LG-120907

LG-120907
Clinical data
Other names	1,2,3,4-Tetrahydro-2,2-dimethyl-6-trifluoromethyl-8-pyridono[5,6-g]quinoline
Drug class	Nonsteroidal antiandrogen
Identifiers
	IUPAC name 2,2-Dimethyl-6-(trifluoromethyl)-1,9-dihydropyrido[3,2-g]quinolin-8-one;
CAS Number	179897-43-9;
PubChem CID	10851308;
ChemSpider	9026602;
ChEMBL	ChEMBL350877;
Chemical and physical data
Formula	C15H13F3N2O
Molar mass	294.277 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CC1(C=CC2=C(N1)C=C3C(=C2)C(=CC(=O)N3)C(F)(F)F)C;
	InChI InChI=1S/C15H13F3N2O/c1-14(2)4-3-8-5-9-10(15(16,17)18)6-13(21)19-12(9)7-11(8)20-14/h3-7,20H,1-2H3,(H,19,21); Key:MMLSXRYBGYGQEP-UHFFFAOYSA-N;

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 K_i 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 aryl propionamide 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

^ ^a ^b ^c ^d Chengalvala M, Oh T, Roy AK (2005). "Selective androgen receptor modulators". Expert Opinion on Therapeutic Patents. 13 (1): 59–66. doi:10.1517/13543776.13.1.59. ISSN 1354-3776. S2CID 219188263.
^ ^a ^b Mohler ML, Nair VA, Hwang DJ, Rakov IM, Patil R, Miller DD (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. S2CID 96279138.
^ ^a ^b ^c ^d ^e Gao W, Kim J, Dalton JT (August 2006). "Pharmacokinetics and pharmacodynamics of nonsteroidal androgen receptor ligands". Pharmaceutical Research. 23 (8): 1641–1658. doi:10.1007/s11095-006-9024-3. PMC 2072875. PMID 16841196.
^ ^a ^b Nyrönen TH, Söderholm AA (January 2010). "Structural basis for computational screening of non-steroidal androgen receptor ligands". Expert Opinion on Drug Discovery. 5 (1): 5–20. doi:10.1517/17460440903468680. PMID 22823968. S2CID 21630468.
^ Hoffmann J, Sommer A (30 January 2007). "Anti-hormone therapy: principles of endocrine therapy of cancer.". In Bradbury R (ed.). Cancer. Springer Science & Business Media. pp. 19-82 (67). ISBN 978-3-540-33120-9.

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