Enzalutamide: Difference between revisions

==History==

Enzalutamide was discovered by [[Charles Sawyers]] who is now{{when|date=December 2019}} at [[Memorial Sloan–Kettering Cancer Center]] and [[Michael E. Jung|Michael Jung]] at the [[University of California, Los Angeles]].<ref name="Borman2008">{{cite journal | vauthors = Borman S | title = New prostate cancer agent class | journal = Chemical & Engineering News | year = 2008 | volume = 86 | issue = 38 | pages = 84–87 | doi = 10.1021/cen-v086n038.p084}}</ref><ref name="pmid20218717">{{cite journal | vauthors = Jung ME, Ouk S, Yoo D, Sawyers CL, Chen C, Tran C, Wongvipat J | title = Structure-activity relationship for thiohydantoin androgen receptor antagonists for castration-resistant prostate cancer (CRPC) | journal = Journal of Medicinal Chemistry | volume = 53 | issue = 7 | pages = 2779–96 | date = April 2010 | pmid = 20218717 | pmc = 3180999 | doi = 10.1021/jm901488g }}</ref><ref name="pmid20853390">{{cite journal | vauthors = Liu B, Su L, Geng J, Liu J, Zhao G | title = Developments in nonsteroidal antiandrogens targeting the androgen receptor | journal = ChemMedChem | volume = 5 | issue = 10 | pages = 1651–61 | year = 2010 | pmid = 20853390 | doi = 10.1002/cmdc.201000259 | s2cid = 23228778 }}</ref> They and their colleagues [[chemical synthesis|synthesized]] and evaluated nearly 200 [[wikt:thiohydantoin|thiohydantoin]] [[chemical derivative|derivative]]s of [[RU-59063]], an [[structural analog|analogue]] of [[nilutamide]], for AR antagonism in human prostate cancer cells, and identified enzalutamide and [[RD-162]] as lead compounds.<ref name="pmid19359544" /><ref name="pmid20853390" /> These compounds were [[patent]]ed in 2006 and described in 2007.<ref name="US20070004753">Sawyers, C., Jung, M., Chen, C., Ouk, S., Welsbie, D., Tran, C., ... & Yoo, D. (2006). U.S. Patent Application No. 11/433,829. https://www.google.com/patents/US20070004753</ref> Enzalutamide was developed and marketed by [[Medivation]] for the treatment of prostate cancer.<ref name="AdisInsight">{{Cite web | url=http://adisinsight.springer.com/drugs/800026688 | title=Enzalutamide - Astellas Pharma/Medivation - AdisInsight}}</ref> It was approved by the U.S. [[Food and Drug Administration]] (FDA) for the treatment of mCRPC in the United States in August 2012, and for the treatment of nonmetastatic castration-resistant prostate cancer in July 2018.<ref name="pmid24076589" /><ref>{{Cite web|url=https://www.healio.com/hematology-oncology/prostate-cancer/news/online/%7Bc932ba92-2ba2-4572-af33-51b20462cedc%7D/fda-expands-xtandi-approval-for-prostate-cancer|title=FDA expands Xtandi approval for prostate cancer|website=www.healio.com|access-date=2018-07-17}}</ref> Enzalutamide was the first new AR antagonist to be approved for the treatment of prostate cancer in over 15&nbsp;years, following the introduction of the first-generation NSAA [[bicalutamide]] in 1995.<ref name="pmid26236143">{{cite journal |vauthors=Gohil K |title=Exciting Therapies Ahead in Prostate Cancer |journal=P & T |volume=40 |issue=8 |pages=530–1 |date=August 2015 |pmid=26236143 |pmc=4517537 }}</ref> It was the first second-generation NSAA to be introduced.<ref name="SaadHeinrich2013">{{cite journal | vauthors = Saad F, Heinrich D | title = New Therapeutic Options for Castration-resistant Prostate Cancer | journal = The Journal of Oncopathology | volume = 1 | issue = 4 | year = 2013 | pages = 23–32 | quote = [...] enzalutamide was the first second-generation AR antagonist to be approved by the FDA in 2012 and by the EMA and Health Canada in 2013 [...]| doi = 10.13032/tjop.2052-5931.100072 }}</ref>

 

==Research==