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Antitumor Antibiotics

MAO

  1. Inhibit DNA function by binding to & forming intercalated bonds
  2. Increase expression of topoisomerase I

Individual agents

  1. Doxorubicin        
  2. Daunorubicin              
  3. Epirubicin              
  4. Idarubicin        
  5. Mitomycin            
  6. Bleomycin            
  7. Mitoxantrone                
  8. Streptozotocin
  9. Plicamycin (Mithramycin)      
  10. Actinomycin D 

1. Doxorubicin

  1. Broadest spectrum
  2. Most efficacious
  3. DOC
    1. Breast cancer
    2. Works better in large tumors
  4. Major side effect is cardiac toxicity
  5. Free radical mediated cardiac damage occurs  

2. Daunorubicin

 

Less cardiotoxic alternative


3. Epirubicin
 
Used in breast cancer

 

4. Idarubicin

 

Used in leukemia

 

5. Mitomycin

 

Dual drug; descried earlier

 

6. Mitoxantrone

 

Used in multiple sclerosis

 

7. Streptozotocin

  1. Nitrosourea
  2. DOC for insulinoma 

8. Plicamycin

  1. Used in tumor induced hypercalcemia
  2. Glucorticoids are used more commonly 

9. Actinomycin D

  1. 2nd drug of choice for ectopic pregnancy
  2. DOC for Wilm’s tumor      

10. Bleomycin :

  1. Only antibiotic which is cell cycle specific
  2. Require oxygen and iron for its anticancer activity
  3. Can be given by any route
  4. Metabolized by bleomycin hydrolase enzyme which is deficient in two places in human body:
  5. Skin 2) lung
  6. When given by systemic route bleomycin will lead to skin toxicity and pulmonary fibrosis as its side effects.
  7. Pulmonary fibrosis if irreversible and serious side effect.
  8. Lung injury is because of type I cell destruction and type II cell proliferation,which leads to fibrosis.
  9. Local side effect of bleomycin is raynaud’s phenomenon.





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