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Izumerogant

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Izumerogant
Clinical data
Other namesIMU-935
Drug classRORγ agonist/DHODH inhibitor
Identifiers
  • 4-[4-[3-(2-chloro-6-fluorophenyl)-4-pyrimidin-2-yl-1,2-oxazol-5-yl]-5-(trifluoromethyl)pyrazol-1-yl]-2-methylbutan-2-ol
CAS Number
PubChem CID
UNII
Chemical and physical data
FormulaC22H18ClF4N5O2
Molar mass495.86 g·mol−1
3D model (JSmol)
  • CC(C)(CCN1C(=C(C=N1)C2=C(C(=NO2)C3=C(C=CC=C3Cl)F)C4=NC=CC=N4)C(F)(F)F)O
  • InChI=1S/C22H18ClF4N5O2/c1-21(2,33)7-10-32-19(22(25,26)27)12(11-30-32)18-16(20-28-8-4-9-29-20)17(31-34-18)15-13(23)5-3-6-14(15)24/h3-6,8-9,11,33H,7,10H2,1-2H3
  • Key:MRJLIFZIFUEXQG-UHFFFAOYSA-N

Izumerogant (IMU-935) is a drug which acts as both a selective antagonist of the receptor RAR-related orphan receptor gamma (RORγ), and also an inhibitor of the enzyme dihydroorotate dehydrogenase (DHODH). It has antiinflammatory and broad-spectrum antiviral effects, and is also of interest in the treatment of cancer.[1][2][3][4]

References

[edit]
  1. ↑ Polasek TM, Leelasena I, Betscheider I, Marolt M, Kohlhof H, Vitt D, et al. (May 2023). "Safety, Tolerability, and Pharmacokinetics of IMU-935, a Novel Inverse Agonist of Retinoic Acid Receptor-Related Orphan Nuclear Receptor γt: Results From a Double-Blind, Placebo-Controlled, First-in-Human Phase 1 Study". Clinical Pharmacology in Drug Development. 12 (5): 525–534. doi:10.1002/cpdd.1243. PMID 36938862.
  2. ↑ Herrmann A, Gege C, Wangen C, Wagner S, Kögler M, Cordsmeier A, et al. (November 2024). "Orally bioavailable RORγ/DHODH dual host-targeting small molecules with broad-spectrum antiviral activity". Antiviral Research. 231 106008. doi:10.1016/j.antiviral.2024.106008. PMID 39306285.
  3. ↑ Wu H, Zhong X, Ma N, He Z, Wang G, Lu G, et al. (2 January 2026). "Selective disruption of RORγt-CBFβ interaction by IMU-935 prevents RORγt-dependent Th17 autoimmunity but not thymocyte development". The Journal of Clinical Investigation. 136 (1) e185942. doi:10.1172/JCI185942. PMC 12721887. PMID 41480759.
  4. ↑ Grochot R, Guo C, Carreira S, Crespo M, Welti J, Miranda S, et al. (March 2026). "An Open-label, Phase 1 Dose-finding Study of Single-agent IMU-935, a Novel RORγ/RORγt Inverse Agonist, in Patients with Progressive Metastatic Castration-resistant Prostate Cancer". European Urology Oncology: S2588–9311(26)00051–9. doi:10.1016/j.euo.2026.02.014. PMID 41820163.
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