Linustedastat

Linustedastat
Clinical data
Other names	FOR-6219; OG-6219; 3-[(17E)-4-Fluoro-17-(hydroxyimino)estra-1,3,5(10)-trien-15β-yl]-N-(5-fluoropyridin-2-yl)propanamide
Identifiers
	IUPAC name 3-[(8R,9S,13S,14S,15R,17E)-4-fluoro-17-hydroxyimino-13-methyl-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-15-yl]-N-(5-fluoropyridin-2-yl)propanamide;
CAS Number	2254299-48-2;
PubChem CID	171390018;
ChemSpider	133325688;
UNII	PP3PLL7GZY;
KEGG	D13078;
Chemical and physical data
Formula	C26H29F2N3O2
Molar mass	453.534 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C[C@]1\2CC[C@H]3[C@H]([C@@H]1[C@@H](C/C2=N\O)CCC(=O)NC4=NC=C(C=C4)F)CCC5=C3C=CC=C5F;
	InChI InChI=1S/C26H29F2N3O2/c1-26-12-11-18-17-3-2-4-21(28)19(17)7-8-20(18)25(26)15(13-22(26)31-33)5-10-24(32)30-23-9-6-16(27)14-29-23/h2-4,6,9,14-15,18,20,25,33H,5,7-8,10-13H2,1H3,(H,29,30,32)/b31-22+/t15-,18-,20-,25+,26-/m1/s1; Key:RMMVCLGAUPAFAI-MLXDORPZSA-N;

Linustedastat (developmental code names FOR-6219 and OG-6219) is a 17β-hydroxysteroid dehydrogenase 1 (17β-HSD1; HSD17B1) inhibitor which is under development for the treatment of endometriosis.^[1]^[2]^[3]^[4]^[5] It is a steroidal compound derived from estrone and works by preventing the formation of the more potent estrogen estradiol from the minimally active precursor estrone.^[1]^[2]^[5] This in turn results in antiestrogenic effects that may be useful in the treatment of estrogen-dependent conditions.^[1]^[2]^[5] As of November 2023, the drug is in phase 2 clinical trials for endometriosis.^[1]^[2] It is also under preclinical investigation for treatment of breast cancer and endometrial cancer.^[5]