Irosustat: Difference between revisions

'''Irosustat''' ({{abbrlink|INN|International Nonproprietary Name}}, {{abbrlink|USAN|United States Adopted Name}}; developmental code names '''STX-64''', '''667-coumate''', '''BN-83495'''; also known as '''oristusane''') is an [[oral administration|orally active]], [[irreversible inhibitor|irreversible]], [[nonsteroidal]] [[enzyme inhibitor|inhibitor]] of [[steroid sulfatase]] (STS) and member of the aryl sulfamate ester class of drugs that was under development by Sterix Ltd and [[Ipsen]] for the treatment of [[hormone-sensitive cancer]]s such as [[breast cancer]], [[prostate cancer]], and [[endometrial cancer]] but has not yet been marketed.<ref name="AdisInsight">{{Cite web | url=http://adisinsight.springer.com/drugs/800020388 |title = Irosustat - AdisInsight}}</ref><ref name="pmid21342037">{{cite journal | vauthors = Palmieri C, Januszewski A, Stanway S, Coombes RC | title = Irosustat: a first-generation steroid sulfatase inhibitor in breast cancer | journal = Expert Rev Anticancer Ther | volume = 11 | issue = 2 | pages = 179–83 | year = 2011 | pmid = 21342037 | doi = 10.1586/era.10.201 | url = }}</ref> The drug<ref>{{Cite journal|vauthors=Woo LW, Purohit A, Malini B, Reed MJ, Potter BV|date=2000|title=Potent active site-directed inhibition of steroid sulphatase by tricyclic coumarin-based sulphamates |url=|journal= Chemistry & Biology|volume=7|issue=10|pages=773–791|via=|doi=10.1016/S1074-5521(00)00023-5}}</ref><ref>{{Cite journal|last=Woo|first=L W L, Ganeshapillai D, Thomas M P, Sutcliffe O B, Malini B, Mahon M F, Purohit A & Potter B V L Structure-Activity Relationship of the Clinical Steroid Sulfatase Inhibitor Irosustat (STX64, BN83495).|date=2011|title=Structure-Activity Relationship of the Clinical Steroid Sulfatase Inhibitor Irosustat (STX64, BN83495).|url=|journal=ChemMedChem|volume=6|issue=11|pages=2019–2034|via=|doi=10.1002/cmdc.201100288|pmid=21990014|pmc=3262147}}</ref> was designed and synthesized in the group of Professor [[Barry V. L. Potter|Barry V L Potter]] at the Department of Pharmacy & Pharmacology, [[University of Bath]], working together with Professor [[Michael J. Reed]] at [[Imperial College London|Imperial College]], London and its initial development was undertaken through the university spin-out company Sterix Ltd and overseen by Cancer Research UK ([[Cancer Research UK|CRUK]]). Results of the "first-in-class" [[clinical trial]] in breast cancer of an STS inhibitor in humans were published in 2006<ref>{{Cite journal|last=Stanway|first=S, Purohit A, Woo L W L, Sufi S, Vigushin D, Ward R, Wilson R, Stanczyk F Z, Dobbs N, Kulinskaya E, Elliott M, Potter B V L, Reed M J and Coombes R C|date=2006|title=Phase I study of STX64 (667 Coumate) in breast cancer patients: the first study of a steroid sulphatase inhibitor|url=|journal=Clin Cancer Res|volume=12|issue=5|pages=1585–1592 |doi=10.1158/1078-0432.CCR-05-1996|pmid=16533785}}</ref> and dose optimisation studies and further clinical data have been reported.<ref>{{Cite journal|vauthors=Coombes RC, Cardoso F, Isambert N, Lesimple T, Soulié P, Peraire C, Fohanno V, Kornowski A, Ali T, Schmid P|date=2013|title=A phase I dose escalation study to determine the optimal biological dose of irosustat, an oral steroid sulfatase inhibitor, in postmenopausal women with estrogen receptor-positive breast cancer.|url=|journal=Breast Cancer Res. Treat.|volume=140|issue=1|pages=73–82 |doi=10.1007/s10549-013-2597-8|pmid=23797179}}</ref>