Proxalutamide

Proxalutamide
Clinical data
Other namesPruxelutamide; GT-0918
Routes of
administration		By mouth
Drug classNonsteroidal antiandrogen
ATC code
  • None
Identifiers
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
CAS Number
PubChem CID
ChemSpider
UNII
Chemical and physical data
FormulaC24H19F4N5O2S
Molar mass517.50 g·mol−1
3D model (JSmol)
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
InChI
  • 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), also known as pruxelutamide (INN),[1] 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.[2][3][4][5][6] 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.[2]

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.[7][8]

Other indications

Proxalutamide is in phase Ic clinical trial in China.[2][9]

See also

References

  1. ↑ https://cdn.who.int/media/docs/default-source/international-nonproprietary-names-(inn)/pl125.pdf?sfvrsn=af269747_5&download=true
  2. 1 2 3 "Proxalutamide - Suzhou Kintor Pharmaceuticals". AdisInsight. Springer Nature Switzerland AG.
  3. ↑ 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.
  4. ↑ 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.
  5. ↑ Applied Biology, Inc. (2020-12-29). "Anti-Androgen Treatment for COVID-19". {{cite journal}}: Cite journal requires |journal= (help)
  6. ↑ "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.
  7. ↑ "Product Pipeline". Kintor Pharmaceutical. Retrieved 2021-01-29.
  8. ↑ 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.
  9. ↑ "Safety, Tolerability, and Pharmacokinetics of Proxalutamide Therapy in Women With Metastatic Breast Cancer". Clinical trials. 24 September 2019. Retrieved 2021-01-29.
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