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34 Cards in this Set
- Front
- Back
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Methotrexate
Trimetrexate |
Antimetabolites
Folate antagonists Folic acid mimic that inhibits the enzyme DHFR Prodrug activated by enz. addition of several glu |
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tetrahydrofolate (THF)
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Required methyl and methylene group donor for thymidine and purine biosynthesis
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leucovorin rescue
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Reduced folates
used with high dose MTX regimes to restore pools of folate so normal cells survive |
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Hydroxyurea
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Deoxynucleotide synthesis antagonist
Inhibits ribonucleotide reductase (reduces NDPs to dNDPs) |
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Fluoropyrimidines
(5-FU, fluorodeoxyuridine, ftorafur) |
Pyrimidine synthesis antagonists
- active 5-F-dUMP covalently modifies thymidylate synthase (TS converts dUMP to TMP) -Can also cause strand breaks - Leucovorin enhances binding of 5-FU to TS 5-FU must be activated by TP, TK and pyrm. kinases |
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6-mercaptoprine
6-thioguanine |
Purine Biosynthesis Antagonists
-competitive inhibitors of enzymes in purine syn pathway -RNA and DNA incorporation |
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Gemcitabine
Cytosine arabinoside Fludarabine 5-azacytidine 2-chlorodeoxyadenosine |
Inhibitors of DNA Polymerase
-nucleoside analogues -BLOCK DNA STRAND ELONGATION |
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Imatinib (Gleevec)TM
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Signal Transduction Inhibitor
-Receptor and Non-Receptor Protein Kinases Inhibitor --Inhibits autophosphorylation of three TKs remember BCR-ABL |
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Trastuzumab (Herceptin)
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Signal Transduction Inhibitor
-Receptor Protein Kinase Inhibitor --humanized MAb, binds HER2 BREAST CANCER |
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Cetuximab
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Signal Transduction Inhibitor
-Receptor Protein Kinase Inhibitor -- anti-EGFR MAb COLORECTAL CANCER, HEAD-AND-NECK TUMORS |
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Gefitinib
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Signal Transduction Inhibitor
--EGFR tyrosine kinase inhibitor(TKI) NON-SMALL CELL LUNG CANCER |
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Protease Inhibitors
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Anti-angiogenesis drugs
Block breakdown of ECM ex: Neovastat |
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Gleevec (Part II)
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Anti-angiogenesis drug
**Inhibitor of endothelial cell proliferation PK (PDGF, VEGF, FGF) Inhibitors |
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Endostatin, angiostatin
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Anti-angiogenesis drugs
Inhibitors of endothelial cell proliferation |
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Fumagillin
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Anti-angiogenesis drug
**Inhibitor of endothelial cell proliferation Fungal product |
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Bortezomib or Velcade
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Proteasome Inhibition
Boronic acid dipeptide inhibitor -Targets chymotrypsin-like active site of proteasome Inhibition of proteasome--> no degradation of IkB--> IkB blocks txn NF-kB ( NF-kB promotes cancer cell survival) |
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mechlorethamine
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Alkylating agent
Nitrogen mustard Use: Hodgkin's Disease Acute toxicity- nausea/vomiting, phlebitis Dose-limiting- Bone marrow suppression |
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melphalan
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Alkylating agent
"Substituted" nitrogen mustard Use: multiple myeloma Dose-lim: bone marrow supp |
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chlorambucil
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Alkylating agent
"Substituted" nitrogen mustard Use: CLL Dose-lim: Bone marrow supp |
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cyclophosphAMIDE
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Alkylating agent
Modified nitrogen mustard **Most commonly used alkylating agent Metabolic act. by CYP450s Use: non-Hodgkin's Lymphoma, Breast cancer Delayed/Dose-limiting- Bone marrow supp, Hemorrhagic cystitis (from acrolein) |
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ifosfAMIDE
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Alkylating agent
Modified nitrogen mustard Structural analog of cyclophosphamide Use: Sarcomas Tox: bone marrow supp, hemorrhagic cystitis Metabolic act. by CYP450s |
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carmustine
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Alkylating agent
Nitrosurea Use: brain tumors Tox: bone marrow suppression |
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streptozotocin
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Alkylating agent
A Nitrosurea An Antibiotic Use: islet cell tumors Tox: n/v, nephrotoxicity, hepato-, bms, DM |
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thiotepa
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Alkylating agent
Aziridines Use: breast cancer Tox: bms |
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mitomycin C
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Alkylating agent
Aziridines antibiotic tox: fever, n/v, bms Rare side effects: hemolyticuremic syndrome (HUS) |
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busulfan
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Alkylating agent
Alkane sulfonate Use: bone marrow tx Side effects: bms |
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procarbAZINE
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Alkylating agent
Methylating agent Tox: bms, secondary leukemia |
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dacarbAZINE
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Alkylating agent
Methylating agent Use: Hodgkin's disease Side effects: bms |
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cisPLATIN
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Platinum compound
Use: cancers in epithelial organs, and testis cancer Side effects:**nephrotoxicity, ototoxicity, peripheral neuropathy, bms, SEVERE N/V KEY LETHAL AGENT MAY BE SQUELCHING MECH. VIA DNA-PROTEIN CROSSLINK |
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carboPLATIN
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Platinum compound
Use: cancers in epithelial organs, and testis cancer side effects: bms |
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oxaliPLATIN
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Platinum compound
Side effects: bms, neurotoxicity, diarrhea |
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bifunctional alkylating agents
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INTRAstrand DNA crosslinking
INTERstrand DNA crosslinking Crosslinking DNA to proteins, RNA, other macromolecules |
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monofunctional alkylating agents
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mispairing of modified base leading to mutation
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Why are hematopoietic stem cells resistant to cyclophosphamide?
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Aldehyde dehydrogenase
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