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40 Cards in this Set
- Front
- Back
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Cyclophosphamide MOA
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Alkylating agents:
Form covalent bonds w/ DNA (esp. 7 position of guanine), RNA, or proteins Not cell cycle specific, but require proliferating cells Nitrogen mustard, binds to DNA |
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What phase does Cyclophosphamide interrupt?
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S phase
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is Cyclophosphamide cell specific?
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No --> alkylating agents target proliferating cells
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Side effects of Cyclophosphamide?
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Myelosuppression
Gonadal dysfunction |
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What are the resistant mechanisms to alkylating agents?
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Resistance mechanisms: enhanced DNA repair, glutathione conjugation
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What is Cisplatin's MOA?
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Alkylating agents:
Form covalent bonds w/ DNA (esp. 7 position of guanine), RNA, or proteins Not cell cycle specific, but require proliferating cells Platinum agent, causes inter- and intra-strand DNA cross-links leading to DNA adducts → difficult for DNA synthesis to occur |
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What phase does Cisplatin act in the cell cycle
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S phase
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What is Cisplatin's side effects
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Myelosuppression
Gonadal dysfunction |
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Is Cisplatin cell specific?
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No, it effects any proliferating cell
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Methotrexate MOA?
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FOLATE ANALOG
Inhibits dyhydrofolate reductase |
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Can Methotrexate cross the Blood Brain Barrier?
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YES!!!
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How is methotrexate excreted?
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Renal
Impaired renal excretion with ASA, NSAID’s, penicillins, probenecid, cephalosporins |
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What are methotrexate's side effects?
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Stomatitis (Mouth sores), diarrhea, myelosuppression
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What part of the cell cycle does methotrexate impact?
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S phase
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What is Leucovorin used for?
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Repletes folate preferentially in normal cells after treatment with Methotrexate b/c methotrexate can take a while to dilute out
In 5FU --> potentiates its action by increasing 5,10 methylene THF |
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What is 5-Fluorouracil (5-FU) MOA
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pyrimidine analog, inhibits thymidylate synthase & pyrimidine incorporation into RNA/DNA
Acts as a toxic precursor resulting in fluorinated pyrimidines - blocks enzymes in pyrimidine metabolism, and pyrimidine incorporation into DNA |
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Does 5FU impact DNA or RNA?
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DNA
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What part of cell cycle does 5FU impact
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S phase
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How is fluoroucil metabolized?
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Dihydropyrimidine dehydrogenase (DPD)
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What is toxicity in patients w/ 5FU?
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pts w/ DPD deficiency → severe toxicity
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What is Vincristine & what is the MOA
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Natural products: Vinca Alkaloids
Blocks polymerization of microtubules; cannot make a spindle |
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What cell cycle phase does vincristine work in?
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M phase
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What are the side effects of vincrsitine?
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Neuropathy
Myelosuppression |
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What is Bleomycin and what is its MOA
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Antibiotic:
intercalates into DNA → Spontaneous oxidation and free-radical formation leading to strand breakage |
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What phase of cell cycle does Bleomycin act in?
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G2 phase
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What is Bleomycin's toxicity?
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PULMONARY FIBROSIS!!! KNOW THIS!
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What is doxorubicin and what is its MOA?
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Anthracyclines (derived from fungus)
Cause intercalation between DNA base pairs and inhibit DNA Topoisomerases |
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What is an important toxicity of doxorubicin?
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CARDIOTOXICITY!!!!
Also causes myelosuppression & stomatitis |
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What is paclitaxel & what is its MOA?
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Microtubule agents that promote microtubular assembly and stability, leading to M phase arrest
Spindle becomes too rigid to allow chromosome segregation |
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What cell cycle phase does Paclitaxel work in?
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M phase!
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What are the toxicities associated w/ Paclitaxel?
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Neuropathy, myelosuppression
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What sort of cells does Paclitaxel work on?
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Cells that are not growing as fast hence why it can effect Neurons
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rituximab MOA?
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Targeted therapy of antibody type..
Chimeric monoclonal antibody against CD-20 Can be used alone or conjugated to radioactive isotope |
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What is Rituximab used for?
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B cell lymphoma!
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What is imatinib and what is its MOA?
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Oral tyrosine kinase inhibitor of bcr-abl, c-kit, PDGFRα:
Acts as an ATP analog → blocks use of ATP by tyrosine kinase → inhibits proliferation, induces apoptosis |
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What is Imatinib used for?
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chronic myeloid leukemia (CML)
Gastrointestinal stromal tumor (GIST) |
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What are potential resistances to Imatinib?
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Bcr-ABL amplification
Mutations in bcr-abl |
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What is bevacizumab and what is its MOA?
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Humanized (93%) VEGF antibody → binds to VEGF with high affinity & prevents it from binding to its receptors, thus prevents angiogenesis to tumor
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What sorts of cancers is bevacizumab used in?
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Colorectal, lung, & kidney cancers
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What has more toxicity? Targeted therapy or chemotherapy?
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Chemotherapy
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