Proxalutamide

{{Short description|Chemical compound}}

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| IUPAC_name = 4-[4,4-dimethyl-3-[6-[3-(1,3-oxazol-2-yl)propyl]pyridin-3-yl]-5-oxo-2-sulfanylideneimidazolidin-1-yl]-3-fluoro-2-(trifluoromethyl)benzonitrile

| image = Proxalutamide skeletal.svg

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| routes_of_administration = By mouth

| class = Nonsteroidal antiandrogen

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| CAS_number = 1398046-21-3

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| PubChem = 60194102

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| ChemSpiderID = 52084193

| UNII = QX6O64GP40

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| synonyms = Pruxelutamide; GT-0918

| C=24 | H=19 | F=4 | N=5 | O=2 | S=1

| SMILES = CC1(C(=O)N(C(=S)N1C2=CN=C(C=C2)CCCC3=NC=CO3)C4=C(C(=C(C=C4)C#N)C(F)(F)F)F)C

| StdInChI_Ref =

| StdInChI = 1S/C24H19F4N5O2S/c1-23(2)21(34)32(17-9-6-14(12-29)19(20(17)25)24(26,27)28)22(36)33(23)16-8-7-15(31-13-16)4-3-5-18-30-10-11-35-18/h6-11,13H,3-5H2,1-2H3

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Proxalutamide (developmental code name GT-0918) is a nonsteroidal antiandrogen (NSAA) – specifically, a selective high-affinity silent antagonist of the androgen receptor (AR) – which is under development by Suzhou Kintor Pharmaceuticals, inc., a subsidiary of Kintor Pharmaceutical Limited, for the potential treatment of COVID-19, prostate cancer, and breast cancer.{{cite web | title = Proxalutamide - Suzhou Kintor Pharmaceuticals | url = https://adisinsight.springer.com/drugs/800046361 | work = AdisInsight | publisher = Springer Nature Switzerland AG}}{{cite journal| vauthors = Tong Y, Chen C, Wu J, Yang J, Zhang H, Wu X, Duan Y, Gao W, Qian W, Niu X, Mi L | display-authors = 6 | title = Proxalutamide (GT0918), a potent androgen receptor pathway inhibitor | journal = Cancer Research|volume=74|issue=19 Supplement|year=2014|pages=614|issn=0008-5472|doi=10.1158/1538-7445.AM2014-614}}{{cite journal | vauthors = Tong Y, Chen C, Wu J, Zhang H, Wu X, Duan Y, Gao W, Niu X, Ma L, Guo C | title = Discovery of potent androgen receptor antagonists for treating CRPC and AR+ breast cancer |journal=Cancer Research|volume=73|issue=8 Supplement|year=2014|pages=2460|issn=0008-5472|doi=10.1158/1538-7445.AM2013-2460 }}{{Cite web |website=ClinicalTrials.gov |date=2020-12-29|title=Anti-Androgen Treatment for COVID-19|url=https://clinicaltrials.gov/ct2/show/NCT04446429}}{{Cite press release |agency=EQS |date=2021-01-10 |title=Kintor's Proxalutamide (GT0918) COVID-19 Clinical Trial Shows Positive Results in Treatment of Male and Female |language=en |website=Bloomberg.com |url=https://www.bloomberg.com/press-releases/2021-01-11/eqs-news-kintor-s-proxalutamide-gt0918-covid-19-clinical-trial-shows-positive-re-sults-in-treatment-of-male-and-female |url-status=dead |archive-url=https://web.archive.org/web/20210301111858/https://www.bloomberg.com/press-releases/2021-01-11/eqs-news-kintor-s-proxalutamide-gt0918-covid-19-clinical-trial-shows-positive-re-sults-in-treatment-of-male-and-female |archive-date=2021-03-01 |access-date=2025-01-09}}{{void|Fabrickator|comment|Alternate presentation: https://www.eqs-news.com/news/corporate/kintors-proxalutamide-gt0918-covid-19-clinical-trial-shows-positive-re-sults-in-treatment-of-male-and-female-patients/1416847 }}{{cbignore}} It was approved in Paraguay for the treatment of COVID-19 in July 2021, but has not been approved at this time in other countries.

Research

= Prostate cancer =

Proxalutamide is in phase III studies for mCRPC as monotherapy and in combination with abiraterone. In the United States, it is in phase II study as monotherapy for mCRPC.{{Cite web |title=Product Pipeline |url=https://en.kintor.com.cn/intro/30.html |access-date=2021-01-29 |website=Kintor Pharmaceutical |archive-date=2021-02-03 |archive-url=https://web.archive.org/web/20210203080612/https://en.kintor.com.cn/intro/30.html |url-status=dead }}{{Cite journal | journal = Clinical Trials |author = Suzhou Kintor Pharmaceutical |date=2020-03-13|title=An Extended/Phase 2, Multi-Center, Randomized, Open-Label Study to Evaluate the Safety and Tolerability of GT0918 in Subjects With Metastatic Castrate Resistant Prostate Cancer (mCRPC) Who Failed Either Abiraterone or Enzalutamide | publisher = US |url= https://clinicaltrials.gov/ct2/show/NCT03899467}}

= Other indications =

Proxalutamide is in phase Ic clinical trial in China.{{Cite journal|title=Safety, Tolerability, and Pharmacokinetics of Proxalutamide Therapy in Women With Metastatic Breast Cancer|url= https://clinicaltrials.gov/ct2/show/NCT04103853|access-date=2021-01-29 |website=Clinical trials|date= 24 September 2019}}

See also

References