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Updated: Dec 26 2021

Targeted Therapy

4.3

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(4)

  • Overview
      • Targeted Therapy
      • Drugs/Antibodies
      • Mechanism of Action
      • Toxicity
      • Hydroxyurea
      • Inhibits ribonucleotide reductase
      • GI upset and myelosupression
      • Trastuzumab
      • Anti-HER-2 (erb-B2) monoclonal antibody
      • Cardiotoxicity
      • Tamoxifen and raloxifene
      • Selective estrogen receptor modulator
      • ↑ risk of endometrial carcinoma and hot flashes
      • Imatinib
      • bcr-abl tyrosine kinase inhibitor
      • Fluid retention
      • Rituximab
      • anti-CD20 monoclonal antibody
      • -
      • Vemurafenib
      • Inhibitor of BRAF
      • -
  • Hydroxyurea
    • Mechanism
      • inhibits ribonucleotide reductase
      • leads to decreased DNA synthesis
        • S-phase specific
    • Clinical use
      • melanoma
      • CML
      • sickle cell disease
        • via increased HbF
    • Toxicity
      • myelosuppression
      • GI upset
  • Trastuzumab (Herceptin)
    • Mechanism
      • anti-HER-2 (erb-B2) monoclonal antibody
    • Clinical use
      • HER-2 positive breast cancer
    • Toxicity
      • cardiotoxicity
  • Tamoxifen, raloxifene
    • Mechanism
      • selective estrogen receptor modulator (SERM)
      • estrogen antagonist in estrogen receptor-positive breast cancer cells
      • estrogen agonist in other tissues
        • bone
    • Clinical use
      • breast cancer
      • prevent osteoporosis
    • Toxicity
      • ↑ risk of endometrial carcinoma
        • tamoxifen only
          • via partial agonist effects
        • raloxifene is endometrial antagonist
      • hot flashes
  • Imatinib (Gleevec)
    • Mechanism
      • Philadelphia chromosome bcr-abl tyrosine kinase inhibitor
        • t(9;22) translocation
    • Clinical use
      • CML
      • GI stromal tumors
    • Toxicity
      • fluid retention
  • Rituximab
    • Mechanism
      • anti-CD20 monoclonal antibody
        • most B cell neoplasms are CD20 positive
    • Clinical use
      • non-Hodgkin's lymphoma
      • chronic lymphocytic leukemia
      • rheumatoid arthritis
        • with methotrexate
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