Targeted Therapies- Antineoplastic Flashcards
How do BCR-ABL inhibitors work?
Block TK, which blocks the downstream pathway that leads to cell proliferation
What does a Philadelphia Chromosome translocation lead to?
An expression of BCR and ABL, leading to unctrollable cell proliferation
What cancer is the Philadelphia chromosome closely related to?
Chronic myeloid leukemia
What are the BCR-ABL tyrosine kinase inhibitors?
Imatinib, Dasatinib, nilotinib
What it unique about dasatinibs ability compared to others in its class?
It can inhibit many TKs, but it can overcome Imatanib resistance
Which has higher binding affinity to Abl, Nilotinib or Imatinib?
Nilotinib
What are the Multi kinase RTKs Inhibitors?
Sunitinib, sorafenib, pazopanib
What do the Muli kinase RTKs inhibitors do?
Inhibit multiple receptor kinasases
What is the action of epidermal growth factor receptors?
Leads to cell proliferation, invasion, metastasis, and angiogenesis
This is overexpressed in several solid tumors
What is the murine percent of Mouse (omab)?
Chimeric (Ximab)?
Humanize (zumab)?
Human (umab)? Human
100%
33%
10%
100%
What is cetuximabs MOA?
chimeric mAb directed against extracellular EGFR domain
What can we know by looking at cetuximabs name?
xi, so highest murine content, so definitely hypersensitivity problems
What is critical to know about cetuximabs administration?
Should not be given with radiation of head/neck, can cause sudden death
What is panitumumabs MOA?
Fully humanized EGFR inhibitor
What is erlotinib and Lapatinibs MOA?
Inhibits INTRAcellular tyrosine kinase domain on EGFR
How is erlotinib and Lapatinib metabolized?
CYP3A4