Anti-neoplastics Mechanism

Question 1

Bi-functional alkylating agent that produces DNA cross links

Answer 1

Mechlorethamine

Question 2

Activated by liver cytochrome P450 system

Answer 2

Cyclophosphamide

Question 3

Highly lipophilic, rapidly crosses BBB

Answer 3

Carmustine

Question 4

Folate analog; binds to dihydrofolate reductase and prevents formation of tetrahydrofolate; binds to serum albumin so avoid other drugs that will displace it from albumin

Answer 4

Methotrexate

Question 5

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

Answer 5

5-Fluorouracil

Question 6

Cytidine analog; competes with cytidine for all 3 phosphorylation steps to dCTP; Causes DNA chain termination
S-phase specific

Answer 6

Cytarabine

Question 7

Purine analog that is converted in cells to ribonucleotide that inhibits RNA and DNA synthesis
S-phase specific

Answer 7

Mercaptopurine

Question 8

Binds to tubulin, inhibits proper formation of microtubules and mitotic spindle

Answer 8

Vinblastine

Question 9

Blocks late in G2 phase; enhances assembly and stability of microtubules of binding to B-subunit of tubulin

Answer 9

Paclitaxel

Question 10

Antitumor antibody; intercalates between DNA base pairs distorting DNA helix
Causes lipid peroxidation and free radical generation
Binds to DNA and topoisomerase II

Answer 10

Doxorubicin

Question 11

Glycopeptides that bind DNA; causes oxidative-like damage to DNA which leads to DNA strand breaks
Specific for G2

Answer 11

Bleomycin

Question 12

Stabilizes DNA-topoisomerase II complexes resulting in double-strand DNA breaks
Late G2 phase effects

Answer 12

Etoposide

Question 13

Stimulates granulocyte production by marrow

Answer 13

Filgrastim

Question 14

Monoclonal antibody that binds HER2 receptor

Answer 14

Trastuzumab

Question 15

Platinum coordination complex, activated species which causes DNA cross links
Cycle-specific phase-non-specific

Answer 15

Cisplatin

Question 16

Activated in vivo to a methylating agent which causes chromosomal damage
Most effective in G1 and S phase

Answer 16

Procarbazine

Question 17

Binds to steroid receptors
Depresses RNA synthesis of many growth-related genes
Induces nucleases that may modulate cell lysis
May arrest cells in G1
Anti-emetic effect
Palliative therapy

Answer 17

Prednisone

Question 18

Anti-estrogen that blocks estrogen receptors; Activated by CYP2D6

Answer 18

Tamoxifen

Question 19

Aromatase inhibitor, inhibits conversion of androgens to estrogens in all tissues

Answer 19

Letrozole

Question 20

Analog of gonadotropin-releasing hormone (GnRH)

Desensitizes GnRH signaling, inhibiting LH/FSH secretion to decrease testosterone synthesis to castration levels

Answer 20

Leuprolide

Question 21

Anti-androgen that blocks androgen receptors

Answer 21

Flutamide

Question 22

Kinase inhibitor

Answer 22

Imatinibmesylate

Question 23

Folinic acid

A fully reduced folate that does not require reduction by DHFR

Answer 23

Leucovorin

Question 24

Inhibits ribonucleotide reductase, blocking DNA synthesis; Arrest at G1-S interface

Answer 24

Hydroxyurea