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