Development of RNA aptamers for therapeutics

Abstract

In recent years, RNA aptamers have been regarded as the next generation of antibody therapeutic drugs. RNA aptamers are selected by in vitro selection referred to as SELEX and after going through truncation and modification, they become candidates for therapeutic drugs. PEGylation is used for substantial improvement of pharmacokinetics. An aptamer itself is potentially a therapeutic drug, but it can also be used as a drug delivery agent by conjugating it with an agent such as an anti-cancer agent. In this review, developmental processes and typical properties of aptamer therapeutic drugs will be reviewed. vWF aptamer, which is now in phase II clinical studies, and MK aptamer, which is being developed by RIBOMIC Inc., will be also reviewed. © 2008, THE JAPAN SOCIETY OF DRUG DELIVERY SYSTEM. All rights reserved.