Antineoplastic Agents

Question 1

Cyclophosphamide

Answer 1

Less reactive derivative of mechlorethamine
DNA alkylating activity requires activation in liver or tumor
Oral administration

Question 2

Mechlorethamine

Answer 2

Nitrogen mustard
Alkylating agent
Highly reactive DNA alkylating/damaging agent
Causes necrosis at the site of injection

Question 3

Nitrosoureas

Answer 3

Alkylating agent
Crosses BBB
Used against brain tumors

Question 4

Procarbazine

Answer 4

Alkylating agent
Carcinogenic
Metabolized to alkylating and free radical intermediates
Used for Hodgkin's disease
Leukemogenic

Question 5

Cisplatin

Answer 5

Platinum coordination complex
Inhibits DNA biosynthesis
Tx: ovarian and testicular cancer
SE: nephrotoxicity, acoustic nerve dysfunction

Question 6

Methotrexate

Answer 6

Anti-tumor antimetabolite
Folic acid analog
Dihydrofolate Reductase inhibitor
Blocks synthesis of DNA, RNA, and protein precursors
S phase-specific

Question 7

Leucovorin(folinic acid)

Answer 7

Rescue drug for chemo
Used as antidote to Methotrexate (poison/chemo)
Also used to treat Rheumatoid Arthritis

Question 8

5-Fluorouracil

Answer 8

Pyrimidine antagonist
Inhibits thymidylate synthetase
Metabolites are incorporated into DNA and RNA
S phase-specific

Question 9

Capecitabine

Answer 9

Pyrimidine antagonist
Oral prodrug of Fluorouracil
Colon and breast cancer treatment

Question 10

Cytosine arabinoside

Answer 10

Pyrimidine antagonist
AKA Cytarabine and araC
araC–>araCMP–>araCTP which inhibits DNA synthesis and leads to breaks and mutations
Metabolic activation requires deoxycytidine

Question 11

6-mercaptopurine

Answer 11

Purine antagonist
Interfere with DNA and RNA synthesis by inhibiting purine synthesis
S phase-specific
Activated by HGPRT
Metabolically inactivated by xanthine oxidase (cow’s milk)

Question 12

6-thioguanine

Answer 12

Purine antagonist
Interfere with DNA and RNA synthesis by inhibiting purine synthesis
S phase-specific
Activated by HGPRT

Question 13

Bleomycin

Answer 13

Anti-tumor AB/Anthracycline
Cuts DNA strands
Causes pulmonary fibrosis at large doses
Useful in combination regimens

Question 14

Daunorubicin

Answer 14

Anti-tumor AB/Anthracycline
Binds to DNA topoisomerase II, cuts DNA, causes mutations and carcinogenic
SE: irreversible cardiac toxicity at high doses

Question 15

Doxorubicin

Answer 15

Anti-tumor AB/Anthracycline
Has -OH group
Binds to DNA topoisomerase II, cuts DNA, causes mutations and carcinogenic
SE: irreversible cardiac toxicity at high doses

Question 16

Paclitaxel

Answer 16

Mitotic spindle poison
Tx: metastatic ovarian and breast cancer
Comes from bark/leaves of yew tree
Blocks microtubule disassembly

Question 17

Vinblastine

Answer 17

Mitotic spindle poison
M phase-specific
Inhibits microtubule polymerization
SE: nausea, vomiting, bone marrow depression
Tx: Hodgkin and other lymphomas
Tubulin gene mutations cause resistance

Question 18

Vincristine

Answer 18

Mitotic spindle poison
Binds to microtubules and stops mitosis
SE: no acute, mild bone marrow depression, muscle weakness
Tx: acute childhood leukemia, Hodgkin’s lymphoma
Tubulin gene mutations cause resistance

Question 19

Irinotecan

Answer 19

Camptothecin
Blocks religation of single-strand break by binding to the cleavable complex of the DNA topoisomerase I and DNA
S phase-specific

Question 20

Topotecan

Answer 20

Camptothecin
Blocks religation of single-strand break by binding to the cleavable complex of the DNA topoisomerase I and DNA
S phase-specific

Question 21

Etoposide

Answer 21

DNA topoisomerase II inhibitor

Forms complex with topo2 and DNA

Question 22

Tamoxifen

Answer 22

Comp inhibitor of estrogen
Partial agonist
low toxicity
SE: hot flashes
Tx: female and male breast and uterine cancers

Question 23

Raloxifene

Answer 23

Selective estrogen response modulator
Tx: breast cancer in patients with osteoporosis
Lower risks of endometrial cancer and thrombosis than tamoxifen.

Question 24

Anastrozole

Answer 24

Aromatase inhibitor
Inhibit conversion of androgens to estrogen
Blocks estrogen production in postmenopausal women
More effective than Tamoxifen for postmenopausal women
SE: joint pain, dec bone density

Question 25

Letrozole

Answer 25

Aromatase inhibitor
Inhibit conversion of androgens to estrogen
Blocks estrogen production in postmenopausal women
More effective than Tamoxifen for postmenopausal women
SE: joint pain, dec bone density

Question 26

Exemestane

Answer 26

Aromatase inhibitor
Inhibit conversion of androgens to estrogen
Blocks estrogen production in postmenopausal women
More effective than Tamoxifen for postmenopausal women
SE: joint pain, dec bone density
Reduces risk of breast cancer in high risk postmenopausal women

Question 27

Leuprolide

Answer 27

Anti-androgen
Analog of GnRH
Pulsatile delivery: inc levels of androgens in men and estrogens in women
Continuous high dose: lowers androgens in men and estrogen in premenopausal women (chemical castration)
Tx: prostate cancer

Question 28

Flutamide

Answer 28

Anti-androgen
Androgen receptor antagonist on the prostate
Used with leuprolide

Question 29

Prednisone

Answer 29

Adrenocorticosteroid
Induces apoptosis in leukemia cells
Tx: leukemia, lymphoma, myeloma
Doesn't cure leukemias
Reduces inflammation and nausea

Question 30

Lapatinib

Answer 30

EGFR and HER2 kinase inhibitor

Tx: breast cancer

Question 31

Erlotinib

Answer 31

EGFR kinase inhibitor

Tx: non-small cell lung cancer, head and neck cancers

Question 32

Imatinib

Answer 32

bcr/abl kinase inhibitor

Tx: CML (bcr/abl mutation)

Question 33

Cetuximab

Answer 33

Chimeric EGFR antibody

Tx: colon cancer, head and neck cancer

Question 34

Trastuzumab

Answer 34

Humanized HER2 antibody in HER2+ breast cancers
Tx: metastatic breast cancer
Immune system-mediated effects

Question 35

Brentuximab vedotin

Answer 35

CD30 surface antigen targeter
Chimeric IgG conjugated to toxic spindle poison (vedotin)
Tx: Hodgkin lymphoma, anaplastic large cell lymphoma