Anticancer Drugs

Question 1

What is the Log kill hypothesis.

Answer 1

Theory that cytotoxic drugs kill fixed percentage of tumor cells not a fixed number. Follow 1st order kinetics.

Question 2

What is growth fraction meaning.

Answer 2

tumors with high turn over

Question 3

Name a few cytotoxic agents that are S phase specific.

Answer 3

• cytarabine
• 6-mercaptopurine
• 6-thioguanine
• 5-FU
• methotrexate
• hydroxyurea
• irinotecan (blocks topoisomerase I)
• etoposide (blocks topoisomerase II)

Question 4

Name some cytotoxic agents that are non-cell cycle specific.

Answer 4

• alkylating agents (cyclophosphamide, cisplatin, procarbazine)
• antitumor antibiotic (doxorubicin, daunorubicin)
• nitrosoureas (lomustine, carmustine)

Question 5

What are the cytotoxic agents that inhibit the M phase of the cell cycle?

Answer 5

vinblastine
vincristine
* blocks tubular polymerization

Paclitaxel
(blocks depolymerization of microtubules)

colchicine and griseofulvin also act via this mechanism

Question 6

What are the cytotoxic agents that act by inhibiting the G2 phase of the cell cycle?

Answer 6

Bleomycin (antibiotic)

Question 7

What is the MOA of cyclophosphamide?

Answer 7

alkylating agent basically alkylates DNA by attacking guanine N7 - dysfunctional DNA

Question 8

S/E of cyclophosphamide?

Answer 8

BMS, hemorrhagic cystitis

Question 9

Antidote cyclophosphamide toxicity? How does it work?

Answer 9

mesna which traps the toxic metabolite acrolein and is protective

Question 10

Uses for cyclophosphamide?

Answer 10

really it is used for many conditions including but not limited to non hodgkin lymphoma, ovarian, breast cancer, neuroblastoma

Question 11

MOA cisplatin?

Answer 11

alkylating agent- cross-links DNA strands

Question 12

Indications for cisplatin?

Answer 12

testicular, ovarian, bladder, lung cancer

Question 13

S/E of using cisplatin?

Answer 13

nephrotoxicity; neurotoxicity (deafness)

Question 14

What drug would you use to protect the kidneys for the nephrotoxic side effects of using cisplatin?

Answer 14

amifostine

Question 15

What is the MOA procarbazine?

Answer 15

alkylating agent

Question 16

Indication procarbazine?

Answer 16

Hodgkin

Question 17

S/E of procarbazine?

Answer 17

BMS, leukemogenic

Question 18

MOA Doxorubicin?

Answer 18

Intercalator (meaning it can insert mini grooves in DNA and cause DNA strand breaks), forms free radicals, inhibits topoisomerase

Question 19

Indications Doxorubicin?

Answer 19

Hodgkin, breast, endometrial, lung, and ovarian cancers

Question 20

S/E doxorubicin?

Answer 20

BMS - delayed CHF

Question 21

Antidote to cardio toxicity caused by doxorubicin?

Answer 21

dexrazoxane which is an iron-chelating agent that prevents the formation of free radicals; it is not a free radical “trapper”

Question 22

Methotrexate MOA?

Answer 22

antimetabolite- inhibits DHF reductase (S phase)

Question 23

Indications for methotrexate?

Answer 23

leukemias, lymphomas, breast cancer; rheumatoid arthritis, psoriasis

Question 24

S/E methotrexate use?

Answer 24

BMS

Question 25

Antidote for methotrexate?

Answer 25

folinic acid (leucovorin rescue)

Question 26

What is the S/E of 5-FU?

Answer 26

BMS

Question 27

MOA Capecitabine?

Answer 27

pyrimidine antimetabolite (S phase) bio activated to inhibit thymidilate synthetase

Question 28

S/E capecitabine?

Answer 28

BMS

Question 29

Indications capecitabine?

