view full sequnce in fasta |
Functional Classification | IIa |
Molecular Weight | N.A. |
Chemical Formula | N.A. |
Isoelectric Point | N.A. |
Hydrophobicity | N.A. |
Melting Point (℃) | N.A. |
Half Life | 7.5 days (range: 4-11 days) |
Description | Panitumumab (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/Disease | For the treatment of EGFR-expressing, metastatic colorectal carcinoma that is refractory to fluoropyrimidine-, oxaliplatin-, and irinotecan- containing chemotherapy regimens. |
Pharmacodynamics | Panitumumab 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 Action | Panitumumab 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. |
Toxicity | Panitumumab 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. |
Metabolism | N.A. |
Absorption | N.A. |
Volume of Distribution | N.A. |
Clearance | 4.9± 1.4 mL/kg/day [Following single-dose administrations of panitumumab as 1-hour infusions] |
Categories | N.A. |
Patents Number | N.A. |
Date of Issue | N.A. |
Date of Expiry | N.A. |
Drug Interaction | N.A. |
Target | Epidermal growth factor receptor |
Information of corresponding available drug in the market |
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Brand Name | Vectibix |
Company | Amgen Inc |
Brand Discription | Vectibix (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 for | N.A. |
Chemical Name | N.A. |
Formulation | single-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 Appearnce | Sterile, 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 Administration | N.A. |
Recommended Dosage | N.A. |
Contraindication | N.A. |
Side Effects | Dermatologic 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 Link | http://www.rxlist.com/vectibix-drug.htm http://www.drugs.com/vectibix.html http://www.vectibix.com/preparation-and-administration.html |
PubMed ID | 20481659, 18343240, 17355997 |
3-D Structure | N.A. |