Ralimetinib

Ralimetinib (LY2228820) is a small molecule experimental cancer drug in development by Eli Lilly. Although originally thought to be a p38 mitogen-activated protein kinase (MAPK) inhibitor,[1] it has since been reported that it acts instead as an epidermal growth factor receptor (EGFR) inhibitor.[2]

Ralimetinib
Ralimetinib structural formula
Clinical data
Other namesLY2228820
Routes of
administration		PO
ATC code
  • none
Identifiers
  • 5-[2-tert-Butyl-4-(4-fluorophenyl)-1H-imidazol-5-yl]-3-(2,2-dimethylpropyl)imidazo[4,5-b]pyridin-2-amine
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC24H29FN6
Molar mass420.536 g·mol−1
3D model (JSmol)
  • C12C(=CC=C(N=1)C1=C(N=C(N1)C(C)(C)C)C1C=CC(=CC=1)F)N=C(N2CC(C)(C)C)N
  • InChI=1S/C24H29FN6/c1-23(2,3)13-31-20-17(28-22(31)26)12-11-16(27-20)19-18(14-7-9-15(25)10-8-14)29-21(30-19)24(4,5)6/h7-12H,13H2,1-6H3,(H2,26,28)(H,29,30)
  • Key:XPPBBJCBDOEXDN-UHFFFAOYSA-N

A phase II trial for treatment of ovarian cancer has completed.[3][4]

References
  1. Patnaik A, Haluska P, Tolcher AW, Erlichman C, Papadopoulos KP, Lensing JL, et al. (March 2016). "A First-in-Human Phase I Study of the Oral p38 MAPK Inhibitor, Ralimetinib (LY2228820 Dimesylate), in Patients with Advanced Cancer". Clinical Cancer Research. 22 (5): 1095–102. doi:10.1158/1078-0432.CCR-15-1718. PMID 26581242.
  2. Bhattacharjee, Debanjan; Bakar, Jaweria; Chitnis, Surbhi P.; Sausville, Erin L.; Ashtekar, Kumar Dilip; Mendelson, Brianna E.; Long, Kaitlin; Smith, Joan C.; Heppner, David E.; Sheltzer, Jason M. (2023). "Inhibition of a lower potency target drives the anticancer activity of a clinical p38 inhibitor". Cell Chemical Biology. doi:10.1016/j.chembiol.2023.09.013.
  3. Clinical trial number NCT01663857 for "A Study LY2228820 for Recurrent Ovarian Cancer" at ClinicalTrials.gov
  4. Vergote I, Heitz F, Buderath P, Powell M, Sehouli J, Lee CM, et al. (January 2020). "A randomized, double-blind, placebo-controlled phase 1b/2 study of ralimetinib, a p38 MAPK inhibitor, plus gemcitabine and carboplatin versus gemcitabine and carboplatin for women with recurrent platinum-sensitive ovarian cancer". Gynecologic Oncology. 156 (1): 23–31. doi:10.1016/j.ygyno.2019.11.006. PMID 31791552.
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