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Ligand-Targeted Drug Delivery

Safety and efficacy constitute the major criteria governing regulatory approval of any new drug. The best method to maximize safety and efficacy is to deliver a proven therapeutic agent with a targeting ligand that exhibits little affinity for healthy cells but high affinity for pathologic cells. The probability of regulatory approval can conceivably be further enhanced by exploiting the same targeting ligand, conjugated to an imaging agent, to select patients whose diseased tissues display sufficient targeted receptors for therapeutic efficacy. The focus of this Review is to summarize criteria that must be met during design of ligand-targeted drugs (LTDs) to achieve the required therapeutic potency with minimal toxicity. Because most LTDs are composed of a targeting ligand (e.g., organic molecule, aptamer, protein scaffold, or antibody), spacer, cleavable linker, and therapeutic warhead, criteria for successful design of each component will be described. Moreover, because obstacles to successful drug des...

Authors:   Madduri Srinivasarao; Philip S. Low
Journal:   Chemical Reviews
Year:   2017
DOI:   10.1021/acs.chemrev.7b00013
Publication date:   12-Sep-2017
Facts, background information, dossiers
  • safety
  • receptors
  • imaging
  • drugs
  • drug delivery
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