4. ALKYLATING AGENTS Mechanism of action : Target DNA, produce alkylation through formation of intermediates. No phase-specific drugs Busulfan Chlorambucil Cisplatin, Carboplatin, Oxaliplatin Cyclophosphamide, Ifosfamide Dacarbazine Mechlorethamine (Nitrogen Mustard) Melphalan Nitrosoureas Procarbazine Streptozotocin Temozolomide Thiotepa
5. ANTIMETABOLITES Mechanism of action : Interfere with DNA synthesis. They are structural analogs or they inhibit several enzymes. S-phase specific Aracytidine Cytarabin Fludarabine Fluorouracil Leucovorin Capecitabine Gemcitabine Hydroxyurea Mercaptopurine Methotrexate Pemetrexed Pentostatin Raltitrexed Thioguanine Trimetrexate Uracil / Tegafur (UFT)
6. ANTITUMOR ANTIBIOTICS Mechanism of action : A variety of mechanisms. They are derived from microorganisms. Cell cycle specific drugs Actinomycin-D Bleomycin Daunorubicin Doxorubicin Doxorubicin Liposomal Epirubicin Idarubicin Mitomycin Mitoxantrone
7. MITOTIC SPINDLE AGENTS Mechanism of action : Bind to microtubular proteins, thus inhibit microtubule assembly resulting in dissolution of the mitotic assembly structure. M- phase specific drugs. Docetaxel Paclitaxel Vinblastine Vincristine Vindesine Vinorelbine
8. TOPOISOMERASE INHIBITORS Mechanism of action : DNA Topoisomerases I and II are essential enzymes for transcription, replication and mitosis. The following drugs are able to inhibit these enzymes. Topoisomerease I inhibitors Irinotecan Topotecan Topoisomerase II inhibitors Etoposide Teniposide
17. CHEMOTHERAPY TOXICITIES ( I ) Bone m arrow s uppression (anemia, leucopenia, thrombocytopenia) Almost all Erythropoietin, G-CSF, blood transfusions TOXICITY DRUG INDUCED ANTIDOTE Nausea- v omiting Platinum Anthracyclines Alkylating s Centrones (serotonin block): granisetron , ondasetron Alopecia Anthracyclines Taxanes Scalp-cooling techniques (not universally accepted) Cardiotoxicity Anthracyclines Cyclophosphamide 5-FU Early detection . Dexrazoxane
18. CHEMOTHERAPY TOXICITIES ( II ) Pulmonary toxicity Bleom y c i n Alkylating s Gemcitabine Early detection . Corticosteroids Nephrotoxicity Platinum Methotrexate (âdose) Adequate hydration Neurotoxicity Alkaloids Platinum Taxanes Early detection Gonadal d amage Alkylatings Others Sperm preservation Second m alignancies Alkylating s Avoid if possible responsible drugs and/or RT in curable diseases
34. SMALL MOLECULES AND INTRACELLULAR SIGNAL TRANSDUCTION TYROSINE KINASE INHIBITORS
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Hinweis der Redaktion
The original hypothesis for Iressa was that in a number of tumours EGFR expression was associated with a poor prognosis and that inhibition of the enzyme would have a number of effects that would impact on tumour growth. This hypothesis was supported by preclinical data.