Chemistry:Ralimetinib

From HandWiki
Short description: Chemical compound
Ralimetinib
Ralimetinib.png
Ralimetinib structural formula
Clinical data
Other namesLY2228820
Routes of
administration
PO
ATC code
  • none
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
Chemical and physical data
FormulaC24H29FN6
Molar mass420.536 g·mol−1
3D model (JSmol)

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]

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

References

  1. "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): 1095–1102. March 2016. doi:10.1158/1078-0432.CCR-15-1718. PMID 26581242. 
  2. "Inhibition of a lower potency target drives the anticancer activity of a clinical p38 inhibitor". Cell Chemical Biology 30 (10): 1211–1222.e5. October 2023. doi:10.1016/j.chembiol.2023.09.013. PMID 37827156. 
  3. Clinical trial number NCT01663857 for "A Study LY2228820 for Recurrent Ovarian Cancer" at ClinicalTrials.gov
  4. "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. January 2020. doi:10.1016/j.ygyno.2019.11.006. PMID 31791552.