Anti-Neoplastic Agents

    .

    UNDER CONSTRUCTION

    Hematology

    • Lenalidomide --> increased risk of thrombosis especially if combined with dexamethasone.
    • Thalidomide --> increased risk of thrombosis.

     

    General Chemotherapy

    • Drug Indications Most Common S/E Notes

      5-FU

      "FOXFOX" - Colon Ca 

         Folinic Acid, 5FU, Oxaliplatin

         Folinic Acid (Leukovorin) enhances 5FU

      Colon Ca

      Anal Ca

         

      Capecitabine

      (Oral pro-drug of 5-FU)

      "CapOx" - Capecitabine + Oxaliplatin

      Colon Ca (Stage III-IV)

      Rectal Ca (Stage II-IV)

      - Oral Version

        (GI diarrhea/mucositis.)

      - "Hand-Foot Syndrome"

       Red discoloration of hands + feet

       leads to blistering and desquamation

       Can improve by adjusting dose or

       shortening therapy

       

      Mitomycin

      - Very toxic with limited utility

      - Only given one single dose 

      - Not used in any other cancer (anal only)

      Anal Cancer

        (with 5FU)

         

    Anti-Rejection Drugs

    • Tacrolimus
      • Lots of drug interactions (classically azole antifungals and macrolides antibiotics).
        • Azithromycin is ok (less cytochrome P450 interaction).
      • Toxicity:
        • Nephropathy
          • AKI (Creat, BUN increase).
          • Tubular disorders.
          • HUS
        • HTN, Neurotoxicity, metabolic abnormalities (hypeglycemia, hypekalemia, magnesium).
    • Mycophenilate mofetil
      • Antibiotics have no effect on drug levels. 
      • Toxicity:
        • GI Side-effects.
        • Bone marrow suppression.

     

    Hormonal Therapy

    • Drug Indications S/E
      Breast Cancer    
      Tamoxifen

      - Pre-menopausal Breast Cancer

      (Primary estrogen from ovaries)

      - Eyes: Cataracts

      - Vessels: Thromboembolism, hot flashes

      - Uterine: Endometrial cancer

      Aromatase Inhibitors

      - Post-menopausal Breast Cancer

      (Primary estrogen aromatase enzyme)

      No increased VTE risk.

      No increased endometrial cancer risk.

      Larger loss of bone mineral density/fractures.

      • Use bisphosphonates.

      MSK/arthralgia syndrome --> symmetric pain and joint stiffness. (discontinue to resolve).

     

    Targeted Therapies

    •  

       

      Agent

      Mechanism of Action

      Applicable Diseases

      Toxicities

      VEGF Inhibitors    

      Bevacizumab

      (IV/SC antibody)

      VEGF monoclonal antibody

      (No marker, just used in some cancers)

      Colon, lung, brain, ovary, breast, renal

      Side-Effect on NORMAL VASCULATURE!

      Hypertension, poor wound healing, nephrotic syndrome, bleeding/thrombosis, abdo perf

      Sunitinib, sorafenib

      (Oral)

      Tyrosine kinase inhibitor,

      blocks VEGF, and raf, PDGFR

      Renal Cell Ca

      GIST,

      Hepatocellular Ca

      Hypertension, rash, hypothyroidism, thrombosis, cardiotoxicity,

      Pazopanib

      Axitinib

        RCC  
      mTOR Inhibitors    
      Temsirolimus mTOR inhibitor RCC  
      Everolimus mTOR inhibitor RCC  
             

      Imatinib

      Tyrosine kinase inhibitor, blocks BCR-ABL and k-KIT

      CML, GIST tumors

      Rash, edema, fatigue, diarrhea, cytopenias

      Gefitinib

      Gefitinib

      Tyrosine kinase inhibitor, blocks EGFR

      Non-small cell lung ca
      Trastuzumab Her2neu receptor positive Breast Cancer  

      EGFR: epidermal growth factor receptor

      GIST = gastrointestinal stromal tumor

      PDGFR = platelet-derived growth factor receptor

      VEGF: vascular endothelial growth factor --> makes more vasculature

    • VEGF Inhibitors
      • Bevacizumab
      • Sunitinib (tyrosine kinase inh.)
      • Sorafenib
      • Pazopanib
      • Axitinib
    • mTOR Inhibitors
      • Temsirolimus
      • Everolimus
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