anti cancer drug

• Cell cycle-specific anticancer drugs:

  • S phase specific drugs: Antimetabolites, Epipodophyllotoxins, Camptothecins
  • G1 phase specific drug: L-asparaginase
  • G2 phase specific drug: Bleomycin
  • M phase specific drugs: Taxanes, Vinca alkaloids
• Cell cycle non-specific anticancer drugs:

  • Alkylating agents: Cyclophosphamide, Busulfan, Lomustine
  • Antitumor antibiotics: Actinomycin D, Mitomycin C
  • Anthracyclines: Doxorubicin, Daunorubicin
  • Platinum analogues: Cisplatin, Oxaliplatin, Carboplatin
• Role of drug combinations in cancer therapy:

  • Enhanced effect by achieving maximal cell killing
  • Broaden the range of attack as drugs in the combination kill heterogeneous cells
  • Reduce resistance by early/rapid cell kill
  • Reduction in the toxicity of individual drugs as lower dose of individual drugs is sufficient to kill cells
• General toxicities of anticancer drugs:

  • Toxic to rapidly dividing normal cells
  • Bone marrow cells: myelosuppression, thrombocytopenia, leukopenia
  • Gut mucosa: GI bleeding and ulcers
  • Skin and hair: Alopecia
  • Gonads: Infertility
  • Fetus: Fetal death and teratogenic effects
  • Tumor Lysis Syndrome: hyperuricemia, urate nephropathy, hyperphosphatemia
  • Hypersensitivity reactions: rashes, chills, fever, anaphylaxis
  • Nausea and vomiting
• Specific toxicities of anticancer drugs:

  • Cyclophosphamide: hemorrhagic cystitis
  • Doxorubicin: cardiotoxicity
  • Bleomycin: pulmonary fibrosis
  • Vincristine: neuropathy, syndrome of inappropriate antidiuretic hormone secretion
  • Cisplatin: nephrotoxicity, ototoxicity
  • Methotrexate: hepatotoxicity, nephrotoxicity, megaloblastic anemia
• Oral and dental problems associated with cancer chemotherapy:

  • Xerostomia (treated with artificial saliva, amifostine - cytoprotective agent)
  • Drugs given in pulses with 2-3-week intervals for normal cells to recover improve the efficacy of therapy: malignant cells recovering more slowly
• Measures to minimize and/or treat the toxicities of anticancer drugs:

  • Ondansetron, a 5-HT3 antagonist for cytotoxic drug-induced vomiting
  • Granulocyte-macrophage colony-stimulating factor (GM-CSF) for neutropenia
  • Platelet transfusion for severe thrombocytopenia
  • Thrombopoietic growth factors like oprelvekin for preventing thrombocytopenia
  • Blood transfusion for severe anemia
  • Human recombinant erythropoietin for preventing anemia
  • Amifostine for prophylaxis of cisplatin-induced nephrotoxicity
  • Leucovorin (folinic acid) for treating methotrexate toxicity
• • Mesna for preventing hemorrhagic cystitis caused by cyclophosphamide and ifosfamide
  • Dexrazoxane as an iron chelating agent to reduce the risk of cardiotoxicity from doxorubicin
  • Allopurinol, alkalinization of urine, and plenty of fluids for reducing urate nephropathy
  • Xerostomia treated with artificial saliva, amifostine
  • Drugs given in pulses with 2-3-week intervals for normal cells to recover
• classification of anticancer drugs

  1. alkylating agent
  2. antimetabolites
  3. anticancer antibiotics
  4. platinum drugs
  5. tyrosine kinase inhibitor
  6. epipodophyllotoxin
  7. camptothecins
  8. vinca alkaloids
  9. taxanes
  10. hormones & antagonists