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Hormonal Drugs

  1. Estrogens (New Drug: Estramustine)
    a. Ca prostate


  1. Deep vein thrombosis          
  2. Nausea/vommiting              
  3. Gynecomastia

2. Fulvestrant

  1. Estrogen receptor blocker
    → Advanced Ca breast/Ca ovary  

3. Tamoxifen

  1. SERM                                            
  2. Partial agonist      
  3. Works well in hormone positive cancers (ER/PR-ER>>PR)
  4. Long acting                                  
  5. Food increases absorption    
  6. Eliminated by bile                        
  7. Works well in both pre & postmenopause


  1. Prophylaxis of Ca breast (Not in healthy)      
  2. Painful gynecomastia  
  3. Adjuant in advanced Ca


  1. Flushing
  2. Hyperlipidemia
  3. Protects against osteoporosis
  4. Endometerial hyperplasia
    i. Ca-endometrium

4. Raloxifen

  1. does not cause endometrial hyperplasia
  2. Causes vascular thrombosis

Toremefen is a drug similar to tamoxifen

5. Aromatase Inhibitors

  1. Exemastane (irreversible)
  2. Aminoglutethimide (also anti-glucocorticoid; remember ketoconazole also is antiandrogen and antiglucocoticoid)
  3. Letrozole
  4. Anistrazole
    1. Used in postmenopausal women (ovarian cancer)
    2. Act on fat; reduce estrogen synthesis
    3. Side effects include osteoporosis and joint disorders

6. GnRH analogues

  1. Example
    1. Neferelin      
    2. Goserelin      
    3. Buserelin
  2. DOC
    i. Ca prostate
  3. s/e-osteoporosis
  4. C/I
    i. Hormone positive cancer, acromegaly, head injury  

7. Other new drugs:

  1. Clofarabine  and Nelarabine are two new purine analogues approved for the treatment of leukemia and lumphomas
  2. Varinostat and Romidepsin  are two new histone deacetylase inhibitor ,approved for the treatment of cutaneous T cell lymphoma
  3. Tembirolime and Everolimus are mTOR inhibitors. Use as immunosuppressant as well as approved for the treatment of renal cell carcinoma and resistant brain tumors
  4. Demileukin diftitox : combination of interleukin -2 and diphtheria toxin. Approved for the treatment of cutaneous Tcell lymphoma ad side effects are because of diphtheria toxin.

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