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Anti-Cancer Drugs
Antineoplastic Agents
| Question | Answer |
|---|---|
| Alkylating agents ? | * Nitrogen mustard - cyclophosphamide and mechlorethamine ..... * procarbazine |
| Antimetabolites ? | * Antifolates - methotrexate .... * Pyrimidine antimetabolites - cytarabine..... * Purine antimetabolites - 6-mercaptopurine, 6-thioguanine, fludarabine |
| Natural products ? | * Antimitotic drugs - vincristine and vinblastine |
| Antibiotics ? | * doxorubicin - daunorubicin - idarubicin |
| Enzymes ? | * L-asparginase |
| Retinoids ? | * ATRA |
| Glucocorticoids ? | * prednisone and dexamethasone |
| Antibodies ? | * rituximab |
| Protein tyrosine kinase inhibitors ? | * imatinid and dasatinib |
| Histone deacetylase (HDAC) inhibitors ? | * vorinostat |
| Proteasome inhibitors ? | * bortezomib |
| MOA of Alkylating agents ? | * alkylate the N7 position of guanine in DNA and cross-links covalently bind two together --> causes strand breaks and apoptosis |
| why the toxicity ? | * excessive cross-linking |
| Alkylating Agents SEs ? | * potentially carcinogenic, can cause sterility, VOD (venous occlusive disease)of liver |
| Nitrogen mustards - Alkylating agent MOA and SEs ? | * cross link DNA.... * SEs = see BM depression (dose related) |
| 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 |
| Cyclophosphamide metabolism metabolites ? | * phosphoramide mustard = anti-cancer metab .... * acrolein - toxic metab where we see bladder hemorrhaging |
| Cyclophosphamide SEs ? | * BM depression ..... * Hemorrhagic Cystitis - treat with hydration and of Mesna or N-acetylcysteine (NAC) |
| Mechlorethamine basics and SEs ? | * not as broad spectrum as Cyclophos ..... * See high emetic frequency with even looking at this drug |
| procarbazine use ? | * Treatment of Hodgkin lymphoma |
| Procarbazine MOA ? | * Inhibits DNA, RNA, and protein synthesis ---- Inhibits transmethylation of methyl groups of methionine into transfer RNA |
| Procarbazine – Side effects ? | * CNS toxicity and disulfiram-like reaction ( puke with alcohol) ...... * Inhibits MAO - watch tyramine rich foods in these pts. |
| Antimetabolites general MOA and SEs? | * act by starving the DNA precursors so they can't be used .... * see BM depression and GI issues |
| Antifolates - methotrexate use ? | * leukemias, lymphomas, and RA |
| MTX MOA ? | * Folic acid analog (antagonist) --- inhibits dihydrofolate reductase (DHFR) ---> loss of TMP |
| 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 |
| MTX SEs ? | * BMD and GI ulcerations |
| 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 |
| Purine analogs - 6-Mercaptopurine and 6-thioguanine uses ? | * AML, ALL, CML |
| 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 |
| 6-mercaptopurine also blocks ? | * inhibits AMP synthesis along with its guanine inhibition |
| When must 6-Mercaptopurine dose be lowered ? | * when using allopurinol concurrently bc it inhibits xanthine oxidase, which breaks down 6-Merc... --> higher toxicities |
| Side effects/toxicities of Purine Analogs ? | * BMD , Hyperuricemia , and Hepatotoxicity |
| Anti-metabolite -- Fludarabine use ? | * CLL |
| Fludarabine MOA ? | * Inhibits DNA synthesis (deoxyadenosine analog) --- by DNA polymerase, DNA primase, DNA ligase |
| Fludarabine SEs ? | * black box for -- Autoimmune effects , Bone marrow suppression, Neurotoxicity..... * also see Progressive multifocal leukoencephalopathy -- usually fatal ...... * Tumor lysis syndrome |
| Antimetabolites - Summary ? | * cell cycle dependant (needs cells to divide to work) |
| Antimitotic Drugs -- Vincristine and Vinblastine MOA ? | * Binds to beta-tubulin --> inhibits microtubule polymerization |
| Vincristine uses ? | * Leukemias, lymphomas (non-Hodgkin’s ) -- Treatment of choice to induce remissions in lymphocytic leukemia ..... * Hodgkin’s disease ..... * Wilms’ tumor..... * neuroblastoma |
| Vincristine SEs ? | * Neurological toxicity (dose-limiting) .... * FATAL if given intrathecally |
| Vinblastine uses ? | * Hodgkin's and non-Hodgkin's lymphoma ...... * Testicular cancer; breast cancer; Kaposi sarcoma |
| Vinblastine SEs ? | * Myelosuppression --- dose limiting BMD ( vinBlastine ) ...... * no neuro |
| 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) |
| Anthracycline that is most broad spectrum and the least ? | * Most = Doxorubicin ..... * Least = Idarubicin (AML only) |
| Anthracycline SEs ? | * BMD and Cardiotoxicity (ruby red for heart) |
| Enzymes - L-Asparaginase use and MOA? | * Standard agent for treating lymphocytic leukemia including ALL .... * Hydrolyzes circulating L-asparagine needed for cells (starves them) |
| L-Asparaginase Side Effects ? | * Anaphylaxis and serious allergic reactions ..... * Coag issues .... * Pancreatitis ..... * Azotemia |
| Retinoids - ATRA use and MOA ? | * Use: acute promyelocytic leukemia (APL).... * MOA: provides homeostasis back to AML cells |
| ATRA SEs ? | * Black Box: APL differentiation syndrome and Leukocytosis ..... * abnormal LFTs and hypertriglyc/cholesterolemia |
| Glucocorticoids - Prednisone and Dexamethasone uses ? | * Suppresses lymphocyte proliferation |
| Targeted agents - Antibodies -- Rituximab use and MOA ? | * Use: CD20-pos issues ...... * MOA: monoclonal antibody directed against the CD20 antigen on B-lymphocytes |
| Rituximab SEs ? | * Black Box: HBV Reactivation (so get HepB tested), infusion-related reactions |
| Tyrosine kinase inhibitor - Imatinib use and MOA ? | * USE: CML .... * MOA: Inhibits Bcr-Abl tyrosine kinase --> signal transduction inhibition |
| Imatinib SEs ? | * fluid retention/edema , CV HF/LVD , |
| Tyrosine kinase inhibitor - Dasatinib MOA ? | * Inhibit both Bcr-Abl and Src kinases --- HIGHLY more potent on BCR than Imatinib, and good against BCR mutations.... * |
| Dasatinib SEs ? | * QT prolongation --- Pulmonary arterial hypertension (PAH) |
| 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 |
| Vorinostat SEs ? | * Hyperglycemia ---- QTc prolongation --- Thromboembolism --- Myelosuppresion --> thrombocytopenia and anemia |
| Proteasome inhibitors - Bortezomib Use and MOA ? | * Use: multiple myeloma ...... * Reversibly inhibits 26S proteasome -- disrupts various cell signaling pathways - (ex. inhibits nuclear factor (NF)-kappaB) |
Created by:
thamrick800
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