
Oditrasertib
SAR443820; DNL788
| Molecular Formula | C14H15F2N3O2 |
| Molecular Weight | 295.2846 |
- UNII-I1YQT8HC89
- I1YQT8HC89
- cas 2252271-93-3
- 4-(3,3-Difluoro-2,2-dimethylpropanoyl)-3,5-dihydro-2H-pyrido(3,4-F)(1,4)oxazepine-9-carbonitrile
PYRIDO(3,4-F)-1,4-OXAZEPINE-9-CARBONITRILE, 4-(3,3-DIFLUORO-2,2-DIMETHYL-1-OXOPROPYL)-2,3,4,5-TETRAHYDRO-
Oditrasertib (SAR443820) is an orally active, BBB-penetrable and selective reversible inhibitor of RIPK1. Oditrasertib can be used in the research of chronic inflammatory central nervous system diseases, such as amyotrophic lateral sclerosis and multiple sclerosis.
Oditrasertib is a serine/threonine kinase (STK) inhibitor.
OriginatorHarvard University
DeveloperDenali Therapeutics Inc; Sanofi
ClassAntidementias; Small molecules
Mechanism of ActionRIPK1 protein inhibitors
- 24 Feb 2025Sanofi terminates its license for DNL 788 from Denali Therapeutics
- 21 Nov 2024Chemical structure information added.
- 08 Nov 2024Discontinued – Phase-II for Multiple sclerosis (In adults) in Canada, China, France, Italy, Poland, Germany, Belgium, Spain (PO)
SCHEME
WO2018213632

PATENT
[WO2018213632A1]
https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2018213632



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- [1]. Fidalgo JDV, et al. Preparation of substituted oxazepines and related compounds as RIPK1 inhibitors and uses thereof. WO2018213632A1. 2018-11-22.[2]. Hincelin-Mery A, et al. Safety, pharmacokinetics, and target engagement of a brain penetrant RIPK1 inhibitor, SAR443820 (DNL788), in healthy adult participants. Clin Transl Sci. 2024 Jan;17(1):e13690. [Content Brief][3]. Montalban X, et al. Effect of RIPK1 inhibitor, SAR443820, on serum neurofilament light levels in patients with multiple sclerosis: a phase 2 trial design (P6-3.011)[J]. Neurology, 2023, 100(17_supplement_2): 2178.
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