Lecture 2.5 - Targeted Cancer Drugs

Question 1

tyrosine kinase inhibitors all end in “ -____”

Answer 1

tinib

Question 2

_____ is a tyrosine kinase inhibitor of BCR-ABL (as in ____) and also ____ (common in GI stromal tumors)

Answer 2

imatinib;
CML;
c-kit

Question 3

main side effect of imatinib:

Answer 3

fluid retention

Question 4

sirolimus/rapamycin bind to ____ and inhibit _____, which is a protein kinase of the PI3K pathway

Answer 4

FKBP, mTOR

Question 5

main toxicity of sirolimus/rapamycin to watch out for?

notably, they are not ___toxic

Answer 5

pancytopenia;

nephro

Question 6

bortezomib and carfilzomib both inhibit _____, inducing arrest at the ____ phase and causing apoptosis

Answer 6

proteosomes;

G2-m

Question 7

bortezomib and carfilzomib are used to treat ____ and mantle cell lymphoma; side effects include _____ and _____ reactivation

Answer 7

multiple myeloma;

peripheral neuropathy, herpes zoster

Question 8

_____ is a monoclonal antibody against HER-2, which is a _____ receptor

Answer 8

trastuzumab, tyrosine kinase (c-ERB2)

Question 9

2 ways that trastuzumab kills cancer cells

Answer 9

inhibts HER2 initiated cell signalling;

antibody dependent cytotoxicity

Question 10

according to FA, herceptin can treat HER2 positive breast and ____ cancer. main side effect?

Answer 10

gastric;

cardiotoxicity

Question 11

_____ is a monoclonal AB against EGFR that is used to treat stage IV _____ cancer and also head and neck cancer

Answer 11

cetuximab;

colon

Question 12

bevacizumab is an antibody against _____ and it inhibits ______

Answer 12

VEGF, angiogenesis

Question 13

bevacuzumab is used to treat solid tumors as well as ______;

side effects include _____ and ______

Answer 13

wet macular degeneration;

hemorrhage/bleeding;
GI perforation

Question 14

sorafenib and sunitinib are _____ inhibitors that inhibit _____

Answer 14

VEGFR, angiogenesis

Question 15

vismodegib is a inhibitor the ______ ______ signalling pathway. can be used to treat advanced ______ _____ carcinoma

Answer 15

sonic hedgehog;

basal cell

Question 16

______ is a GnRH analog. it is an antagonist when used in _____ Fashion. used for ____ cancer

Answer 16

leuprolide;
continuous;
prostate

Question 17

main side effect of leuprolide

Answer 17

vasodilation;

also weakness

Question 18

flutamide is a ______ inhibitor at _____ receptors. used to treat advanced ______

Answer 18

competitive, androgen;

prostate cancer

Question 19

DES is a _____ agonist. it is indicated to treat _____ cancer. increased risk of _____ cancer to females exposed in utero

Answer 19

estrogen;
prostate;
vaginal adenocarcinoma

Question 20

______ is an estrogen antagonist at the breast and an agonist at the bone and uterus. thus, increased risk of _____ cancer

Answer 20

tamoxifen;

endometrial

Question 21

raloxifen is an estrogen antagonist at the ____ and _____ and is an agonist at the _____

Answer 21

breast, uterus;

bone

Question 22

both tamoxifen and raloxifen have increased risk of ______

Answer 22

thromboembolism

Question 23

anastrolze, letrozole, and exemestane are _____ inhibitors. used to treat _____ breast cancer in ___menopausal women

Answer 23

aromatase;
ER+;
post

Question 24

_____ is an estrogen receptor down regulator that is used to treat resistant ER+ breast cancer.

Answer 24

fulvestrant

Question 25

histone deacetylase (HDAC) inhibitors _____ gene expression. used primarily to treat ____ T-cell lymphoma and various heme cancer

Answer 25

increase;

cutaneous

Question 26

_____ is a Poly(ADP-ribose) polymerase (PARP) inhibitor. used to treat BRCA mutated _____ cancer

Answer 26

olaparib;

ovarian