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ORGANIC SPECTROSCOPY

Read all about Organic Spectroscopy on ORGANIC SPECTROSCOPY INTERNATIONAL 

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DR ANTHONY MELVIN CRASTO Ph.D

DR ANTHONY MELVIN CRASTO Ph.D

DR ANTHONY MELVIN CRASTO, Born in Mumbai in 1964 and graduated from Mumbai University, Completed his Ph.D from ICT, 1991,Matunga, Mumbai, India, in Organic Chemistry, The thesis topic was Synthesis of Novel Pyrethroid Analogues, Currently he is working with AFRICURE PHARMA, ROW2TECH, NIPER-G, Department of Pharmaceuticals, Ministry of Chemicals and Fertilizers, Govt. of India as ADVISOR, earlier assignment was with GLENMARK LIFE SCIENCES LTD, as CONSUlTANT, Retired from GLENMARK in Jan2022 Research Centre as Principal Scientist, Process Research (bulk actives) at Mahape, Navi Mumbai, India. Total Industry exp 32 plus yrs, Prior to joining Glenmark, he has worked with major multinationals like Hoechst Marion Roussel, now Sanofi, Searle India Ltd, now RPG lifesciences, etc. He has worked with notable scientists like Dr K Nagarajan, Dr Ralph Stapel, Prof S Seshadri, etc, He did custom synthesis for major multinationals in his career like BASF, Novartis, Sanofi, etc., He has worked in Discovery, Natural products, Bulk drugs, Generics, Intermediates, Fine chemicals, Neutraceuticals, GMP, Scaleups, etc, he is now helping millions, has 9 million plus hits on Google on all Organic chemistry websites. His friends call him Open superstar worlddrugtracker. His New Drug Approvals, Green Chemistry International, All about drugs, Eurekamoments, Organic spectroscopy international, etc in organic chemistry are some most read blogs He has hands on experience in initiation and developing novel routes for drug molecules and implementation them on commercial scale over a 32 PLUS year tenure till date Feb 2023, Around 35 plus products in his career. He has good knowledge of IPM, GMP, Regulatory aspects, he has several International patents published worldwide . He has good proficiency in Technology transfer, Spectroscopy, Stereochemistry, Synthesis, Polymorphism etc., He suffered a paralytic stroke/ Acute Transverse mylitis in Dec 2007 and is 90 %Paralysed, He is bound to a wheelchair, this seems to have injected feul in him to help chemists all around the world, he is more active than before and is pushing boundaries, He has 100 million plus hits on Google, 2.5 lakh plus connections on all networking sites, 100 Lakh plus views on dozen plus blogs, 227 countries, 7 continents, He makes himself available to all, contact him on +91 9323115463, email amcrasto@gmail.com, Twitter, @amcrasto , He lives and will die for his family, 90% paralysis cannot kill his soul., Notably he has 38 lakh plus views on New Drug Approvals Blog in 227 countries......https://newdrugapprovals.wordpress.com/ , He appreciates the help he gets from one and all, Friends, Family, Glenmark, Readers, Wellwishers, Doctors, Drug authorities, His Contacts, Physiotherapist, etc He has total of 32 International and Indian awards

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Linustedastat

November 1, 2025 6:01 am / Leave a comment


Linustedastat

CAS 2254299-48-2

MFC26H29F2N3O2 MW 453.5 g/mol

FOR-6219, OG-6219, FOR 6219, OG 6219, PP3PLL7GZY, Phase 2, Endometriosis

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-fluoro-2-pyridinyl)propanamide

3-[(17E)-4-fluoro-17-(hidroxiimino)estra-1,3,5(10)-trien-15β-il]-N-(5-fluoropiridin-2-il)propanamida
inhibidor de la hidroxiesteroide 17-beta deshidrogenasa 1(HSD17B1)

  • OriginatorHormos Medical; Solvay Pharmaceuticals B.V.; University of Turku
  • DeveloperOrganon
  • ClassSmall molecules
  • Mechanism of ActionEstradiol dehydrogenase inhibitors
  • Phase IIEndometriosis
  • 02 Jul 2025Efficacy data from the phase II ELENA trial in Endometriosis released by Organon
  • 28 May 2025Organon completes a phase-II clinical trials in Endometriosis (In adults) in Latvia, Sweden, Poland, Italy, France, Hungary, Germany, Czech Republic, Czech Republic, Bulgaria, Belgium, USA (PO) (NCT05560646)
  • 28 Nov 2023No recent reports of development identified for phase-I development in Endometriosis(In volunteers) in United Kingdom (PO)

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]

A Study to Investigate Efficacy and Safety of OG-6219 BID in 3 Dose Levels Compared With Placebo in Participants Aged 18 to 49 With Moderate to Severe Endometriosis-related Pain

CTID: NCT05560646

Phase: Phase 2

Status: Completed

Date: 2025-05-29

Pat

WO2018224736

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2018224736&_cid=P21-MHFVBM-49409-1

Compound 26

3-((13S,15R,E)-3-fluoro-17-(hydroxyimino)-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-15-yl)-N-(5-fluoropyridin-2-yl)propanamide

Example 26 was prepared in 94% yield from the compound 25 by the same method as with Example 2 in three hours reaction time.

1H NMR (200 MHz, DMSO-d6): 1.03 (s, 3 H), 1.12 – 2.48 (m, 15 H), 2.57 – 2.78 (m, 1 H), 2.80 – 2.95 (m, 2 H), 6.79 – 7.01 (m, 2 H), 7.18 – 7.38 (m, 1 H), 7.72 (td, 1 H), 8.15 (dd, 1 H), 8.31 (d, 1 H), 10.18 (s, 1 H), 10.64 (s, 1 H). MS m/z (TOF ES+): 454 (M+1).

SYNTHESIS

str1

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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
IUPAC name
CAS Number2254299-48-2
PubChem CID171390018
UNIIPP3PLL7GZY
KEGGD13078
Chemical and physical data
FormulaC26H29F2N3O2
Molar mass453.534 g·mol−1
3D model (JSmol)Interactive image
SMILES
InChI

References

  1.  “FOR 6219”. AdisInsight. 28 November 2023. Retrieved 15 August 2024.
  2.  “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. hdl:11380/1201688. 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.  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 […]

//////////Linustedastat, FOR-6219, OG-6219, FOR 6219, OG 6219, PP3PLL7GZY, Phase 2, Endometriosis

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