New Drug Approvals

Home » Uncategorized » Ocadusertib

Ocadusertib

DRUG APPROVALS BY DR ANTHONY MELVIN CRASTO .....FOR BLOG HOME CLICK HERE

ORGANIC SPECTROSCOPY

Read all about Organic Spectroscopy on ORGANIC SPECTROSCOPY INTERNATIONAL 

Archives

Categories

Recent Posts

Blog Stats

  • 4,847,733 hits

Unknown's avatar

Enter your email address to follow this blog and receive notifications of new posts by email.

Join 37.9K other subscribers

add to any

Share

Ocadusertib

CAS 2382811-41-6

MF C25H25N5O4 MW 459.5 g/mol

5-benzyl-N-[(3S)-7-(3-hydroxy-3-methylbut-1-ynyl)-5-methyl-4-oxo-2,3-dihydro-1,5-benzoxazepin-3-yl]-1H-1,2,4-triazole-3-carboxamide

5-benzyl-N-[(3S)-7-(3-hydroxy-3-methylbut-1-yn-1-yl)-5-methyl-4-oxo-2,3,4,5-tetrahydro-1,5-benzoxazepin-3-yl]-1H-1,2,4-triazole-3-carboxamide
serine/threonine kinase inhibitor, LY3871801, R552, LY 3871801, R 552, S53J4A7ME4

  • OriginatorRigel Pharmaceuticals
  • DeveloperEli Lilly and Company; Rigel Pharmaceuticals
  • ClassAnti-inflammatories; Antirheumatics; Small molecules
  • Mechanism of ActionRIPK1 protein inhibitors
  • Phase IIRheumatoid arthritis
  • No development reportedUnspecified
  • 28 Mar 2025No recent reports of development identified for phase-I development in Unspecified(In volunteers) in Singapore (PO, Suspension)
  • 14 Nov 2024Pharmacodynamics data from preclinical trials in Rheumatoid arthritis presented at the ACR Convergence 2024 (ACR-2024)
  • 14 Nov 2024Safety and pharmacokinetics data from a phase I trial in Rheumatoid arthritis presented at the ACR Convergence 2024 (ACR-2024)

Ocadusertib (LY3871801/R552) is an oral, potent, and selective small-molecule RIPK1 inhibitor developed by Rigel Pharmaceuticals and Eli Lilly for autoimmune and inflammatory diseases. It is currently in Phase 2 clinical trials for treating moderate-to-severe rheumatoid arthritis. ACR Meeting AbstractsACR Meeting Abstracts +4

Key Aspects of Ocadusertib:

  • Mechanism of Action: It inhibits receptor-interacting serine/threonine-protein kinase 1 (RIPK1), which blocks necroptotic (cell death) responses and, consequently, reduces inflammation.
  • Target Indications: Primarily focused on rheumatoid arthritis, it has also been investigated for psoriasis and general inflammatory joint conditions.
  • Development Status: As of late 2025, it is in Phase 2 clinical trials (NCT05848258), with previous trials evaluating its safety, tolerability, and pharmacokinetics in healthy volunteers.
  • Characteristics: It is designed to be a selective inhibitor, showing no significant inhibition in a broad panel of other kinases. ACR Meeting AbstractsACR Meeting Abstracts +3

Ocadusertib is a small molecule drug. The usage of the INN stem ‘-sertib’ in the name indicates that Ocadusertib is a serine/threonine kinase inhibitor. Ocadusertib is under investigation in clinical trial NCT05848258 (An Adaptive Phase 2a/2b Study of LY3871801 in Adult Participants With Rheumatoid Arthritis). Ocadusertib has a monoisotopic molecular weight of 459.19 Da.

  • An Adaptive Phase 2a/2b Study of LY3871801 in Adult Participants With Rheumatoid ArthritisCTID: NCT05848258Phase: Phase 2Status: RecruitingDate: 2025-12-09
  • A Study of LY3871801 in Healthy Asian and Non-Asian ParticipantsCTID: NCT05960851Phase: Phase 1Status: CompletedDate: 2024-01-10
  • A Drug Interaction Study of LY3871801 in Healthy ParticipantsCTID: NCT05602675Phase: Phase 1Status: CompletedDate: 2023-04-18
  • A Study of LY3871801 in Healthy ParticipantsCTID: NCT05222399Phase: Phase 1Status: CompletedDate: 2022-03-18

SYN

PAT

PAT

WO 2014/125444

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2014125444&_cid=P20-MM02QM-54301-1

PAT

I-30: (S)-5-benzyl-N-(7-(3-hydroxy-3-methylbut-1-yn-1-yl)-5-methyl-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-yl)-1H-1,2,4-triazole-3-carboxamide;

(S)-5-benzyl-N-(5-methyl-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-yl)-4H-1,2,4-triazole-3-carboxamide (WO 2014/125444), having a structure as illustrated below, was used as a comparative compound and was examined using a similar protocol as described by WO 2014/125444. This comparison

compound exhibited 93% inhibition at a dose of 30 mg/kg according to WO 2014/125444; however, in the inventors hands, the compound inhibited only 70% at 30 mg/kg. In comparison, compound I-30 of the present disclosure achieved greater than 85% inhibition at a dose of just 5 mg/kg using the similar assay protocol described above.

PAT

str1

AS ON OCT2025 4.511 LAKHS VIEWS ON BLOG WORLDREACH AVAILABLEFOR YOUR ADVERTISEMENT

wdt-16

join me on Linkedin

Anthony Melvin Crasto Ph.D – India | LinkedIn

join me on Researchgate

RESEARCHGATE

This image has an empty alt attribute; its file name is research.jpg

join me on Facebook

Anthony Melvin Crasto Dr. | Facebook

join me on twitter

Anthony Melvin Crasto Dr. | twitter

+919321316780 call whatsaapp

EMAIL. amcrasto@gmail.com

///////ocadusertib, serine/threonine kinase inhibitor, LY3871801, R552, LY 3871801, R 552, S53J4A7ME4

Tags: , , , , ,

By in Uncategorized on .

Leave a comment

This site uses Akismet to reduce spam. Learn how your comment data is processed.

DR ANTHONY CRASTO

Follow New Drug Approvals on WordPress.com

Enter your email address to follow this blog and receive notifications of new posts by email.

Join 37.9K other subscribers
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

View Full Profile →

bloglovin

Follow my blog with Bloglovin The title of your home page You could put your verification ID in a comment Or, in its own meta tag Or, as one of your keywords Your content is here. The verification ID will NOT be detected if you put it here.