chapter 38/39: anti-neoplastic Flashcards by Anna Woods

what is the clinical application of Gefitinib

non-small cell lung cancer

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what are some adverse reactions seen with Gefitinib

interstitial lung disease, corneal erosion; rash, diarrhea

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what is the mechanism of action of Gefitinib

reversible inhibitor of the EGFR (ErbB1) cytoplasmic tyrosine kinase domain; competes with ATP binding to the kinase domain

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who has the most favorable response to Gefitinib

patients with bronchoalveolar cell carcinoma

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what is the clinical application of Erlotinib

non-small cell lung cancer; carcinoma of pancreas

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what are some adverse rxns seen with Erlotinib

MI, DVT, microangiopathic hemolytic anemia, elevated liver enzymes, stroke, conjunctivitis

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what is the mechanism of action of Erlotinib

reversible inhibitor of EGFR (ErbB1) cytoplasmic tyrosine kinase domain

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what is the clinical application of cetuximab

colorectal cancer; head and neck cancer

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what are some adverse reactions seen with cetuximab

cardiac arrest, Pulmonary embolism, rash, diarrhea, hypomagnesemia, asthenia

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what is the mechanism of action of cetuximab

monoclonal IgG antibody that binds to extracellular domain EGFR (ErbB1)

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development of what is predictive of tumor response when cetuximab is used

development of rash

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what is the clinical application of trastuzumab

breast cancer or metastatic gastric caner with HER2 over expression

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what are some adverse reactions seen with trastuzumab

cardiotoxicity, nephrotic syndrome, leukopenia

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what is the mechanism of action of trastuzumab

monoclonal IgG antibody against ErbB2 (HER2)

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what is the clinical application of imatinib

CML expression the philadelphia chromosome; GI stroll tumor GIST expressing Kit (CD117); idiopathic hypereosinophilic syndrome

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what are some adverse reactions see with imatinib

edema, myelosuppresion, nausea, muscle cramps, diarrhea, rash

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what is the mechanism of action of sorafenib

inhibits both wild type and mutant B-RAF (RAS/MAP kinase pathway inhibitor)

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what is the mechanism of action of rapamycin (sirolimus)

inhibits mTor but also blocks downstream targets of mTOR such as cyclin D1, c-MYC, BAD, and Hif-1

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what is the mechanism of action of bortezomib

inhibits an active site N-terminal threonine residue within the 20S catalytic subunit of the proteasome

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what is the clinical application of sorafenib

renal cell carcinoma, hepatocellular carcinoma

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what is the clinical application of rapamycin (sirolimus)

prophylaxis for renal transplant rejection

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what is the clinical application of bortezomib

multiple myeloma; mantle cell lymphoma

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what are some adverse effects seen with sorafenib

CV disease, erythema multiform, hand-foot rash, elevated lipase and amylase levels; depressed blood cell counts; neuropathy

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what are some adverse effects seen with rapamycin (sirolimus)

increased susceptibility to infection, lymphoma, malignancy; thrombotic microangiopathy; renal toxicity

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what are some adverse effects seen with bortezomib

HF, neutropenia, thrombocytopenia, neuropathy, hypotension, arthralgia

what else does sorafenib inhibit besides B-RAF

VEGFR-2, PDGFR-2

what drugs should be avoided when using rapamycin (sirolimus)

drugs that induce or inhibit CYP 450

what is the clinical application of bevacizumab

metastatic colorectal cancer; non-small cell lung cancer

what are some adverse reactions seen with bevacizumab

arterial thromboembolism; hypertensive crisis; nephrotic syndrome

what is the mechanism of action of bevacizumab

monoclonal IgG1 antibody against VEFF-A

what is the clinical application of sunitinib

renal cell carcinoma; GI stromal tumor

what is the clinical application of thalidomide

multiple myeloma; erythema nodosum leprosum

what is the clinical application of lenalidomide

multiple myeloma; myelodysplastic syndrome

what are some adverse effects seen with sunitinib

left ventricular dysfunction, anemia; hepatotoxicity; inflammation of mucous membrane; thyroid dysfunction

