The role of transporters in the drug absorption, distribution and elimination and its significance in the new drug development

The effects of drug transporters on the drug disposition were introduced and the possible utility in the developing of new drugs was discussed. The properties of the transporters can be used to increase the bioavailability of the drugs, to deliver the drug to the target organ or avoid distribution to other organs, thereby increase the therapeutic effects and reduce the chance of toxic effects. Forevermore, they can also be used to control the elimination speed of the compounds. There are two methods can be utilized to reach the purposes described as above, one is selecting a leading compound does or does not interact with special transporters, another is the use of inhibitors of some transporters. It is well accepted in recent years that the pharmacokinetic properties of a drug should be studied in its early stage of development. High-throughput screening systems established bases on transporters will be an efficient tools in the new drug developments.