Polymyxins

a new hope in combating Gram-negative superbugs?

Research output: Contribution to journalReview ArticleResearchpeer-review

32 Citations (Scopus)

Abstract

Polymyxins have emerged as an important last-line of defense against Gram-negative 'superbugs'. Unfortunately, the effective use of polymyxins in the clinic has been hampered by their nephrotoxic side effects. Over the last 10 years various industry and academic groups across the globe have been trying to develop new polymyxins that are safer and more efficacious than the currently approved polymyxin B and colistin. However these drug discovery programs are yet to deliver a new and improved polymyxin drug into the clinic. In this piece we provide an overview of the current state of these polymyxin drug discovery programs from a medicinal chemistry perspective as well as some thoughts on how future drug discovery efforts may ultimately find success.

Original languageEnglish
Pages (from-to)1017-1025
Number of pages9
JournalFuture Medicinal Chemistry
Volume8
Issue number10
DOIs
Publication statusPublished - 1 Jun 2016

Keywords

  • Drug discovery
  • Nephrotoxicity
  • Polymyxins
  • Resistance

Cite this

@article{2f1a70ac9776468cb88a22609efcb133,
title = "Polymyxins: a new hope in combating Gram-negative superbugs?",
abstract = "Polymyxins have emerged as an important last-line of defense against Gram-negative 'superbugs'. Unfortunately, the effective use of polymyxins in the clinic has been hampered by their nephrotoxic side effects. Over the last 10 years various industry and academic groups across the globe have been trying to develop new polymyxins that are safer and more efficacious than the currently approved polymyxin B and colistin. However these drug discovery programs are yet to deliver a new and improved polymyxin drug into the clinic. In this piece we provide an overview of the current state of these polymyxin drug discovery programs from a medicinal chemistry perspective as well as some thoughts on how future drug discovery efforts may ultimately find success.",
keywords = "Drug discovery, Nephrotoxicity, Polymyxins, Resistance",
author = "Tony Velkov and Roberts, {Kade D} and Thompson, {Philip E} and Jian Li",
year = "2016",
month = "6",
day = "1",
doi = "10.4155/fmc-2016-0091",
language = "English",
volume = "8",
pages = "1017--1025",
journal = "Future Medicinal Chemistry",
issn = "1756-8919",
publisher = "Future Science",
number = "10",

}

Polymyxins : a new hope in combating Gram-negative superbugs? / Velkov, Tony; Roberts, Kade D; Thompson, Philip E; Li, Jian.

In: Future Medicinal Chemistry, Vol. 8, No. 10, 01.06.2016, p. 1017-1025.

Research output: Contribution to journalReview ArticleResearchpeer-review

TY - JOUR

T1 - Polymyxins

T2 - a new hope in combating Gram-negative superbugs?

AU - Velkov, Tony

AU - Roberts, Kade D

AU - Thompson, Philip E

AU - Li, Jian

PY - 2016/6/1

Y1 - 2016/6/1

N2 - Polymyxins have emerged as an important last-line of defense against Gram-negative 'superbugs'. Unfortunately, the effective use of polymyxins in the clinic has been hampered by their nephrotoxic side effects. Over the last 10 years various industry and academic groups across the globe have been trying to develop new polymyxins that are safer and more efficacious than the currently approved polymyxin B and colistin. However these drug discovery programs are yet to deliver a new and improved polymyxin drug into the clinic. In this piece we provide an overview of the current state of these polymyxin drug discovery programs from a medicinal chemistry perspective as well as some thoughts on how future drug discovery efforts may ultimately find success.

AB - Polymyxins have emerged as an important last-line of defense against Gram-negative 'superbugs'. Unfortunately, the effective use of polymyxins in the clinic has been hampered by their nephrotoxic side effects. Over the last 10 years various industry and academic groups across the globe have been trying to develop new polymyxins that are safer and more efficacious than the currently approved polymyxin B and colistin. However these drug discovery programs are yet to deliver a new and improved polymyxin drug into the clinic. In this piece we provide an overview of the current state of these polymyxin drug discovery programs from a medicinal chemistry perspective as well as some thoughts on how future drug discovery efforts may ultimately find success.

KW - Drug discovery

KW - Nephrotoxicity

KW - Polymyxins

KW - Resistance

UR - http://www.scopus.com/inward/record.url?scp=84977103552&partnerID=8YFLogxK

U2 - 10.4155/fmc-2016-0091

DO - 10.4155/fmc-2016-0091

M3 - Review Article

VL - 8

SP - 1017

EP - 1025

JO - Future Medicinal Chemistry

JF - Future Medicinal Chemistry

SN - 1756-8919

IS - 10

ER -