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Proxalutamide

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
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
PubChemCID
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 nameGT-0918) is anonsteroidal antiandrogen (NSAA) – specifically, aselective high-affinitysilentantagonist of theandrogen receptor (AR) – which is under development by Suzhou Kintor Pharmaceuticals, inc., a subsidiary of Kintor Pharmaceutical Limited, for the potential treatment ofCOVID-19,prostate cancer, andbreast cancer.[1][2][3][4][5] It was approved inParaguay 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 formCRPC as monotherapy and in combination withabiraterone. 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

[edit]

References

[edit]
  1. ^abc"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. ^"Anti-Androgen Treatment for COVID-19".ClinicalTrials.gov. 2020-12-29.
  5. ^"Kintor's Proxalutamide (GT0918) COVID-19 Clinical Trial Shows Positive Results in Treatment of Male and Female".Bloomberg.com (Press release). EQS. 2021-01-10. Archived fromthe original on 2021-03-01. Retrieved2025-01-09.
  6. ^"Product Pipeline".Kintor Pharmaceutical. Archived fromthe original on 2021-02-03. Retrieved2021-01-29.
  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. Retrieved2021-01-29.
ARTooltip Androgen receptor
Agonists
SARMsTooltip Selective androgen receptor modulator
Antagonists
GPRC6A
Agonists
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