Anti cancer Drugs 3

Question 1

Fulvestrant is an SERD (selective estrogen receptor downregulators). What is its mechanism

Answer 1

Binds to ER and inhibits its dimeriztain and increases its degradation

Question 2

The only source of estrogen in post menopausal women is from the ocversoin of _________ to _______ by _________

Answer 2

Androstenedione; estrone; aromatase

Question 3

Aromatase inhibitors are the used for ________

Answer 3

Adjuvant therapy for post menopausal women with hormone receptor positive breast cancer

Question 4

Nonsteroidal aromatose inhibitors

Answer 4

Anastrozole and letrozole Reversible competitive inhibitor of aromatase

Question 5

Steroidal aromatase inhibitors

Answer 5

Exemestane Irreversible inhibitor of aromatase

Question 6

Examples of GnRH agonists and what do they do?

Answer 6

goserelin and leuprolide They cause an initial surge in LH and FSH followed by an inhibition of gonadotropin release

Question 7

To prevent the intital increase of testosterone when administering GnRH agonsts, give _______

Answer 7

Flutamide

Question 8

Mechanism of flutamide

Answer 8

It is a non steroidal anitandrogen that is a competitive antagonist at the androgen receptor

Question 9

Mechanism of imatinib

Answer 9

Inhibitor fo tyrosine kinase of Bcr-Abl

Question 10

Mechanism of Trastuzumab

Answer 10

Monoclonal antibody against ErB2

Question 11

Mechanism of asparaginase

Answer 11

It hydrolyzes serum asparagine and thus depriving the tumor cells of the asparagine that is necessary for protein synthesis (Neoplastic tissues require exogenous source of asparagine)

Question 12

Adverse effects of asparaginase

Answer 12

HS, ↓ in clotting factors (but paradoxically have more thrombotic events), liver abnormalities, pancreatitis (asparaginase can activate enzymes while they are in the pancreas), and seizures and coma due to ammonia toxicity

Question 13

Hydroxyurea inhibits ______ causing …

Answer 13

Ribonucleotide reductase; depletion of deoxynucleoside triphasophate pools and thus arresting DNA synthesis /

Question 14

Hydroxyurea kills cells in the ____ phase

Answer 14

S

Question 15

Interferon α is used to treat:

Answer 15

• hairy cell leukemia - CML - malignant melanoma - kaposi sarcoma

Question 16

Mechanism of interferon α

Answer 16

• increase the expression of HLA molecules on tumor cells so they can be destroyed - activates NK cells to destroy tumor cells

Question 17

Mechanism of vinca alkaloids

Answer 17

Binds to β tubulin and hinhits it’s ability polymerize to microtubules and cells arrest in metaphase and die by apoptosis

Question 18

Adverse effects of vincristine

Answer 18

Peripheral neuropathy with MILD bone marrow depression

Question 19

Adverse effects of vinblastine

Answer 19

Myelosuppresion is the dose limiting diverse effects and other adverse effects include alopecia and peripheral neuropathy

Question 20

What is the difference in adverse effects between vincristine and vinblastine?

Answer 20

Vincristine has mild bone marrow suppression while that is the dose limiting adverse effect for vinblastine Vincristine has much worse peripheral neuropathy

Question 21

Mechanism of taxaxes (paclitaxel and docetaxel)

Answer 21

Bind to β tubules but they allow for the polymerization of microtubules but PREVENTS DEPOLYMERIZATION

Question 22

What is the difference between the mechanism of vinca alkaloids and taxanes?

Answer 22

Vinca alkaloids do not allow for the polymerization of the microtubules while taxanes do but with taxanes no depolymerization

Question 23

Adverse effects of paclitaxel

Answer 23

HS, myelosuppresoin, peripheral neuropathy and alopecia

Question 24

Adverse effects of docetaxel

Answer 24

Peripheral neuropathy is not as bad as in paclitaxel

Question 25

\_\_\_\_\_\_\_\_\_ is required to prevent fluid retention when taking docetaxel

Answer 25

Dexamethasone

Question 26

\_\_\_\_\_\_\_\_\_\_ is dose limiting in docetaxel

Answer 26

Myelosuppresion

Question 27

Etoposide inhibits _____________ and blocks the cell at \_\_\_\_\_\_\_

Answer 27

Topoisomerase II (breaks DNA on BOTH strands) S-G2 phase

Question 28

Campothecins inhibits \_\_\_\_\_\_\_\_\_\_\_\_\_

Answer 28

Topoisomerase I

Question 29

Prednisone is used for ___________ and what is its mechanism

Answer 29

Acute leukemia and malignant lymphomas Prednisone is a glucocorticoid and they are lymphocytic and suppress mitosis in lymphocytes

Question 30

Selective estrogen receptor modulators act as agonists on _______ and as antagonists on \_\_\_\_\_\_\_\_

Answer 30

Bone, endometrium; breast

Question 31

Tamoxifen is an _________ on breast cancer and is used for ____________ breast cancer

Answer 31

Antagonist; receptor positive

Question 32

Raloxifene is a SERM that acts as an ___________ on the bone to inhibit \_\_\_\_\_\_\_\_

Answer 32

Agonist; resorption

Question 33

\_\_\_\_\_\_\_\_\_ is a SERM that does not have risk for endometrial cancer when using it

Answer 33

Raloxifene

Question 34

What are some uses for raloxifene?

Answer 34

Prevention of post menopausal osteoporosis and prophylaxis of breast cancer in high risk post menopausal women