Drug Delivery: Tumor-Targeted Systems

Authored by: Yu Li , Chao-Pin Lee

Encyclopedia of Pharmaceutical Science and Technology

Print publication date:  July  2013
Online publication date:  July  2013

Print ISBN: 9781841848198
eBook ISBN: 9781351124874
Adobe ISBN:


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Unsatisfactory therapeutic efficacy and substantial systemic toxicity have been the major hurdles in developing small-molecule anti-cancer drugs, as these drugs often lack the selectivity between tumor and healthy tissues. The uptake of cytotoxic anti-cancer drugs by normal tissues usually causes undesired toxicity that can lead to the termination of a treatment regimen. An ideal approach to overcome these hurdles is to develop drugs that only kill tumor cells without any harm to normal tissues. Examples of such drugs include Herceptin (Trastuzumab) (1) for the treatment of metastatic breast cancer and Gleevec (imatinib mesylate) (1) for the treatment of chronic myeloid leukemia and certain types of gastrointestinal stromal tumors. Alternatively, developing tumor-targeted drug delivery systems has been recognized as a valuable approach to enhance the therapeutic efficacy of existing small-molecule anti-cancer drugs. These systems, constructed with tumor-targeting constituents, are designed to modify the pharmacokinetics and biodistribution of cytotoxic anti-cancer drugs, and thus to reduce toxic side effects. Extensive studies have demonstrated the effectiveness of tumor targeted drug delivery systems, and several have been approved for clinical use.

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