Pharmacology
Summary
Kinase inhibitors are antineoplastic agents that target specific kinases (the enzymes involved in cell signaling pathways) in order to regulate uncontrolled cell growth often seen in cancers and other diseases.
Imatinib is a tyrosine kinase inhibitor that effectively treats chronic myeloid leukemia by targeting the BCR-ABL fusion protein, and gastrointestinal stromal tumors by blocking c-kit tyrosine kinase. Erlotinib blocks the tyrosine kinase domain of epidermal growth factor receptor (EGFR), and is mainly used to treat non-small cell lung cancer. Sunitinib and Sorafenib inhibit the vascular endothelial growth factor receptor (VEGFR) tyrosine kinase, and treat cancers with VEGFR overexpression (e.g. renal cell carcinoma). Vemurafenib serves as a B-Raf kinase inhibitor, and is employed in the treatment of V600E BRAF positive malignant melanoma. Side effects of kinase inhibitors include ankle and periorbital edema (imatinib), papulopustular acneiform rash and diarrhea (erlotinib), and hyperkeratosis and skin rashes (sunitinib and sorafenib).
Lesson Outline
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FAQs
The "-nib" suffix refers to a type of small molecule kinase inhibitor. These are a class of agents used to treat a variety of cancers, including hematologic and solid malignancies. Different "-nib" drugs work by blocking different types of tyrosine kinase enzymes, which play a key role in cell growth and survival.
Imatinib works by selectively blocking the tyrosine kinase activity of specific proteins such as BCR-ABL fusion protein and c-kit tyrosine kinase. This action can interrupt signaling pathways which encourage the growth and division of cancer cells, making it particularly effective in treating conditions like chronic myeloid leukemia (CML) and gastrointestinal stromal tumors (GIST).
Erlotinib is a small molecule tyrosine kinase inhibitor that blocks the activity of the epidermal growth factor receptor (EGFR) tyrosine kinase. EGFR is often overexpressed in conditions like NSCLC, driving the growth and survival of cancer cells. Thus, erlotinib can help to inhibit tumor growth in these cases.
Sunitinib and sorafenib are types of small molecule tyrosine kinase inhibitors that chiefly act by blocking the activity of the vascular endothelial growth factor receptor (VEGFR) tyrosine kinase. This action interrupts blood vessel formation, thus curbing the growth of cancer cells in conditions like renal cell carcinoma.
Vemurafenib is a small molecule kinase inhibitor that specifically targets the B-Raf kinase. It is particularly effective in the treatment of malignant melanomas that test positive for the V600E BRAF mutation. By inhibiting B-Raf kinase, vemurafenib disrupts the cell signaling pathways that contribute to melanoma growth and survival.
