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39 Cards in this Set
- Front
- Back
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Cyclophosphamide
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Causes irreversible DNA crosslinking, crosslinks proteins and RNA
Side Effects: teratogenic, mutagenic and carcinogenic |
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Methotrexate
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Antimetabolite: Folic acid analog, inhibits dihydrofolate reductase
Retards DNA/RNA synthesis, interferes with methionin synthesis a causing protein synthesis problems |
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Mercaptopurine (6-MP)
Azathioprine 6-Thioguanine (6-TG) |
Antimetabolites: Thiopurines
Pair with C and T, causing mutations in DNA and prevent de novo purine synthesis (inhibit thiopurine methyl transferase) Delayed toxicitity because it needs to pass through S-phase |
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Fluorouracil (5-FU)
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Antimetabolite
1. FdUMP - Blocks thymidylare synthase 2. FdUTP - induced nucleotide excision repair, which leads to strand breaks 3. FUTP - Incorporated into RNA, has wide effects on cell metabolism and viability |
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Vinblastine / Vinca Alkaloids
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Bind tubulin, prevent mitotic spindle formation (metaphase arrest)
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Paclitaxel
Taxol |
Taxoids from yew tree bark
Induces polymerization and stabilization of microtubules |
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Actinomycin D
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Streptomyces derived
Large planar structure, intercalates in DNA and inhibits DNA transcription and synthesis |
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Doxorubicin
Adriamycin |
Streptomyces derived
Large planar structure, intercalates in DNA and inhibits DNA transcription and synthesis |
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Mitomycin
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Streptomyces derived
Activated intracellularly, reactive -NH group binds with DNA and inhibits synthesis |
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Bleomycin
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Large structure with lots of sulfur and nitrogens
Chelates metal ions, producing reactive free-radical oxygen species |
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Topotecan
Irinotecan |
Camptothecins
Inhibits topoisomerase I leading to single-strand DNA breaks Inhibits replication and transcription |
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Etoposide
Teniposide |
Epopodophyllotoxins
Inhibit topoisomerase II, leading to double-strand DNA breaks |
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Cisplatin
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Platinum based
Crosslinks DNA |
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Arsenic trioxide
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It's potent, but don't kill your patient okay
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Asparaginase
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Bacteria derived enzyme
Asn -> Asp + NH3 depletes Asn levels Conjugate to polyethylene glycol (PEG) |
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Flutamide
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anti-androgen
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Tamoxifen
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anti-estrogen
affects α- and β-receptors differently, acting as an agonist or antagonist (selective receptor modulators) |
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Tretinoin
All-trans retinoic acid (ATRA) |
Disease: Acute promyelocytic lukemia
Activity: Binds to t(15;17) fusion protein, activiting retionic acid receptor (RAR) and re-enabling blocked gene activity Side effects: Teratogenic, sunlight sensitivity, skin irritation |
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Alitretinoin
9-cis-retinoic acid |
Disease: AIDS-related Kaposi's sarcome
Activity: Similiar to tretinoin, but binds to both RAR and RXR receptors |
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Bexarotene
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Disease: cutaneous T cell lymphoma (off-label: lung cancer, breast cancer, Kaposi's sacroma)
Activity: Targets RXR |
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Gleevec
Imatinib |
Disease: Chronic Myeloid lukemia Ph+; Acute lymphocytic lukemia Ph+; gastrointestinal stromal tumors
Activity: Tyrosine kinase inhibitor (Abl intracellularly, cKit and PDGFR membrane receptors) |
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Herceptin
Trastuzumab |
Disease: Breast, ovarian, and endometrial cancer that over-expresses HER2/Neu
Activity: humanized monoclonal antibody, interferes with dimerization of HER2/Neu and slows cell proliferation Side effects: Cardiac dysfunction |
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Lapatinib
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Disease: Breast, ovarian, and endometrial cancer overexpressing HER2/Neu or EGFR
Activity: Kinase inhibitor SE: Nausea, vomiting, heartburn, fatigue |
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Erlotinib
Tarceva |
Disease: Advanced non-small cell lung carcinoma (NSCLC)
Activity: Epidermal Growth Factor Receptor (EGFR) Kinase inhibitor SE: Rash, diarrhea, fatigue |
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Gefitinib
Iressa |
Disease: Non-small cell lung carcinoma (NSCLC)
Activity: Epidermal Growth Factor Receptor (EGFR) SE: Acne, diarrhea, nausea, vomiting |
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Cetuximab
Erbitux |
Disease: Squamous cell carcinoma and colon cancer
Activity: Monocolonal Antibody which prevents EGF receptor binding. Only effective in absence of K-Ras mutations |
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Bevacizumab
Avastin |
Disease: Metastatic colorectal cancer, NSCLC (off-label: age-related macular degeneration)
Activity: Vascular Endothelial Growth Factor (VEGF) antibody, prevents VEGF receptor binding (angiogenesis inhibitor) SE: bleeding, bowel perforation |
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Sunitinib
Sutent |
Diease: Renal cell carcinoma (RCC), imatinib-resistant gastrointestinal stromal tumor (GIST)
Activity: VEGFR, PDGFR, and cKit inhibitor (angiogenesis inhibitor) |
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Sorafenib
Nexavar |
Disease: Renal cell carcinoma (RCC) and unresectable hepatoceuular carcinoma
Activity: Inhibitor of VEGFR2, VEGFR3, PDGFR, cKit, Raf-1, B-Raf (angiogenesis inhibitor) |
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Vemirafenib
Zelboraf |
Disease: Late-stage melanoma
Activity: Inhibits V600E B-Raf, but not wild-type B-Raf (seen in 60% of melanoma) |
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Bortezomib
Velcade |
Disease: Multiple myeloma
Activity: Inhibits 26S subunit of proteasome |
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Azacitidine
Vidaza |
Disease: myelodysplastic syndrome (pre-lukemia)
Activity: Identical structure to cytosine except position 5 of the pyrimidine ring is a N instead of C. Incorporated into DNA and RNA, and irreversibly inhibits DNA methyltransferase (DNMT). (DNA demethylating agent) |
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5-Aza-2'-deoxycytidine
Decitabine |
Disease: Myelodysplastic syndrome
Activity: Identical structure to cytosine except 5' of the pyrimidine ring is a N instead of C and is deoxy at the 2' ribose. Incorporated into DNA, and irreversibly inhibits DNA methyltransferase (DNMT). (DNA demethylating agent) |
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Vorinostat/SAHA
Zolinza |
Disease: Cutaneous T-cell lymphoma
Activity: histone deacetylase inhibitor |
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Romidepsin
Istodax |
Disease: Cutaneous T-cell lymphoma
Activity: Histone deacetylase inhibitor |
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Interleukin-2
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Disease: Metastatic renal cell carcinoma; malignant melanoma
Activity: Increases immune activity SE: T-cell induced capillary damage |
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Interferon-α 2a (IFN-α 2a)
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Disease: Renal cell carcinoma
Activity: Increases immune activity SE: life-threatening myelosuppression; flu-like symptoms |
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Interferon-γ (INF-γ)
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Disease: Renal cell carcinoma
Activity: Increases immune activity SE: GI upset, flu-like symptoms |
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Levamisole
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Disease: Colon, head and neck cancer, melanoma
Activity: Non-specific immunostimulator SE: suppresses leukocyte production; inflammatory destruction of blood vessels Fun Fact: Founds in 82% of seized cocaine |
