Cancer Chemotherapy

Question 1

Alkylating Agents

Answer 1

CELL CYCLE NON-SPECIFIC
Mechlorethamine
Cyclophosphamide
Isofosfamide
Carmustin/Lomustin
Busulfan
Cisplatin

Question 2

Antimetabolites

Answer 2

CELL CYCLE SPECIFIC
Methotrexate
6-MP
Fluorouracil
Capecitabine
Cytarabine

Question 3

Antibiotics

Answer 3

CELL CYCLE NON-SPECIFIC - except Bleo
Doxorubicin
Epirubicin
Dactinomycin
Bleomycin

Question 4

From plants

Answer 4

CELL CYCLE SPECIFIC
Vincristine
Vinblastine
Paclitaxel (Taxol)
Docetaxel
Etoposide

Question 5

Aromatase Inhibitors

Answer 5

Exemestane
Letrozole
Anastrozole

Question 6

RTK Inhibitors

Answer 6

Tamoxifen

Imatinib

Question 7

Monoclonal Antibodies (RTK)

Answer 7

Trastuzumab
Cetuximab
Bevacizumab

Question 8

Raf/Mek Inhibitors

Answer 8

Sorafenib

Vemurafenib

Question 9

Mechlorethamine

Answer 9

Reactive nitrogen mustard
Must be mixed right before administration
Nausea, vomiting, BM toxicity

(not in FA)

Question 10

Cyclophosphamide

Answer 10

Crosslink DNA at guanine N7
Prodrug that is activated by CYP450 in liver

TX: Highly effective against Burkitt’s

Acrolein - toxic compound that causes hemorrhagic cystitis. Must take with lots of water.
MESNA - will bind toxic acrolein and reduce its effects

SE: Hematuria
Myelosuppression

Question 11

Isofosfamide

Answer 11

Greater activity than Cyclophosphamide, must give with MESNA

SE: Neurotoxicity, Nephrotoxicity, Hematuria, Cardiac tox at high dose
Myelosuppression

Question 12

Carmustin/Lomustin

Answer 12

Nitrosoureas
Lipid soluble - can cross BBB

TX: Brain tumors

SE: Delayed myelosuppression, PULMONARY FIBROSIS, CNS toxicity

Question 13

Busulfan

Answer 13

TX: CML

SE: Myelosuppression, Pulmonary Fibrosis

Question 14

Cisplatin

Answer 14

Cross-links GC base pairs with platinum

TX: Treat testicular cancer
(Bleomycin, Etoposide, Vinblastine - 85% cure)

SE: Renal damage, Ototoxicity, Peripheral neuropathy

Question 15

Methotrexate

Answer 15

Folate analog - Inhibits DHFR
No THF (dTMP) generated
S-phase specific

TX: Pediatric ALL, Choriocarcinoma
(Psoriasis, IBD, RA, Vasculitis)

SE: Hepatic Necrosis, Myelosuppression, Pulmonary Fibrosis, Mucositis

Reversal: Leucovorin

Question 16

6-Mercaptopurine

Answer 16

(same as Azathioprine - Aza is metabolized to 6-MP)
Inhibits guanine synthesis

TX: Maintenance of ALL

SE: Myelosuppression

Question 17

Fluorouracil (5-FU)

Answer 17

Pyrimidine analog
Inhibits Thymidylate Synthase - prevent dTMP
Potentiated by leucovorin

TX: Colon cancer, Pancreatic cancer, Basal Cell Carcinoma

SE: PHOTOSENSITIVITY, Oral/GI ulcers, Hand Foot Syndrome, Myelosuppression

Question 18

Capecitabine

Answer 18

Orally prodrug of 5-FU

not GI toxic

Question 19

Cytarabine

Answer 19

Cytosine analog - Inhibits DNA polymerase

TX: AML, Hairy Cell Leukemia

SE: Myelosuppression with Megaloblastic anemia, Pancytopenia

Question 20

Doxorubicin

Answer 20

Free radicals that bind to topo II nicked DNA

TX: Solid tumors, breast cancer

SE: Dilated Cardiomyopathy, severe local tissue damage with extravasation, Myelosuppression

