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Review

New-generation efflux pump inhibitors

, &
Pages 429-440 | Published online: 10 Jan 2014
 

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.

Financial & competing interests disclosure

The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

No writing assistance was utilized in the production of this manuscript.

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