Anti-neoplastics

Question 0

Activated by liver cytochrome P450 system; broad spectrum of activity; for Hodgkin’s disease and non-Hodgkin’s lymphoma, multiple myeloma, neuroblastoma, leukemias, carcinoma of endometrium, breast, lung; may cause sterile hemorrhagic cystitis

Answer 0

Cyclophosphamide

Question 1

bi-functional alkylating agent that produces DNA cross-links; for Hodgkin and non-Hodgkin’s lymphoma

Answer 1

Mechlorethamine

Question 2

Nitrosureas; Highly lipophilic, rapidly crosses BBB; Treatment of brain tumors, multiple myeloma, melanoma

Answer 2

Carmustine

Question 3

Folate analog; binds to dihydrofolate reductase and prevents formation of tetrahydrofolate; High doses followed by “rescue” of host cells with leucovorin; Binds to serum albumin so avoid other drugs that will displace it from albumin; Treatment of acute lymphocytic leukemia, choriocarcinoma

Answer 3

Methotrexate

Question 4

Pyrimadine Analog; Activated in cells to FUTP which inhibits RNA synthesis, and FdUMP which interferes with thymidylate synthetase and ultimately DNA synthesis; S-phase specific; IV for carcinoma of stomach, colon, pancreas, ovary, head and neck, breast, bladder; topical cream for basal cell carcinoma

Answer 4

5-Fluorouracil

Question 5

Cytidine analog; Competes with cytidine for all 3 phosphorylation steps to dCTP; Causes DNA chain termination; S-phase specific; Treatment of acute leukemias

Answer 5

Cytarabine

Question 6

Purine analog that is converted in calls to ribonucleotide that inhibits RNA and DNA synthesis; S-phase specific; Treatment of acute leukemias

Answer 6

Mercaptopurine

Question 7

Inhibits ribonucleotide reductase, blocking DNA synthesis; Arrest at G1-S interface; Treatment of chronic granulocytic leukemia, head and neck cancer

Answer 7

Hydroxyurea

Question 8

Treatment of Hodgkin’s and non-Hodgkin’s lymphoma, breast cancer; M-phase specific; binds to tubulin, inhibiting proper formation of microtubules and mitotic spindle

Answer 8

Vinblastine

Question 9

Treatment of acute lymphocytic leukemia, Hodgkin’s and non-Hodgkin’s lymphomas, Wilm’s tumor, neuroblastoma, and rhabdomyosarcoma

Answer 9

Vincristine

Question 10

Blocks late in G2 phase; enhances assembly and stability of microtubules of binding to B-subunit of tubulin; Treatment of refractory ovarian cancer and breast cancer

Answer 10

Paclitaxel

Question 12

Antitumor antibody; Intercalates between DNA base pairs distorting DNA helix, causes lipid peroxidation and free radical generation, binds to DNA and topoisomerase II; Treatment of Hodgkin’s and non-Hodgkin’s lymphomas, breast, ovary, small-cell lung cancers

Answer 12

Doxorubicin

Question 13

Glycopeptides that bind DNA; causes oxidative-like damage to DNA which leads to DNA strand breaks; Phase-specific for G2; Treatment of germ cell tumors of testes, ovaries, head, neck, lung, lymphomas

Answer 13

Bleomycin

Question 14

Stabilizes DNA-topoisomerase II complexes, resulting in double-strand DNA breaks; Late G2 phase effects; Treatment of lymphomas, acute nonlymphocytic leukemia, small cell carcinoma of the lung, testicular tumors

Answer 14

Etoposide

Question 15

Stimulates granulocyte production by marrow; Given after myelosuppressive agents to speed neutrophil recovery

Answer 15

Filgrastim

Question 16

Monoclonal antibody that binds to HER2 receptor; Treatment of metastatic breast cancers that over express HER2

Answer 16

Trastuzumab

Question 17

Platinum coordination complex, activated species which causes DNA cross links; Cycle-specific phase-nonspecific; Wide anti tumor spectrum– treatment of cancer of testis, ovary, head, neck, bladder, colon, esophagus, small cell lung

Answer 17

Cisplatin

Question 18

Activated in vivo to a methylating agen which causes chromosomal damage; Most effective in G1 and S phase; Treatment of Hodgkin’s

Answer 18

Procarbazine

Question 19

Binds to steroid receptors, depresses RNA synthesis of many growth-related genes, induces nucleases which may modulate cell lysis; May arrest cells at G1; May also have anti-emetic effect; Palliative therapy, limited myelosuppression; Treatment for acute and chronic lymphocytic leukemia, Hodgkin’s disease, non-Hodgkin’s lymphoma, breast cancer

Answer 19

Prednisone

Question 20

Antiestrogen that blocks estrogen receptors; Activated by CYP2D6; Used for breast cancer and breast cancer prophylaxis in women that are at high risk

Answer 20

Tamoxifen

Question 21

Aromatase inhibitor, inhibits conversion of androgens to estrogens in all tissues; Treatment for breast carcinoma in post-menopausal women

Answer 21

Letrozole

Question 22

Analog of gonadotropin-releasing hormone (GnRH); After 2-4 wks it desensitizes GnRH signaling, inhibiting LH/FSH secretion thereby decreasing testosterone synthesis to castration levels

Answer 22

Leuprolide

Question 23

Antiandrogen that blocks androgen receptors; Treatment for metastatic prostate cancer

Answer 23

Flutamide

Question 24

Kinase inhibitor

Answer 24

Imatinibmesylate (Gleevec)

Question 25

Partially prevents sterile hemorrhagic cystitis from cyclophosphamide

Answer 25

Mesna

Question 26

Used as a rescue for host cells after high doses of Methotrexate; Folinic acid, a fully reduced folate that does not require reduction by DHFR

Answer 26

Leucovorin

Question 27

Class of alkylating agents; includes Carmustine; Cycle non-specific, cross the blood brain barrier well, Treat brain tumors, multiple myeloma, melanoma

Answer 27

Nitrosoureas