Clinical data
Synonyms 1,2,3,4-Tetrahydro-2,2-dimethyl-6-trifluoromethyl-8-pyridono[5,6-g]quinoline
Drug class Nonsteroidal antiandrogen
PubChem CID
Chemical and physical data
Formula C15H13F3N2O
Molar mass 294.277 g/mol
3D model (JSmol)

LG-120907 is a nonsteroidal antiandrogen (NSAA) of the quinoline group which was developed by Ligand Pharmaceuticals along with selective androgen receptor modulators (SARMs) like LG-121071 and was never marketed.[1][2] [3][4] The drug is a high-affinity antagonist of the androgen receptor (AR) with a Ki value of 26 nM and has been found to inhibit growth of the ventral prostate and seminal vesicles in male rats without increasing circulating levels of luteinizing hormone or testosterone.[1][2][3] However, this tissue selectivity has not been assessed in humans.[5] LG-120907 is orally active and shows greater oral potency than the arylpropionamide NSAA flutamide.[1][3][4]

The 7-fluoro derivative of LG-120907, LG-105, is also a potent NSAA, and appears to possess greater potency in comparison.[3] Conversely, the 6-ethyl, 8-didesmethyl analogue of LG-120907, LG-121071, is a SARM with potent androgenic activity equivalent to that of dihydrotestosterone (DHT).[1][3]


  1. 1 2 3 4 Chengalvala, Murty; Oh, Thomas; Roy, Arun K (2005). "Selective androgen receptor modulators". Expert Opinion on Therapeutic Patents. 13 (1): 59–66. doi:10.1517/13543776.13.1.59. ISSN 1354-3776.
  2. 1 2 Mohler, Michael L; Nair, Vipin A; Hwang, Dong Jin; Rakov, Igor M; Patil, Renukadevi; Miller, Duane D (2005). "Nonsteroidal tissue selective androgen receptor modulators: a promising class of clinical candidates". Expert Opinion on Therapeutic Patents. 15 (11): 1565–1585. doi:10.1517/13543776.15.11.1565. ISSN 1354-3776.
  3. 1 2 3 4 5 Gao W, Kim J, Dalton JT (2006). "Pharmacokinetics and pharmacodynamics of nonsteroidal androgen receptor ligands". Pharm. Res. 23 (8): 1641–58. doi:10.1007/s11095-006-9024-3. PMC 2072875. PMID 16841196.
  4. 1 2 Nyrönen TH, Söderholm AA (2010). "Structural basis for computational screening of non-steroidal androgen receptor ligands". Expert Opin Drug Discov. 5 (1): 5–20. doi:10.1517/17460440903468680. PMID 22823968.
  5. Rob Bradbury (30 January 2007). Cancer. Springer Science & Business Media. pp. 67–. ISBN 978-3-540-33120-9.

This article is issued from Wikipedia. The text is licensed under Creative Commons - Attribution - Sharealike. Additional terms may apply for the media files.