Thursday, 11 December 2014

Pharmacology of anticancer agents

Here is another important topic for the GPAT preparation. Every year you well get fair amount of questions in the GPAT exam from this topic. We have tried to explain this topic simply and interactively. Don't forget to mention your any doubt in the comment below. We will be happy to clarify it by the experts of our team.

Classification of anticancer agents

Classification of anticancer agents
Pharmacology of individual Class

a) Alkylating agents:


Alkylating agents


 Mechanism of action:

  • Alkylation of DNA (mainly N7 of guanine).
  • Misleading in DNA replication-----> Cell Death.
  • Alkylation in G1 & S phase.
  • Cell death in G2 phase.
  • Related drugs to alkylating agents: Procarbazine, Cisplatin & Dacarbazine

b) Antimetabolites:

1. Methotrexate: Folic acid antagonists.
  • Binds to dihydrofolate reductase------> No folic acid synthesis.
  • Lack of folic acid-------> No synthesis of adenine, guanine, thiamine & cytosil.
2. Purine antagonists ( Adenine, Guanine)

  • Thiopurines: 6-mercaptopurines & 6- Thioguanine
  • Cladibrine
  • Fludarabines
3. Pyrmidine antagonists (Cytosine, Thiamine)

  • 5-flurouracil
  • Cytarabine
c) Plant alkaloids:

1. Vinca alkaoids: Vincristine & Vinblastin (Tubule synthesis inhibitor).

2. Epidophyllotoxins: Inhibits Topoisomerase-II-------> DNA breakage.

3. Campothecin: Inhibits Topoisomerase-II.

4. Taxanes: Acts as spindle poison (mitotic).

d) Antiestrogen: Tamoxifen  (Breast cancer).

e) Miscellaneous drugs:

Miscellaneous anticancer agents




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