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Tykerb Delivered As A Kinase Inhibitor
To Treat Invasive Ductal Carcinoma
University of Pittsburgh
Abigail Doyle and Katherine Gaines
Background of Cancer
• Cancer cells divide uncontrollably, causing an excess of cells called tumors that
can spread into nearby tissues.
• Breast cancer begins in breast milk glands, milk ducts, or sometimes breast tissue
and spreads dangerously fast if it reaches the lymph nodes or blood stream..
• 80% of breast cancer is diagnosed as invasive ductal carcinoma (IDC) , which
spreads from the epithelial cells in the milk duct to the surrounding breast tissue
(Figure 1).
• In most cases, the patient has an excess amount of the human epidermal growth
factor receptor 2 gene (HER2), which signals the cell to grow more than normal.
• There are over 320,000 new cases of breast cancer diagnosed each year and 40,000
cases result in death. These cases contribute to the continually rising $90 billion
spent on cancer treatment each year in the United States.
Cancer
Treatment
Radiation
Therapy
Description
•
•
Hormone
Therapy
•
•
Target Drug
Therapy
•
•
Creates small breaks in a cell’s DNA,
inhibiting its ability to divide and
spread
May damage DNA in normal cells,
causing undesirable side effects
Typically decreases a person’s
estrogen, which is needed for regular
cell division
May actually increase the risk of cancer
reoccurrence
Only acts on specific parts of the body
Either destroys the cells itself or serves
as a marker on the cancer cell to help
chemotherapy reach the designated
cells better and more accurately
The Future Outlook
• There has already been research conducted to improve its absorption by creating a
human serum albumin, the most prevalent protein found in the blood, which is
loaded with Tykerb nanoparticles.
• Researchers are also working to make Tykerb available to men, younger women,
and pregnant women,
Figure 1 – IDC Cells
Sustainability
• GlaxoSmithKline (GSK), the pharmaceutical company that owns and markets
Tykerb, has begun to further develop their global pricing strategies.
• Through negotiations, GSK provides Tykerb at a discounted price to those with
private or no insurance.
• GSK has partnered with other pharmaceutical companies, expanding its market,
and making it a proprietary global oncology drug.
Tykerb
• Tykerb, a specific brand of Lapatinib, is a dual tyrosine kinase inhibitor.
• This target drug blocks HER2 protein receptors, stopping phosphorylation,
which is the process that adds a phosphate group and allows cancer cells to
divide.
• Tykerb was approved by the FDA in 2010 for postmenopausal women.
• Monoclonal antibodies can either attach to the antigen to kill the cell
themselves or the antibodies can carry other cancer treatment drugs. When
the breast cancer is resistant to monoclonal antibodies, oncologists use target
drugs.
• Tykerb is a protein kinase inhibitor that interrupts signal transduction and
prevents the normal function and cell communication of the protein kinase,
which controls cell growth. This stops a phosphate from being added, which
turns the HER2 protein off and stops the cell from receiving signals to
continue growing.
• Tykerb nanoparticles are more effective than monoclonal antibodies because
it enters the cells to connect to the HER2 receptors (Figure 2) rather than
attaching to the antigens on the outside of the cell.
Figure 2 – HER2 Inhibition
Advantages
Distinguishes between
cancerous and
noncancerous cells to
minimize damage unlike
chemotherapy
Fewer and less severe side
effects
More accessible because it
is taken as a pill rather than
intravenously.
Can be taken in
combination with other
cancer treatments when
other drugs are not effective
or when the patient has
developed a resistance to
them.
Causes cells to destroy
themselves, eliminating a
need for surgery
Disadvantages
Low oral absorption
Requires a large daily
dosage
Only approved for
postmenopausal women
A month’s supply of Tykerb
can cost $5,000 to $6,000
Not all healthcare plans
cover cost of Tykerb
Acknowledgements
A special thank you to our writing instructor Julianne McAdoo, our librarian Judy
Brink, our co-chair Morgan Austin, our chair Brandon Marshall, and our friend
Hailey Honeycutt for their guidance, knowledge, and suggestions.