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Technical information

Drug Transporters

  Transporters are membrane proteins indispensable for life, carrying endogenous active materials, such as sugars, amino acids and hormones, across cell membranes. However, certain drugs are carried by these transporters as well, and therefore a detailed understanding of transporters is increasingly important for pharmaceutical companies engaged in development of new drugs, as well as for academia.

 

Mechanism of Drug Transfer by Transporters

  It is considered that certain drugs are recognized by transporters owing to structural similarity to the endogenous substrates. Consequently these drugs are transferred across cell membranes by the transporters.

 

Research on Drug Transporter 

  Only 10% of candidate drugs are successfully developed; most drop out during the process of development. One of the main reasons for this is inappropriate ADME (absorption, distribution, metabolism, and excretion) properties of drugs, resulting in low bioavailability, unexpected distribution, or toxicity. These effects probably reflect the combined actions of transporters  and drug-metabolizing enzymes in drug distribution (see figure below), as well as other factors.
  It should be possible to reduce the costs and risks in drug development if interactions of drugs with metabolizing enzymes and transporters can be evaluated at an early stage of development.
  Drug-metabolizing enzymes have been well investigated, whereas research on transporters started relatively recently, partly because of the difficulty of handling membrane proteins.  It is, however, expected that studies on the role of transporters will become increasingly important in drug development.

  GenoMembrane’s aim is to support drug development as a pioneer of transporter research.

 

Figure; Drug transport and metabolism in cells