Antitumoral Flashcards
Toceranib (Palladia) is
tyrosine kinase inhibitor
For what is toceranib used
to treat Patnaik grade II or III, recurrent, cutaneous mast cell tumors with or without regional lymph node involvement…
Most common AE with toceranib
-diarrhoea
- loss of appetite, weight loss
-lameness,
- hematochezia
Nasal depigmentation
Can toceranib be used in cats ?
yes
What receptors does toceranib inhibit?
-RTK (receptor tyrosine kinase) called c-KIT
-VEGFR2 and PDGFR-beta
MOA of toceranib
Tyrosine kinase inhibitors competitively inhibits ATP binding in target RTKs (receptors)
Blocks TK from transferring a phosphate group from ATP to proteins (ie prevents receptor phosphorylation)
Prevents downstream signal transduction and results in cell cycle arrest and tumour apoptosis
The c-KIT gene (proto-oncogene) in mast cells encodes the c-KIT receptor (tyrosine kinase receptor) for _______ cell factor (SCF).
stem
A gain of function mutation in the c-KIT gene results in constitutive ________ of the c-KIT receptor even in the absence of SCF binding.
activation
The most common type of mutation is an internal tandem duplication (ITD) in exons 8 or ___ of the c-KIT gene.
11
Mast cell tumours with c-KIT mutations tend to have a ________ prognosis and shorter survival time than those with wild-type c-KIT.
poorer
Ki-67 and c-KIT are both immunohistochemical markers which help to determine the ______ in dogs with MCTs.
prognosis