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Targeted Therapy: Specific Targeted Molecules Needed For Carcinogenesis and Tumor Growth

Targeted therapy is a type of cancer medication that blocks specific molecules needed for tumor growth rather than all rapidly dividing cells. It may be more effective and less harmful than chemotherapy. Targeted therapy was shown to reverse cancer phenotypes using monoclonal antibodies on Her2/neu transformed cells. The main targeted therapies are small molecule drugs and monoclonal antibodies. Imatinib blocks leukemia and gastrointestinal tumor growth while Rituximab targets CD20 on B-cells for lymphoma treatment.

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Malueth Angui
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201 views9 pages

Targeted Therapy: Specific Targeted Molecules Needed For Carcinogenesis and Tumor Growth

Targeted therapy is a type of cancer medication that blocks specific molecules needed for tumor growth rather than all rapidly dividing cells. It may be more effective and less harmful than chemotherapy. Targeted therapy was shown to reverse cancer phenotypes using monoclonal antibodies on Her2/neu transformed cells. The main targeted therapies are small molecule drugs and monoclonal antibodies. Imatinib blocks leukemia and gastrointestinal tumor growth while Rituximab targets CD20 on B-cells for lymphoma treatment.

Uploaded by

Malueth Angui
Copyright
© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
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Download as PPT, PDF, TXT or read online on Scribd
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TARGETED THERAPY

 Targeted therapy is a type of medication that blocks the growth of cancer cells by
interfering with specific targeted molecules needed for carcinogenesis and tumor
growth rather than by simply interfering with rapidly dividing cells (e.g. with
traditional chemotherapy).
 Targeted cancer therapies may be more effective than current treatments and less
harmful to normal cells.
 The definitive experiments that showed that targeted therapy would reverse the
malignant phenotype of tumor cells involved treating Her2/neu transformed cells
with monoclonal antibodies in vitro and in vivo by Mark Greene’s laboratory.
 The main categories of targeted therapy are;
1) Small molecules
2) Monoclonal antibodies.
   
Mechanism of imatinib
Small molecules
 These include;
1) Imatinib mesylate (Gleevec)
2) Gefitinib (Iressa)
3) Erlotinib (Tarceva)
4) Bortezomib (Velcade)
5) Tamoxifen (selective estrogen receptor modulator)
6) Other newer agents;
 Bcl-2 inhibitors (e.g. obatoclax in clinical trials, ABT-263, and
Gossypol.
 PARP inhibitors (e.g. Iniparib, Olaparib in clinical trials)
 Apatinib is a selective VEGF Receptor 2 inhibitor
 Imatinib mesylate (Gleevec, also known as STI–571) is approved for chronic
myelogenous leukemia, gastrointestinal stromal tumor and some other types of
cancer. Early clinical trials indicate that imatinib may be effective in treatment of
dermatofibrosarcoma protuberans.
 Gefitinib (Iressa, also known as ZD1839), targets the epidermal growth factor
receptor (EGFR) tyrosine kinase and is approved in the U.S. for non small cell
lung cancer. EGFR is also overexpressed in the cells of other solid tumors, such
as lung and breast cancers. This leads to inappropriate activation of the
apoptotic Ras signal transduction cascade, eventually leading to uncontrolled
cell proliferation. Gefitinib inhibits EGFR tyrosine kinase by binding to the
adenosine triphosphate (ATP)-binding site of the enzyme. Thus the function of
the EGFR tyrosine kinase in activating the Ras signal transduction cascade is
inhibited; and malignant cells are inhibited.
 Erlotinib (marketed as Tarceva). Erlotinib inhibits epidermal growth factor receptor,[5]
and works through a similar mechanism as gefitinib. Erlotinib has been shown to
increase survival in metastatic non small cell lung cancer when used as second line
therapy. Because of this finding, erlotinib has replaced gefitinib in this setting.
 Bortezomib (Velcade) is an apoptosis-inducing proteasome inhibitor drug that causes
cancer cells to undergo cell death by interfering with proteins. It is approved in the
U.S. to treat multiple myeloma that has not responded to other treatments.
 The selective estrogen receptor modulator tamoxifen has been described as the
foundation of targeted therapy.
 Bcl-2 inhibitors (e.g. obatoclax in clinical trials, ABT-263, and Gossypol.
 PARP inhibitors (e.g. Iniparib, Olaparib in clinical trials)
 Apatinib is a selective VEGF Receptor 2 inhibitor which has shown encouraging anti-
tumor activity in a broad range of malignancies in clinical trials.[8] Apatinib is currently
in clinical development for metastatic gastric carcinoma, metastatic breast cancer and
advanced hepatocellular carcinoma.[9]
Monoclonal antibodies
1) Rituximab (marketed as MabThera or Rituxan) targets CD20 found on B cells. It is
used in non Hodgkin lymphoma
2) Trastuzumab (Herceptin) targets the Her2/neu (also known as ErbB2) receptor
expressed in some types of breast cancer.
3) Cetuximab (marketed as Erbitux) targets the epidermal growth factor receptor. It is
used in the treatment of colon cancer and non-small cell lung cancer.
4) Bevacizumab (marketed as Avastin) targets circulating VEGF ligand. It is approved
for use in the treatment of colon cancer, breast cancer, non-small cell lung cancer,
and is investigational in the treatment of sarcoma. Its use for the treatment of brain
tumors has been recommended
 Many oncologists believe that targeted therapies are the chemotherapy of the future.

 As solid tumor cancer continues to be viewed as a chronic condition, methods for long-

term treatment, with fewer side-effects

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