Ralimetinib

Ralimetinib
	Ralimetinib structural formula
Clinical data
Other names	LY2228820
Routes of; administration	PO
ATC code	none;
Identifiers
	IUPAC name 5-[2-tert-Butyl-4-(4-fluorophenyl)-1H-imidazol-5-yl]-3-(2,2-dimethylpropyl)imidazo[4,5-b]pyridin-2-amine;
CAS Number	862505-00-8 ;
PubChem CID	11539025;
ChemSpider	9713805;
UNII	73I34XW4HD;
KEGG	D10658 ;
CompTox Dashboard (EPA)	DTXSID00235456 ;
Chemical and physical data
Formula	C24H29FN6
Molar mass	420.536 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES 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 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;

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[edit]

^ 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): 1095–1102. doi:10.1158/1078-0432.CCR-15-1718. PMID 26581242.
^ Bhattacharjee D, Bakar J, Chitnis SP, Sausville EL, Ashtekar KD, Mendelson BE, et al. (October 2023). "Inhibition of a lower potency target drives the anticancer activity of a clinical p38 inhibitor". Cell Chemical Biology. 30 (10): 1211–1222.e5. doi:10.1016/j.chembiol.2023.09.013. PMID 37827156. S2CID 263962827.
^ Clinical trial number NCT01663857 for "A Study LY2228820 for Recurrent Ovarian Cancer" at ClinicalTrials.gov
^ 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.