Cancer Chemotherapy

Question 1

Alkylating agents

Answer 1

Cyclophosphamide, cisplatin, Procarbazine, Dacarbazine, Busulfan, Carmustine

Question 2

Antimetabolites

Answer 2

5-fluorouracil, methotrexate

gemcitabine, 6-mercaptopurine, cytarabine

Question 3

Natural products

Answer 3

Etoposide, paclitaxel, vincristine, Vinblastine

Question 4

Antitumor antibiotics

Answer 4

Bleomycine, doxorubicin, mitomycin, actinomycin D,

Question 5

Miscellaneous

Answer 5

Imatinib, cetuximab

Question 6

Hormonal

Answer 6

Prednisone, tamoxifen

Question 7

Log-kill hypothesis

Answer 7

anticancer drugs kill a fixed proportion of a tumor cell population, not a fixed number of tumor cells

Question 8

Cell Cycle Nonspecific Drugs (CCNS)

Answer 8

G0 phase (CCNS)
Cisplatin
Antitumor antibiotics,
Nitrosureas (Lomustine, carmustine)

Question 9

Cell cycle Specific Drugs (CCS) S phase

Answer 9

S phase (66 MECH)
6-mercaptopurine, 6 thioguanine, Methotrexate
Etoposide, Cytarabine, Hydroxyurea,

Question 10

Cell cycle Specific Drugs (CCS) G2 phase

Answer 10

Bleomycine

Question 11

Cell cycle Specific Drugs (CCS) M phase

Answer 11

Vinblastine
Vincrisine
Paclitaxel

Question 12

Use of chemotherapy in patients with localized cancer before performing local therapy (surgery)

Answer 12

Neoadjuvant Chemotherapy

Question 13

Chemotherapy done after local treatment procedures such as surgery or radiation

Answer 13

Adjuvant chemotherapy

Question 14

Rescue drug for methotrexate toxicity

Answer 14

Leucoverin

Question 15

Rescue drug for cyclophosphamide toxicity

Answer 15

MESNA (mercaptoethane sulfate)

Question 16

Rescue drug for doxorubicin toxicity

Answer 16

Dexrazoxane

Question 17

Rescue drug for Cisplatin toxicity

Answer 17

Amifostine

Question 18

Class Alkylating agent
MOA: Forms DNA cross-links resulting in inhibition of DNA synthesis and function.
Uses: Non-hodgkin’s lymphoma, CLL
AE: bone marrow suppression, HEMORRHAGIC CYSTITIS

Answer 18

Cyclophosphamide

Question 19

Class Alkylating agent
MOA: Forms DNA cross-links resulting in inhibition of DNA synthesis and function.
Uses: Testicular CA, Ovarian CA, Advanced colon CA
AE: Nephrotoxicity

Answer 19

Cisplatin

Advanced colon CA (Oxaliplatin)

Question 20

Class Alkylating agent
MOA: Forms hydrogen peroxide w/c generates free radicals that cause DNA strand scission
Uses: Hodgkin’s lymphoma, Non-hodgkin’s lymphoma
AE: Leukemogenic, Disulfiram rxn, BMS

Answer 20

Procarbazine

Question 21

Class Alkylating agent
MOA: Forms hydrogen peroxide w/c generates free radicals that cause DNA strand scission
Uses: Hodgkin’s lymphoma, Non-hodgkin’s lymphoma
AE: BMS, Phototoxicity, Flu-like syndrome

Answer 21

Dacarbazine

Question 22

Class Alkylating agent
MOA: Forms DNA cross-links resulting in inhibition of DNA synthesis and function.
Uses: CML
SE: Pulmonary fibrosis, Adrenal insufficiency , Skin pigmentation
Notes: SPAREs the bone marrow

Answer 22

Busulfan

Question 23

Class Alkylating agent
MOA: Forms DNA cross-links resulting in inhibition of DNA synthesis and function.
Uses: BRAIN TUMORS, melanoma, skin CA
SE: CNS toxicity

Answer 23

Carmustine

- highly lipophilic, able to pass the BBB

Question 24

Class: Antimetabolite, DMARD
MOA: Inhibits dihydrofolate reductase. Decrease synthesis of thymidylate, AA, purine nucleotides.
Uses: ChorioCA, Primary CNS lymphoma, RA, Psoriasis, Ectopic pregnancy
SE: BMS

Answer 24

Methotrexate

Question 25

Class: Antimetabolite MOA: Inhibits de novo purine nucleotide synthesis. Activated by HGPRT. Uses Acute Leukemias (ALL, AML), CML SE: BMS, Hepatotoxicity

Answer 25

6 Mercaptopurine (purine)

Question 26

6 MP metabolism is inhibited by?

Answer 26

Allopurinol and febuxostat

Question 27

Class Antimetabolite MOA Inhibits thymidylate synthase Uses: Colorectal CA, Bladder CA, Skin CA (basal cell ca, actinic keratoses) SE: BMS

Answer 27

5 Fluorouracil (pyrimidine)

Question 28

Class Antimetabolite MOA: Inhibits DNA synthesis and repair. Inhibits ribonucleotide reductase with reduced formation of dNTPs. Uses: Acute leukemias (ALL,AML), CML in blast crisis Notes: Most specific for S phase cell cycle

Answer 28

Cytarabine (pyrimidine)

Question 29

Class Antimetabolie MOA: Inhibits DNA synthesis and repair. Inhibits ribonucleotide reductase with reduced formation of dNTPs. Uses: Pancreatic CA

