Flashcards in clinical: Targeted therapies Deck (14)
Target therapies can be Mabs or Ibs. What are each?
Mabs are monoclonal antibodies
Ibs are signal transduction inhibitors
Myeleproliferative disorders tend to have a mutation that cause what?
Constitutively active tyrosine kinase receptor
Pathophysiology of CML: fusion of what two regions of which chromosomes renders the tyrosine kinase constitutively active
Break point cluster region (BCR) and Ableson Oncogene product (Abl)
What is a proteosome?
Enzyme complexes present in both healthy and cancerous cells. Proteasomes degrade intracellular proteins in a regulated manner
Imatinib is a signal transduction inhibitor that binds where?
Binds the ATP binding domain of the Abl kinase preventing substrate phosphorylation and signaling preventing downstream signaling
MOA of Ruxolitinib and indicated for tx of what disease that causes erythrocytosis
Block cytokine signaling and amplified cytokine and growth factor expression, effectively a JAK2 inhibitor and used for tx of Polycythemia Vera
MOA of Ibrutinib and indicated for tx of what disease that causes high levels of IgM in the blood leading to hyperviscosity and is associated with lymphoplasmacytic lymphoma
BTK inhibitor in b-cell receptor signaling used to treat Waldenstrom macroglobulinemia
CYP3A4 (lots of drug drug interactions) and can also be used for mantle cell lymphoma
Idelalisib inhibits what part of the BCR cascade?
P13K 2nd messenger used for tx of CLL or relapsed follicular B cell non-hodgkins lymphoma of FL/relapsed SLL
bortezomib is a _______inhibitor
26s proteosome inhibitor
the Abl ATP biniding domain mutates and can become resistant to imatinib. What other treatments are there if this happens in a pt with CML?
Dasatinib or Nilotinib
Imatinib adverse effects
What are some potentially fatal adverse effects of idelalisib (P13K inhibitor that treats relapses CLL/SLL, Relapsed follicular B-Cell NHL)
Idelalisib can have many drug drug interactions because
it's a CYP3A4 inhibitor