Anti-Tumor agents

Question 1

EX of alkylating agent

Answer 1

Cyclophosphamide

Question 2

Cells with ____ are resistant to cyclophosphamide

Answer 2

High ALDH

*** hematopoietic and intestinal cells have high levels so this drug has low toxicity compare to other alkylating agents

Question 3

Resistance to alkylating agents (3)

Answer 3

• High levels of GSH
• removal of alkyl group
• cross link repair

Question 4

Toxicity of alkylating agents (5)

Answer 4

• hematopoietic
• GI
• Gonadal
• Alopecia
• Carcinogenesis

Question 5

Cisplatin and analogues

Answer 5

Crosslink DNA

Question 6

Pt compounds resistance (5)

Answer 6

• Reduced accumulation
• inactivation
• increased DNA repar
• Increased tolerance for DNA damage

Question 7

Cisplatin toxixity

Answer 7

nephrotoxivity

Question 8

carboplatin toxicity

Answer 8

myelosupression

platelet toxicity

Question 9

oxaliplatin toxicity

Answer 9

sensory neuropathy

Question 10

2 EX of antimetabolites

Answer 10

1. Methotrexate

2. 5- fluorouracil

Question 11

Methotrexate is a ___, ___ inhibitor of ___

Answer 11

reversible, competitive

dihydro folate reductase (DHFR)

Question 12

MTX is metabolized to

Answer 12

polyglutamated MTX

Question 13

MTX resistance (3)

Answer 13

• decreased capacity to make polyglutamated MTX
• Increased expression of DHFR
• Mutant DHFR

Question 14

DHFR is required for _____ synthesis

Answer 14

purine

Question 15

5_flurouracil is a ___ analog

Answer 15

pyrimadine

Question 16

5-FU resistance (2)

Answer 16

• alterations in target enzyme (TS, causes dTTP depletion)

- Increased levels of TS

Question 17

5-FU toxicity

Answer 17

• hematological
• GI
• alopecia
• derm problems

Question 18

Topoisomerase inhibitors are derived from

Answer 18

natural products

Question 19

Topoisomerase inhibitors inhibit

Answer 19

DNA relegation to leave DNA breakes

Question 20

camptothecins

Answer 20

Topo I and II inhibitors

Question 21

Anthracyclines

Answer 21

Topo II inhibitors (doxorubicin)

Question 22

Topoisomerase inhibitors resistance (2)

Answer 22

• increased drug efflux

- mutations in toposiomerases

Question 23

Topo drugs toxicity

Answer 23

• myelosupression

- secondary malignancies

Question 24

anthracyclins toxicity

Answer 24

cardiotoxicity

Question 25

2 antimicrotubule agents

Answer 25

1. Vinca alkaloids | 2. Taxanes

Question 26

Vinca alkaloids ____ microtubules

Answer 26

stabilize

Question 27

Taxanes ___ microtubules

Answer 27

de stabilize

Question 28

Vinca alkaloids resistance (2)

Answer 28

- increased drug efflux | - mutations is tubulin that alter binding

Question 29

Vinka alkaloids toxicity (2)

Answer 29

- NEUROTOXICITY | - myelosuppression

Question 30

Taxanes resistance (3)

Answer 30

- drug efflux - mutations in tubulin - inhibition of apoptosis

Question 31

Taxanes toxicity (3)

Answer 31

- myelosuppresion - peripheral neuropathy - alopecia

Question 32

Tamoxifen

Answer 32

ER inhibitor

Question 33

antiandrogens (2 examples) and action

Answer 33

- bicalutamide, flutamide | bind to AR and inhibit function as tf

Question 34

Steroid receptor resistance

Answer 34

- activate recptor by other mechanisms | - mutations in receptor cause drug binding to activate rather than inactivate

Question 35

mutations in receptor in response to flutamide

Answer 35

- activate rather than inhibit

Question 36

Aromatase inhibitor (1 EX) and action

Answer 36

Letrozole | inhibit synthesis of estrogen from androgens

Question 37

Gonadotropin-releasing hormone analogues

Answer 37

leuprolide | Inhibit testosterone production

Question 38

Hormonal agents toxicities

Answer 38

- altered steroid function

Question 39

Rituximab

Answer 39

Anti CD20 used to treat B cell tumors - dependent on different stages

Question 40

Trastuzumab/ Herceptin

Answer 40

Anti- Her2 breast cancer

Question 41

Bevacizumab/ Avastin

Answer 41

anti-VEGF colon cancer

Question 42

Antibody function against cancer (2)

Answer 42

- inhibit function of target | - cell mediated toxicity

Question 43

Poster child for kinase inhibitors

Answer 43

Imatinib/Glebevec

Question 44

Imatinib treats

Answer 44

CML and GIST | Bcr-ABL translocation

Question 45

Resistance to imatinib

Answer 45

inhibitor insensitive BCR-ABL alleles (alter drug binding)