Targeted therapy Flashcards
What are the two types of molecule seen in targeted therapy
small molecules
large molecules
what are small molecules referred to as
tyrosine kinase inhibitors
what are large molecules referred to as
monoclonal antibodies
what is the suffix of a tyrosine kinase inhibitor
nib
how are small molecule drugs delivered vs large molecule drugs
oral for small
parenteral for big
How do small molecules exert an affect
they affect the intracellular mechanisms
how do large molecules cause an effect
they target extracellular targets and enable a change within the cell
what is the primary intra cellular target of small molecules
protein kinase
what does protein kinase do
when it is dysregualted leading to an increase in proliferative signalling
how to protein kinase inhibitors work
they inhibit the phosphorylation of proteins that are involve in cellular signal transduction pathways
what is the most common small molecule drug
imatinib
what is a monoclonal antibody
they are a type of y shaped antibody that are man made and are involved in eliminating pathogens.
what are the different sources that monoclonal antibodies produce copies from in the lab.
animals
mice
humanized
human
what are the two ways in which monoclonals work
direct and indirect mechanism
outline the two direct mechanisms of monoclonal antibodies
monoclonal antibodies bind with a target receptor and block the signals needed for growth
monoclonal antibodies combine with other cytotoxic agents and facilitate the direct delivery of a toxic substance to the cell
what are the 5 types of indirect mechanism of monoclonal antibodies
antibody dependent cellular cytotoxicity
complement dependent cytotoxicity
antibody dependent cellular phagocytosis
immune checkpoint blockade
binding and delivery
what is antibody dependent cellular cytotoxicity
activation of NK, macrophage and neutrophils leading to apoptosis
what is complement dependent cytotoxicity
activate cytokines that attack the cell leading to apoptosis
what is antibody dependent cellular phagocytosis
engagement of macrophages which phagocytose the cancer
what is immune checkpoint blockade
involves interruption of immunosuppresive extracellular signallingw
what is binding and delivery
mab carries the cancer cell to the immune effect to enable immune mediated tumour cell
what is CD20 a common antigen of
non hodjkins lymphoma
where can CD20 be found
surface of beta cells
what type of drugs interact with CD20
rituximab
obinutuzumab
brentuximab
what does cd20 do
proliferation
differention
how does angiogenesis occur
due to the need for blood and tumours growth they release
VEGF
FGF
transforming growth factor beta
this stimulates endothelial cell proliferation and formation of new blood vessels
How can drugs interact with VEGF
bind to VEGF itself and restrict its ability to bind
inhibit the activation of VEGF receptors