Anticancer drugs Kaplan

Question 1

What are the non-cell cycle specific cancer drugs?

Answer 1

• Alkyalting agents (cyclophosphamide, cisplatin, and procarbazine)
• Antitumor Abx (doxorubicin, daunorubicin)
• Nitrosureas (lomustine, carmustine)

Question 2

What are the S phase specific cancer drugs?

Answer 2

• Hydroxyurea
• Methotrexate
• Irinotecan
• Cytarabine
• Etoposide
• 6-mercaptopurine
• 6-thioguanine
• 5-fluorouracil

Question 3

What is the G2 phase specific cancer drug?

Answer 3

Bleomycin

Question 4

What are the M phase specific cancer drugs?

Answer 4

• Vinblastine
• Vincristine
• Paclitaxel

Question 5

What is the specific MOA of cyclophosphamide?

Answer 5

-Alkylating agent-attacks guanine N7-dysfunctional DNA

Question 6

What are the side effects of cyclophosphamide?

Answer 6

• Bone marrow suppression

- Hemorrhagic cystitis

Question 7

What is used to treat the hemorrhagic cystitis caused by cyclophosphamide and what is its MOA?

Answer 7

Mesna-traps acrolein and is protective

Question 8

What is the specific MOA of doxorubicin?

Answer 8

• Intercalator -> forms free radicals

- Inhibits topoisomerase

Question 9

What are the side effects of doxorubicin?

Answer 9

• Bone marrow suppression

- Delayed CHF (heart damage is caused by the free radicals)

Question 10

What is used to prevent the free radicals formed by doxorubicin?

Answer 10

Dexrazoxane-iron chelating agent that prevents the formation of free radicals

Question 11

What is the specific MOA of methotrexate?

Answer 11

-Antimetabolite-inhibits DHF reductase (S phase)

Question 12

What is the main side effect of methotrexate?

Answer 12

Bone marrow suppression

Question 13

What is used to prevent the toxicity of methotrexate?

Answer 13

Leucovorin (folinic acid) rescue

Question 14

What is the specific MOA of 5-fluorouracil/capecitabine (oral form)?

Answer 14

Pyrimidine antimetabolite (S phase) bioactivated to inhibit thymidylate synthetase

Question 15

What is the specific MOA of bleomycin?

Answer 15

Complexes with Fe and oxygen -> DNA strand scission (G2 phase)

Question 16

What are the main side effects of bleomycin?

Answer 16

Pulmonary fibrosis and pneumonitis

Question 17

What is the specific MOA of vincristine/vinblastine?

Answer 17

Inhibition of microtubular polymerization - spindle poisons (M phase)

Question 18

What is the main side effect of vincristine?

Answer 18

Neurotoxicity

Question 19

What is the specific MOA of all-trans retinoic acid?

Answer 19

-Differentiating agent, promotes differentiation of promyelocytes

Question 20

All-trans retinoic acid is used to treat what specific cancer?

Answer 20

Acute myelogenous leukemia (AML), M3

Question 21

What are the main side effects of all-trans retinoic acid?

Answer 21

“Differentiation syndrome”-with respiratory distress, pleural and pericardial effusions, CNS symptoms

Question 22

Explain the what causes the “thymineless death of fungal cells and neoplastic cells” and which agents are used for each

Answer 22

Flucytosine (FC) and 5-fluorouracil (5-FU) are bioactivated to 5-FdUMP which inhibits thymidylate synthetase -> thymineless death

• FC is used for fungal cells
• 5-FU is used for neoplastic cells

Question 23

What is the specific MOA of paclitaxel?

Answer 23

Blocks depolymerization of microtubules

Question 24

What is the specific MOA of irinotecan?

Answer 24

Blocks topoisomerase 1

Question 25

What is the specific MOA of etoposide?

Answer 25

Blocks topoisomerase 2

Question 26

What is the target of imatinib?

Answer 26

BCR-ABL

Question 27

Imatinib is used in the treatment of what specific cancer?

Answer 27

CML

Question 28

What is the target of cetuximab?

Answer 28

ErbB1

Question 29

Cetuximab is used in the treatment of what specific cancers?

Answer 29

Cancers of the head, neck, and colon

Question 30

What is the target of trastuzumab?

Answer 30

ErbB2 (HER2/neu) (EGFR inhibitor)

Question 31

Trastuzumab is used in treatment of what specific cancer?

Answer 31

Breast cancer

Question 32

What is the target of bevacizumab?

Answer 32

VEGF-A

Question 33

What is the target of sorafenib?

Answer 33

RAF kinase

Question 34

Cisplatin is associated with toxicity of what organ?

Answer 34

Renal (nephrotoxicity)

Question 35

Bleomycin is associated with toxicity of what organ?

Answer 35

Pulmonary

Question 36

Doxorubicin is associated with toxicity of what organ?

Answer 36

Cardiac

Question 37

Vincristine is associated with toxicity of what organ?

Answer 37

Neurologic

Question 38

Cyclophosphamide is associated with toxicity of what organ?

Answer 38

Bladder (hemorrhagic cystitis)

Question 39

Name the bone marrow "sparing" cancer drugs

Answer 39

- Vincristine - Cisplatin - Asparaginase - Bleomycin

Question 40

What type of cancer drugs are more effective against tumors with high growth fractions (leukemias/lymphomas)?

Answer 40

Cell cycle specific drugs

Question 41

Non-cell cycle specific drugs are effective against?

Answer 41

Tumors with high or low growth fractions

Question 42

What is the antidote used to prevent the nephrotoxicity caused by cisplatin?

Answer 42

Amifostine

Question 43

What is aldesleukin?

Answer 43

- IL-2 | - Increases lymphocyte differentiation and NKs

Question 44

What does IL-11 do?

Answer 44

Increases platelet formation

Question 45

What is filgrastim?

Answer 45

- G-CSF | - Increases granulocytes

Question 46

What is sargramostim?

Answer 46

- GM-CSF | - Increases granulocytes and macrophages

Question 47

What is the log-kill hypothesis?

Answer 47

The cytotoxic actions of anticancer drugs follow first order kinetics - kill a fixed PERCENTAGE of cancer cells