Antineoplastic Agents
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| Alkylating agents ? | * Nitrogen mustard - cyclophosphamide and
mechlorethamine ..... * procarbazine
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| Antimetabolites ? | * Antifolates - methotrexate .... * Pyrimidine antimetabolites - cytarabine..... * Purine antimetabolites - 6-mercaptopurine,
6-thioguanine, fludarabine
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| Natural products ? | * Antimitotic drugs - vincristine and
vinblastine
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| Antibiotics ? | * doxorubicin
- daunorubicin -
idarubicin
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| Enzymes ? | * L-asparginase
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| Retinoids ? | * ATRA
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| Glucocorticoids ? | * prednisone and dexamethasone
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| Antibodies ? | * rituximab
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| Protein tyrosine kinase inhibitors ? | * imatinid and dasatinib
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| Histone deacetylase (HDAC) inhibitors ? | * vorinostat
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| Proteasome inhibitors ? | * bortezomib
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| MOA of Alkylating agents ? | * alkylate the N7 position of guanine in DNA and cross-links covalently bind two together --> causes strand breaks and apoptosis
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| why the toxicity ? | * excessive cross-linking
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| Alkylating Agents SEs ? | * potentially carcinogenic, can cause sterility, VOD (venous occlusive disease)of liver
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| Nitrogen mustards - Alkylating agent MOA and SEs ? | * cross link DNA.... * SEs = see BM depression (dose related)
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| Cyclophosphamide ? | * most versatile and used alkylating agent and is used in lots of cancers .... * Requires hepatic activation (P450)
-- a prodrug requiring metabolic activation in the liver
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| Cyclophosphamide metabolism metabolites ? | * phosphoramide mustard = anti-cancer metab .... * acrolein - toxic metab where we see bladder hemorrhaging
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| Cyclophosphamide SEs ? | * BM depression ..... * Hemorrhagic Cystitis - treat with hydration and of Mesna or N-acetylcysteine (NAC)
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| Mechlorethamine basics and SEs ? | * not as broad spectrum as Cyclophos ..... * See high emetic frequency with even looking at this drug
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| procarbazine use ? | * Treatment of Hodgkin lymphoma
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| Procarbazine MOA ? | * Inhibits DNA, RNA, and protein synthesis
---- Inhibits transmethylation of methyl groups of methionine into transfer RNA
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| Procarbazine – Side effects ? | * CNS toxicity and disulfiram-like reaction
( puke with alcohol) ...... * Inhibits MAO - watch tyramine rich foods in these pts.
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| Antimetabolites general MOA and SEs? | * act by starving the DNA precursors so they can't be used .... * see BM depression and GI issues
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| Antifolates - methotrexate use ? | * leukemias, lymphomas, and RA
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| MTX MOA ? | * Folic acid analog (antagonist)
--- inhibits dihydrofolate reductase (DHFR)
---> loss of TMP
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| High Dose Methotrexate ? | * Used for CNS prophylaxis in pts with leukemia and high-risk lymphoma.... * give with Leucovorin --> reduces toxicity (DHFR inhibition) in normal cells and gives the body back its folate
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| MTX SEs ? | * BMD and GI ulcerations
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| Pyrimidine Antimetabolites - cytarabine uses and SEs ? | * Prodrug converted to ara-CTP
competes with dCTP & inhibits DNA synthesis
and is rapidly cleared, constant infusion is needed.... * Uses: Hematological (AML, ALL, NHL) .... * SEs = BMD and HYPERuricemia
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| Purine analogs - 6-Mercaptopurine and 6-thioguanine uses ? | * AML, ALL, CML
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| 6-Mercaptopurine and 6-thioguanine MOA ? | * turns in to a nucleotide analog and then inhibits synthesis of purine nucleotides -->
leads to decreased RNA & DNA synthesis..... * inhibits the rate limiting step of guanine synthesis, IMPDH
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| 6-mercaptopurine also blocks ? | * inhibits AMP synthesis along with its guanine inhibition
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| When must 6-Mercaptopurine dose be lowered ? | * when using allopurinol concurrently bc it inhibits xanthine oxidase, which breaks down 6-Merc... --> higher toxicities
