Molecular Targeted Agents

Question 1

Imatinib MOA (inhibits 3 things) “Gleevac”

Answer 1

1. Inhibits the constitutively active fusion produce BCR-ABL arising from the PHILADELPHIA CHROMOSOME of CML
2. Inhibits c-kit (TKR), overexpressed in GISTs
3. Inhibits PDGFR

Question 2

Name the two EGFR TKIs

Answer 2

Erlotinib (Tarceva) and Gefitinib (Iressa)

Question 3

MOA Bortezomib

Answer 3

Reversible proteasome inhibitor (which is involved in degradation and recycling of cellular proteins)

Question 4

MOA Tipifarnib (Zarnestra)

Answer 4

Oral farnesyltransferase inhibitor which inhibits signaling from the RAS ONCOGENE