Term
| How do cancer cell acquire invasiveness? |
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Definition
| Expression of metalloproteases and tolerance to normal survival factors secreted by neighboring cells |
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Term
| In general, when do you prefer to use a Cell Cycle Specific Chemo drug? |
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Definition
| For hematologic malignancies and solid tumors w/ high growth fraction |
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Term
| In general, when do you prefer to use a Cell Cycle Non-Specific Chemo drug? |
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Definition
| For solid tumors w/ high or low growth fraction |
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Term
| What are 5 general chronic toxicities associated w/ cancer drugs? |
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Definition
| Leukemia, cardiotoxicity (esp w/ anthracyclines), sterility, neuropathy, and nephropathy |
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Term
| MOA for alkylating agents? |
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Definition
| transfer of alkyl group to cellular constituents. Typically at N7 of guanine --> cross linking of DNA --> cytotoxic. Classified as CCNS |
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Term
| How do cells become resistant to alkylating agents and what are some adverse effects? |
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Definition
increased DNA repair, decrease permeability, and increase glutathione
Standard + mucositis + busulfan causes pulmonary fibrosis and hepatic toxicity. |
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Term
| Cyclophosphamide MOA? Toxic effects? Treatment for effects? Uses? |
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Definition
Prodrug converted to Acrolein in liver. May cause hemorrhagic cystitis. Treat w/ mesna. SEs - hepatotoxicity. Treats NHL, ovarian, breast, and neuroblastoma
Alkylating agent -> CCNS |
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Term
Nitrosoureas (carmustine and lomustine)
What class? Special property? |
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Definition
Alkylating agent.
Lipid soluble and crosses BBB |
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Term
Procarbazine
Class? adverse effects? |
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Definition
Alkylating agent.
adverse effects - myelosuppression, pulmonary toxicity, neurotoxicity, leukomogenic, and teratogenic |
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Term
| Platinum Analog MOA? Adverse Effects? Uses? main example? |
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Definition
CCNS - complexes w/ DNA --> strand links --> cytotoxicity.
Nephrotoxicity, ototoxicity from neurotoxicity.
Uses - solid tumors: testicular, ovarian, bladder, lung.
Cisplatin |
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Term
Carboplatin
Dose-limiting SE?
other adverse effects?
Uses? |
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Definition
myelosuppression is Dose limiting
Used for solid tumors: testicular, ovarian, lung, bladder. |
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Term
| General MOA for antimetabolites? |
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Definition
| targets aspects of cellular metabolism that makes them more susceptable to cancer drugs. Thus they generally do not cause acute toxicities. |
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Term
Methotrexate
MOA?
Resistance mechanism?
Adverse Effects? Rescue from effects with?
Uses? |
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Definition
CCS antimetabolite
Folic acid analong that prevents DHFR causing block in thymidilate production -> DNA and RNA synthesis block. Does not cross BBB.
Resistant via decreased permiability, increase DHFR, low DHFR affinity for MTX, decreased retention
Adverse Effects - mucositis, myelosuppression, nephrotoxicity. Rescue w/ leucovorin
Uses - Leukemia, lymphoma, breast cancer |
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Term
6-thiopurines (6-mercaptopurine and 6-thioguanine)
Class? MOA? Adverse Effects? |
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Definition
purine antagonist antimetabolite
convereted by HGPRT to incorporate into DNA and RNA -> cytotoxicity
SEs - myelosuppression, immunosuppression, hepatotoxicity |
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Term
Fludarabine and Cladribine
Class? MOA? |
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Definition
Purine antagonist antimetabolite
both must be phosphoryloated to triphosphate to be active. |
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Term
5-Fu
Class? MOA?
give with what to potentiate effects?
Adverse Effects?
Uses? |
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Definition
Pyrimidine antagonist antimetabolite CCS
Prodrug that undergoes series of rxns -> FdUMP preventing synthesis of thymidine
Give w/ leucovorin to potentiate effects by stabilizing the THF, FdUMP, TS complex.
SEs - nausea, diarrhea, mucositis, bone marrow suppression, alopecia
Hand Foot syndrome is dose limiting
Used for breast, ovarian, head and neck cancers |
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Term
Capecitabine
class? MOA? SEs? |
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Definition
pyrimidine antagonist antimetabolie CCS
prodrug that eventually is converted to 5-Fu in the tumor cell by thymidilate phosphorylase giving more specificity. then same MOA as 5-Fu. Same SEs as 5-Fu. |
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Term
Cytarabine
Class?
MOA?
