Updated: 7/28/2020

Targeted Therapy

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Overview

 

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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