title: New-generation efflux pump inhibitors.
abstract: The development of novel efflux pump inhibitors is an emerging and challenging research field. Besides the use of such excipients in cancer therapy, efflux pump inhibitors are gaining increasing interest with regards to drug delivery. In particular, inhibition of efflux pumps located in the intestine and the blood-brain barrier offers promising prospects. Nowadays, third-generation inhibitors, such as elacridar, zosuquidar, laniquidar, OC144-093 and tariquidar, have been evaluated in clinical trials. Apart from these small, molecular inhibitors, which will be discussed within the current review, a focus has been set on polymeric or polymer-based inhibitors, including poly(ethylene glycol) and derivatives, poloxamers and thiomers.
authors.affiliation: Department of Drug Delivery Technology and Science, Laboratory of Pharmaceutical Engineering, Gifu Pharmaceutical University, 5-6-1 Mitahora-Higashi, Gifu 502-8585, Japan and ThioMatrix GmbH, Research Center Innsbruck, Mitterweg 24, 6020 Innsbruck, Austria. martin.werle@uibk.ac.at.
authors.forename: Martin
authors.initials: M
authors.lastname: Werle
authors.forename: Hirofumi
authors.initials: H
authors.lastname: Takeuchi
authors.forename: Andreas
authors.initials: A
authors.lastname: Bernkop-Schnürch