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| Side effects/toxicities of Purine Analogs ? | * BMD , Hyperuricemia , and Hepatotoxicity
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| Anti-metabolite -- Fludarabine use ? | * CLL
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| Fludarabine MOA ? | * Inhibits DNA synthesis (deoxyadenosine analog)
--- by DNA polymerase, DNA primase, DNA ligase
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| Fludarabine SEs ? | * black box for -- Autoimmune effects , Bone marrow suppression, Neurotoxicity..... * also see Progressive multifocal leukoencephalopathy
-- usually fatal ...... *
Tumor lysis syndrome
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| Antimetabolites - Summary ? | * cell cycle dependant (needs cells to divide to work)
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| Antimitotic Drugs -- Vincristine and Vinblastine MOA ? | * Binds to beta-tubulin -->
inhibits microtubule polymerization
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| Vincristine uses ? | * Leukemias, lymphomas (non-Hodgkin’s )
-- Treatment of choice to induce remissions in lymphocytic leukemia
..... * Hodgkin’s disease
..... * Wilms’ tumor..... * neuroblastoma
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| Vincristine SEs ? | * Neurological toxicity (dose-limiting)
.... * FATAL if given intrathecally
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| Vinblastine uses ? | * Hodgkin's and non-Hodgkin's lymphoma
...... * Testicular cancer; breast cancer; Kaposi sarcoma
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| Vinblastine SEs ? | * Myelosuppression --- dose limiting BMD ( vinBlastine ) ...... * no neuro
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| Antibiotics - doxorubicin, daunorubicin , idarubicin MOA ? | * Intercalates into DNA
---> blocks DNA and RNA synthesis
..... * Inhibits topoisomerase II
leads to strand breaks and apoptosis
...... * Free radical formation b/c powerful iron chelator (sponge)
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| Anthracycline that is most broad spectrum and the least ? | * Most = Doxorubicin ..... * Least = Idarubicin
(AML only)
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| Anthracycline SEs ? | * BMD and Cardiotoxicity (ruby red for heart)
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| Enzymes - L-Asparaginase use and MOA? | * Standard agent for treating lymphocytic leukemia including ALL .... * Hydrolyzes circulating L-asparagine needed for cells (starves them)
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| L-Asparaginase Side Effects ? | * Anaphylaxis and serious allergic reactions
..... * Coag issues .... * Pancreatitis ..... * Azotemia
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| Retinoids - ATRA use and MOA ? | * Use: acute promyelocytic leukemia (APL).... * MOA: provides homeostasis back to AML cells
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| ATRA SEs ? | * Black Box: APL differentiation syndrome and
Leukocytosis ..... * abnormal LFTs and hypertriglyc/cholesterolemia
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| Glucocorticoids - Prednisone and Dexamethasone uses ? | * Suppresses lymphocyte proliferation
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| Targeted agents - Antibodies -- Rituximab use and MOA ? | * Use: CD20-pos issues ...... * MOA: monoclonal antibody directed against the CD20 antigen on B-lymphocytes
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| Rituximab SEs ? | * Black Box: HBV Reactivation (so get HepB tested), infusion-related reactions
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| Tyrosine kinase inhibitor - Imatinib use and MOA ? | * USE: CML .... * MOA: Inhibits Bcr-Abl tyrosine kinase --> signal transduction inhibition
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| Imatinib SEs ? | * fluid retention/edema , CV HF/LVD ,
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| Tyrosine kinase inhibitor - Dasatinib MOA ? | * Inhibit both Bcr-Abl and Src kinases
--- HIGHLY more potent on BCR than Imatinib, and good against BCR mutations.... *
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| Dasatinib SEs ? | * QT prolongation
--- Pulmonary arterial hypertension (PAH)
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| Histone deacetylase (HDAC) inhibitors --- Vorinostat Use and MOA ? | * Use: Cutaneous T-cell lymphoma ...... * MOA: Inhibits histone deacetylase (HDAC)
---> remove acetyl groups --> Alters/Shuts Down transcription factors ….. Leads to cell cycle arrest
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| Vorinostat SEs ? | * Hyperglycemia
---- QTc prolongation --- Thromboembolism
--- Myelosuppresion -->
thrombocytopenia and anemia
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| Proteasome inhibitors - Bortezomib Use and MOA ? | * Use: multiple myeloma
...... * Reversibly inhibits 26S proteasome --
disrupts various cell signaling pathways
- (ex. inhibits nuclear factor (NF)-kappaB)
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