Merestinib Explained

Iupac Name:N-(3-Fluoro-4-phenyl)-1-(4-fluorophenyl)-6-methyl-2-oxo-1,2-dihydropyridine-3-carboxamide
Width:300
Routes Of Administration:PO
Cas Number:1206799-15-6
Unii:5OGS5K699E
Atc Prefix:none
Kegg:D11763
Chemspiderid:29361338
C:30
H:22
F:2
N:6
O:3
Smiles:Cc1ccc(c(=O)n1c2ccc(cc2)F)C(=O)Nc3ccc(c(c3)F)Oc4cc5cnn(c5cc4c6c[nH]nc6)C
Stdinchi:1S/C30H22F2N6O3/c1-17-3-9-23(30(40)38(17)22-7-4-20(31)5-8-22)29(39)36-21-6-10-27(25(32)12-21)41-28-11-18-16-35-37(2)26(18)13-24(28)19-14-33-34-15-19/h3-16H,1-2H3,(H,33,34)(H,36,39)
Stdinchikey:QHADVLVFMKEIIP-UHFFFAOYSA-N

Merestinib (LY2801653) is an experimental cancer drug in development by Eli Lilly. It is a small molecule inhibitor of MET and several other receptor tyrosine kinases such as MST1R, FLT3, AXL, MERTK, TEK, ROS1, NTRK1/2/3, and DDR1/2.[1]

Meristinib is part of a phase II clinical trial for advanced billiary tract cancer. The study is expected to be complete in April 2018. Phase II clinical trials for non-small cell lung cancer and solid tumors began in November 2016.[2]

Notes and References

  1. Konicek BW, Capen AR, Credille KM, Ebert PJ, Falcon BL, Heady GL, Patel BK, Peek VL, Stephens JR, Stewart JA, Stout SL, Timm DE, Um SL, Willard MD, Wulur IH, Zeng Y, Wang Y, Walgren RA, Betty Yan SC . 6 . Merestinib (LY2801653) inhibits neurotrophic receptor kinase (NTRK) and suppresses growth of NTRK fusion bearing tumors . Oncotarget . 9 . 17 . 13796–13806 . March 2018 . 29568395 . 5862616 . 10.18632/oncotarget.24488 .
  2. Web site: Merestinib - Eli Lilly . AdisInsight . Springer Nature Switzerland AG .