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Proxalutamide
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Proxalutamide
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
CompTox Dashboard (EPA)
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

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Prostate cancer

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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

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

See also

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References

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