drugs Flashcards
Monoclonal antibody against CD20 B cells
Rituximab
Rituximab
Monoclonal antibody against CD20 B cells
Area of antibody that binds to CD20
fc region
type of toxicity displayed by rituximab
Antibody dependant cellular cytotoxicity
action of CD20
Cell cycle initiation
Ca channel
condition rituximab used in
NHL
mechanism of resistance to retuximab
downregulation of cd20- resistant clones
Poor antibody dependant cellular cytotoxicity as fc region is neutralised
mutation od CD20 c terminal by epigenetic methylation
vemurafinib mechanism of action
BRAF V600E inhibitor
serine threonine kinase inhibitor
SE of vemurafanib
QT elongation
tumouor promotion in BRAF WT
% of melanomas with V600E mutation
40-60%
what is the V600E mutation
valine for glycine at codon 600 in exon 15
resistance to vemurafaib
Loss of PTEN allows PI3K pathway
10-35% of melanomas
-LOH, methylation or deletion mutations
Herceptin mechanism
monoclonal AB against HER-2 human oestrogen receptor-2
overexpression of HER2
non trade name for herceptin
trastuzumab
resistence to HER2
Downstream mutation
-Tyrosine kinase inhibitors can overcome
obsticles for binding- truncated HER2 mutation resultsin constitutively active receptor
PTEN mutation in 50%- upregulation of PI3K
Ivacaftor used in…
used in cf
ivacaftor MOA
potentiator of CFTR, meaning it increases the length of time channels are open, allowing Chlorie ion to pass through the pore
How many CFTR mutation classes recognised?
6
G551D CF mutation
CFTR gets to the membrane, but chnnel regulation is defective, with decreased channel conductance
mutaion ivacaftor targets
G551D
how many cf patients will benefit from ivaaftor
4%
alternative to ivacaftor for CF patients
Lumacaftor
machanism of action of Lumacaftor
Acts as a chaperone during protein folding, increasing number of CFTR receptors are on the cell surface