Dexrazoxane - Prevents cardiac myopathy. Iron chelating agent

Question 21

Epirubicin

Answer 21

Doxorubicin analog
Can use it at higher doses than Doxorubicin

SE: Chronic cardiac toxicity
Interacts with Cimetidine (H2 Receptor blocker) - serum concentration will rise

Question 22

Dactinomycin

Answer 22

Intercalates DNA between adjacent GC base pairs
Inhibits RNA pol
Blocks topo II nicked strands

TX: Pediatric Rhabdomyosarcoma, Wilm’s Tumor, Ewing’s sarcoma
(along with surgery, Vincristine/Cyclophosphamide)

SE: Severe tissue damage with extravasation, Myelosuppression

Question 23

Bleomycin

Answer 23

Generates free radicals (O2 and OH-) that fragment DNA

TX: Hodgkin lymphoma, squamous cell carcinomas, testicular cancer, germ cell tumor of ovary

SE: PULMONARY FIBROSIS, Minimal Myelosuppression

Question 24

Mild Bone Marrow Suppression

Answer 24

Bleomycin and Vincristine

Question 25

Vincristine

Answer 25

Inhibits tubulin polymerization M-Phase specific TX: Pediatric leukemia, Non-Hodgkin lymphomas SE: Sensory neuropathy, paralytic ileus *Mild myelosuppression*

Question 26

Vinblastine

Answer 26

TX: Testicular cancer (w/ Bleo and cisplatin) SE: Myelosuppression, less neurotoxic

Question 27

Paclitaxel/Docetaxel

Answer 27

Stabilizes polymerized microtubules TX: Cisplatin resistant solid tumors SE: Peripheral neuropathy

Question 28

Etoposide

Answer 28

Inhibits topoisomerase II - causes ds breaks TX: Testicular cancer, SCLC leukemias, lymphomas SE: Myelosuppression

Question 29

Vinblastine/Cisplatin/Bleomycin/Etoposide

Answer 29

Testicular Cancer

Question 30

Exemestane, Letrozole, Anastrozol

Answer 30

Aromatase inhibitors - block conversion of androgen to estrogen TX: Estrogen receptor positive breast cancer SE: MSK pain, Headache, Fatigue, Difficulty breathing

Question 31

Tamoxifen

Answer 31

Inhibits Estrogen Receptor directly TX: Estrogen dependent breast cancer SE: Can increase the risk of endometrial cancer Prevents bone loss and reduces serum cholesterol

Question 32

Imatinib

Answer 32

Inhibits BCR-ABL TX: CML, CMML SE: Inhibits platelet derived growth factor

Question 33

Trastuzumab

Answer 33

Inhibits Her2 TX: Her2 positive metastatic breast cancer SE: Weakening of heart muscle, CHF, neutropenia, anemia, hypersensitivity reactions

Question 34

Cetuximab

Answer 34

Inhibits EGFR (Her1) TX: EGFR positive colorectal cancer SE: Severe infusion reactions, Hypotension, Serum sickness, Papulopustular acneiform rash

Question 35

Bevacizumab

Answer 35

Inhibits VEGF Blocks angiogenesis and neovascularization TX: Colorectal Cancer SE: Hypertension, CHF, Proteinuria, Hemorrhage, GI perforation

Question 36

Sorafenib

Answer 36

C-Raf, VEGF, PDGFR inhibitor TX: Kidney, Liver, Thyroid cancer SE: Hemorrhage, Hypertension

Question 37

Vemurafenib/Dabrafenib

Answer 37

B-Raf inhibitor TX: METASTATIC MELANOMA carrying V600E B-Raf mutation Given with Trametinib