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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.

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:

Angiogenesis inhibitors 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-targeted agents 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.
Anti-CD20 monoclonal antibodiesThese 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) inhibitorsThese 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 inhibitorsThese 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.

Other cancer treatments

Because an individual’s cancer cells are unique, different people may receive different treatments, even if their cancer type is the same. Doctors will recommend the best treatment for an individual based on the type and stage of cancer, its genetic make-up, the person’s age and their general health.

Aside from targeted therapy, other treatments for cancer include surgery, chemotherapy, radiation therapy, hormone therapy, and immunotherapy.

These treatments may be used on their own or in combination. For example, you may have surgery to remove a tumour, followed by a targeted therapy drug to kill any remaining cancer cells.

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Understanding Targeted Therapy

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This information is reviewed by

This information was last reviewed June 2018 by the following expert content reviewers: Dr Fiona Day, Medical Oncologist, Calvary Mater Newcastle, and Conjoint Senior Lecturer, University of Newcastle, NSW; Dawn Bedwell, 13 11 20 Consultant, Cancer Council Queensland; Jennifer Cardwell, Consumer; Christine Henneker, Nurse Practitioner Cancer Services, WA Country Health Service, WA; Dr Rohit Joshi, Medical Oncology Consultant, Calvary Central Districts Hospital, and Clinical Lecturer, University of Adelaide, SA; Prof Ross McKinnon, Director, Flinders Centre for Innovation in Cancer, SA; Prof Miles Prince, Haematologist, Director of Molecular Oncology and Cancer Immunology, Epworth HealthCare, VIC; Prof Ben Solomon, Medical Oncologist, and Group Leader, Molecular Therapeutics and Biomarkers Laboratory, Peter MacCallum Cancer Centre, VIC; Dr Subotheni Thavaneswaran, Medical Oncologist, The Kinghorn Cancer Centre and St Vincent’s Hospital, and Translational Research Fellow, Garvan Institute of Medical Research, NSW; A/Prof Kathy Tucker, Clinical Cancer Geneticist, Nelune Comprehensive Cancer Centre, NSW.