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Linustedastat

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]

Linustedastat
Clinical data
Other namesFOR-6219; OG-6219; 3-[(17E)-4-Fluoro-17-(hydroxyimino)estra-1,3,5(10)-trien-15β-yl]-N-(5-fluoropyridin-2-yl)propanamide
Identifiers
  • 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
PubChem CID
UNII
Chemical and physical data
FormulaC26H29F2N3O2
Molar mass453.534 g·mol−1
3D model (JSmol)
  • 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=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

References

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  1. ^ a b c d "FOR 6219". AdisInsight. 28 November 2023. Retrieved 15 August 2024.
  2. ^ a b c d "Delving into the Latest Updates on Linustedastat with Synapse". Synapse. 3 August 2024. Retrieved 15 August 2024.
  3. ^ Barra F, Romano A, Grandi G, Facchinetti F, Ferrero S (June 2019). "Future directions in endometriosis treatment: discovery and development of novel inhibitors of estrogen biosynthesis". Expert Opin Investig Drugs. 28 (6): 501–504. doi:10.1080/13543784.2019.1618269. PMID 31072144.
  4. ^ Perrone U, Evangelisti G, Laganà AS, Bogliolo S, Ceccaroni M, Izzotti A, Gustavino C, Ferrero S, Barra F (December 2023). "A review of phase II and III drugs for the treatment and management of endometriosis". Expert Opin Emerg Drugs. 28 (4): 333–351. doi:10.1080/14728214.2023.2296080. PMID 38099328.
  5. ^ a b c d Rižner TL, Romano A (2023). "Targeting the formation of estrogens for treatment of hormone dependent diseases-current status". Front Pharmacol. 14: 1155558. doi:10.3389/fphar.2023.1155558. PMC 10175629. PMID 37188267. Several compounds with inhibitory action on the enzyme HSD17B1 have been developed and one steroidal compound, a competitive HSD17B1 inhibitor (OG-6219) recently entered the clinical phase for endometriosis [...] and it is in the preclinical phase for endometrial and breast cancer (Husen et al., 2006a; Husen et al., 2006b; Konings et al., 2018b; Jarvensivu et al., 2018; Xanthoulea et al., 2021). [...] Only the C15 estrone derivative developed by Organon Finland, former Forendo pharma (compound FOR-6219/OR-6219) reached the clinical phase for endometriosis with three clinical trials registered in the database Clinical Trails (Table 2). Phase 1 and 1b trials NCT04686669 and NCT03709420 determined the bio-availability of the compound administered orally as gelatine capsule in 12 subjects (NCT04686669) and then the safety, tolerability, food interactions, the pharmacokinetics and pharmacodynamics of escalating doses of the drug in 87 subjects (NCT03709420). The phase 2 randomized, double-blind, Elena study (NCT05560646) is currently recruiting patients and aims at evaluating the efficacy and safety of OG-6219 in women with moderate to severe endometriosis [...]
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