Uses? |
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Definition
pyrimidine antagonise antimetabolite CCS
S-phase specific effects limiting its use to hematologic malignancies (particularly ALL) |
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Term
Gemcitabine
class? MOA? Toxicity? |
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Definition
pyrimidine antagonist antimetabolite CCS
MOA: analog of deoxycytidine that must be phosphorylated to be active
Myelosuppression is dose limiting |
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Term
Vinblastine, Vincristine, vinorelbine
MOA? adverse affects shared by all three? |
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Definition
inhibits microtubule formation via binding of B subunit.
SEs - rapid action causes hyperuricemia which may precipitate gout. give allopurinol.
If extravastated --> cellulitis. |
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Term
| Vinblastine side effects? Uses? |
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Definition
Bone marrow suppression
low neurotoxicity
GI problems.
Hodgkins, NHL, Breast, Testicular |
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Term
Vincristine
Side Effects?
Uses? |
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Definition
limited myelosuppression but higher neurotoxic effects.
Less GI effects.
ALL, Hodgkins, Leukemias, Wilms |
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Term
|
Definition
intermediate myelosuppression
low neurotoxicity
most likely cause granulocytopenia |
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Term
Paclitaxel and Docetaxel
Class?
Adverse Effects? |
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Definition
plant alkaloids Taxanes CCS
causes myelosuppression
Cumulative effects causing neurotoxicity.
Hypersensitivity rxn - treat w/ CS and antihistamines beforehand. |
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Term
Etoposide, and Teniposide
Class?
MOA?
Adverse effects? |
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Definition
plant alkaloid Epipodophyllotoxin
MOA: inhibits DNA topoisomerase II causing strand breakage. blocking late S-G2 phase
SEs - dose reduction in renal pts. |
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Term
Topotecan
Class?
MOA?
Adverse Effects? |
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Definition
plant alkaloid camptothecin
MOA: inhibits topoisomerase I
Reduce dose for renal pts |
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Term
Irinotecan
Class? MOA? Adverse Effects? |
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Definition
plant alkaloid camptothecins
Inhibits topoisomerase I
Reduce dose in liver dysfunction pts. |
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Term
what class does the -rubicin and mitoxantrone drugs fall into? MOA?
Dose limiting Adverse effects?
Adverse effects that are a result of its MOA? |
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Definition
all drugs ending in rubicin are antitumor antibiotics of the anthracycline class
They inhibit topoisomerase II and generate free radicals.
Myelosuppression is dose limiting. and cardiotoxicity from the free radicals. |
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Term
| MOA and adverse effects for anthracyclines |
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Definition
inhibition of topoisomerase II leading to DNA strand breakage
SEs - myelosuppression is dose limiting. |
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Term
Bleomycin
class? MOA? adverse effects? |
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Definition
antitumor antibiotic that is CCS
MOA: bifunctional molecules that bind DNA w/ one end and chelates Fe2+ with the other end
SEs - pulmonary fibrosis is dose limiting. Mucocutaneous reactoins |
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Term
| Prednisone effect on cancer? |
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Definition
| decreases lymphoid mass and induces remission of ALL |
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Term
Tamoxifen
class? MOA? Uses? |
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Definition
Hormonal agen
MOA: competitive partial agonist inhibitor of estrogen
Used in breast cancer |
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Term
Flutamide and Bicalutamide
Class? MOA? |
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Definition
Hormonal agent
Antagonist at the androgen receptor (testosterone promotes growth of the prostate) |
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Term
Leuprolide and goserelin
Class? MOA? Uses? |
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Definition
GnRH agonist
MOA: initial surge in LH and FSH followed by inhibition of LH and FSH release and inhibition of testosterone release.
Treats prostate cancer. |
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Term
Anastrozole, letrozole, and exemestane
Class? |
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Definition
| Hormonal agenst that inhibit aromatase and prevents conversion of steroids into androgens |
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Term
| Ways that monoclonal antibodies are used in cancer? 5 ways |
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Definition
Ab dependent lysis
Complement dependent lysis
Localized delivery of radiation
Localized delivery of chemo
Inhibit angiogenesis. |
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Term
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Definition
| binds to circulating VEGF and prevents angiogenesis. Used in colon and lung cancer |
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Term
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Definition
| Binds to CD20 on B-Cells causing AB dependent or complement dependent lysis. Treats NHL. |
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Term
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Definition
| Used to treat breast cancer because it binds to HER-2/Neu and causes Ab dependent lysis. |
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Term
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Definition
Tyrosine kinase inhibitor
MOA: inhibits PDGF
Treats CML |
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Term
| name 3 bone marrow sparing agents |
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Definition
| cisplatin, bleomycin and vincristine |
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Term
| What are the general toxicities associated w/ chemo drugs? acute and chronic |
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Definition
Acute: nausea, vomitting, bone marrow suppression, alopecia, neutropenai and thrombocytopenia
Chronic: Leukemia, Cardiotoxicity (Anthracyclines), sterility, neuropathy, nephropathy |
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