Fitz - Targeted Therapy & Biologicals

Question 1

occupies the ATP cofactor binding site on Bcr-Ab causing inhibition of phosphate transfer to tyrosine kinase

Answer 1

imatinib

Question 2

resistance to imatinib

Answer 2

mutation in ATP binding pocket

Question 3

can overcome imatibib resistance

Answer 3

dasatinib

Question 4

tx: imatinib

Answer 4

CML, GIST

Question 5

tx: basatinib

Answer 5

CML, ALL

Question 6

receptors specific for GIST

Answer 6

c-kit, PDFR (membrane)

Question 7

tx of imatinib-resistant GIST

Answer 7

sunitinib

Question 8

membrane ass’d RTK inhibitors

Answer 8

• gefitinib
• erlotinib
• lapatinib
• sunitinib
• sorafenib

Question 9

RTK overexpression seen 25% of breast cancers

Answer 9

HER2

Question 10

drugs that inhibit EGFR

Answer 10

• gefitinib
• erlotinib
• lapatinib

Question 11

drugs that inhibit HER2

Answer 11

lapatinib

Question 12

drugs that inhibit PDFR and VEGFR

Answer 12

• sunitinib

- sorafenib

Question 13

tx: gefitinib, erlotinib

Answer 13

NSCLC

Question 14

tx: sunitinib

Answer 14

• GIST

- RCC

Question 15

tx: sorafenib

Answer 15

RCC

HCC

Question 16

tx: lapatinib

Answer 16

breast cancer

Question 17

inhibits mutant BRAF V600E

Answer 17

vemurafinib

Question 18

antibodies that target EGFR

Answer 18

• cetuximab

- panitumab

Question 19

antibodies that target HER2R

Answer 19

trastuzumab

Question 20

antibodies that target VEGF ligand

Answer 20

bevacizumab

Question 21

tx: cetuximab

Answer 21

colorectal, H/N cancer (not KRAS mutants)

Question 22

tx: panitumumab

Answer 22

colorectal ca (not KRAS mutants)

Question 23

tx: bevacizumab

Answer 23

advanced solid tumors - RCC, colon, lung brain ca

Question 24

tx: trastuzumab

Answer 24

HER2+ breast ca

Question 25

target for rituxomab

Answer 25

CD20+ - B cell lymphomas