EGFR
HER 1
HER 2
HER 3
HER 4
Gefitinib,  Erlotinib

Lapatinib, XL 647**,
ARRY 543
Canertinib
Oral anti-EGFR-TKs* inhibit
enzyme cascades that are
activated by stimulation of
Her 1,2, 3 & 4 membrane receptors
* inhibitors of tyrosine kinases triggered
by EGFR stimulation
** XL 647 also inhibits VEGFR2 & EphB4
Anti EGFR or anti Her2 monoclonals prevent these receptors from being activated.
If they are IgG1s, they can also increase ADCC (antibody dependent cell cytotoxicity) :
                                  trastuzumabcetuximab,

Panitumumab
Cetuximab
Trastuzumab
T-DM1
HealthValue
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EGFR close-up
Some patients with non small cell lung cancer respond particularly well to oral anti-EGFR-TKs if they carry "facilitating" mutations in their EGFRs (the letters and numbers indicate which amino acids are mutated).

On these CT scans one can see the enormous tumoral mass on the left, considerably regress on the right, after 6 weeks of treatment with an oral anti EGFR-TK, in a 32 year old patient bearing an EGFR mutation
Biotech & Cancer : the EGF system
These two illustrations (3D reconstruction of mutated zones, CT scan) are reproduced with authorization from the authors  (Daniel A. Haber) and from the New England Journal of Medicine : Lynch TJ, Bell DW, Sordella R, et al. Activating Mutations in the Epidermal Growth Factor Receptor Underlying Responsiveness of Non-Small-Cell Lung Cancer to Gefitinib. N. Engl J Med 2004;350:2129-39. Copyright 2004 Massachussets Medical Society. All rights reserved.
These new Bio-Medicines, inhibiting receptors
(monoclonals) or cascades (oral anti EGFR  tyrosine kinases ), devoid of cytotoxic effects of classical anticancer chemotherapies, play a growing part in anti-cancer strategy



Zalutumumab, nimotuzumab,
matuzumab, ch 806

SHEDDASES activate these receptors, click
EGFR agonists &
pathways, click
Details on agonists
& pathways, click
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Visit key other pages :
EGF system
EGF receptor
EGF agonists & pathways
Sheddases & ADAMs
VEGF
Cancer & Biotech drugs
Monoclonals
Pertuzumab
inhibits Her2/Her3 dimerization
ARRY 380
In Afro-Americans mutations are rare, but high increase of EGFR numbers might induce higher sensitivity to erlotinib, gefitinib; Chicago Sympo Thoracoc Oncol. Nov 14, 2008
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