Introduction to Targeted Therapy
The modern-day approach to cancer management is an increasingly multidisciplinary one, consisting primarily of surgery, radiation therapy and chemotherapy, in varying combinations. However, any approach is only as good as its individual components....

Part One: Introduction to Small Molecule Tyrosine Kinase Inhibitors
In the past several years, tyrosine kinase inhibitors have taken on an increasingly important role in the treatment of cancer. Tyrosine kinases function to transfer phosphate groups from a molecule known as ATP (adenosine triphosphate) to tyrosine...

Small Molecule Tyrosine Kinase Inhibitors with VEGFR as a Target
Sunitinib and Sorafenib Tumor cells, like normal cells, need an adequate blood supply in order to perform vital cellular functions. In fact, as cells multiply and grow in number and size, access to nutrients and blood supply becomes increasingly...

Anti-Angiogenesis Antibody: Bevacizumab
Review of Pivotal Bevacizumab Studies – Colorectal Cancer Phase I clinical trials (Gordon et al., Margolin et al.) established a half-life of 21 days, lack of dose-limiting toxicity, and safety/tolerability when bevacizumab is given...

Anti-Angiogenesis Small Molecules
Vatalanib (PTK 787/ZK 222584) Vatalanib is an oral drug that selectively inhibits all three types of VEGFR, as well as platelet-derived growth factor receptor (PDGFR) and c-KIT. (Note: c-KIT is a tyrosine kinase receptor pathway that is...

Anti-Angiogenesis Soluble Receptor
VEGF Trap VEGF Trap is a fully human fusion protein designed from components of VEGFR-1 and -2. It is soluble (travels freely in blood) and is able to bind VEGF-A more tightly than monoclonal antibodies. In addition to VEGF-A, this drug also...