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Anti-cancer Agents (Alkylating Agents (Nitrosoureas (E.g- CARMUSTINE,…
Anti-cancer Agents
Alkylating Agents
Nitrogen mustards
Derivatives of mustard gas which forms bifunctional DNA adducts. The prodrugs are activated in the liver by Cytochrome P450 enzymes. E.g- CYCLOPHOSPHAMIDE and IFOSFAMIDE
Nitrosoureas
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Alkylation of DNA and forms carbamoyl adducts with proteins. Can also pass through the BBB so it can be used for the treatment of brain tumours, myelomas and Hodgkin's lymphoma
Form covalent bond with DNA which then inhibits DNA synthesis during S phase. They form irreversible bonds on guanine residues on the same or adjacent strands. Intra and inter chain linking occurs and during replication some parts of the DNA is unpaired making it more susceptible to alkylation.
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Antimetabolites
Folate antagonists
Folate metabolism- Required for the synthesis of purine nucleotides and thymidylate which are essential for DNA synthesis and cell division. FOLATE--> DHF-->THF--> CH2THF-->CH3THF--> Purine Biosynthesis
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METHOTREXATE- Inhibits the metabolism of folates by inhibiting the action of Dihydrofolate Reductase which converts folate to THF. Maximal effects are S-phase specific (specific to the synthesis phase)
Folinic Acid is used with a high dose of MTX as a form of rescue for the highly proliferating cells of the bone marrow and GI mucosa
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General MOA: Acts by competition, block or subvert metabolic pathways in the biosynthesis of DNA
Cytotoxic Antibiotics
Antracyclines
DOXORUBICIN- Interacts with DNA by intercalation and prevents correct uncoiling and exposure of DNA by stabilising DNA-topoisomerase complex 2. Used to treat leukaemias, lymphomas and solid tumours. Adverse effects: cardiac toxicity- produces oxygen radical which are normally inactivated by catalase and glutathione peroxidase
They are flat molecules which interpose themselves between the coils of DNA strands and cause inhibition of macromolecular biosynthesis
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