Ralimetinib Explained
| Iupac Name: | 5-[2-''tert''-Butyl-4-(4-fluorophenyl)-1''H''-imidazol-5-yl]-3-(2,2-dimethylpropyl)imidazo[4,5-''b'']pyridin-2-amine |
| Routes Of Administration: | PO |
| Cas Number: | 862505-00-8 |
| Unii: | 73I34XW4HD |
| Atc Prefix: | none |
| Pubchem: | 11539025 |
| Chemspiderid: | 9713805 |
| Kegg: | D10658 |
| Synonyms: | LY2228820 |
| C: | 24 |
| H: | 29 |
| F: | 1 |
| N: | 6 |
| 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 |
| Stdinchi: | 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) |
| Stdinchikey: | 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]
Notes and References
- Patnaik A, Haluska P, Tolcher AW, Erlichman C, Papadopoulos KP, Lensing JL, Beeram M, Molina JR, Rasco DW, Arcos RR, Kelly CS, Wijayawardana SR, Zhang X, Stancato LF, Bell R, Shi P, Kulanthaivel P, Pitou C, Mulle LB, Farrington DL, Chan EM, Goetz MP . 6 . 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 . 26581242 . 10.1158/1078-0432.CCR-15-1718 . free .
- Bhattacharjee D, Bakar J, Chitnis SP, Sausville EL, Ashtekar KD, Mendelson BE, Long K, Smith JC, Heppner DE, Sheltzer JM . 6 . 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 . 37827156 . 10.1016/j.chembiol.2023.09.013 . 263962827 .
- Vergote I, Heitz F, Buderath P, Powell M, Sehouli J, Lee CM, Hamilton A, Fiorica J, Moore KN, Teneriello M, Golden L, Zhang W, Pitou C, Bell R, Campbell R, Farrington DL, Bell-McGuinn K, Wenham RM . 6 . 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 . 31791552 . 10.1016/j.ygyno.2019.11.006 . free .
