Types of targeted therapy

Each type of targeted therapy drug works on a specific molecular target. The two main groups of drugs are monoclonal antibodies and small molecule inhibitors.

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Monoclonal antibodies

These medicines are manufactured (synthetic) versions of immune system proteins called antibodies, which are part of the body’s natural defence against infections. The synthetic antibodies lock onto a protein on the surface of cells or surrounding tissues to interfere with the growth or survival of cancer cells in some way.

Monoclonal antibodies can be classified as either a targeted therapy or immunotherapy, depending on the type of monoclonal antibody. Examples of targeted therapy monoclonal antibodies include:

These drugs are designed to reduce the blood supply to a tumour to slow or stop it growing. They target various receptors or proteins linked with the growth of cancer cells and stop them from working. For example, bevacizumab targets vascular endothelial growth factor (VEGF), a protein that helps new blood vessels form.
HER2 is a protein that causes cancer cells to grow uncontrollably. Some targeted therapy drugs destroy the HER2 positive cancer cells, or reduce their ability to divide and grow. Examples include trastuzumab and pertuzumab, which are used to treat HER2 positive breast cancer.
monoclonal antibodies
These drugs target a protein called CD20 found on some B-cell leukaemias and non-Hodgkin lymphomas. Examples include rituximab and obinutuzumab.

Small molecule inhibitors

These drugs can get inside cancer cells and block certain enzymes and proteins that tell cancer cells to grow. Examples of small molecule inhibitors include:

Tyrosine kinase
inhibitors (TKIs)
These drugs block a group of enzymes called tyrosine kinases from sending signals that tell cancer cells to grow, multiply and spread. Without this signal, the cancer cells die. Examples of TKIs include erlotinib, sunitinib, lapatinib and ibrutinib.
Mammalian target of rapamycin (mTOR)
These drugs block mTOR, an enzyme that tells cancer cells to grow and spread. Everolimus is an mTOR inhibitor approved for use for some types of kidney cancer.
PARP inhibitors These drugs stop the protein known as PARP from repairing damaged DNA in cancer cells. Olaparib is a PARP inhibitor approved for use in some ovarian, fallopian tube and peritoneal cancers.
This information was last reviewed in June 2018
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