Proxalutamide

From Wikipedia, the free encyclopedia
Proxalutamide
Proxalutamide skeletal.svg
Clinical data
Other namesPruxelutamide; GT-0918
Routes of
administration
By mouth
Drug classNonsteroidal antiandrogen
ATC code
  • None
Identifiers
  • 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
CAS Number
PubChem CID
ChemSpider
UNII
Chemical and physical data
FormulaC24H19F4N5O2S
Molar mass517.50 g·mol−1
3D model (JSmol)
  • 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
  • InChI=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
  • Key:KCBJGVDOSBKVKP-UHFFFAOYSA-N

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.[1][2][3][4][5] 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.[1]

Research[edit]

Prostate cancer[edit]

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.[6][7]

Other indications[edit]

Proxalutamide is in phase Ic clinical trial in China.[1][8]

See also[edit]

References[edit]

  1. ^ a b c "Proxalutamide - Suzhou Kintor Pharmaceuticals". AdisInsight. Springer Nature Switzerland AG.
  2. ^ Tong Y, Chen C, Wu J, Yang J, Zhang H, Wu X, et al. (2014). "Proxalutamide (GT0918), a potent androgen receptor pathway inhibitor". Cancer Research. 74 (19 Supplement): 614. doi:10.1158/1538-7445.AM2014-614. ISSN 0008-5472.
  3. ^ Tong Y, Chen C, Wu J, Zhang H, Wu X, Duan Y, Gao W, Niu X, Ma L, Guo C (2014). "Discovery of potent androgen receptor antagonists for treating CRPC and AR+ breast cancer". Cancer Research. 73 (8 Supplement): 2460. doi:10.1158/1538-7445.AM2013-2460. ISSN 0008-5472.
  4. ^ Applied Biology, Inc. (2020-12-29). "Anti-Androgen Treatment for COVID-19". {{cite journal}}: Cite journal requires |journal= (help)
  5. ^ "EQS-News: Kintor's Proxalutamide (GT0918) COVID-19 Clinical Trial Shows Positive Re-sults in Treatment of Male and Female". Bloomberg.com. 2021-01-11. Retrieved 2021-01-29.
  6. ^ "Product Pipeline". Kintor Pharmaceutical. Retrieved 2021-01-29.
  7. ^ Suzhou Kintor Pharmaceutical (2020-03-13). "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". Clinical Trials. US.
  8. ^ "Safety, Tolerability, and Pharmacokinetics of Proxalutamide Therapy in Women With Metastatic Breast Cancer". Clinical trials. 24 September 2019. Retrieved 2021-01-29.