The Modification Strategies for Enhancing the Metabolic Stabilities and Pharmacokinetics of Aptamer Drug Candidates

Aptamers are single-stranded DNA or RNA that can mimic the functional properties of monoclonal antibodies. Aptamers have high affinity and specificity for their target molecules, which can make them a promising alternative to therapeutic antibodies or peptide ligands. However, many aptamer drug candidates in clinical development have been discontinued due to suboptimal metabolic stabilities and pharmacokinetics. To address these issues, chemical modification can be used to enhance the metabolic stability and prolong the half-life of aptamer candidates. The chapter reviewed published data regarding the metabolic stability and pharmacokinetics of aptamer drug candidates from preclinical and clinical studies. The benefits and possible shortcomings of current modification strategies used in these aptamers were briefly discussed.