Jump to content

Proxalutamide

Edit links
From Wikipedia, the free encyclopedia

This is an old revision of this page, as edited by DMacks (talk | contribs) at 06:28, 23 June 2020 (Remove malformatted |molecular_weight= when infobox can autocalculate it, per Wikipedia talk:WikiProject Pharmacology#Molecular weights in drugboxes (via WP:JWB)). The present address (URL) is a permanent link to this revision, which may differ significantly from the current revision.

Proxalutamide
Clinical data
Other namesGT-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 for the treatment of prostate cancer.[1][2][3] It inhibits AR-mediated gene transcription more potently than bicalutamide (by ~5- to 10-fold) and enzalutamide (by 2- to 5-fold) and maintains silent antagonism in castration-resistant prostate cancer (CRPC) cells.[2] It has also been found to downregulate the AR, which could further confer it greater efficacy against CRPC compared to existing NSAAs.[2] Unlike enzalutamide, the drug showed low central nervous system distribution and no induction of seizures in animals.[2][3] As of 2017, it is in phase II clinical trials for prostate cancer.[1] It is also in preclinical investigation for the treatment of AR-positive breast cancer.[1][2][3]

See also

References

  1. ^ a b c http://adisinsight.springer.com/drugs/800046361
  2. ^ a b c d e Tong, Youzhi; Chen, Chunyun; Wu, Juan; Yang, Jiangtao; Zhang, Huihui; Wu, Xiaojun; Duan, Yanmei; Gao, Wei; Qian, Weidong; Niu, Xiaoxia; Mi, Lili; Guo, Chuangxing (2014). "Abstract 614: 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. ^ a b c Tong, Youzhi; Chen, Chunyun; Wu, Juan; Zhang, Huihui; Wu, Xiaojun; Duan, Yanmei; Gao, Wei; Niu, Xiaoxia; Ma, Linglan; Guo, Chuangxing (2014). "Abstract 2460: 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.



Stub icon

This antineoplastic or immunomodulatory drug article is a stub. You can help Wikipedia by expanding it.

Retrieved from "https://en.wikipedia.org/w/index.php?title=Proxalutamide&oldid=964034540"