GMS6540: TARGETED THERAPIES EXAM QUESTIONS AND ANSWERS WITH COMPLETE SOLUTIONS VERIFIED

GMS6540: TARGETED THERAPIES EXAM QUESTIONS AND

ANSWERS WITH COMPLETE SOLUTIONS VERIFIED


growth factors

-stimulate the growth and division of cells

growth factor receptors important in cancer

-epidermal growth factor receptor = EGFR

-human epidermal growth factor receptor 2= HER2/Neu

-platelet derived growth factor receptor = PDGFR

EGFR

-sits on transmembrane protein

-receptor part is extracellular

-EGF ligand binds = dimerization

-intracellular parts form dimer = kinase domain

-autophosphorylation occurs

-Ras and PI3K acitivated

classes of EGFR inhibitors

-antibodies = block extracellular ligand binding

-tyrosine kinase inhibitors = block intracellular signaling

EGFR antibodies

-Cetuximab

Cetuximab

, -EGFR antibody

-bind extracellular domain III

-blocks EGFR binding and induces antibody-dependent cell-mediated cytotoxicity =

ADCC

-administered as loading dose + weekly by IV

-used for colon cancer = combined with chemo for KRAS WT or single agent for chemo-

resistant cancers

-used for head and neck squamous cell carcinoma = combined with radiation or

cisplatin or single-agent for cisplatin resistant cancer

ADCC

-antibodies bind antigens on surface of target cells

-NK cell CD16 Fc receptors recognize cell-bound antibodies

-cross-linking of CD16 triggers degranulation into a lytic synapse

-tumor cells die by apoptosis

EGFR tyrosine kinase inhibitors

-erlotinib, gefitinib, osimertinib

erlotinib, gefitinib, osimertinib

-EGFR tyrosine kinase inhibitors

-inhibit ATP binding = prevents kinase activity

erlotinib/gefitinib

-EGFR tyrosine kinase inhibitors

-inhibit ATP binding = prevents kinase activity

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