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Chemical compound
Ralimetinib
Ralimetinib structural formula
Other names LY2228820
Routes of administration PO
ATC code
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 )
Formula C 24 H 29 F N 6
Molar mass 420.536 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
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
^ 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 .