what is the mechanism of action of sunitinib

inhibits VEGFR-1, VEGFR-2, PDGFR, and other receptor tyrosine kinases

what are some adverse effects seen with thalidomide

teratogenesis, thrombotic disorder, SJS; peripheral neuropathy

what are some contraindications for thalidomide use

pregnancy; women capable of becoming pregnant; males not using latex condom

what is the mechanism of action of thalidomide

inhibits basic fibroblast growth factor (bFGF)-induced angiogenesis; also costimulates T cells

what is thalidomide used in combination with as first line regimen for multiple myeloma

dexamethasone

what are some adverse effects seen with rituximab

significant immunosuppression; anaphylactoid reaction related to chimeric antibodies; hematologic abnormalities; infusion reactions

what is the mechanism of action of lenalidomide

analogue of thalidomide with enhanced inhibition of TNF-alpha and improved T-cell costimulatory properties, while maintaining antiangiogenic activity

what is the mechanism of action of rituximab

anti-CD20 antibody

what is the clinical application of fluorouracil (5-FU)

breast cancer, GI cancers, skin cancer (topical application)

what are some adverse reactions seen with fluorouracil

coronary atherosclerosis, cerebellar syndrome, visual changes, stenosis of lacrimal system; photosensitivity

what are some contraindications to fluorouracil use

severe bone marrow depression, poor nutritional state, serious infection, dihydropyrmidine dehydrogenase deficiency, pregnancy

what is the mechanism of action of fluorouracil

inhibits thymidylate synthase by binding to the deoxyuridylate (substrate) site on the enzyme

what can be used to potentiate the action of fluorouracil

folinic acid

what is the clinical application of capecitabine

metastatic colorectal cancer; breast cancer

what are the contraindications to capecitabine use

dihydropyrimidine dehydrogenase deficiency; severe renal impairment

what is the orally available prodrug for of 5-FU

capecitabine

what is the mechanism of action of 6-mercaptopurine (6-MP) and azathioprine

inhibits IMPDH and other synthetic enzymes, thereby interfering with AMP and GMP synthesis

what is the main clinical application of 6-mercaptopurine

acute lymphoblastic leukemia

what are the clinical applications of azathioprine

immunosuppression in renal transplantation, rheumatoid arthritis, IBD

what are some adverse reactions seen with 6-mercaptopurine (6-MP) and azathioprine

pancreatitis, myelosuppresion, hepatotoxicity, infection; gastritis

what is a contraindication for 6-mercaptopurine (6-MP) and azathioprine

pregnancy

what is the mechanism of action of hydroxyurea

inhibit ribonucleotide reductase (enzyme that converts ribonucleotides to deoxyribonucleotides)

what are the clinical applications of hydroxyurea

myeloproliferative disorders, hematologic malignancies, head/neck cancers, melanoma, ovarian carcinoma; sickle cell anemia (adults only)

what are some adverse reactions seen with hydroxyurea

secondary leukemia with long term use; GI toxicity; skin ulcer

what is a contraindication for hydroxyurea use

severe bone marrow depression

what is the mechanism of action of thioguanine

incorporation into DNA and RNA results in inhibition of DNA polymerase, thereby causing cell death

what is the clinical application of thioguanine

acute myelogenous leukemia

what are some adverse reactions seen with thioguanine

hyperuricemia, intestinal perforation, hepatotoxicity

what analogue is cladribine

adenosine

what is the clinical application of cladribine

hairy cell leukemia, multiple sclerosis

what are some adverse reactions seen with cladribine

febrile neutropenia, neurotoxicity

what analogue is cytarabine

cytidine

what are the clinical applications of cytarabine

acute lymphoblastic and myelogenous leukemia; CML; meningeal leukemia; hodgkin's disease; non-hodgkin lymphoma

