All About Targeted Therapies

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...
Small Molecule Tyrosine Kinase Inhibitors with the EGF or HER2 Receptors as a Target As we briefly touched on in the introduction to targeted therapies, the epidermal growth factor receptor (EGFR) family comprises EGFR itself (also known as human epidermal receptor type 1 [HER1] or ErbB1), HER2 (ErbB2), HER3 (ErbB3), and HER4...
Small Molecule Tyrosine Kinase Inhibitors with BCR-ABL and C-Kit as Targets Imatinib mesylate Drs. Peter Nowell and David Hungerford, two Philadelphia researchers, were experimenting with cells from various types of leukemia when one noticed a smaller-than-normal chromosome number 22 on the cancer cells of two individuals...
Part Two: Targeting Signal Transduction with Antibodies To begin the second section of our examination of targeted therapies, we will transition from small molecule tyrosine kinase inhibitors (TKIs) to antibody-based targeted therapies. Please feel free to refer as needed to Part One, which presented the...
Antibodies Targeting the Vascular Endothelial Growth Factor (VEGF) Receptor As discussed in the section on TKIs, vascular endothelial growth factor (VEGF) is a signaling protein that helps govern the birth of new blood vessel, a process referred to in the oncological literature as "angiogenesis". Expression of VEGF...
Antibodies targeting the HER2 Receptor Trastuzumab Trastuzumab (Herceptin, NO 34) is a monoclonal antibody that targets cancer cells overproducing the HER2 protein, which is a member of the HER family of TK receptors that we have discussed extensively, particularly in the context of our...
Antibodies Targeting the Epidermal Growth Factor Receptor The agents listed above are presented in alphabetical order and are the current FDA-approved antibody agents currently used in the treatment of various cancers. In the following section, we will review these agents in greater detail. Note, because...
Antibodies Used in the Treatment of Lymphomas and other Hematological Malignancies In the following section, we will cover antibody therapies used in the treatment of lymphomas and other hematological malignancies, including chronic lymphocytic leukemia and acute myeloid leukemia. Despite advances in cancer biology, immunology, and...