Irosustat: Difference between revisions

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'''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) that was under development by [[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">http://adisinsight.springer.com/drugs/800020388</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 was designed and synthesized by the Potter group of Professor Barry Potter at the Department of Pharmacy & Pharmacology, University of Bath, working together with the group of Professor Mike Reed at Imperial College, London and its initial development was undertaken through the university spin-out company Sterix Ltd overseen by Cancer Research UK. Results of the first clinical trial of an STS inhibitor in humans were published in 2006.<nowiki><ref> Stanway 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 (2006). Phase I study of STX64 (667 Coumate) in breast cancer patients:  the first study of a steroid sulphatase inhibitor. </nowiki>''Clin Cancer Res'' '''12''' (5): 1585-1592. doi 10.1158/1078-0432.CCR-05-1996 <nowiki></ref></nowiki>
 
In 2004 Sterix Ltd was acquired by Ipsen and the drug continued in development through formal academic-industry partnerships by Ipsen with the University of Bath and Imperial College. The drug reached [[Phases of clinical research#Phase II|phase II]] [[clinical trial]]s in hormone-dependent breast cancer and endometrial cancer prior to the discontinuation of its initial development as a monotherapy by Ipsen.<ref name="AdisInsight" /><ref name="AvendanoMenendez2015">{{cite book|author1=Carmen Avendano|author2=J. Carlos Menendez|title=Medicinal Chemistry of Anticancer Drugs|url=https://books.google.com/books?id=VEibBwAAQBAJ&pg=PA105|date=11 June 2015|publisher=Elsevier Science|isbn=978-0-444-62667-7|pages=105–}}</ref> It also reached a phase I trial in the USA for prostate cancer. However, the development of Irosustat has continued with clinical trials designed to explore its activity in early breast cancer and also in combination with an aromatase inhibitor. The results of these trials were published in 2017 and showed evidence of clinical benefit in patients.