Answer 29

Gemcitabine

Question 30

``` Class: Vinca Alkaloid MOA: Prevents microtubule assembly. Causes cell arrest at metaphase Use: Acute Leukemias, Lymphomas SE: Peripheral neuritis, paralytic ileus Note: Spares Bone marrow ```

Answer 30

Vinblastine

Question 31

Class: Vinca Alkaloid MOA: Prevents microtubule assembly. Causes cell arrest at metaphase Uses: Testicular CA, Kaposi's sarcoma SE: BMS

Answer 31

Vincristine

Question 32

Class: Podophyllotoxin MOA: Inhibits DNA topoisomerase II. Inhibits mitochondrial electron transport. Uses: Lung CA, Prostate CA, Hodgkin's lymphoma SE: BMS, GI irritation, Alopecia

Answer 32

Etoposide

Question 33

Class Camptothecin MOA Inhibits topoisomerase I Uses: Advance ovarian ca (2nd line), small cell lung ca Metastatic Colorectal CA

Answer 33

Topotecan: Advance ovarian ca (2nd line), small cell lung ca Irinotecan: Metastatic Colorectal CA

Question 34

Class: Taxane MOA: interferes with mitotic spindle. Prevents microtubule disassembly into tubulin monomers. Uses: Advance breast and ovarian CA

Answer 34

Paclitaxel

Question 35

SE of Paclitaxel

Answer 35

Neutropenia, thrombocytopenia, peripheral neuropathy

Question 36

SE of Docetaxel

Answer 36

Neurotoxicity, BMS

Question 37

Class: Antitumor antibiotic MOA: generates free radicals, w/c cause DNA strand breaks, Intercalates with DNA Use: Testicular CA SE: Pulmonary fibrosis Notes: Specific for G2 phase of cell cycle

Answer 37

Bleomycin

Question 38

Class: Antitumor antibiotic MOA Binds to dsDNA. Inhibits DNA-dependent RNA synthesis. CCNS Use: Melanoma, Wilm's Tumor, Rhabdomyosarcoma SE: BMS

Answer 38

Actinomycin D

Question 39

Class Tyrosine Kinase Inhibitors MOA: Inhibits tyrosine kinase activity of the protein product of bcr-abl oncogene in CML; Inhibits c-kit tyrosine kinase in GIST Use: CML, GIST SE: Fluid retention, Drug interactions

Answer 39

Imatinib

Question 40

Class Monoclonal antibody MOA: acts against breast ca cells that overexpress the HER2/neu receptor for epidermal growth factor Uses: Metastatic breast CA SE: Cardiotoxicity (CHF)

Answer 40

Trastuzumab

Question 41

Class: Monoclonal antibody MOA: inhibits binding of VEGF to VEGFR leading to inhibition of VEGF signaling. Inhibits tumor vascular permeability but enhances tumor blood flow and drug delivery Use: Metastatic Colorectal CA, Non-small cell Lung CA, Diabetes retinopathy SE: Gastrointestinal perforation

Answer 41

Bevacizumab

Question 42

Class: Monoclonal antibody MOA: Binds to surface protein in NHL cells. Induces complement mediated lysis. Direct cytotoxicity and induction of apoptosis Uses: Nonhodgkins lymphoma (low grade)

Answer 42

Rituximab

Question 43

Class Interferon MOA: Endogenous glycoproteins with antineoplastic, immunosuppressive and antiviral actions Uses: Hair cell leukemia, T-cell lymphoma SE: Neurologic dysfunction, alopecia, myalgia, depression Notes: CI include autoimmune disease, history of cardiac arrhythmias and pregnancy

Answer 43

Interferon Alpha

Question 44

Class: substrate-depleting enzyme MOA: depletes serum asparagine Uses: ALL SE Acute pancreatitis

Answer 44

Asparaginase

Question 45

``` Class Vitamin A derivative MOA: Allows DNA transcription and differentiation of immature leukemic promyelocytes into mature granulocytes (differentiation therapy) Uses: Acute promyelocytic leukemia SE: Retinoic acid syndrome Notes: Only vitamin that can cure cancer Does not directly kill cancer cells ```

Answer 45

All trans retinoic acid

Question 46

Retinoic Acid Syndrome

Answer 46

Dyspnea, fever, wt gain, peripheral edema

Question 47

DOC Retinoic Acid Syndrome

Answer 47

Dexamethasone

Question 48

MOA: suppresses inflammation and immune response. May trigger apoptosis and work on nondividing cancer cells Use: CLL, Hodgkin's lymphomas SE: adrenal suppression, growth inhibition, muscle wasting

Answer 48

Prednisone

Question 49

Class: Selective Estrogen Receptor modulator MOA: Estrogen antagonist actions in breast tissue and CNS. Estrogen agonists effects in uterus, liver & bone Uses: Hormone responsive breast ca SE: Endometrial hyperplasia, endometrial ca Notes: prevents osteoporosis and decrease risk for atherosclerosis

Answer 49

Tamoxifen

Question 50

Class: Androgen antagonist MOA Competitive antagonist at androgen receptor Uses: Prostate CA, surgical castration SE: gynecomastia, hot flushes

Answer 50

Flutamide Surgical castration (nilutamide) Notes: less hepatotoxicity with bicalutamide and nilutamide GnRH analogs (leuprolide) must be co-administered with flutamide to prevent acute flare-up of prostate CA

Question 51

Class: GnRH analog MOA: Increased LH and FSH secretion with intermittent administration. Reduced LH and FSH secretion with prolonged continuous administration Uses: Prostate CA, Precocious puberty SE: Hot flushes, sweats, headache,

Answer 51

Leuprolide

Question 52

Class: Estrogen synthesis inhibitor MOA: Reduces estrogen synthesis by inhibiting aromatase Uses: Breast CA, Precocious puberty Notes: effective against Breast CA that have become resistant to tamoxifen

Answer 52

Anastrozole