Chemotherapy MOAs

Question 1

Name 6 alkylating agents

Answer 1

Mustargen (aka mechlorethamine)
Melphalan
Cyclophosphamide (aka Cytoxan)
Chlorambucil
Lomustine (aka CCNU)
Procarbazine

Question 2

At what point in the cell cycle do alkylating agents work best?

Answer 2

They are cell cycle phase nonspecific

Question 3

What drug class includes mustargen, melphalan, cyclophosphamide, and chlorambucil?

Answer 3

Nitrogen mustards

Question 4

Name two anti-tumor antibiotics

Answer 4

doxorubicin and mitoxantrone

Question 5

How are mitoxantrone and doxorubicin related?

Answer 5

Mitoxantrone is a synthetic analog of doxorubicin

Question 6

Name 4 anti-metabolite chemotherapeutics

Answer 6

Cytosine Arabinoside (aka Cytarabine, brand name Cytosar-U)
Methotrexate
Gemcitabine
Rabacfosadine (brand name Tanovea)

Question 7

At what point in the cell cycle do anti-metabolite chemotherapeutics work best?

Answer 7

S phase

Question 8

What drug class includes vincristine, vinblastine, vinorelbine, and vindesine?

Answer 8

Vinca alkaloids

Question 9

What group of chemotherapeutics describes the vinca alkaloids?

Answer 9

anti-microtubule agents

Question 10

At what point in the cell cycle do platinum anti-cancer agents work best?

Answer 10

S phase

Question 11

What is the drug classification for Palladia?

Answer 11

tyrosine kinase inhibitor

Question 12

What is the generic name for Palladia?

Answer 12

Toceranib phosphate

Question 13

What is the brand name for Toceranib phosphate?

Answer 13

Palladia

Question 14

What is the brand name for Rabacfosadine?

Answer 14

Tanovea

Question 15

What is the generic name for Tanovea?

Answer 15

Rabacfosadine

Question 16

What is the MOA of mustargen?

Answer 16

Hydrolyzes to nucleophilic reactive centers capable of forming DNA crosslinks. Interferes with DNA replication, RNA transcription, and protein synthesis

Question 17

What is the MOA of Melphalan?

Answer 17

Bifunctional alkylating agent that interferes with RNA transcription and DNA replication, thereby disrupting nucleic acid function. Does not require activation by the liver. Actively transported into tumor cells by amino acid transporters

Question 18

What is the MOA of cyclophosphamide?

Answer 18

Prodrug is metabolized and the metabolite enters cells and rapidly decomposes into alkylating agents that interfere with DNA replication and RNA transcription and replication to ultimately disrupt nucleic acid function

Question 19

What is the MOA of Chlorambucil?

Answer 19

Enters cells through passive diffusion. Primary cytotoxic effect is due to alkylation of cancer cell DNA strands resulting in cross-linking and cellular apoptosis

Question 20

What is the MOA of Lomustine?

Answer 20

MOA not completely understood; believed to inhibit DNA, RNA, and protein synthesis through alkylation and carbamoylation. Enters cells through passive diffusion.

Question 21

What is the MOA of procarbazine?

Answer 21

Prodrug. precise MOA is not well understood, but it is considered to be an alkylating agent, and it appears to inhibit protein, RNA, and DNA synthesis. Procarbazine is auto-oxidized into hydrogen peroxide, which may also directly damage DNA

Question 22

What is the MOA of Doxorubicin?

Answer 22

Inhibits DNA synthesis, DNA-dependent RNA synthesis, and protein synthesis by inhibiting DNA and RNA polymerases and impairing topoisomerase II, as well as through generation of free radicals. Doxorubicin alters transcription and replication by intercalating with DNA base pairs

Question 23

What is the MOA of mitoxantrone?

Answer 23

Synthetic doxorubicin analog. DNA-reactive agent that binds in between DNA base pairs, causing crosslinks and strand breaks. Also interferes with RNA synthesis and is a potent topoisomerase II inhibitor. Does NOT cause oxidative destruction to cell and has reduced potential to produce ROS

Question 24

What is the MOA of Cytarabine?

Answer 24

converted intracellularly into aracytidine triphosphate, which competes with deoxycytidine triphosphate to inhibit DNA polymerase, resulting in inhibition of DNA synthesis. Enters cells via active transport

Question 25

What is the MOA for methotrexate?

Answer 25

inhibits folic acid reductase, preventing the reduction of dihydrofolate to tetrahydrofolate and affecting the production of purines and pyrimidines. Enters cells via active transport

Question 26

What is the MOA for gemcitabine?

Answer 26

Metabolized intracellularly into a diphosphate and triphosphate form. The diphosphate inhibits ribonucleotide reductase. The triphosphate competes with dTCP (the “normal nucleotide”) for incorporation into DNA strands. DNA polymerase epsilon is unable to recognize the abnormal nucleotide (gemcitabine) and repair the DNA strand. Enters cells via active transport

Question 27

What is the MOA for Tanovea?

Answer 27

Guanine nucleotide analogue. The pro-drug is processed by the body and in it’s active form, the drug is a potent, chain-terminating inhibitor of the major DNA polymerases, causing inhibition of DNA synthesis and resulting in S phase arrest

Question 28

What is the MOA for Vinblastine/Vicristine?

Answer 28

Binds to β-tubulin to block microtubule formation and prevent mitotic spindle formation. Some can bind and dismantle formed tubules. Also interferes with amino acid metabolism by inhibiting glutamic acid utilization and preventing purine synthesis, citric acid cycle, and urea formation

Question 29

What is the MOA for carboplatin/cisplatin?

Answer 29

Causes intra- and interstrand DNA cross-linking that causes single- and double-stranded DNA breakage, impairs DNA replication, RNA transcription, and protein synthesis, leading to cell death and inhibition of tumor growth

Question 30

What is the MOA for Elspar?

Answer 30

Catalyzes asparagine into ammonia and aspartic acid. Some malignant cells are unable to synthesize asparagine and are dependent on exogenous asparagine for DNA and protein synthesis

Question 31

What is the drug classification for palladia?

Answer 31

Tyrosine kinase inhibitor

Question 32

What is the MOA for Palladia?

Answer 32

Competitively inhibits ATP binding in target receptor tyrosine kinases, preventing receptor phosphorylation and subsequent downstream signal transduction.

Question 33

What is the MOA for zoledronate?

Answer 33

impedes osteoclast activity and induces osteoclast apoptosis to inhibit bone resorption. Increases urinary excretion of calcium and phosphorus

Question 34

What is the drug classification for zoledronate?

Answer 34

bisphosphanate