what are some adverse reactions seen with cytarabine

neuropathy, nephrotoxicity, liver dysfunction; ulcers of mouth and anus

what is the mechanism of action of cyclophosphamide

covalently bind DNA, often cross-like to DNA or associated proteins

what are the clinical applications of cyclophosphamide

autoimmune diseases, leukemias & lymphomas; advanced mycosis fungoides; neuroblastoma; ovarian cancer; retinoblastoma; malignant histiocytosis

what are some adverse reactions seen with cyclophosphamide

cardiomyopathy, SJS, hemorrhagic cystitis, azoospermia, alopecia, amenorrhea

what is a contraindication for cyclophosphamide use

severely depressed bone marrow function

what metabolite of cyclophosphamide can cause hemorrhagic cystitis and how can it be prevented

acrolein; prevented with co-administration of meson

what is the clinical application of mitomycin

gastric pancreatic cancer

what is the clinical application of thiotepa

bladder cancer

what is the clinical application of carmustine

brain cancer

what is the clinical application of dacarbazine

hodgkins disease

what is the clinical application mom procarbazine

hodgkins disease

what is the clinical application of altretamine

ovarian cancer

what is a contraindication for mitomycin use

coagulation disorder or renal impairment

what is a contraindication for thiotepa use

hepatic, renal or bone marrow dysfunction

what is a alkylating antibiotic that targets hypoxic tumor cells

mitomycin

what is the mechanism of action of cisplatin and carboplatin

cross-link intrastrand guanine bases

what is the clinical application of cisplatin and carboplatin

genitourinary cancers; lung cancers

what is the dose limiting toxicity of cisplatin

nephrotoxicity

what are some contraindications for cisplatin and carboplatin use

severe bone marrow depression; renal/hearing impairment

what can be co-administered with cisplatin to limit nephrotoxicity

amifostine

what is the mechanism of action of bleomycin

binds oxygen and chelates Fe(II); binds DNA and leads to strand breaks via generation of oxidative intermediates

what is the clinical application of bleomycin

testicular cancer; hodgkin disease

what is the dose-limiting toxicity of bleomycin

pulmonary fibrosis

what is the clinical application of irinotecan

colorectal cancer

what is the clinical application of topotecan

small cell lung cancer, cervical carcinoma, ovarian cancer

what are some adverse reactions seen with irinotecan and topotecan

life-threatening diarrhea, febrile neutropenia, alopecia, eosinophilia

what stage in the cell cycle are irinotecan and topotecan specific for and what do they inhibit

S phase; inhibit topoisomerase 1

what are the clinical applications of doxorubicin

leukemias, lymphomas, breast cancer, bladder cancer, thyroid cancer, GI cancer, nephroblastoma, osteosarcoma, ovarian cancer, small cell lung cancer; soft tissue sarcoma

what is a major adverse reaction seen with doxorubicin

heart failure

what are some contraindications for doxorubicin

preexisting heart failure, severe bone marrow depression

what does doxorubicin inhibit and what stage of the cell cycle does it target

inhibits topoisomerase 2; G2 phase

what is the clinical application of etoposide

testicular and lung cancer; leukemia

what does etoposide inhibit and what stage of the cell cycle does it target

inhibits topoisomerase 2; action is specific to late S phase and G2 phases

what is the mechanism of action of vinblastine

bind tubular subunits and prevent microtubule polymerization

what are some adverse reactions seen with vinblastine

myelosuppresion, azoospermia, alopecia, bone pain

what are some contraindications for vinblastine use

bacterial infection; significant granulocytopenia

what is the dose-limiting toxicity of vinblastine

bone marrow suppression

what are some contraindications for vincristine use

charcot-marie-tooth syndrome; intrathecal use

what is the dose limiting effect of vincristine

peripheral neuropathy

what agent that inhibits microtubule polymerization can lead to diplopia as an adverse effect

vincristine

what is the dose limiting toxicity of paclitaxel

peripheral neuropathy

what is the clinical application of paclitaxel

ovarian cancer, non-small cell lung cancer; AIDS-related kaposis sarcoma

what are the most common clinical uses for docetaxel

breast cancer; non-small cell lung cancer

what is the dose limiting toxicity of docetaxel

myelosuppression