Answer 29

breast, ovarian, head and neck cancer, topical for basal cell cancer and keratoses; colorectal cancer

Question 30

6-mercaptopurine MOA.

Answer 30

purine antimetabolite bio activated by HGPR transferase.

Question 31

Indications for 6-mercaptorpurine.

Answer 31

acute lymphocytic leukemia; immunosuppression

Question 32

S/E 6 mercaptopurine.

Answer 32

BMS

Question 33

Bleomycin MOA?

Answer 33

complexes with Fe and O2 > DNA strand scission

Question 34

Indications bleomycin?

Answer 34

Hodgkin, testicular, head, neck, skin cancer

Question 35

S/E bleomycin

Answer 35

pneumonitis, pulmonary fibrosis

Question 36

VInblastine MOA.

Answer 36

dec micro tubular polymerization (spindle poison)

Question 37

Vincristine MOA.

Answer 37

dec micro tubular polymerization (spindle poison)

Question 38

Indication vinblastine.

Answer 38

Hodgkin, testicular cancer, Kaposi

Question 39

Indication Vincristine.

Answer 39

Hodkin, leukemias, Wilms

Question 40

VInblastine S/E?

Answer 40

BMS

Question 41

Vincristine S/E?

Answer 41

neurotoxicity

Question 42

MOA All-trans retinoid acid (ATRA)

Answer 42

differentiating agent, promotes differentiation of promyelocytes

Question 43

Indication for ATRA?

Answer 43

acute myelogenous leukemia (AML) M3

Question 44

S/E of ATRA?

Answer 44

differentiation syndrome with respiratory distress, pleural and pericardial effusions, CNS symptoms

Question 45

Target of Imatinib

Answer 45

BCR-ABL (treats CML, GI stromal tumors GIST)

Question 46

Cetuximab target?

Answer 46

ErbB1 (head and neck and colon cancer)

Question 47

Trastuzumab target?

Answer 47

ErbB2 (HER2/neu) (breast cancer)

Question 48

Bevacizumab target?

Answer 48

VEGF-A

Question 49

Sorafenib target?

Answer 49

RAF kinase

Question 50

What are the more marrow sparing cytotoxic medications?

Answer 50

cisplatin, bleomycin, vincristine

Question 51

Popular nephrotoxic medications cytotoxic?

Answer 51

cisplatin, methotrexate

Question 52

Popular cytotoxic medications implicated in pulmonary toxicity?

Answer 52

bleomycin, busulfan, procarbazine

Question 53

Popular cardiotoxic cytotoxic meds?

Answer 53

Doxorubicin, daunorubicin

Question 54

Popular neurotoxic cytotoxic meds?

Answer 54

Vincristine, cisplatin

Question 55

Popular immunosuppressive cytotoxic meds?

Answer 55

cyclophosphamide, methotrexate

Question 56

What asparaginase causes what notable side effect?

Answer 56

pancreatitis

Question 57

CSF, erythropoietin and thrombopoietin therapy can be supportive in care for cancer in what way?

Answer 57

helps to reduce infections and need for antibiotics

Question 58

Aldesleukin MOA

Answer 58

IL-2 analog; inc. lymphocyte differential and inc. NKs

Question 59

Indication aldesleukin?

Answer 59

used in renal cell cancer and metastatic melanoma

Question 60

Interleukin 11 indications.

Answer 60

inc. platelet formation used in thrombocytopenia

Question 61

Filgrastim MOA

Answer 61

G-CSF inc. granulocytes

Question 62

Filgrastim indications?

Answer 62

marrow recovery

Question 63

Sargramostim indications.

Answer 63

inc. granulocytes and macrophages - used for marrow recovery

Question 64

MOA Sargramostim?

Answer 64

GM-CSF

Question 65

Erythropoeitin indications.

Answer 65

anemia, especially associated with renal failure

Question 66

Thrombopoietin indications.

Answer 66

thrombocytopenia