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20 Cards in this Set
- Front
- Back
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DNA Polymerase Inhibitors must be converted to this form before becoming active.
What enzymes convert them to this form? |
Triphosphate nucleotides
Kinases - phosphorylation |
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How do DNA polymerases then work?
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They are taken up into cells, phosphorylated to their active form and then mistakenly incorporated into the growing DNA chain. They arrest further elongation.
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Name the two cytidine based DNA polymerase inhibitors.
How are they metabolized? |
Cytarabine
Gemcitabine By Cytidine deaminases to inactive uracil analogs |
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Name 3 adenosine based DNA polymerase inhibitors.
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Fludarabine
Cladribine Clofarabine |
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What are the 2 main classes of mitosis inhibitors?
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Taxanes
Vinca alkaloids |
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What is the MOA for taxanes?
Name 2 taxanes. |
They prevent microtubule disassembly
Paclitaxel - Ovarian/ non-small cell Docetaxel - Similar indications to paclitaxel but not used for ovarian and greater water solubility. |
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What is the MOA for vinca alkaloids?
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Prevent assembly of tubulin into microtubules. M phase specific
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Name the 3 vinca alkaloids.
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Vincristine
Vinblastine Vinorelbine |
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Vinca alkaloids have two portions. What are they?
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Catharanthine
Vindoline Both are essential for high affinity tubulin binding. |
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What effect does acetylation of hydroxyl groups on vinca alkaloids have?
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Destroys antineoplastic activity.
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What are epipdophyllotoxin's?
What is their MOA? |
Topoisomerase Poisons
They increase DNA degradation by interacting with Topo II. |
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What are two examples of this type of drug?
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Etoposide
Teniposide |
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What type of drug inhibits Topo I?
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Camptothecins - S phase specific
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Name two camptothecins.
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Topotecan
Irinotecan |
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What is the MOA of antiandrogens?
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They decrease the action of endogenous androgens such as testosterone and DHT in patients with prostate cancer.
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Name 3 antiandrogens.
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Flutamide
Nilutamide Bicalutamide |
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What is the MOA for Luteinizing Hormone-releasing Hormone Agonists
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Inhibit LH production from the pituitary after it is stimulated, thereby reducing production of testosterone from the gonads.
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name 3 LHRH agonists.
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Leuprolide
Goserelin Buserelin |
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What is the MOA for antiestrogens?
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Compete with estrogen for binding of estrogen receptor in breast cancer cells.
Decreased estrogen stimulation decreases transcription of genes that affect cell growth. Tamoxifen |
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What are aromatase inhibitors?
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They are drugs that inhibit the conversion of androgens to estrogens which is mediated by aromatase enzymes. (Anastrozole, Letrozole, Exemestane)
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