Kinase Inhibitors

Question 1

Name the Kinase Inhibitors

(“Broken nib”)

Answer 1

Imatinib
(“Imitating”)

Erlotinib
(“Earl Geoffrey”)

Sunitinib
(“Rising sun”)

Sorafenib
(“Soaring eagle”)

Vemurafenib
(“Venom”)

Question 2

Imatinib
(“Imitating”)

MOA

Answer 2

tyrosine kinase inhibitor
(“Inhibited tire swing”)

• imatinib blocks the tyrosine kinase domain of the BCR/ABL fusion protein →in CML
  (“BREAKABLE”)
• ​imatinib blocks the c-kit tyrosine kinase →in GIST (“Congress kit”)

Question 3

Imatinib can be used to treat

Answer 3

-treat a variety of hematologic and solid malignancies

• chronic myeloid leukemia -CML (increased levels of mature granulocytes – eosinophils, neutrophils, basophils [[BCR/ABL]]
  (“Copious pink, white, and blue granules”)
• ​gastrointestinal stromal tumors (GIST) [[c-kit]]
  (“Crab buttons on belly”)

(“Cracked crab”)

Question 4

Imatinib Side Effects

Answer 4

can cause fluid retention→ ankle and periorbital edema

(“Baggy pantaloons”)

Question 5

Erlotinib MOA

(“British Earl”)

Answer 5

Blocks the epidermal growth factor receptor (EGFR) tyrosine kinase

(“Earl Geoffrey”)

Question 6

Erlotinib

(“British Earl”)

Answer 6

treats solid tumors with EGFR overexpression

• e.g. non-small cell lung cancer – NSCLC
  (“Big lapel with crab badge”)

Question 7

Erlotinib Side Effects

Answer 7

can cause a papulopustular acneiform rash
(“Spotty rash”)

can cause diarrhea
(“Muddy pantaloons”)

Question 8

Sunitinib/Sorafenib

MOA

(“Rising sun”)
(“Soaring eagle”)

Answer 8

inhibits the vascular endothelial growth factor receptor →VEGFR tyrosine kinase

(“Inhibiting vegetables”)

Question 9

Sunitinib and Sorafenib can treat…

Answer 9

cancer with VEGFR overexpression

• e.g. renal cell carcinoma
  (“Flank crab buckles”)

Question 10

sunitinib and sorafenib
Side effects

Answer 10

can cause hyperkeratosis and skin rashes

VEGF-targeted therapies are associated with an increased risk of hemorrhage
(“Bleeding wound”)

(“Callused and sunburned”)

Question 11

Vemurafenib MOA

(“Venom”)

Answer 11

-blocks B-Raf kinase

(“B. Fra”)

Question 12

Vemurafenib can treat…

Answer 12

vemurafenib treats V600E BRAF positive malignant melanoma

(“Disseminated ink”)