AntiNeoplastic Drugs

Question 1

Mechloethamine

1) Use
2) Mechanism of Action

Answer 1

1) Neoplasm
2) DNA Alkylating/Damaging agent, binds guanine
* IV only administration*

Question 2

Cyclophosphamide

1) Use
2) Mechanism of Action

Answer 2

1) Neoplasm
2) DNA Alkylating/Damaging agent, binds guanine
* PO administration-less reactive prodrug*

Question 3

Nitrosourea

1) Use
2) Mechanism of Action

Answer 3

1) Brain Tumors
2) DNA Alkylating agent
* Little cross reaction w/other Alkylating agents*

Question 4

Methotrexate

1) Use
2) Mechanism of Action

Answer 4

1) Neoplasm

2) Dihydrofolate reductase (DHFR) Inhibitor

Question 5

6-Mercaptopurine

1) Use
2) Mechanism of Action

Answer 5

1)Neoplasm
2)Purine antagonists- activated by the enzyme hypoxanthine-guanine phosphoribosyl transferase (HGPRT) causes fraudulent nucleotide base incorporation
Inhibits de novo purine synthesis

Question 6

6-thioguanine

1) Use
2) Mechanism of Action

Answer 6

1)Neoplasm
2)Purine antagonists- activated by the enzyme hypoxanthine-guanine phosphoribosyl transferase (HGPRT) causes fraudulent nucleotide base incorporation
Inhibits de novo purine synthesis

Question 7

Fluorouracil (5-FU)

1) Use
2) Mechanism of Action

Answer 7

1) Colorectal CA
2) Pyrimidine Antagonists- 5-FU metabolite, fluorodeoxyuridine monophosphate (FdUMP) inhibits thymidylate synthetase which stops the production of thiamine nucleotides
* Co-administered w/Leucovorin=synergistic toxicity*

Question 8

Capecitabine

1) Use
2) Mechanism of Action

Answer 8

1) Colon & Breast CA

2) Pyrimidine antagonists- Prodrug of 5-FU activated by thymidine phosphorylase

Question 9

Gemcitabine

1) Use
2) Mechanism of Action

Answer 9

1) Neoplasm (Broad Spectrum)

2) Pyrimidine Antagonists- inhibits ribonucleotide reductase (RNR)

Question 10

Daunorubicin

1) Use
2) Mechanism of Action

Answer 10

1) Neoplasm (Broad Spectrum)

2) Anthracycline- anti-tumor antibody that inhibits DNA synthesis by intercalating between base pairs of the DNA strand

Question 11

Doxorubicin

1) Use
2) Mechanism of Action

Answer 11

1) Neoplasm (Broad Spectrum)

2) Anthracycline- anti-tumor antibody that inhibits DNA synthesis by intercalating between base pairs of the DNA strand

Question 12

Bleomycin

1) Use
2) Mechanism of Action

Answer 12

1) Neoplasm (Broad Spectrum)

2) Anthracycline- anti-tumor antibody that breaks DNA strands (DNA strand scission)

Question 13

Vinblastine

1) Use
2) Mechanism of Action

Answer 13

1) Hodgkin’s Lymphoma
2) Mitotic Spindle Poison (Vinca Alkaloid)- binds tubulin inhibiting microtubule elongation causing mitotic arrest in metaphase (M-phase)

Question 14

Vincristine

1) Use
2) Mechanism of Action

Answer 14

1) Hodgkin’s Lymphoma, Acute Childhood Leukemia
2) Mitotic Spindle Poison (Vinca Alkaloid)- binds tubulin inhibiting microtubule elongation causing mitotic arrest in metaphase (M-phase)

Question 15

Paclitaxel

1) Use
2) Mechanism of Action

Answer 15

1) Ovarian and Advanced Breast CA

2) Mitotic Spindle Poison (Taxane)- enhances tubulin polymerizaton blocking microtubule disassembly

Question 16

Cisplatin

1) Use
2) Mechanism of Action

Answer 16

1) Ovarian and Testicular CA

2) Platinum Coordinated Complexes- DNA crosslinking agent that inhibits DNA synthesis

Question 17

Tamoxifen

1) Use
2) Mechanism of Action

Answer 17

1) Female & Male Breast CA, Uterine endometrium CA
2) Selective Estrogen Receptor Modulators (SERMs)- competitive inhibitor of estrogen binding to estrogen receptors, also works as a partial estrogen receptor agonist

Question 18

Raloxifen

1) Use
2) Mechanism of Action

Answer 18

1)Prevention of Breast CA in osteoporosis pts
2Selective Estrogen Receptor Modulators (SERMs)- competitive inhibitor of estrogen binding to estrogen receptors, also works as a partial estrogen receptor agonist

Question 19

Letrozole

1) Use
2) Mechanism of Action

Answer 19

1) Estrogen Receptor(+) Breast CA

2) Aromatase inhibitors- inhibits conversion of androgens to estrogens (especially in postmenopausal women)

Question 20

Leuprolide

1) Use
2) Mechanism of Action

Answer 20

1) Prostate CA (continuous high doses)
2) Gonadotropin-releasing hormone receptor agonist (on pituitary), causes negative feedback to hypothalamus and decreases androgen production

Question 21

Flutamide

1) Use
2) Mechanism of Action

Answer 21

1) Prostate CA (w/leuprolide)

2) Androgen receptor antagonist- blocks initial pulse of androgen levels @ start of leuprolide

Question 22

Prednisone

1) Use
2) Mechanism of Action

Answer 22

1) Inducing remission & Mutlidrug therapy for Leukemia, Lymphoma, Myeloma, Palliative
2) Adrenocorticosteroids- inducing apoptosis in leukemia cells

Question 23

Erlotinib

1) Use
2) Mechanism of Action

Answer 23

1)Non-small cell lung CA
2)Targeted agent inhibits the function of activated oncogenes/proteins necessary for tumor cell proliferation/angiogenesis
Kinase inhibitor- epidermal growth factor receptor (EGFR) kinase inhibitor

Question 24

Imatinib

1) Use
2) Mechanism of Action

Answer 24

1)Chronic Myelogenous Leukemia (CML)
2)Targeted agent inhibits the function of activated oncogenes/proteins necessary for tumor cell proliferation/angiogenesis
Kinase inhibitor of ABL protein tyrosine kinase and activated BCR-ABL fusion protein

Question 25

Vermuratenib

1) Use
2) Mechanism of Action

Answer 25

1)B-Raf V600E mutant melanomas
2)Targeted agent inhibits the function of activated oncogenes/proteins necessary for tumor cell proliferation/angiogenesis
Kinase inhibitor of B-Raf protein serine/threonine kinase

Question 26

Cetuximab

1) Use
2) Mechanism of Action

Answer 26

1)Colon CA, Head and Neck CA
2)Humanized antibody that kills cells by direct immune-system mediated mechanisms
Epidermal growth factor receptor (EGFR) antibody

Question 27

Brentuximab vedotin

1) Use
2) Mechanism of Action

Answer 27

1) Hodgkin lymphoma, Anaplastic Large cell Lymphoma
2) Humanized anti-CD-30 IgG antibody conjugated to a highly toxic mitotic spindle poison (vedotin) w/ cleavable linker (brings toxin into the tumor cell)