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Class III Natural Products
- Antimitotic Drugs
- DNA Topoisomerase Inhibitors
- Antibiotics
- Enzymes
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DNA Topoisomerase Inhibitors
- Camptothecins
- Podophyllotoxins
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Antibiotics
- Anthracycline
- Dactinomycin/Actinomycin D
- Bleomycin
- Mitomycin
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Vinca Alkaloids
- block cells in mitosis by binding to B-tubulin and inhibiting its ability to polymerize with a-tubulin into microtubules.
- M-Phase Specific
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Taxanes
- Binds to site on B-Tubulin that promotes microtuble formation
- M-Phase specific
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Camptothecins
- Bind to and stabilize DNA topoisomerase I cleavable complex
- S-Phase specific
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Podophyllotoxins
- Form a ternary complex with topoisomerase II and DNA preventing resealing of the break.
- S and G2 phase specific
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Anthracycline
- form tripartite complex with topoisomerase II and DNA
- Intercalate in DNA directly affecting transcription and replication
- tetracyclic ring connected to daunosamine sugar.
- S-Phase specific
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Dactinomycin/Actinomycin D
- phenoxazone ring intercalates in DNA while polypeptide chains block transcription of DNA by RNA polymerase
- S-Phase specific
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Bleomycin
- DNA Cleaving antibiotic
- Basic water soluble glycopeptides
- S-phase specific
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Mitomycin
- Bifunctional or trifunctional alkylating agent after activation
- Radiosensitizer
- Structure contains azaurdine group and quinone group with mitosane ring
- Non-phase specific
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L-Asparaginase
- Hydrolysis of Asparagine to aspartic acid and ammonia, depriving cells of asparagine necessary for growth
- Non-phase specific.
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Class IV Antineoplastic Drugs : Miscellaneous Agents
- Hydroxyurea
- Differentiating Agents
- Protein Tyrosine Kinase inhibitors
- Proteasome Inhibitor
- Monoclonal Antibodies
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Hydroxyurea
- inhibits ribonucleoside diphosphate reductase
- -conversion of ribonucleotides to deoxyribonucleotides
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Differentiating Agents
- Vitamin D, Retinoids, HDAC inhibitors
- Induce differentiation of cancerous cells
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Protein Tyrosine Kinase inhibitors
- Imatinib/Gleevec
- Gefitinib
- Erlotinib/Tarceva
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Imatinib/Gleevec
Inhibits BCR-ABL Kinase
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Gefitinib
Inhibits EGFR/ErbB1/Her1 Kinase
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Erlotinib/Tarceva
Inhibits EGFR/ErbB1/Her1 Kinase
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Bortezomib
- Reversible inhibitor of chymotrypsin-like activity of proteosome
- -disrupts signaling cascades
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Proteasome Inhibitors
Bortezomib
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Monoclonal Antibodies
- Trastuzumab/Herceptin
- Bevacizumab/Avastin
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Trastuzumab/Herceptin
Inhibits dimerization of ErbB2/Her2 kinase
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Bevacizumab/Avastin
Inhibits VEGF, blocking angiogenesis
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