Therapeutic Targeting of Cancer Cells
Era of Molecularly Targeted Agents
Summary of Key Points
• Molecularly targeted anticancer agents (MTAs) are those that selectively target specific molecular features of cancer cells such as aberrations in genes, proteins, or pathways that regulate tumor growth, progression, and survival.
• Molecular targets include the following: products of activating mutations and translocations, growth factors and receptors, aberrant signal transduction and apoptotic pathways, factors that control tumor angiogenesis and microenvironment, dysregulated proteins, DNA repair machinery, and aberrant epigenetic mechanisms.
• The development of MTAs requires innovative strategies that differ from those traditionally applied to nontargeted conventional chemotherapy.
• Successful development of an MTA depends largely on the importance of the target in controlling tumor cell proliferation and survival and effective modulation of the target in the tumor at clinically achievable concentrations.
