Description
Panitumumab is a recombinant, fully human IgG2 kappa monoclonal antibody
that is highly selective for the epidermal growth factor receptor (EGFR),
and it is indicated for the treatment of EGFR-expressing, metastatic colorectal
carcinoma (mCRC) with disease progression on or following fluoropyrimidine-,
oxaliplatin-, and irinotecan-containing chemotherapy regimens. Overexpression
of EGFR is detected in many human cancers, including those of the colon and
rectum. Panitumumab blocks the binding of ligands such as epidermal growth
factor (EGF) and transforming growth factor (TGF-a) to various EGFR-expressing
cell lines, which results in inhibition of EGF-dependent tumor cell activation,
induction of apoptosis, and decreased pro-inflammatory cytokine and vascular
growth factor production. In vitro, panitumumab binds EGFR with high affinity
(KD ? 50pM; IC50 ? 3 nM) in human cervical epidermal cell line A-431.
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Clinical Use
Monoclonal antibody:
Treatment of metastatic colorectal cancer
Drug interactions
Potentially hazardous interactions with other drugs
Cytotoxics: avoid with bevacizumab, fluorouracil,
irinotecan and oxaliplatin.
Folinic acid: avoid concomitant use.
Live vaccines: avoid concomitant use.
Metabolism
Saturable elimination mediated via reticuloendothelial
system, and internalisation and degradation of EGFR.
