Chemistry:LG-120907
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| Other names | 1,2,3,4-Tetrahydro-2,2-dimethyl-6-trifluoromethyl-8-pyridono[5,6-g]quinoline |
| Drug class | Nonsteroidal antiandrogen |
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| Formula | C15H13F3N2O |
| Molar mass | 294.277 g·mol−1 |
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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]
References
- ↑ 1.0 1.1 1.2 1.3 "Selective androgen receptor modulators". Expert Opinion on Therapeutic Patents 13 (1): 59–66. 2005. doi:10.1517/13543776.13.1.59. ISSN 1354-3776.
- ↑ 2.0 2.1 "Nonsteroidal tissue selective androgen receptor modulators: a promising class of clinical candidates". Expert Opinion on Therapeutic Patents 15 (11): 1565–1585. 2005. doi:10.1517/13543776.15.11.1565. ISSN 1354-3776.
- ↑ 3.0 3.1 3.2 3.3 3.4 "Pharmacokinetics and pharmacodynamics of nonsteroidal androgen receptor ligands". Pharmaceutical Research 23 (8): 1641–1658. August 2006. doi:10.1007/s11095-006-9024-3. PMID 16841196.
- ↑ 4.0 4.1 "Structural basis for computational screening of non-steroidal androgen receptor ligands". Expert Opinion on Drug Discovery 5 (1): 5–20. January 2010. doi:10.1517/17460440903468680. PMID 22823968.
- ↑ "Anti-hormone therapy: principles of endocrine therapy of cancer.". Cancer. Springer Science & Business Media. 30 January 2007. pp. 19-82 (67). ISBN 978-3-540-33120-9. https://books.google.com/books?id=fdtDAAAAQBAJ&pg=PA67.
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